Time filter

Source Type

Gurunath S.,Vaagdevi Institute of Pharmaceutical science | Pradeep Kumar S.,Vaagdevi Institute of Pharmaceutical science | Patil P.A.,Vaagdevi Institute of Pharmaceutical science
Journal of Pharmacy Research | Year: 2013

Amorphous solid dispersions are one of the most promising strategies to improve the oral bioavailability of sparingly water-soluble drugs. Drug particle size reduction improved the drug wettability and bioavailability significantly. Poorly soluble drugs may benefit from formulation approaches that overcome poor solubility and dissolution rate limited bioavailability. The solubility of a compound in the amorphous form is higher than the more stable crystalline form because the Gibbs free energy is higher. In addition, glasses or amorphous forms are kinetically trapped high energy disordered materials that lack the periodicity of crystals but behave mechanically as solids. Lipophilic molecules, especially those belonging to the biopharmaceutics classification system (BCS) class II and IV, dissolve slowly, like incomplete release from the dosage form, poor bioavailability, increased food effect, and high inter-patient variability. Hence, several formulation approaches can be taken to improve the solubility and dissolution of poorly water-soluble compounds, such as formulating the API in an amorphous form. Amorphous solid dispersions of poorly water-soluble drugs with water-soluble carriers have been reduced the incidence of these problems and enhanced dissolution. This review is mainly focus on advantages, methods of preparation, and characterization of the amorphous solid dispersion. © 2013, JPR Solutions; Published by Reed Elsevier India Pvt. Ltd.


Gurunath S.,Vaagdevi Institute of Pharmaceutical science | Patil P.A.,KLE University
Drug Development and Industrial Pharmacy | Year: 2015

Objective: The aim of the study is to explore the pharmacokinetic behavior of candesartan solid dispersions prepared by different pharmaceutical interventions using P-gp inhibitor in rabbits to validate the effectiveness of naringin as a pharmaceutical excipient in enhancing the oral delivery of lipophilic candesartan cilexetil. Methods: Male albino rabbits (1-1.5kg) were orally administered pure CAN suspensions and various candesartan solid dispersions (10mg/kg) with and without naringin (15mg/kg) and blood samples were collected at specified time points. CAN plasma samples were measured using HPLC. Key findings: After oral dosing of pure CAN suspension, the mean AUC0-8h was found to be 0.14±0.09μgh/ml which was increased significantly, i.e. 0.52±0.13μgh/ml with freeze-dried solid dispersions in the presence of naringin (p<0.01). Similarly, the mean Cmax of pure CAN suspension increased from 35.81±0.13μg/ml (without naringin) to 112.23±0.13μg/ml (freeze-dried solid dispersions with naringin) (p<0.01). A 3.7-folds increase in apparent bioavailability was noticed with freeze-dried solid dispersions with naringin as compared to free CAN suspension administered alone. Conclusion: These results are quite stimulating for further development of a clinically useful oral formulation of candesartan cilexetil based on P-gp inhibition using naringin, a natural flavonoid as a pharmaceutical excipient. © 2015 Informa Healthcare USA, Inc. All rights reserved.


Prasad D.K.,Vaagdevi Institute of Pharmaceutical science | Prasad D.K.,Pacific University at Udaipur | Sriharsha S.N.,Pacific University at Udaipur
International Journal of Pharmacy and Technology | Year: 2015

This study was designed to investigate the effect of Murraya Koeinigii (MK) extracts in several neuropharmacological experimental models like General behavioral tests, motor coordination activity and locomotor activity, anxiolytic activity like Light-dark model transition, Cognitive activity by Morris water maze spatial navigation, antidepressant activity like Forced Swim Test (FST) and Tail Suspension Test (TST), antiepileptic activity by INH Induced epilepsy and antistress activity by Restraint stress (RS) model. The extracts dose was identified by using acute toxicity studies and determined for activity. The optimum safe concentration was 50, 100 and 200 mg/kg body weight for the methanol (ME), Hydro alcoholic (HE) and Aqueous (AQE) extracts of MK. The effective dose in all the extracts are MEMK, HEMK, is 200mg/kg. & Hydroalcholic extract is found to be more effective. The Hydro alcoholic extract had shown better results than other extracts. Hydroacohlic fraction showed a significant (#p<0.05) decrease in immobility time in FST. The results were comparable to those of fluoxetine. Moreover it also showed significant (#p<0.05) reduction in spontaneous locomotor activity and significant facilitation of learning and memory which may be due to enhanced cholinergic function. They have been shown to possess significant reduction of DPPH radicals can be observed by decreases in absorbance at 517 nm. That indicates acts an antioxidant activity due to amount of phenolic compounds present in extracts. That indicates acts an antioxidant activity. The presence of more percentage of Alkaloids and phytosterols, it showed better Neuropharmacololgical activity and can be infered that the content in extracts is responsible for the activity. © 2015, International Journal of Pharmacy and Technology. All rights reserved.


Behera A.,Vaagdevi Institute of Pharmaceutical science | Srikanth P.,Vaagdevi Institute of Pharmaceutical science | Rao Y.M.,Vaagdevi Institute of Pharmaceutical science | Sahoo S.K.,Utkal University
Immunology, Endocrine and Metabolic Agents in Medicinal Chemistry | Year: 2016

In the present day scenario, even if many advances in diabetic therapy have been sought, but it is still in its formative years. Nanotechnology has brought a range of novel promises into biological discovery and medical practice. Nanoparticulate drug delivers have revolutionized drug delivery, allowing therapeutic agents to be selectively targeted for organs, tissues and cell specific levels, minimizing exposure of healthy tissues to drugs. Keeping all the views in mind, Glimepiride loaded PLGA nanoparticles (NPs) were prepared by the solvent evaporation method. Physicochemical characterization of NPs included dynamic laser spectroscopy and atomic force microscopy confirmed the mean particle diameter of NPs was ~300 nm with spherical morphology. Fourier transform infrared spectroscopy and differential scanning calorimetry analysis depicted no interaction between the drug and polymer in formulation. Drug encapsulation efficiency was found to be ~55 % and it released from NPs in a sustained manner. Blood glucose level of glimepiride loaded NPs treated to diabetic rats was reduced significantly to normal level compared with native drug treated group. Thus, this system could facilitate to achieve a sustained formulation resulting in reduced dose frequency and improved patient compliance for type-2 diabetes mellitus management. © 2016 Bentham Science Publishers.


Surampalli G.,Vaagdevi Institute of Pharmaceutical science | Nanjwade B.K.,KLE University | Patil P.A.,Omer Al Mukhtar University
Journal of Pharmacy and Pharmacology | Year: 2015

Objective In this study, a comprehensive and comparative cytotoxic evaluation of morin against verapamil on rat intestinal epithelium as P-gp inhibitors through in-vitro gastrointestinal short-term toxicity assays involving permeability studies for safety evaluation was investigated. Methods In this study, the effect of morin (1 mM or 10 mM) or verapamil (1 mM or 10 mM) or sodium deoxycholate (10 mM) was investigated on intestinal epithelium and isolated brush border membrane using biomarker assays. Cytotoxicity was determined using 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay. The nutrients transport was assessed using everted sacs studies. Paracellular permeability was measured using Lucifer yellow, followed by morphometric analysis of intestinal sacs. Key findings Our results indicated that morin was effective in maintaining cell viability with no significant changes (P > 0.05) in the activity of intestinal brush border markers, membrane integrity and morphometric analysis as compared with control. On the contrary, dramatic (P < 0.01) changes were noticed in the release of membrane markers, cell viability and surface characteristics of intestinal segments when treated with verapamil or sodium deoxycholate as compared with control or morin. Conclusions Our findings confirm that morin is non-toxic to rat intestinal epithelium against verapamil demonstrating the potential use of bioflavonoid as safe and novel pharmaceutical adjuvant as P-gp inhibitor. © 2015 Royal Pharmaceutical Society.


PubMed | KLE University, Vaagdevi Institute of Pharmaceutical science and Omer Al Mukhtar University
Type: Comparative Study | Journal: Drug delivery | Year: 2016

To assess the effect of naringenin on the intestinal biochemical composition, function and histology for gastrointestinal toxicity since it has not yet been adequately exploited for safety through standard assays.Here, we describe naringenin (1mM, 10mM and 100mM, respectively) or sodium deoxycholate (10mM) effects on isolated brush border membrane from intestinal segments with single pass intestinal perfusion using lactate dehydrogenase, alkaline phosphatase and protein assays. MTT assay was used for cytotoxicity studies. Everted gut sac studies were used for evaluating the transport of nutrients across the intestinal segments. Lucifer yellow was used for paracellular permeability, followed by histological changes and surface characteristic studies of intestinal sacs.The results indicated no significant alterations with naringenin, although significant (p<0.01) changes were noticed with sodium deoxycholate in the activity of the rat intestinal brush border associated enzymes such as LDH, followed by intact cell viability with marked decrease in the villi height of the intestinal segments.These observations indicate that naringenin was harmless upon exposure to rat gastrointestinal epithelium, clearly demonstrating the potential use of naturally occurring bioflavonoid as safe and novel pharmaceutical adjuvant in oral dosage forms as P-gp inhibitor.


PubMed | KLE University, Vaagdevi Institute of Pharmaceutical science and Omer Al Mukhtar University
Type: Journal Article | Journal: The Journal of pharmacy and pharmacology | Year: 2015

In this study, a comprehensive and comparative cytotoxic evaluation of morin against verapamil on rat intestinal epithelium as P-gp inhibitors through in-vitro gastrointestinal short-term toxicity assays involving permeability studies for safety evaluation was investigated.In this study, the effect of morin (1mM or 10mM) or verapamil (1mM or 10mM) or sodium deoxycholate (10mM) was investigated on intestinal epithelium and isolated brush border membrane using biomarker assays. Cytotoxicity was determined using 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay. The nutrients transport was assessed using everted sacs studies. Paracellular permeability was measured using Lucifer yellow, followed by morphometric analysis of intestinal sacs.Our results indicated that morin was effective in maintaining cell viability with no significant changes (P>0.05) in the activity of intestinal brush border markers, membrane integrity and morphometric analysis as compared with control. On the contrary, dramatic (P<0.01) changes were noticed in the release of membrane markers, cell viability and surface characteristics of intestinal segments when treated with verapamil or sodium deoxycholate as compared with control or morin.Our findings confirm that morin is non-toxic to rat intestinal epithelium against verapamil demonstrating the potential use of bioflavonoid as safe and novel pharmaceutical adjuvant as P-gp inhibitor.


PubMed | Vaagdevi institute of pharmaceutical science and Kakatiya University
Type: | Journal: Drug research | Year: 2016

Isradipine (ID), is an antihypertensive drug, having low oral bioavailability (15-24%) due to poor aqueous solubility (0.01mg/mL) and also hepatic first-pass metabolism. Among various approaches, Solid lipid nanoparticles (SLNs) were developed using stearic acid, glyceryl monostearate as lipid matrices for improving the oral bioavailability of ID. ID-SLNs were prepared by using hot homogenization followed by ultrasonication. The prepared SLNs were characterized for size, PDI, zeta potential (ZP), entrapment efficiency (EE) and drug content.


Prasad D.K.,Vaagdevi Institute of Pharmaceutical science | Spoorthy S.,Vaagdevi Institute of Pharmaceutical science
International Journal of Pharmacy and Technology | Year: 2015

Inflammation is a pathophysiological response of living tissue to injury that leads to local accumulation of plasmatic fluid and blood cells. In recent years, research is focused on existing molecules and their modifications in order to reduce their side effects and to explore their pharmacological and biological effects. Most of anti-inflammatory drugs exert their beneficial effect by inhibiting either release of lysosomal enzymes orstabilizing membrane. Isatin Spiropyrazoline is an endogenous compound and it has a wide variety of pharmacological activities like anticancer, anti-inflammatory, antifungal and antibacterial. Anti-inflammatory was evaluated in animal models with a doses of 75 and 150 mg/kg as a test doses and using diclofenac (0. 45mg/kg) as a standard. Anti-inflammatory activity by carrageenan induced rat paw edema and cotton pellet granuloma, respectively the % inhibition of paw volume and granuloma tissue. Synthetic test compound (ISP) shows high significant with (***p<0. 001) level of inhibition against proteinases which is implicated in the development of inflammation which is further supported by the biochemical parameters SGPT, SGOT and ALP showed extremely significant(***P<0. 001),which helps to conclude the result that test compound able to reduce the enzyme activity which is the main cause of the inflammation. Inhibition of albumin denaturation and proteinase inhibitory activity, the test compound (ISP) showed anti-inflammatory activity with dose dependent effect when compared with the control group. In inflammatory condition 150mg/kg dose of the test drug possessed greater significance (***p<0. 001), the results of experimental findings suggest that ISP act as anti-inflammatory activity in the treatment of inflammation. © 2015, International Journal of Pharmacy and Technology. All rights reserved.


Pore D.,Medicinal Chemistry Research Division | Alli R.,Vaagdevi Institute of Pharmaceutical science | Prabhakar A.S.C.,Medicinal Chemistry Research Division | Alavala R.R.,Medicinal Chemistry Research Division | And 2 more authors.
Letters in Organic Chemistry | Year: 2012

Turmeric contains three important analogs, curcumin, demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC), collectively called as curcuminoids. Curcumin, the most abundant of these curcuminoids is reported to have antioxidant, anti-inflammatory, neuroprotective, antimicrobial, nematocidal, antimutagenic, anticarcinogenic, antiretroviral and chemopreventive activities. Curcumin (a symmetric β diketone) analogs 3a-e were synthesized from β-diketones and aromatic aldehydes using solid phase microwave irradiation method in presence of boric acid in diethanolamine, acetic acid (1:1) with reduced reaction time and enhanced %yield. Various clays like Alumina (neutral), Silica gel and Montmorillonite K 10 were used as solid phase catalysts where alumina was found to be efficient in the synthesis of curcumin analogs. © 2012 Bentham Science Publishers.

Loading Vaagdevi Institute of Pharmaceutical science collaborators
Loading Vaagdevi Institute of Pharmaceutical science collaborators