tel Perd Center

Ahmadābād, India

tel Perd Center

Ahmadābād, India
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Shah B.,tel Perd Center | Khunt D.,Indian National Institute of Pharmaceutical Education and Research | Bhatt H.,Indian National Institute of Pharmaceutical Education and Research | Misra M.,Indian National Institute of Pharmaceutical Education and Research | Padh H.,Sardar Patel University
Journal of Drug Delivery Science and Technology | Year: 2016

The objective of the present investigation was to optimize and develop venlafaxine (VLF) loaded nanostructured lipid carrier (NLC) using QbD and risk assessment approach. Full factorial 32 design was applied using two independent variables viz., X1: Drug to total lipid ratio and X2: Surfactant concentration whereby their effect on dependent variables viz., Y1: Size, Y2: PDI and Y3: %EE was studied. Compritol 888 ATO and Capmul MCM EP showed highest solubility for VLF as solid and liquid lipid respectively which depicted superior miscibility at solid: liquid lipid ratio of 70:30% w/w. VLF NLC were formulated based on optimized formula obtained from design space which gave experimental values for CQA (Size: 77.08 ± 3.45 nm, PDI: 0.234 ± 0.062 and %EE: 81.33 ± 3.05). FTIR, DSC and XRD studies revealed formation of less ordered crystalline structure of lipid matrix favouring higher encapsulation of VLF. Ex-vivo diffusion study showed higher flux value with VLF NLC (14.2 ± 0.40 μg/cm2/h) in comparison to VLF solution (9.62 ± 0.59 μg/cm2/h) across goat nasal mucosa. VLF NLC did not show toxicity and nasal mucosa was intact indicating safety for intranasal administration. Overall, QbD approach sounds to be apt for the successful development of VLF NLC. © 2016 Elsevier B.V.


Shah B.,tel Perd Center | 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
European Journal of Pharmaceutical Sciences | Year: 2016

Systemic drug delivery in schizophrenia is a major challenge due to presence of obstacles like, blood-brain barrier and P-glycoprotein, which prohibit entry of drugs into the brain. Quetiapine fumarate (QF), a substrate to P-glycoprotein under goes extensive first pass metabolism leading to limited absorption thus necessitating frequent oral administration. The aim of this study was to develop QF based microemulsion (ME) with and without chitosan (CH) to investigate its potential use in improving the bioavailability and brain targeting efficiency following non-invasive intranasal administration. QF loaded ME and mucoadhesive ME (MME) showed globule size, pH and viscosity in the range of 29–47 nm, 5.5–6.5 and 17–40 cP respectively. CH-ME with spherical globules having mean size of 35.31 ± 1.71 nm, pH value of 5.61 ± 0.16 showed highest ex-vivo nasal diffusion (78.26 ± 3.29%) in 8 h with no sign of structural damage upon histopathological examination. Circular plume with an ovality ratio closer to 1.3 for CH-ME depicted ideal spray pattern. Significantly higher brain/blood ratio of CH-ME in comparison to QF-ME and drug solution following intranasal administration revealed prolonged retention of QF at site of action suggesting superiority of CH as permeability enhancer. Following intranasal administration, 2.7 and 3.8 folds higher nasal bioavailability in brain with CH-ME compared to QF-ME and drug solution respectively is indicative of preferential nose to brain transport (80.51 ± 6.46%) bypassing blood-brain barrier. 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.


Yagnik B.,tel Perd Center | Patel S.,tel Perd Center | Dave M.,tel Perd Center | Sharma D.,tel Perd Center | And 2 more authors.
Indian Journal of Microbiology | Year: 2016

Potential use of Lactococcus lactis (L. lactis) as a heterologous protein expression host as well as for delivery of multiple therapeutic proteins has been investigated extensively using Nisin Inducible Controlled Expression (NICE) system. Optimum inducible expression of heterologous protein by NICE system in L. lactis depends on multiple factors. To study the unexplored role of factors affecting heterologous protein expression in L. lactis using NICE, the present study outlines the optimization of various key parameters such as inducer concentration, host’s proteases and precipitating agent using Outer membrane protein A (OmpA). For efficient expression and secretion of OmpA, pSEC:OmpA vector was successfully constructed. To circumvent the troubles encountered during detection of expressed OmpA, the precipitating agent was switched from TCA to methanol. Nevertheless, detection was achieved accompanied by degraded protein products. Speculating the accountability of observed degradation at higher inducer concentration, different nisin concentrations were evaluated. Lower nisin concentrations were found desirable for optimum expression of OmpA. Consistently observed degradation was eliminated by incorporation of protease inhibitor cocktail which inhibits intracellular proteases and expression in VEL1153 (NZ9000 ΔhtrA) strain which inhibits extracellular protease leading to optimum expression of OmpA. Versatility and complexity of NICE system in L. lactis requires fine-tuning of target protein specific parameters for optimum expression. © 2015, Association of Microbiologists of India.


Khunt D.,Indian National Institute of Pharmaceutical Education and Research | Shah B.,tel Perd Center | Misra M.,Indian National Institute of Pharmaceutical Education and Research
Journal of Drug Delivery Science and Technology | Year: 2017

Purpose of the present investigation was to explore the potential of butter oil (BO) as a novel permeation enhancer to enhance the drug concentration in the brain when given intranasally. Quetiapine fumarate (QF) was selected as a model drug since it undergoes extensive first-pass metabolism leading to poor oral bioavailability of 9%. QF:BO binary mixture was prepared by simple physical mixing in the ratio of 1:9 to 9:1. Diffusion study was performed to obtain optimized QF:BO ratio. QF loaded microemulsion (ME) system (QF ME) was developed by water titration method. The optimized ratio of QF:BO showing higher permeation for QF was added into ME to obtain QF:BO ME. Globule size of QF ME and QF:BO ME was found be 61.59 ± 0.54 and 133.30 ± 1.74 nm, respectively. Nasal diffusion data revealed that QF:BO ME showed higher permeation (85.45 ± 2.14%) for QF in comparison to QF ME (52.07 ± 2.07%) and QF solution (40.00 ± 2.01%). Nearly 4.6 folds higher brain bioavailability of QF:BO ME (384.11 ± 49.10%) compared to QF Solution (83.15 ± 9.82%) suggested higher transport of QF from QF:BO ME to rat brain. Overall, it was concluded that BO enhances the brain bioavailability of poorly permeable drugs across the olfactory neuroepithelium, thereby proving its potential in the area of brain drug delivery system. © 2017 Elsevier B.V.


Pund S.,tel Perd Center | Joshi A.,tel Perd Center | Vasu K.,tel Perd Center | Nivsarkar M.,tel Perd Center | Shishoo C.,tel Perd Center
International Journal of Pharmaceutics | Year: 2011

Rifampicin, a first line anti-tubercular drug, has maximum solubility and permeability in the stomach. An oral multi-particulate formulation with site specific sustained delivery of rifampicin was developed. This oral gastroretentive rifampicin formulation consisted of rifampicin pellets for immediate release as the loading dose and a bio/mucoadhesive rifampicin tablet for extended release. Immediate release pellets of rifampicin were prepared by extrusion-spheronization process and were evaluated for physico-mechanical properties: usable yield, size, shape, abrasion resistance, mechanical crushing force, residual moisture and drug release. For the mucoadhesive rifampicin formulation, statistical experimental strategy was utilized to simultaneously optimize the effect of two independent variables namely amount of Carbopol and MCC. The two dependent responses selected were, work of adhesion; estimated using Texture Analyzer and T 50%; determined from dissolution studies. Graphical and mathematical analysis of the results allowed the identification and quantification of the formulation variables influencing the selected responses. To study the gastrointestinal transit of the optimized gastroretentive formulation, the in vivo gamma scintigraphy was carried out in six healthy human volunteers, after radiolabeling the formulation with 99mTc. The transit profiles demonstrated that the dosage form was retained in the stomach for more than 320 min. The human data validates the design concept and signifies the potential of the developed system for stomach targeted delivery of rifampicin for improved bioavailability. © 2011 Elsevier B.V. All rights reserved.


PubMed | tel Perd Center, Indian National Institute of Pharmaceutical Education and Research and Sardar Patel University
Type: | Journal: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences | Year: 2016

Systemic drug delivery in schizophrenia is a major challenge due to presence of obstacles like, blood-brain barrier and P-glycoprotein, which prohibit entry of drugs into the brain. Quetiapine fumarate (QF), a substrate to P-glycoprotein under goes extensive first pass metabolism leading to limited absorption thus necessitating frequent oral administration. The aim of this study was to develop QF based microemulsion (ME) with and without chitosan (CH) to investigate its potential use in improving the bioavailability and brain targeting efficiency following non-invasive intranasal administration. QF loaded ME and mucoadhesive ME (MME) showed globule size, pH and viscosity in the range of 29-47nm, 5.5-6.5 and 17-40cP respectively. CH-ME with spherical globules having mean size of 35.311.71nm, pH value of 5.610.16 showed highest ex-vivo nasal diffusion (78.263.29%) in 8h with no sign of structural damage upon histopathological examination. Circular plume with an ovality ratio closer to 1.3 for CH-ME depicted ideal spray pattern. Significantly higher brain/blood ratio of CH-ME in comparison to QF-ME and drug solution following intranasal administration revealed prolonged retention of QF at site of action suggesting superiority of CH as permeability enhancer. Following intranasal administration, 2.7 and 3.8 folds higher nasal bioavailability in brain with CH-ME compared to QF-ME and drug solution respectively is indicative of preferential nose to brain transport (80.516.46%) bypassing blood-brain barrier. 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.


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.


PubMed | tel Perd Center and Nirma University
Type: Evaluation Studies | Journal: Journal of chromatographic science | Year: 2016

High-performance liquid chromatography method for anti-asthmatic 2-agonist drug bambuterol, its process-related impurities and its major degradation products was developed and validated using quality by design concept. A 3(3) 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.


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


Potential use of Lactococcus lactis (L. lactis) as a heterologous protein expression host as well as for delivery of multiple therapeutic proteins has been investigated extensively using Nisin Inducible Controlled Expression (NICE) system. Optimum inducible expression of heterologous protein by NICE system in L. lactis depends on multiple factors. To study the unexplored role of factors affecting heterologous protein expression in L. lactis using NICE, the present study outlines the optimization of various key parameters such as inducer concentration, hosts proteases and precipitating agent using Outer membrane protein A (OmpA). For efficient expression and secretion of OmpA, pSEC:OmpA vector was successfully constructed. To circumvent the troubles encountered during detection of expressed OmpA, the precipitating agent was switched from TCA to methanol. Nevertheless, detection was achieved accompanied by degraded protein products. Speculating the accountability of observed degradation at higher inducer concentration, different nisin concentrations were evaluated. Lower nisin concentrations were found desirable for optimum expression of OmpA. Consistently observed degradation was eliminated by incorporation of protease inhibitor cocktail which inhibits intracellular proteases and expression in VEL1153 (NZ9000 htrA) strain which inhibits extracellular protease leading to optimum expression of OmpA. Versatility and complexity of NICE system in L. lactis requires fine-tuning of target protein specific parameters for optimum expression.

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