Drug Invention Today
ISSN NO: 0975-7619
Drug Invention Today (DIT) was first published in 2009 by JPR Solutions. It is a journal, which publishes reviews, research papers and short communications . 
• Novel Drug Delivery Systems • Nanotechnology & Nanomedicine • Biotechnology related pharmaceutical technology • Polymeric bio-conjugates • Biological macromolecules • Biomaterials • Drug Information • Drug discovery/development • Screening of drugs from natural & synthetic origins • Novel therapeutic strategies • Combinatorial chemistry and parallel synthesis • Clinical trials • Case Reports
 Impact FactorTM ( India ) = 0.897 as on date (08.05.2017)
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Journal Metrics for this   Drug Invention Today (Source ID: 21100202909): 2014 (SNIP) Source Normalized Impact Per Paper : 0.402; SCImago Journal Rank (SJR):0.301; Impact Per Publication : 0.517 (Top level : Life Science)
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Manuscripts Published

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-DRP-00002135
Title: Challenges in delivery of chemotherapeutic agents for the treatment of brain cancer and the scope of nanoparticulates
Category: Drug Release Profiles
Section: Review Article
Country: India
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Brain tumor remains one of the most dreadful, poorly prognosed cancer despite advances in understanding the molecular basis of carcinogenesis. Treatment of brain tumors requires a multidisciplinary approach that includes combination of surgery, radiation, or chemotherapy. The major hindrance to prognosis of brain tumor is the autoprotective nature of the brain and blood–brain barrier (BBB). The approaches involves deliberate opening of the tight junctions of the BBB or delivery of drugs “through” or “behind” BBB by manipulating the physicochemical properties of the drug and have major drawbacks including irreversible opening of BBB that potentially allows the entry of exogenous material such as viruses and bacteria, and allows limited spatial distribution of drug. Nanoparticles (NPs) focus on the administration of nanometric size particles loaded with chemotherapeutic agent, monoclonal antibodies, genes, proteins, peptides, and other entities. Due to its small size and modifiability warrant their selective uptake by the tumor cells. They can be formulated out of variety of substance and can carry multiple loads of drugs directing the substance toward the tumor cells. Thus in comparison to conventional therapies, NPs reduces the side effects. Number of drug delivery strategies has been developed to overcome challenges presented by the BBB. One technique that holds promise for bypassing the BBB to deliver drugs to the brain the spillover effect of drug to normal tissue is intranasal delivery. The intranasal delivery of NP loaded anticancer drug provides a practical and noninvasive method for delivering therapeutic agents to the brain due to the unique anatomical connections.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002122
Title: Evaluation of in vitro rheumatoid arthritis activity of polyherbal ethanolic extract containing formulations for selected potential Indian herbs
Category: Drug (Discovery/Development)
Section: Research Article
Country: India
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Objective: Arthritis has emerged to be a very common disorder affecting statistically one-third of the population. The present study aims to investigate the effectiveness of a polyherbal formulation Polygonum glabrum, Canthium dicoccum, Ochna obtusata, and Argyreia nervosa in treating the disorder arthritis. Materials and Methods: Ethanolic extract of different portions are used to investigate by in vitro inhibition of protein denaturation method using bovine serum, inhibition of protein denaturation method using egg albumin, and human red blood cell (HRBC) membrane stabilization method. Results: The result revealed that the formulations F2 and F4 possessed significant anti-arthritic activity by protein denaturation inhibition and HRBC membrane stabilization comparing with diclofenac sodium, the standard drug used. Conclusion: The study concluded that the above two formulations are an effective inhibitor of protein denaturation and HRBC membrane stabilization which can be used potent anti-arthritic activity.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002123
Title: A perspective studies on marine Red algae – Hypnea valentiae
Category: Drug (Discovery/Development)
Section: Review Article
Country: India
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Seaweeds are the potential marine living resources in the world. More than 20,000 seaweeds are distributed throughout the world, of which only 221 (1.1%) are commercially utilized, which includes 145 species for food and 110 species for phycocolloid production (Sahoo, 2000). The biodiversity of the marine environment and the associated chemical diversity constitute a practically unlimited resource of new active substances in the field of the development of bioactive products. Carrageenans are galactans extracted mainly from species belonging to Gigartinales. These sulfated galactans, consist of linear chains of D-galactopyranoses linked. Seaweeds constitute some of the most important reservoirs of new therapeutic compounds for humans. Several of them have been shown to have many biological activities, including anticancer activity, in this present review study is mainly focused on Hypnea valentiae.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-CPS-00002124
Title: Synthesis, characterization, and biological evaluation of some new quinolinyl chalcone derivatives
Category: Chemistry and Parallel Synthesis
Section: Research Article
Country: India
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Aim: The aim of the present study is to synthesize, characterize, and biologically evaluate some new quinolinyl chalcone derivatives. Materials and Methods: In the present study, synthesis of different quinolinyl chalcones is done by synthesizing quinoline moiety by Friedlander synthesis, then it is condensed with different aromatic aldehydes by acid or base catalyzed aldol condensation to form new quinolinyl chalcones derivatives using appropriate purifying techniques such as recrystallization and column chromatography. Results and Discussion: All the compounds were characterized by physical (melting point and thin-layer chromatography) and spectral data (infrared, MASS, and H1 nuclear magnetic resonance). The antibacterial activity of these compounds was tested against two Gram-positive strains Bacillus subtilis and Bacillus pumilus and two Gram-negative strains Proteus vulgaris and Escherichia coli, and the antifungal activity of these compounds was tested against Aspergillus niger and Candida albicans using Ciprofloxacin and Miconazole nitrate, respectively, as standards at a concentration of 50 µg/ml. Conclusion: The result shows that the presence of fluorine at 4th position, hydroxyl at 2nd , and nitro at 5th position exhibited better activity and considered as lead compounds for generation of new potential antimicrobial agents in future.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-pp-00002125
Title: Methylenetetrahydrofolate reductase gene polymorphism MTHFR A1298C and Rheumatoid arthritis in south indian population
Category: Pharmacy Practice
Section: Research Article
Country: India
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Aim: The present study evaluated the influence of methylenetetrahydrofolate reductase (MTHFR) A1298C polymorphisms on safety and efficacy of methotrexate (MTX). Objective: In this study, the distribution of this polymorphism was assessed in healthy and rheumatoid arthritis (RA) patients of South India, and then, subset of patients with RA was studied for response and emergence of adverse effects. Methods: A total of 100 RA patients and 50 healthy subjects were participated in the study. The genotype frequencies of different alleles of MTHFR 1298C were assessed by polymerase chain reaction and restriction fragment length polymorphism. The efficacy parameters were mitigation of morning stiffness, reduction in pain scale, tender and swollen joint counts, improvement in health assessment questionnaire, and disease activity score (DAS), calculated with erythrocyte sedimentation rate. The adverse effects identified liver transaminases and gastrointestinal adverse effects, during follow-up visit, scheduled at the 3rd month. Results: The genotype frequencies of MTHFR A1298C polymorphism revealed difference in distribution of the alleles AA, AC, and CC were different in healthy and RA patients. It was also found that the distribution was significantly different in comparison to worldwide population reports. The 1298AA allele was found to have significant improvement in efficacy variables and less prone to harmful effects of MTX, whereas 1298CC genotypes were found to be non-responders and more susceptible to adverse effects, despite folate supplementation. Conclusion: The assessment of genotype frequencies reveals differences in distribution of alleles, and closer observation of 1298CC genotypes is warranted to the physicians, as they could emerge as non-responders and prone to adverse effects.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002126
Title: Formulation and evaluation of hesperidin-loaded chitosan nanosuspension for brain targeting
Category: Drug (Discovery/Development)
Section: Research Article
Country: India
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Aim: Parkinson’s disease is characterized by a progressive loss of dopaminergic neuron in the substantia nigra. Hesperidin is a free radical scavenger that has been shown to have a protective effect against oxidative insults. An antioxidant can neutralize the free radical by accepting or donating an electron to eliminate the unpaired condition. Materials and Methods: Hesperidin- loaded chitosan nanosuspension was prepared by ionic gelation method using tripolyphosphate and chitosan. There was no incompatibility observed between the drug and polymer through Fourier-transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles. Results and Discussion: The average particle size of 188 nm, zeta potential of 48.7 mV, drug content of 0.470 ± 0.25 mg/ml, and entrapment efficiency of 78.2% are obtained with HPN3 formulation. The HPN1 shows the highest drug release followed by HPN2 due to the low concentration of polymer, and HPN4 and HPN5 show less drug release due to the high concentration of polymer. The in vitro release of HPN3 85.2% showed an initial burst release of approximately 60% in the 1st 8 h, followed by a slow and much reduced additional release for about 24 h. Conclusion: HPN3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be taken for the effective treatment of Parkinson’s disease.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002127
Title: A review on applications of natural polymers in gastroretentive drug delivery system
Category: Drug (Discovery/Development)
Section: Review Article
Country: India
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The objective of this review is to provide the overview of the role of natural polymers in gastroretentive drug delivery system (GRDDS), its characteristics, ongoing research, trend of future developments, and applications in the field. Appropriate articles were searched from Medline database using the search term “Natural Polymer and Gastric,” restricted search for the past 5 years and accessed only 21 open access articles to narrate this review. The approach of various natural polymers in industrial applications such as medicine, agriculture, and similar areas is growing rapidly in this era. It was observed biodegradable and non-toxic materials like the natural polymers are evident by the mounting level of its use in the pharmaceutical field. Using various natural polymers have been aiding the drug delivery systems for prolongation of time as the drug transporters with the objective of improving bioavailability and therapeutic efficacy. The use of natural polymers in novel drug delivery like GRDDS to possess floating or mucoadhesive in the gastric system for the benefit of increasing gastric resident time and to improve therapeutic efficacy, particularly those drugs are having narrow therapeutic index such as carvedilol, itopride, and glipizide. The physical characteristics of natural polymers facilitates sustained, swelling, and mucoadhesive nature based on literature reviewed, therefore, natural polymers also suitable to GRDDS as like synthetic or semi-synthetic polymers.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002129
Title: An overview on novel approach of transdermal drug delivery systems
Category: Drug (Discovery/Development)
Section: Review Article
Country: India
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The transdermal drug delivery systems (TDDSs) are polymeric patches with drugs are designed to deliver a therapeutically active agent through the skin. TDDS provides better patient acceptability and compliance over the oral route of administration. The system has improved therapeutic efficacy and safety of the drugs because it deliverers through the skin layer of the patient at a controlled and predetermined rate. As skin is an effective medium from which absorption of the drug takes place and it enters the circulatory system to maintain steady-state blood concentration. The system is a desirable form of drug delivery because of the merits such as pain-free self-administration for patients and avoids the first-pass metabolism over other routes of delivery systems. In this article, an outline of the TDDS, merits over conventional drug delivery system, skin layers, various components of transdermal systems, permeability enhancers, applications, and evaluation parameters of transdermal system were discussed.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-pp-00002130
Title: Effect of patient-specific variables on rifampicin peak serum concentration
Category: Pharmacy Practice
Section: Research Article
Country: India
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Introduction: Tuberculosis (TB) is a common infectious disease with high mortality rate across the globe. In spite of effective strategies and treatment modalities, it remains a global burden due to emergence of drug-resistant bacillary strains. Rifampicin is a potent bactericidal agent used in the antitubercular regimen whose altered pharmacokinetic profile, and decreased systemic bioavailability has been strongly associated with treatment failure and emergence of drug-resistant strains. In our current study, peak serum concentration of rifampicin was studied in pulmonary TB (PTB) patients. Materials and Methods: A total of 60 patients with PTB who volunteered participation were enrolled into the study. Blood samples were collected by venipuncture, and drug concentration was determined using liquid chromatography–mass spectrometry. Logistic regression models were used to determine the effect of patient-specific variables on rifampicin serum concentrations. Results: Interindividual variability was observed in serum rifampicin concentrations. Serum concentrations of rifampicin were found to be decreased in diabetic patients. Body weight, serum albumin, and blood glucose were found to be inversely correlated with rifampicin concentrations. Conclusion: Dosing individualization of rifampicin should be considered in patients with the identified factors so as to decrease the incidence of treatment failures, drug-resistant bacilli emergence, and adverse drug reactions.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-CPS-00002131
Title: Synthesis, characterization, and evaluation of some novel derivatives of Benzoin
Category: Chemistry and Parallel Synthesis
Section: Research Article
Country: India
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Objective: The main objective of the present study is to synthesize some derivatives of Benzoin that shows promising antimicrobial and anthelmintic activity. Methods: In the current research work, some derivatives of benzoin were synthesized by targeting its ketone group by reacting with various hydrazines, semi carboxamide, and hydroxylamine. The purity of the synthesized derivatives and completion of reaction were confirmed by thin-layer chromatography and was characterized by infrared studies. The pure derivatives are then screened for antimicrobial activity against Pseudomonas aeruginosa, Pseudomonas vulgaris, Escherichia coli, Staphylococcus aureus, and Bacillus subtilis at various concentrations (25–200 µl) and anthelmintic activity against Indian adult earthworms (Pheretima posthuma) at the concentrations (100–500 µl). Results: The synthesized derivatives B2, B3, B5, NB3, NB4, and NB5 showed good–to-moderate antibacterial activity comparable with the standard drug and compounds B5, NB3, and NB5 exhibited promising anthelmintic activity when compared with standard. Conclusion: All the synthesized derivatives of benzoin were found to have good antimicrobial activity and anthelmintic activity when compared with standard.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002132
Title: Formulation and evaluation of budenoside loaded PLGA nanoparticles
Category: Drug (Discovery/Development)
Section: Research Article
Country: India
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Objective: The objective of the present study was to formulate and evaluate the nanoparticulate drug delivery system for the controlled release of budesonide to control asthma, inflammatory bowel diseases and its associated disease condition. Materials and Methods: To achieve the above objective, budesonide nanoparticles (NPs) were prepared by solvent displacement technique using various concentrations of PLGA (PNP1-PNP5). The effects of increase in polymer concentration in various parameters like particle size, zeta potential, entrapment efficiency and in-vitro drug release profile were studied. Results: The results showed that the in vitro drug release for PNP1, PNP2, PNP3, PNP4 and PNP5 were found to be 99.57 ± 0.29, 99.61 ± 0.32, 99.54 ± 0.21, 99.58 ± 0.38 and 99.61 ± 0.28 respectively. Based on the in vitro drug release profile of budesonide NP formulations (PNP1-PNP5) the trail PNP5 was selected as the best formulation in which the particle size was 170.3 nm and drug: Polymer in the ratio of 1:3 (budesonide 100 mg: 300 mg of PLGA).The in vitro % drug release of PNP5 formulation was 99.61 ± 0.28 and it was found to be desirable for the controlled release of budesonide. Conclusion: The present study can be concluded that the newly formulated controlled release nanoparticulate drug delivery systems of Budesonide may be ideal and effective to control the asthma, inflammatory bowel disease and other associated disease condition by allowing the drug release continuously for 24 h.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002133
Title: Design, formulation, and in vitro evaluation of sustained release tablets for losartan potassium
Category: Drug (Discovery/Development)
Section: Research Article
Country: India
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Objective: The purpose of the present research investigation was to formulate sustained release (SR) formulations for losartan potassium using 32 factorial designs. Methods: Losartan potassium is an antihypertensive agent, non-peptide angiotensin-II receptor (type AT1) blocker, and BCS class-III agent. SR tablet formulations of losartan potassium were formulated using variable quantities of hydroxymethyl propyl cellulose (HPMC) K100M and xanthan gum in combinations by direct compression technique. The amount of polymers, HPMC K100M, and xanthan gum required to achieve the drug release was selected as independent variables, X1 and X2 , respectively, whereas time required to release 10% (t 10%), 50% (t 50%), 75% (t 75%), and 90% (t 90%) of drug from formulation was selected as dependent variables. Nine formulations were prepared and evaluated for various pharmacopoeial tests. Results: The results reveal that all formulations were found to be with in the pharmacopoeial limits and in vitro drug release profiles of all formulations were subjected to kinetic modeling. The statistical parameters such as intercept, slope, and correlation coefficient were determined. Polynomial equations were developed for dependent variables. Validity of developed polynomial equations was checked by designing two checkpoint formulations (C1 and C2 ). According to SUPAC guidelines, formulation (F4 ) containing mixture of 15% HPMC K100M and 20% xanthan gum is the most identical formulation (similarity factor f2 = 86.747, dissimilarity factor f1 = 1.760, and no significant difference, t = 0.0477) to marketed product (LOSACAR). Conclusion: Best Formulation F4 follows the first-order, Higuchi kinetics, and the mechanism of drug release was found to be non-Fickian diffusion anomalous transport (n = 0.825).

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002134
Title: Formulation and evaluation of non-effervescent floating tablets of linagliptin using low-density carriers
Category: Drug (Discovery/Development)
Section: Research Article
Country: India
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Aim and Objective: The objective of the present work was to formulate floating tablets containing linagliptin to provide a prolonged effect and improve bioavailability in the treatment of type II diabetes. Materials and Methods: Linagliptin is a dipeptidyl peptidase-4 enzyme inhibitor used in the treatment of type-II diabetes. It is rapidly absorbed after oral intake and has 30% of bioavailability while remaining drug is excreted unchanged in urine and enterohepatic system. Due to its lower bioavailability and absorption is more at acidic pH conditions, it is selected as a suitable drug for the design of a gastroretentive floating drug delivery system with a view to improve its bioavailability. Linagliptin non-effervescent floating tablets can be prepared by direct compression method using hydroxypropyl methylcellulose (HPMC) K15, HPMC E15, and chitosan as polymers and Accurel, Gelucire as low-density carriers. Results and Discussion: The Fourier transform-infrared spectra revealed that there was no interaction between polymers an drug; hence, they are compatible. The formulations were evaluated for pharmacopoeial quality control tests and all the physical parameters evaluated were within the acceptable limits. Linagliptin non-effervescent floating tablets were remained buoyant for more than 20 h. The optimized formulation F1 gave 98% of drug release in 20 h with floating lag time of 22 s and total floating time more than 20 h. Conclusion: This study shows that optimum concentration of polymer and low-density carrier increases bioavailability. Stability studies were carried out on the optimized formulation F1 for 3 months at 40°C/75% RH. Finally, it was observed that there was no change in physiochemical and physical properties as well as in drug release profile even after storage at 45°C and 75% for 3 months.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-pp-00002136
Title: Comparison of safety and effectiveness of ondansetron and domperidone in patients with gastrointestinal problems
Category: Pharmacy Practice
Section: Research Article
Country: India
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Objective: The objective of this study was to compare the safety and effectiveness of ondansetron and domperidone in patients with gastrointestinal (GI) problems. Materials and Methods: A prospective observational comparative study design was used with the help of data entry forms and regular ward round participation. The numeric scoring system was used to evaluate the efficacy assessment of ondansetron and domperidone in time interval 0–24 h. Results: The study was conducted in 100 patients. 50 patients were treated with ondansetron. 50 patients were treated with domperidone. 20% was suffering from peptic ulcer. 20% was suffering from GERD. 20% was suffering from duodenal ulcer. 30% was suffering from nonsteroidal anti-inflammatory drugs-induced ulcer. 10% was suffering from other GI problems. Conclusion: In the management of GI disturbance patients, ondansetron was found to be more effective than domperidone, and hence, it is considered better than domperidone as ondansetron shows better efficacy than domperidone.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-Pcol-00002137
Title: Ifosfamide drug stability: A formulation challenge
Category: Pharmacology
Section: Review Article
Country: India
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Although ifosfamide is usually formulated as a sterile solution and delivered as intravenous injection, major efforts in both academic and industrial laboratories have been directed toward developing effective oral formulations and increasing the oral absorption of ifosfamide through the use of formulations that protect the drug and/or enhance its uptake into the intestinal mucosa. However, in spite of these major attempts, relatively little progress has been made. For the efficient delivery of ifosfamide by non-parenteral route, in particular through the gastrointestinal tract, novel concepts are needed to overcome significant diffusion barriers. The properties of ifosfamide, which are of major interest in oral delivery, are highlighted in the article. This article reviews the various problems associated and novel approaches for formulation and development of oral ifosfamide delivery systems.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-pp-00002138
Title: Assessment of knowledge, attitude, and practice of pharmacist in providing patient counseling on urinary tract infection and its treatment
Category: Pharmacy Practice
Section: Research Article
Country: India
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Aim: Urinary tract infections (UTIs) are the most commonly occurring bacterial infections and accounts for 8 million patient visits annually to the hospital and clinics. Health-care professional plays main role in the community health. Objective: Of this study is to assess the knowledge, attitude, and practice (KAP) of pharmacists in providing patient counseling on UTIs. Methods: It is a cross-sectional study with 100 sample sizes of pharmacist and pharmacy students. Questionnaires were prepared and validated after conducting pilot study. The finalized questionnaire was used to assess the KAP of community pharmacist and pharmacy students. The data were collected, scored and then the results were statistically analyzed and compared. Results: KAP score shows that 4.56, 5.34, and 3.88 and 7.02, 6.68, and 6.72 of pharmacist and internship student for their KAP, respectively. Conclusion: From the present study, an unwelcomed result which shows that community pharmacist scored low when compared to the pharmacy internship students. Community pharmacists were directly involved in dispensing the medicines to public, their knowledge to be upgraded is a prerequisite. Academic conclaves involving faculty from universities and customer educating concerts by pharmaceutical marketing teams educating them would improve their current level of knowledge and makes them competent enough for the public health-care service in future.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-pp-00002139
Title: A prospective study on the effect of sodium intake on renal function in hypertensive patients
Category: Pharmacy Practice
Section: Research Article
Country: India
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Objective: The association between salt intake and renal outcome in subjects with preserved kidney functions in hypertension patients remains unclear. However, high salt intake might adversely affect blood pressure (BP) and renal function. The objective of the study was to assess the association between sodium (salt) intake and renal function in patients with hypertension. Methods: About 100 patients (male 76% and female 33%) of mean age 43 ± 8 years diagnosed with hypertensive (systolic BP 140–160 mmHg and diastolic 90–100 mmHg) in a tertiary care hospital were assessed. BP, 24 h urinary salt, and creatinine (Cr) excretion levels were measured. Results: The level of Cr clearance was significantly increased (P = 0.003**) in line with the increase of sodium intake. The study revealed that there was an association between the amounts of sodium intake and reservation of renal function in hypertension state was observed. Conclusion: The results suggest that the high salt intake promotes a decline in renal function in hypertensive patients, and thus, salt restriction is encouraged to prevent renal damage in higher degrees of hypertension.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-PS-00002140
Title: Analgesic and anti-inflammatory activities of Dichrostachys cinerea (L.) Wight and Arn.
Category: Pharmacological Screening
Section: Research Article
Country: India
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Background: Dichrostachys cinerea (Family - Mimosaceae), known as “Viddathalai” in Tamil, is well-known plant used in the traditional system of medicines such as Ayurveda and Siddha. The traditional plant is commonly used by tribal of India and South Africa. The plant is claimed to possess more therapeutic medicinal uses such as anti-inflammatory, analgesic, antipyretic also used in rheumatism, urinary calculi, and in diarrhea, which is evident from traditional knowledge. Methods: Based on the literature review, the proposed study is intended to validate scientifically the folklore claims for its analgesic, anti-inflammatory, and antioxidant activity. Therein, an attempt has been made for screening the various inflammation-associated activities as per standard protocols to prove its efficacy on support of folklore uses. Results: Qualitative phytochemical analysis of leaf, stem bark, and root revealed that petroleum ether extract showed the presence of terpenoid and steroid. Chloroform extract has shown the presence of glycosides, the alcoholic extract showed the presence of tannin, flavonoids, and phenolic compounds. Aqueous extract showed positive test for saponin and tannins. The acute toxicity study of ethanolic extract of D. cinerea leaf (EDCL), ethanolic extract of D. cinerea bark (EDCB), and ethanolic extract of D. cinerea root (EDCR) carried out revealed that all the extracts were not toxic up to 2000 mg/kg. Hence, the tested extracts were found to be within the safe margin. The results of the different parameter carried out for 28 days in subacute toxicity studies of EDCL, EDCB, and EDCR did not reveal any toxic effect in the two dose levels tested by biochemical and histopathological examination and have wide safety margin. The test extracts, namely, leaf, stem bark, and root extract were found to show significant analgesic activity in both centrally and peripherally mediated analgesia. Anti-inflammatory screening indicates that stem bark, leaf, and root were effective in acute model, whereas stem bark is ineffective in chronic model. The results of antioxidant activity act as a prelude for anti-inflammatory study and these are attributed to the presence of phytoconstituents tested in our extracts. Conclusion: The data retrieved from the observations have been formulated into a diagnostic protocol of Dichrostachys cinerea. The promising biological activities will definitely lead to develop a new drug from the plant and also form the foundation for a future research work in bioactivity-guided isolation of active principles.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-BSN-00002141
Title: Application of phytochemicals for the treatment of neurodegenerative diseases
Category: Biomaterials ( Synthetic and Natural )
Section: Review Article
Country: India
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Neurodegeneration is defined as the progressive loss of structure or function of neurons which includes amyotrophic sclerosis, Alzheimer’s disease, and Huntington’s disease. Many neurodegenerative diseases are caused by genetic mutations; however, multiple biological processes can cause neurodegeneration. Synthetic drugs are widely used for the treatment of most neurodegenerative disorders which are reported to cause side effects during the treatment. Researchers identified some naturally occurring chemical compounds in plants, i.e., phytochemical through various research programs, and these are used for the management of neurodegenerative diseases. Phytochemicals are generally accepted to be safe with minimal side effects. In this review, we comprehensively compiled the plant-derived compounds such as polyphenol, isothiocyanate, alkaloid, and cannabinoid, and other important phytochemicals reported possess beneficial effect in neurodegenerative disorders. These phytochemical compounds have various effects such as neuroprotective, antioxidant, and anti-inflammatory actions. In the case of phytochemical studies, different plants and plant parts containing many valuable constituents such as lignans, flavonoids, tannins, triterpenes, and sterols, and these constituents are exhibit neuroregeneration or neuroprotective effect. Many Ayurvedic formulations prepared from various plants are claimed to possess neurostimulant activity, thus improving the symptomatic conditions in patients with neurodegenerative disorders. The folklore medicine has also possessed a significant contribution identifying neurotonic and nerve stimulants. The systematic ethanopharmacological studies had yielded highly reliable results in exploring the phytochemical agents for the treatment of neurodegenerative disorders. This review article will provide the researchers comprehensive information about the plants and the mechanisms elucidated by them through in vivo or in vitro studies.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-Pcol-00002142
Title: A review on the role of estrogen, estrogen receptor and signaling pathways in breast carcinogenesis
Category: Pharmacology
Section: Review Article
Country: India
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Estrogens were one of the primary female sex hormones, and it plays an important role in both reproductive and non-reproductive systems. It can also be synthesized in non-reproductive tissue as liver, heart, muscle, bone, and brain. The estradiol (E2) was considered to be a major estrogen hormone which is involved in the progression of breast cancer, and a majority of the human breast cancers start out as estrogen dependent and express the estrogen receptor (ER). Interruption of ER function mainly (ER)-α in breast cancer is an effective therapeutic strategy. HOXB13, IL17BR, and CHDH are estrogen-regulated genes where their prognostic utility is likely to impact on their regulation through both ER- and HER2-dependent pathways. Genomic and extranuclear signaling pathways are the main two estrogen signaling pathway where estradiol acts on the ER. In the genomic pathway, estradiol (E2) binds to ER-α and relocalizes estrogen to estrogen-responsive elements and promotes target genes expression. In the extranuclear signaling pathways, rapid E2 signaling activates PI3K/Akt/mTOR and eRK/mitogen-activating protein kinase pathway. Thus, estrogen signal regulates cell proliferation, apoptosis, and cell cycle, following control cell or tissue growth.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002143
Title: Docetaxel-loaded chitosan nanoparticles to enhance the chemotherapeutic efficacy in lung cancer
Category: Drug (Discovery/Development)
Section: Research Article
Country: India
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Purpose: The purpose of the research is to prepare an optimized chitosan nanoparticle for Docetaxel. Method: Docetaxel- loaded chitosan nanoparticles were prepared by water in oil emulsion cross-linking method. Response surface methodology using the Box–Behnken design was used to optimize the formulations of docetaxel-loaded chitosan nanoparticles. Results: The drug entrapment efficiency, drug loading efficiency, particle size, and zeta potential of docetaxel-loaded chitosan nanoparticles were 93.10%, 8.17%, 100 nm, and −24.17 mV, respectively. Transmission electron microscope of the optimized nanoparticles showed spherical particles. Furthermore, docetaxel-loaded chitosan nanoparticles displayed the highest cytotoxicity against lung cancer cells. The result indicated that the docetaxel nanoparticle had sustained release efficacy. The results indicated that the nanoparticles could deliver docetaxel mainly to lung after iv. injection to mice and the concentration of docetaxel in lung (781.4 ng/g, 0.25 h) was significantly higher than those in other tissue and plasma. Conclusion: The nanoparticle formulation demonstrated a promising perspective for the targeted delivery of docetaxel for lung cancer.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-pp-00002144
Title: A retrospective study on drug utilization evaluation of analgesics for palliative pain management
Category: Pharmacy Practice
Section: Research Article
Country: India
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Aim: The aim of this present study is to evaluate the use of analgesics for the management of pain in the palliative care patients. The secondary objective was to evaluate the choice of analgesic selection for the management of various kinds of pain in these patients. Objective: The perception of pain is always a point of concern. Chronic malignant pain occurs in a potentially life-threatening illness. The aim of this present study is to evaluate the use of analgesics for the management of pain in palliative care patients. Study Design: A retrospective study has been carried out with the help of patient’s case sheets. Case sheets of 200 patients had been obtained for the study. Data were collected from the case sheets between the years 2012 and 2015. Results: It can be seen that 56.09% patients had lung carcinoma. The most common drug being given for palliative pain management is Morphine. The other drug that was given predominantly was Tramadol. Nonsteroidal anti-inflammatory drugs such as diclofenac and ibuprofen were also been given to the patients. Corticosteroids such as dexamethasone were also given, sodium valproate is also given for the management of neuropathic pain. Opioids were found to be much efficient than non-opioid analgesics (P < 0.001). Conclusion: This study concludes that the goal of physicians is “to cure sometimes, to relieve often, and to comfort always.” Careful attention to the science and art of pain management and comfort is every bit as important as cure. Death is inevitable; suffering is not.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-CDRS-00002154
Title: Effectiveness of chlorhexidine and warm saline mouth rinses against bacterial colonization on silk suture material in third molar surgery - A clinicomicrobiological study
Category: Clinical Drugs Related Study
Section: Research Article
Country: India
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Objective: Sutures are used for approximation of wound margins and to promote wound healing. Post-operative wound care is essential for uneventful wound healing. Normal saline rinse, chlorhexidine mouthwashes, and hydrogen peroxide diluted with saline or fresh tap water are some of the frequently used mouth rinses used to maintain clean sutured wounds in intraoral surgery. The aim of the present study was to evaluate the effectiveness of chlorhexidine and warm saline mouth rinses against bacterial colonization on silk suture material in third molar surgery through microbiological analysis. Methods: This was a split-mouth prospective randomized clinical study involving a total of 25 patients requiring lower third molar surgery bilaterally. After the extraction of the third molar on the left side, all the participants were instructed to use warm saline mouth rinse (Group 1) from the 2nd post-operative day to the 7th post-operative day. 15 days later, the third molar surgery was done on the contralateral side followed by the use of 0.2% concentration of chlorhexidine mouth rinse (Group 2) from the 2nd post-operative day to the 7th post-operative day. Microbial analysis from silk suture was performed; data were analyzed in SPSS software and results obtained. Results: Bacterial adherence to sutures (colony-forming units of bacteria) was more in Group 1 compared to Group 2, and the results were statistically significant (P < 0.05). Wound healing was complete and satisfactory in both the groups on the 15th post-operative day, and none of the patients developed suture site infection. Conclusion: From the present study, it can be concluded that chlorhexidine mouth rinse following third molar surgery plays a promising role in reducing the amount of bacterial colonization on silk suture.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-DFP-00002155
Title: Review on a herbal anticoagulant - Indian Musa species
Category: Drugs from Plants
Section: Review Article
Country: India
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The genus Musa compresses of 70 species. It is a large herb with false stem compound inflorescence with large leaves belong to Musaceae family. It is largely cultivated and used as staple food around the world. In India, it is largely consumed for many therapeutic values. Its medicinally used to treat laxative, constipation, intestinal lesions, diabetes, bladder stone, anticoagulant activity on blood. It was shown that it has been much evaluated for anticoagulant properties. Hence, the present study was aimed to focus for the collection of scientific data to merge together the anticlotting properties of Indian Musa species extract and its isolated phytocompounds. The present review work was concluded.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002156
Title: A review docking studies: In silico methodologies for a better computational approach
Category: Drug (Discovery/Development)
Section: Review Article
Country: India
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Molecular docking methodology explores the behavior of small molecules in the binding site of a target protein. As more protein structures are determined experimentally using X-ray crystallography or nuclear magnetic resonance spectroscopy, molecular docking is increasingly used as a tool in drug discovery. Docking against homology-modeled targets also becomes possible for proteins whose structures are not known. With the docking strategies, the druggability of the compounds and their specificity against a particular target can be calculated for further lead optimization processes. Molecular docking programs perform a search algorithm, in which the conformation of the ligand is evaluated recursively until the convergence to the minimum energy is reached. Finally, an affinity scoring function, ΔG (U total in kcal/mol), is employed to rank the candidate poses as the sum of the electrostatic and Van der Waals energies. The driving forces for these specific interactions in biological systems aim toward complementarities between the shape and electrostatics of the binding site surfaces and the ligand or substrate.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-pp-00002157
Title: Assessment of cardiovascular risk in hypertensive and non-hypertensive postmenopausal women in a tertiary care hospital
Category: Pharmacy Practice
Section: Research Article
Country: India
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Aim and Objective: The aim of the study is to assess the cardiovascular risk in hypertension and non-hypertensive postmenopausal women and impart pharmacist education in hypertension management. Methodology: A prospective observational study was conducted at the tertiary care hospital in Chennai providing comprehensive medical care in all areas. A self-designed questionnaire was used to collect patient data including their demographic details and lipid profile. The patient was initially assessed for cardiovascular risk followed by their blood pressure using mercury sphygmomanometer. Then, pharmacist education for the management of hypertension was provided and followed up for their next visit. Results and Conclusion: On assessing the cardiovascular risk, 52 (52.92%) hypertensive women are in moderate risk whereas only 12 (11.08%) of non-hypertensive women are in moderate risk. During the measurement of baseline blood pressure before intervention, 54 (51.9%) were in pre-hypertensive stage, 26 (25.0%) were in Stage-1, 6 (5.8%) were in Stage-I, and 18 (17.3%) were non-hypertensive. After intervention 34 (32.7%) were in pre-hypertensive stage, 19 (18.3%) were in Stage-1, and non-hypertensive cases were 51 (49.0%). The Chi-square value was found to be 27.417, and the study was significant (P = 0.000).

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-D(DD)-00002158
Title: Development of eco-friendly mosquito repellents with emphasis on herbal formulation and evaluation
Category: Drug (Discovery/Development)
Section: Research Article
Country: India
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Background and Objective: Traditional plants are safe and non-toxic alternative to synthetic chemicals against mosquito- borne diseases. The present investigation is aimed to evaluate the mosquito repellent activity of Ricinus communis oil (seeds), Eugenia caryophyllus (flower buds), Foeniculum vulgare (fruits), and Vitex negundo (leaves) in plant natural form of herbal formulation. Materials and Methods: The plant materials (R. communis oil [seeds], E. caryophyllus [flower buds], F. vulgare [fruits], and V. negundo [leaves]) were collected and subjected to cold maceration for 7 days using castor oil as solvent. The obtained extract were formulated into repellent coil, repellent cream, and repellent candle. These formulations were evaluated for repellent activity using standard methods under proper laboratory conditions. Results: The maximum efficacy was observed in candle when compared with coil and cream formulation. The candle formulation gave protection against mosquito bites without any allergic reaction to the test person. The Aedes aegypti showed prominent highest mortality rate, at the candle formulation with **P < 0.05 statistically significant value. These results established a correlation between the protection percentages with increasing concentration. Conclusion: Discovery of natural products, with potent phytoconstituents that have insecticidal properties, may help overcome problems of chemical insecticide resistance. However, the present study showed that all the three formulations do not harm the subjected persons during the study time.

Journal: Drug Invention Today , Volume: 10, Issue: March
Article Id: JPRS-pp-00002159
Title: Pharmacist-patient interaction and medication history interview on psoriasis patients
Category: Pharmacy Practice
Section: Research Article
Country: India
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Aim: Psoriasis is a common, chronic skin disease labeling from both the community and individuals due to its effects on appearance. Objectives: The main objective of this study is to describe and explain the percentage of the people affected with psoriasis. The present research is a study of patients aimed to evaluate the pharmacist-patient interactions and medication history interview on psoriasis at Limat Multispeciality Hospital, Padur, Chennai. Methods: A total of 100 patients were selected randomly and were interviewed for the psoriasis, in two sessions (morning and evening). Results: After the interview, it was seen that most of the people affected were from semi-urban areas who are earning 1000–3000 mid-aged persons and mostly married male persons are affected with the disease. In most of the people, the detection of the disease is between 1 and 5 years of time period, according to the affected people survey, most of the people were affected on their body with moderate severity. For the psoriasis, the treatment can be through topical, UVB, and oral; nowadays, the treatment mostly used is topical. Conclusion: All the patients are needed a further awareness on the psoriasis and need advanced treatment.