National Institute of Pharmaceutical Education and Research, Ahmedabad

www.niperahm.edu.in
Ahmadabad, India
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Dash R.P.,A And G Pharmaceutical, Inc. | Ellendula B.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Agarwal M.,A And G Pharmaceutical, Inc. | Nivsarkar M.,A And G Pharmaceutical, Inc.
European Journal of Pharmacology | Year: 2015

The aim of this study was to evaluate the change in the expression and the activity of intestinal P-glycoprotein (efflux transporter) with progression of diabetes in rats. Diabetes was induced in Wistar rats using a combination of low dose streptozotocin along with high fat diet. The expression of intestinal P-glycoprotein significantly increased (P≤0.05) with the progression of diabetes which was inferred from the mRNA analysis of mdr1a and mdr1b genes in the ileum segment of rat intestine. Furthermore, a significant increase (P≤0.05) in Na+-K+ ATPase activity was observed in the ileum segment of rat intestine with the progression of diabetes. As a result of this, a significant decrease in the intestinal uptake and peroral bioavailability of the P-glycoprotein substrates (verapamil and atorvastatin) was observed along with the progression of diabetes as compared to normal animals. To address this problem of impaired drug uptake and bioavailability, a reported P-glycoprotein inhibitor, epigallocatechin-3-gallate, was experimentally evaluated. The treatment with epigallocatechin-3-gallate resulted in significant reduction in the expression and activity of P-glycoprotein and subsequent improvement in the intestinal uptake and peroral bioavailability of both verapamil and atorvastatin in normal as well as in diabetic animals. The findings of this study rationalised the use and established the mechanism of action of epigallocatechin-3-gallate to overcome P-glycoprotein mediated drug efflux and will also be helpful in therapeutic drug monitoring in diabetes. © 2015 Elsevier B.V.


Parekh K.D.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Dash R.P.,A And G Pharmaceutical, Inc. | Pandya A.N.,B. V. Patel Pharmaceutical Education and Research Development Center | Vasu K.K.,B. V. Patel Pharmaceutical Education and Research Development Center | Nivsarkar M.,A And G Pharmaceutical, Inc.
Journal of Pharmacy and Pharmacology | Year: 2013

Objectives The objective of this study was to synthesize and identify potential leads for the management of Alzheimer's disease (AD). Methods A series of bis-imidazopyridines were synthesized and assessed preclinically for anti-inflammatory and antioxidant activity in aluminium chloride-induced rat model for AD. The two targets, anti-inflammatory and antioxidant, hold a significant relevance in AD. The compounds were also screened for their role of protein phosphatase 2A (PP2A) activity in brain which is responsible for tau dephosphorylation and alleviation of AD. Key findings The results of our study identified NIPERAMCD-KTB7 (dose: 50 mg/kg bodyweight, orally), as a potential molecule with good inhibitory activity in acute (67% oedema protection) as well as chronic (61% oedema protection) model of inflammation. This compound also showed good antioxidant activity as inferred from the inhibition of lipid peroxidation and superoxide dismutase activity in rats at the dose mentioned above. More significantly, PP2A activity was found to be increased in the brains of the animals treated with NIPERAMCD-KTB7 suggesting its potential role in management of AD. Conclusions These preliminary findings indicate that NIPERAMCD-KTB7 holds potential to serve as a basic lead for further structural modification and development of other new chemical entities for combating AD. © 2013 Royal Pharmaceutical Society.


Upadhyay D.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Dash R.P.,A And G Pharmaceutical, Inc. | Anandjiwala S.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Nivsarkar M.,A And G Pharmaceutical, Inc.
Fitoterapia | Year: 2013

Picrosides I and II are the active chemical constituents, present in the roots and rhizomes of Picrorhiza kurroa Royle (family: Scrophulariaceae). The plant is ethnomedically claimed for the treatment of liver and upper respiratory tract infection, fever, dyspepsia and scorpion sting. This study attempts to determine the in vivo pharmacokinetic profile of picrosides I and II in rats after oral administration of three different preparations namely, kutkin (a mixture of picrosides I and II), P. kurroa extract and Picrolax® capsule (marketed formulation). A simple, precise, specific and sensitive method was developed for simultaneous quantification of picrosides I and II in rat plasma and was applied for the pharmacokinetic study. Pharmacokinetic parameters were calculated from the observed plasma concentration of picrosides I and II. The results showed a significant difference (p ≤ 0.05) in oral bioavailability of picrosides I and II from different preparations. Both the compounds were found to be more bioavailable from P. kurroa extract followed by Picrolax® capsule and kutkin. Moreover, we also developed a novel method for isolation of kutkin from roots of P. kurroa with a high yield of 2.4% w/w. The information gained from this study provides a meaningful basis for clinical application and mechanistic study of such phytochemicals. © 2013 Elsevier B.V.


Patel M.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Antala B.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Barua C.,Assam Agricultural University | Lahkar M.,National Institute of Pharmaceutical Education and Research, Ahmedabad
International Journal of Green Pharmacy | Year: 2013

Background: Anxiety or depressed mood is associated with low levels of serotonin in the brain. A hydroxycitric acid (HCA), constituent of Garcinia indica (GIA), increases serotonin release from isolated rat brain cortex. Aim: To evaluate the anxiolytic activity of aqueous extract of dried fruits of GIA in mice. Materials and Methods: The anxiolytic-like effects of aqueous extract of dried fruits of GIA were evaluated by using elevated plus maze (EPM), hole board and light/dark exploration models in Swiss albino mice. Control mice were treated with an equal volume of saline, and positive control mice were treated with diazepam (1 mg/kg). Results: GIA administered orally, 30 min before the test in different doses (125, 250 and 500 mg/kg of body weight), was able to increase significantly (P < 0.05) the time-spent and entries into open arms of the EPM and reduced the time-spent and entries into closed arms versus control. In the hole-board test, treatment with GIA (250 and 500 mg/kg) significantly increased the number of head-dips and duration of head dipping (P < 0.05). In the light-dark paradigm test, number of transitions and the time spent in the light box increased with reduction in time spent in the dark box and immobility period significantly (P < 0.05) after treatment with GIA. However, no significant changes in locomotor activity were observed versus control. Conclusion: The results of the present study suggest that aqueous extract of dried fruits of GIA is an effective anxiolytic agent for behavioural models in mice.


Vyas T.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Dash R.P.,A And G Pharmaceutical, Inc. | Anandjiwala S.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Nivsarkar M.,A And G Pharmaceutical, Inc.
Fitoterapia | Year: 2011

The oral bioavailability of vasicine (1) was investigated in hard gelatin capsules of lyophilized Vasa Swaras (aqueous extract of Adhatoda vasica Nees.,Fam.: Acanthaceae) The rat pharmacokinetic profile of lyophilized Vasa Swaras, Vasa Swaras, vasicine (1) (chief marker compounds of A. vasica) and a marketed capsule formulation of A. vasica were compared. Vasicine (1) was found to be more orally bioavailable from lyophilized Vasa Swaras, with an overall minor conversion to vasicinone (2). © 2010 Elsevier B.V. All rights reserved.


Zine R.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Sinha M.,National Institute of Pharmaceutical Education and Research, Ahmedabad
Materials Science and Engineering C | Year: 2017

The purpose of wound management is to prevent wound from infection, increase the fibroblast cell growth, and preserve cellular function. The polymeric electrospun nanofiber scaffold made up of natural and/or synthetic polymer provides an extracellular matrix for support and initiates the growth, proliferation and differentiation of fibroblast cells. The present study deals with the development of poly3-hydroxybutyric acid-co-3-hydroxyvaleric acid (PHBV) nanofibrous scaffold imbedded with graphene oxide (GO), and collagen. Nanofibrous PHBV offers advantages like structural resemblance to native extracellular matrix, high porosity and surface area to volume ratio. The nanofibrous mats were morphologically and chemically characterized by Field Emission Scanning Electron Microscopy (FESEM) and Fourier Transform Infrared (FTIR) Spectroscopy. FESEM images showed the nanofiber diameter was decreased and porosity increased by adding GO and collagen into the matrix without any chemical interaction among them. Incorporation of GO into the matrix increases mechanical strength of scaffold in addition to antibacterial activity against E. coli and S. aureus with decrease in pore size and hydrophilicity. In contrast, collagen addition into the nanofibers enhanced hydrophilicity without affecting mechanical strength and porosity significantly. Moreover, collagen enhanced cell proliferation capacity of nanofibers in comparison to the samples of PHBV + GO and virgin PHBV. The combination of collagen and GO with PHBV has balanced properties which can be utilised for the application. © 2017


Shah V.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Choudhury B.K.,National Institute of Pharmaceutical Education and Research, Ahmedabad
AAPS PharmSciTech | Year: 2017

A revolutionary paradigm shift is being observed currently, towards the use of therapeutic biologics for disease management. The present research was focused on designing an efficient dosage form for transdermal delivery of α-choriogonadotropin (high molecular weight biologic), through biodegradable polymeric microneedles. Polyvinylpyrrolidone-based biodegradable microneedle arrays loaded with high molecular weight polypeptide, α-choriogonadotropin, were fabricated for its systemic delivery via transdermal route. Varied process and formulation parameters were optimized for fabricating microneedle array, which in turn was expected to temporally rupture the stratum corneum layer of the skin, acting as a major barrier to drug delivery through transdermal route. The developed polymeric microneedles were optimized on the basis of quality attributes like mechanical strength, axial strength, insertion ratio, and insertion force analysis. The optimized polymeric microneedle arrays were characterized for in vitro drug release studies, ex vivo drug permeation studies, skin resealing studies, and in vivo pharmacokinetic studies. Results depicted that fabricated polymeric microneedle arrays with mechanical strength of above 5 N and good insertion ratio exhibited similar systemic bioavailability of α-choriogonadotropin in comparison to marketed subcutaneous injection formulation of α-choriogonadotropin. Thus, it was ultimately concluded that the designed drug delivery system can serve as an efficient tool for systemic delivery of therapeutic biologics, with an added benefit of overcoming the limitations of parenteral delivery, achieving better patient acceptability and compliance. © 2017 American Association of Pharmaceutical Scientists


Patil S.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Dash R.P.,A And G Pharmaceutical, Inc. | Anandjiwala S.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Nivsarkar M.,A And G Pharmaceutical, Inc.
Biomedical Chromatography | Year: 2012

A sensitive and simple HPLC method was developed for the simultaneous quantification of berberine and lysergol in rat plasma. The chromatographic separation was achieved on a C18 column using isocratic elution with methanol-acetonitrile-0.1% ortho-phosphoric acid (25:20:55, v/v/v), pH adjusted to 6.5 with triethylamine and detected at a UV wavelength of 230nm. The extraction of the berberine and lysergol from the rat plasma with methylene chloride resulted in their high recoveries (82.62 and 90.17%). HPLC calibration curves for both berberine and lysergol based on the extracts from the rat plasma were linear over a broad concentration range of 50-1000ng/mL. The limit of quantification was 50ng/mL. Intra- and inter-day precisions were <15% and accuracy was 87.12-92.55% for berberine and 87.01-92.26% for lysergol. Stability studies showed that berberine and lysergol were stable in rat plasma for short- and long-term period for sample preparation and analysis. The described method was successfully applied to study the pharmacokinetics of berberine as well as lysergol following oral administration in Sprague-Dawley rats. The results of the study inferred that lysergol improved the oral bioavailability of berberine. © 2011 John Wiley & Sons, Ltd.


Chaudhary S.A.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Shahiwala A.F.,Dubai Pharmacy College
Expert Opinion on Drug Delivery | Year: 2010

Importance of the field: Over the years, patient convenience and patient compliance-orientated research in the field of drug delivery has resulted in bringing out potential innovative drug delivery options. Out of which, medicated chewing gum (MCG) offers a highly convenient patient-compliant way of dosing medications, not only for special population groups with swallowing difficulties such as children and the elderly, but also for the general population, including the young generation. Areas covered in this review: In this review, various formulation ingredients, different manufacturing processes, and assessment of in vivo and in vitro drug release from MCG are thoroughly discussed along with the therapeutic potential and limitations of MCG. What the reader will gain: Readers will gain knowledge about the rationale and prominent formulation and performance evaluation strategies behind chewing gum as a drug delivery system. Take home message: The availability of directly compressible co-processed gum material enables rapid, safe and low-cost development of MCG as a drug delivery option. By MCG formulation, revitalization of old products and reformulation of new patented products is possible, to differentiate them from upcoming generics competition in the market. © 2010 Informa UK Ltd.


PubMed | National Institute of Pharmaceutical Education and Research, Ahmedabad
Type: | Journal: Journal of biomedical materials research. Part B, Applied biomaterials | Year: 2016

Bone morphogenetic protein-2 (BMP-2) has unique bone regeneration property. The powerful osteoinductive nature makes it considered as second line of therapy in nonunion bone defect. A large number of carriers and delivery systems made up of different materials have been investigated for controlled and sustained release of BMP-2. The delivery systems are in the form of hydrogel, microsphere, nanoparticles, and fibers. The carriers used for the delivery are made up of metals, ceramics, polymers, and composites. Implantation of these protein-loaded carrier leads to cell adhesion, degradation which eventually releases the drug/protein at site specific. But, problems like ectopic growth, lesser protein delivery, inactivation of the protein are reported in the available carrier systems. Therefore, it is need of an hour to modify the available carrier systems as well as explore other biomaterials with desired properties. In this review, all the reported carrier systems made of metals, ceramics, polymers, composites are evaluated in terms of their processing conditions, loading capacity and release pattern of BMP-2. Along with these biomaterials, the attempts of protein modification by adding some functional group to BMP-2 or extracting functional peptides from the protein to achieve the desired effect, is also evaluated. 2016 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2016.

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