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Ahmadābād, India

Shah B.,tel Perd Center | Shah B.,Nirma University | Khunt D.,Indian National Institute of Pharmaceutical Education and Research | Misra M.,Indian National Institute of Pharmaceutical Education and Research | Padh H.,Sardar Patel University
International Journal of Biological Macromolecules | Year: 2016

The objective of the present investigation was to optimize and develop quetiapine fumarate (QF) loaded chitosan nanoparticles (QF-NP) by ionic gelation method using Box-Behnken design. Three independent variables viz., X1-Concentration of chitosan, X2-Concentration of sodium tripolyphosphate and X3-Volume of sodium tripolyphosphate were taken to investigate their effect on dependent variables (Y1-Size, Y2-PDI and Y3-%EE). Optimized formula of QF-NP was selected from the design space which was further evaluated for physicochemical, morphological, solid state characterization, nasal diffusion and in-vivo distribution for brain targeting following non-invasive intranasal administration. The average particle size, PDI, %EE and nasal diffusion were found to be 131.08 ± 7.45 nm, 0.252 ± 0.064, 89.93 ± 3.85% and 65.24 ± 5.26% respectively. Neither toxicity nor structural damage on nasal mucosa was observed upon histopathological examination. Significantly higher brain/blood ratio and 2 folds higher nasal bioavailability in brain with QF-NP in comparison to drug solution following intranasal administration revealed preferential nose to brain transport bypassing blood-brain barrier and prolonged retention of QF at site of action suggesting superiority of chitosan as permeability enhancer. Overall, the above finding shows promising results in the area of developing non-invasive intranasal route as an alternative to oral route for brain delivery. © 2016 Elsevier B.V.

Pund S.,STESs Sinhgad Institute of Pharmacy | Thakur R.,STESs Sinhgad Institute of Pharmacy | More U.,STESs Sinhgad Institute of Pharmacy | Joshi A.,tel Perd Center
Colloids and Surfaces B: Biointerfaces | Year: 2014

Resveratrol, a dietary non-flavonoid polyphenolic phytoalexin, has gained attention in cancer chemoprevention. However, poor aqueous solubility and cellular bioavailability has limited its therapeutic application. We formulated a lipid based delivery system of resveratrol with self nanoemulsifying ability. Several edible and safe lipids, surfactants and cosolvents were screened for solubilization of resevratrol. Developed formulation comprised of Acrysol K 150 as a lipid and mixture of Labrasol and Transcutol HP as the surfactant system, as these components showed higher solubility. Pseudoternary phase diagram was constructed to identify the region of nanoemulsification. The formulations showed rapid emulsification with an average globule diameter; 85. nm to 120. nm and slight negative zeta potential. The nanocompositions exhibited cloud point above 55. °C and were stable toward the gastrointestinal pH and thermodynamic stress testing. As compared to pristine resveratrol, the developed delivery system showed significant increase in vitro cytotoxicity in MCF-7 breast cancer cells. In vivo chick chorioallantoic membrane assay revealed enhanced antiangiogenic activity of composition with high lipid level. Briefly, lipid based nanoemulsifying resveratrol dramatically enhanced the anticancer and antiangiogenic activities, thus increasing its potential application in cancer chemotherapy. © 2014 Elsevier B.V.

Dhawan D.,tel Perd Center | Padh H.,tel Perd Center
Annals of Human Biology | Year: 2016

Background: Thymidylate synthase (TS) is the major target for fluoropyrimidine drugs like 5-Fluorouracil (5-FU). There are polymorphic tandem repeats in the TYMS gene enhancer region (TSER). The number of tandem repeats varies in different populations. The aim of this study was to determine the frequencies of the TSER tandem repeats (rs34743033) and compare the observed frequencies with those of other populations. Methods: This study genotyped 350 healthy individuals by Polymerase Chain Reaction (PCR). Results: A novel allele *1 (only a single repeat) was observed in four individuals, the individuals were heterozygous (TSER*1/*2) for TYMS. Another variant rs2853542 affecting the expression of Thymidylate synthase was also analysed. The observed genotype frequencies were compared with frequencies observed in other populations for understanding differences between various population groups. There was a statistically significant difference between Indians and Chinese, Kenyans, Ghanians, African-Americans, Americans of European Ancestry, British, Hungarians, Turkish, Australians and Brazilians. Conclusion: This study identified a novel single repeat in the TYMS gene which might have an impact on the expression of this gene, which needs to be confirmed by functional studies. © 2016 Informa UK Limited, trading as Taylor & Francis Group

Mahapatra A.,National Institute of Pharmaceutical Education and Research | Shah P.,National Institute of Pharmaceutical Education and Research | Jivrajani M.,tel Perd Center | Nivsarkar M.,tel Perd Center
Records of Natural Products | Year: 2015

Blastocyst implantation which is analogous to pro-inflammatory response, mediated by different inflammatory mediators and ovarian hormones found to be an effective target for the development of emergency contraceptives. In the present study, a series of derivatives an anti-inflammatory natural scaffold, lupeol were synthesized under mild reaction conditions and good yield. All the compounds were evaluated for acute anti-inflammation. The three active compounds with 62-92% edema protection were screened for chronic anti-inflammation. The analogue 3-(p-chlorocinnamoyl) lupeol (2) with potent anti-inflammatory activity (85% protection) was evaluated for the anti-implantation activity by studying changes in superoxide dismutase (SOD) and lipid peroxidation (LPO) levels, visualization of implantation site and anti-estrogenic activity. As expected, a sharp decrease in superoxide anion radical and increase in SOD activity was seen in the endometrium of treated animals. Also no implantation sites were observed in the uterus of treated animals. The active compound also exhibited anti-estrogenic activity. © 2015 ACG Publications. All rights reserved.

Abiramasundari A.,tel Perd Center | Abiramasundari A.,Nirma University | Joshi A.,tel Perd Center | Joshi R.,tel Perd Center | And 4 more authors.
Journal of Chromatographic Science | Year: 2016

High-performance liquid chromatography method for anti-asthmatic β2-agonist drug bambuterol, its process-related impurities and its major degradation products was developed and validated using quality by design concept. A 33 full factorial design was employed to study the effect of three independent factors, namely, ratio of organic modifiers in mobile phase, pH of the buffer and flow rate of the mobile phase. The responses considered were retention time of the last peak and resolution of poorly separated peaks (drug and PR-4 and drug and DP-3). The optimum conditions for separation were determined with the aid of design of experiments. The optimized ternary solvent composition was a mixture of 10 mM ammonium acetate buffer (pH 6.0), methanol and acetonitrile in the ratio of 90:5: 5 (v/v/v) in solvent reservoir A and 10:45:45 (v/v/v) in solvent reservoir B. The separation of the analytes was achieved by using a gradient method. The predictability criteria of the optimized method demonstrated good correlation between observed and predicted response. The method was validated for specificity, linearity, accuracy, precision and robustness in compliance with the International Conference on Harmonization guidelines Q2R1. © 2015 The Author 2015. Published by Oxford University Press.

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