Indian National Institute of Pharmaceutical Education and Research

Thaltej, India

Indian National Institute of Pharmaceutical Education and Research

Thaltej, India
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Jayakumari S.,Vels University | Ravichandiran V.,Indian National Institute of Pharmaceutical Education and Research
Research Journal of Pharmacy and Technology | Year: 2017

Cyclooxygenase–2 (COX–2) inhibition is an important approach in the management of inflammatory problems. Since synthetic compounds may exaggerate the levels of inflammatory mediators via COX pathway, so many researchers are focusing in search of natural compound or bioguided fraction for COX–2 inhibitors. From the literature review it is evident that natural polyphenols such as flavonoid and tannins have been found exert its anti-inflammatory effects either by decreasing formation of reactive oxygen species or by modulation of proinflammatory gene expression of Cyclooxygenase by acting through Nuclear factor – kappa B (NF-kappa) and Mitogen Activated Protein Kinase signaling. Earlier literature revealed that Terminalia chebula (Fruits); Sida rhombifolia (Root) Leucas cephalotes (Entire plant) were found to contain polyphenolic compounds and steroid and are used in Indian traditional system of medicine for inflammatory associated problems. The earlier scientific reports showed the extract of the above plants have significant anti-inflammatory activity in animal model. Hence the present study is focused to separate the fraction from the selected plants and study the effect of combined fractions for inhibition of inflammatory key enzymes.Further the bioactive fraction was standardized by HPTLC as per standard protocol. The outcome of the present work would pave a pathway for finding a new phytopharmacophore from Indian meditational plants for treatment of inflammatory associated diseases. © RJPT All rights reserved.


Shah B.,Bv Patel 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
European Journal of Pharmaceutical Sciences | Year: 2015

In the present investigation, Quality by Design (QbD) approach was applied on the development and optimization of solid lipid nanoparticle (SLN) formulation of hydrophilic drug rivastigmine (RHT). RHT SLN were formulated by homogenization and ultrasonication method using Compritol 888 ATO, tween-80 and poloxamer-188 as lipid, surfactant and stabilizer respectively. The effect of independent variables (X1 - drug: lipid ratio, X2 - surfactant concentration and X3 - homogenization time) on quality attributes of SLN i.e. dependent variables (Y1 - size, Y2 - PDI and Y3 - %entrapment efficiency (%EE)) were investigated using 33 factorial design. Multiple linear regression analysis and ANOVA were employed to indentify and estimate the main effect, 2FI, quadratic and cubic effect. Optimized RHT SLN formula was derived from an overlay plot on which further effect of probe sonication was evaluated. Final RHT SLN showed narrow size distribution (PDI- 0.132 ± 0.016) with particle size of 82.5 ± 4.07 nm and %EE of 66.84 ± 2.49. DSC and XRD study showed incorporation of RHT into imperfect crystal lattice of Compritol 888 ATO. In comparison to RHT solution, RHT SLN showed higher in-vitro and ex-vivo diffusion. The diffusion followed Higuchi model indicating drug diffusion from the lipid matrix due to erosion. Histopathology study showed intact nasal mucosa with RHT SLN indicating safety of RHT SLN for intranasal administration. © 2015 Elsevier B.V. All rights reserved.


Saha S.,Gujarat University | Goswami G.,Indian National Institute of Pharmaceutical Education and Research
Asian Pacific Journal of Tropical Medicine | Year: 2010

Objective: To investigate the gastroprotective activity of hydroalcoholic extract leaves of Ficus religiosa (F. religiosa) in different experimental models of gastric ulcer in rats. Methods: The hydroalcoholic extract leaves of F. religiosa were studied at two dose levels (250 and 500 mg/kg, oral) in rats against absolute ethanol (0.2 mL oral), aspirin (200 mg/kg) and pyloric ligation induced gastric ulcer. Ranitidine (50 mg/kg, oral) was used as a standard drug. Mean ulcer indices and oxidative stress were measured. Phytochemical tests and acute toxicity tests were also carried out. Results: Administration of F. religiosa to rats significantly decreased the ulcer index value when compared with the control treated group. Ranitidine (50 mg/kg, oral) also produced a significant decrease the ulcer index value when compared with the control treated group. Phytochemical analysis revealed the presence of tannins, sterols, saponins, flavonoids, carbohydrates and proteins. Conclusions: The results suggest that the leaves of the F. religiosa possess significant anti ulcer activity. © 2010 Hainan Medical College.


Vadlamani S.,Indian National Institute of Pharmaceutical Education and Research
Research Journal of Pharmaceutical, Biological and Chemical Sciences | Year: 2015

Statins are used widely for the treatment of hypercholesterolemia [5]. They inhibit HMG-CoA reductase competitively; reduce LDL levels more than other cholesterol-lowering drugs, and decrease triglyceride levels in hypertriglyceridemic patients. In this review current status of statins, structure and their role and applications is briefly discussed.


Dokania S.,Indian National Institute of Pharmaceutical Education and Research | Joshi A.K.,Indian National Institute of Pharmaceutical Education and Research
Drug Delivery | Year: 2015

Self-microemulsifying drug delivery system (SMEDDS) has emerged as a vital strategy to formulate poor water soluble compounds for bioavailability enhancement. However, certain limitations are associated with SMEDDS formulations which include in vivo drug precipitation, formulation handling issues, limited lymphatic uptake, lack of predictive in vitro tests and oxidation of unsaturated fatty acids. These limitations restrict their potential usage. Inclusion of polymers or precipitation inhibitors within lipid based formulations helps to maintain drug supersaturation after dispersion. This, thereby, improves the bioavailability and reduces the variability on exposure. Also, formulating solid SMEDDS helps to overcome liquid handling and stability problems. Usage of medium chain triglycerides (MCT) and suitable antioxidants to minimize oxidation of unsaturated fatty acids are few of the steps to overcome the limitations associated with SMEDDS. The review discussed here, in detail, the limitations of SMEDDS and suitable measures that can be taken to overcome them. © 2014 Informa Healthcare USA, Inc.


Patel N.K.,Indian National Institute of Pharmaceutical Education and Research | Ramandeep,Indian National Institute of Pharmaceutical Education and Research | Bhutani K.K.,Indian National Institute of Pharmaceutical Education and Research
Natural Product Communications | Year: 2014

In the continuous search for new antiinflammatory agents from natural products, dichloromethane (DCM), ethyl acetate (EtOAc) and methanol (MeOH) extracts of Ipomea fistulosa leaves were evaluated for inhibition of production of nitric oxide (NO), interleukin 1beta (IL-1β) and tumor necrosis factor alpha (TNF-a) in lipopolysaccharide (LPS) stimulated J774A.1 cells. Among the tested extracts, the ethyl acetate (EtOAc) extract was found to be most active and activity based fractionation of this extract by column chromatography led to the identification of seven compounds for the first time from this plant. Furthermore, 3,4-dimethoxy cinnamic acid (1) exhibited two folds more potent inhibition of LPS-induced NO production (IC50 = 10.7 μg/mL) as compared with the standard, L-NAME (IC50=19.8 μg/mL). The present study supports the use of Ipomea fistulosa leaves for the treatment of inflammation. Copyright © 2014 Natural Product Communciations Inc.


Patel N.K.,Indian National Institute of Pharmaceutical Education and Research | Pulipaka S.,Indian National Institute of Pharmaceutical Education and Research | Dubey S.P.,Indian National Institute of Pharmaceutical Education and Research | Bhutani K.K.,Indian National Institute of Pharmaceutical Education and Research
Natural Product Communications | Year: 2014

The anti-inflammatory and cytotoxic activity of thirty-six extracts of nine Indian medicinal plants were determined by measuring the inhibition of production of nitric oxide (NO), interleukin 1beta (IL-1β) and tumor necrosis factor alpha (TNF-α) in lipopolysaccharide (LPS) stimulated RAW 264.7 cells. Their cytotoxic activity against macrophages was determined by MTT assay. The ethyl acetate (EtOAc) extract of Cassia occidentalis L. (roots) (IC50 = 21.3 to 43.1 μg/mL) and Mimosa pudica (whole plant) (IC50 = 31.7 to 47.2 μg/mL) and the dichloromethane (DCM) extract of Leucas cephalotes (whole plant) (IC50 = 46.8 to 49.3 μg/mL) exhibited significant anti-inflammatory activity by in vitro inhibition of the production of TNF-α, IL-1β and NO in LPS stimulated RAW 264.7 cells. Furthermore, the five compounds isolated from the ethyl acetate extract of Cassia occidentalis roots were found to suppress LPS-induced IL-1β, TNF-α and NO production in a concentration-dependent manner in these cells at IC50 values ranging from 22.5 to 97.4 μM. Emodin and chrysophanol were also found active in inhibiting pro-inflammatory cytokines in vivo. These findings justify an ethnopharmacological use of C. occidentalis roots as an effective herbal remedy for the treatment and prevention of inflammation and associated ailments.


Kumar D.,Indian National Institute of Pharmaceutical Education and Research | Sailaja Chirravuri S.V.,Indian National Institute of Pharmaceutical Education and Research | Shastri N.R.,Indian National Institute of Pharmaceutical Education and Research
International Journal of Pharmaceutics | Year: 2014

This study aims to evaluate the impact of surface area of silica particles on in vitro release of poorly soluble drug aceclofenac and their in vivo performances. Mesoporous silicas of different surface area and porosity were synthesized and characterized. Aceclofenac loaded silicas were prepared by solvent evaporation technique and characterized for surface area, pore size, DSC, FTIR and p-XRD. The dissolution efficiency (DE) of the mesoporous and nonporous silica was ∼2 times more than that of plain drug and marketed tablets in acidic discriminating media. A significant enhancement of 189% and 164% in oral bioavailability (AUC0-8) was observed for optimized aceclofenac loaded mesoporous formulation (MS11/72) and nonporous silica (NP), respectively, when compared to plain aceclofenac in male Wistar rats. However, no correlation could be established between the enhancements in their oral bioavailability and their corresponding surface area. The surface area of MS11/72 was 5 times more (∼1011 m2/g) when compared to NP (∼200 m2/g) and the enhancement in the oral bioavailability was only 1.15 times. This could be due to the limiting value of effective surface area of the drug available for in vitro dissolution beyond which, any further increase in surface area fails to improve the release rate or its bioavailability. © 2013 Elsevier B.V.


Mittal A.,Indian National Institute of Pharmaceutical Education and Research | Kumar N.,Indian National Institute of Pharmaceutical Education and Research
Pharmaceutical Research | Year: 2012

Purpose: A new, injectable, drug-loaded composite graft was developed to enable infection free wound healing. Methods: The graft was fabricated using gentamicin and biomimetic microparticulate scaffolds in gelatin gel and characterized for biologically relevant properties like fluid uptake, evaporative water loss (EWL), water vapor transmission rate (WVTR), Young's modulus and degradation. It was evaluated for drug release, cytocompatibility and antimicrobial efficacy against Staphylococcus aureus and Pseudomonas aeruginosa. Results: Graft exhibited fluid uptake of 13.79%, EWL of 60-70% in 10 h, WVTR of 5480.31 g/m2/d, and Young's modulus as 2.1-10.8 kPa. It exhibited 99.36% degree of crosslinking and a dual degradation behavior wherein, the carrier gel, gelatin, degraded rapidly leaving the microparticulate scaffolds intact. Drug release studies showed a sustained release of gentamicin for 13 days sufficient to inhibit the infection at the wound site. Cytocompatibility assessment of the graft revealed that graft supported cell adhesion, proliferation and migration. The antibacterial efficacy of the graft was assessed using Kirby-Bauer method and time kill assay, wherein results indicated a quick, effective (≥5-log reduction in CFU/ml) and long lasting antimicrobial effect. Conclusions: These results as a whole indicate that the graft represents an effective alternative for infection-free healing of full thickness wounds. [Figure not available: see fulltext.] © 2012 Springer Science+Business Media, LLC.


Karmase A.,Indian National Institute of Pharmaceutical Education and Research | Birari R.,Indian National Institute of Pharmaceutical Education and Research | Bhutani K.K.,Indian National Institute of Pharmaceutical Education and Research
Phytomedicine | Year: 2013

The study was carried out to investigate the anti-obesity effects of Aegle marmelos leaves extracts and its phytochemical constituents in vitro and in vivo. The dichloromethane (DCM), ethyl acetate (EtOAc) and n-butanol extracts of A. marmelos leaves were studied for their lipolytic effect. Lipolysis was measured by determining the amount of glycerol released at 12 h and 24 h at 50 μg/ml and 100 μg/ml concentrations. Phytochemical investigation of the most active DCM extract yielded 14 compounds. The isolated compounds were evaluated for their lipolytic effects at 50 μM and 100 μM. The most active compounds, umbelliferone and esculetin were further screened for their antiobesity effects in vivo in the high fat diet (HFD) induced obese rat model. Umbelliferone and esculetin reduced body weight, total triglyceride (TG), total cholesterol (TC) and glucose level in their respective HFD groups. A. marmelos DCM extract and compounds isolated from it have the potential of counteracting the obesity by lipolysis in adipocytes. © 2013 Elsevier GmbH. All rights reserved.

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