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Ghāziābād, India

Gaur P.K.,Its Paramedical Pharmacy College | Gaur P.K.,Jodhpur National University | Purohit S.,IMS BHU | Mishra S.,Jamia Hamdard University
Journal of Biomaterials Science, Polymer Edition | Year: 2013

Context: Aceclofenac is an important NSAID; however, it causes GI disturbances whereas employing transdermal route would require permeation enhancer for systemic application, thereby causing skin damage. Ceramide 2 is a natural lipid having an important role in the maintenance of skin. Objective: Aceclofenac-loaded nanovesicles of ceramide-2, cholesterol, palmitic acid, and cholesteryl sulfate were formulated and analyzed for physical and biological properties. Materials and method: Film hydration method was used to prepare the vesicles and physical parameters, in vitro drug release and stability were evaluated. Then, they were formulated into gel and evaluated against a commercial formulation (CF) and gel-containing plain drug (CPG) for ex vivo, in vivo drug permeation, and anti-inflammatory activity. Results: The developed formulations showed best physical profile and ACV-1 gave 92.89% drug release in in vitro studies. Ex vivo studies showed drug permeation between 15.32-31.12 μg/cm2, whereas CPG and CF released 0.47 and 2.81 μg/cm 2, respectively. ACVG-1 and CF showed Cmax of 8.1 and 1.2 μg/ml at 8 and 4 h, respectively. ACVG-1 showed 11.6 times AUC than CF. ACVG-1 inhibited edema by 44% in first hour itself. Discussion: Ceramide 2 and palmitic acid played an important role in the formulation and promotes the drug permeation through stratum corneum and dermis. Ceramide content of the formulation also contributes towards stability and skin protection. Conclusion: The composition of the vesicle formulation performs an important role in physical properties and drug permeation, thereby producing an optimum formulation. © 2013 © 2013 Taylor & Francis.

Gaur P.K.,Its Paramedical Pharmacy College | Mishra S.,Jamia Hamdard University | Purohit S.,Banaras Hindu University
BioMed Research International | Year: 2013

Diclofenac sodium loaded solid lipid nanoparticles (SLNs) were formulated using guggul lipid as major lipid component and analyzed for physical parameters, permeation profile, and anti-inflammatory activity. The SLNs were prepared using melt-emulsion sonication/low temperature-solidification method and characterized for physical parameters, in vitro drug release, and accelerated stability studies, and formulated into gel. Respective gels were compared with a commercial emulgel (CEG) and plain carbopol gel containing drug (CG) for ex vivo and in vivo drug permeation and anti-inflammatory activity. The SLNs were stable with optimum physical parameters. GMS nanoparticle 1 (GMN-1) and stearic acid nanoparticle 1 (SAN-1) gave the highest in vitro drug release. Guggul lipid nanoparticle gel 3 (GLNG-3) showed 104.68 times higher drug content than CEG in receptor fluid. The enhancement ratio of GLNG-3 was 39.43 with respect to CG. GLNG-3 showed almost 8.12 times higher C max than CEG at 4 hours. The AUC value of GLNG-3 was 15.28 times higher than the AUC of CEG. GLNG-3 showed edema inhibition up to 69.47% in the first hour. Physicochemical properties of major lipid component govern the properties of SLN. SLN made up of guggul lipid showed good physical properties with acceptable stability. Furthermore, it showed a controlled drug release profile along with a promising permeation profile. © 2013 Praveen Kumar Gaur et al.

Gaur P.K.,Its Paramedical Pharmacy College | Mishra S.,Jamia Hamdard University | Aeri V.,Jamia Hamdard University
The Scientific World Journal | Year: 2014

Context. Most new drugs have low water solubility and liposome is an important formulation to administer such drugs; however, it is quite unstable and has negligible systemic absorption. Objective. Aceclofenac nanovesicles were made using guggul lipid for formulating stable transdermal formulation. Materials and Methods. Guggul lipid was formulated into vesicles along with cholesterol and dicetyl phosphate using film hydration method. The formulations were analyzed for physicochemical properties and stability. Then its skin permeation and anti-inflammatory activity were determined. Results. Both categories of vesicles (PC and GL) showed optimum physicochemical properties; however, accelerated stability study showed considerable differences. GL-1 was appreciably stable for over 6 months at 4°C. Corresponding gels (PCG-1 and GLG-1) showed Cmax values at 4.98 and 7.32 μg/mL along with the Tmax values at 4 and 8 hours, respectively. GLG-1 inhibited edema production by 90.81% in 6 hours. Discussion. PC liposomes are unstable at higher temperature and upon longer storage. The formulation with higher lipid content (GL-1) showed good drug retention after 24 hours and appreciable stability both at higher temperature and for longer duration. Guggul lipid being a planar molecule might be stacked in vesicle wall with cholesterol. Conclusion. The composition of the nanovesicle played an important role in stability and drug permeation. Guggul lipid is suitable for producing stable vesicles. © 2014 Praveen Kumar Gaur et al.

Gaur P.K.,Jodhpur National University | Gaur P.K.,Its Paramedical Pharmacy College | Purohit S.,IMS BHU | Kumar Y.,Its Paramedical Pharmacy College | And 2 more authors.
Drug Development and Industrial Pharmacy | Year: 2014

Context: The vesicles based on skin lipid have a drug localization effect and its main lipid, ceramide provides protective and regenerative effects while oleic acid (OA) is a penetration enhancer, however, it causes slight irritation, so we have formulated formulation incorporating both of these to develop a transdermal formulation for better permeation. Objective: Present study investigated the preparation and characterization of physicochemical properties and permeation of nanovesicles of ceramide-2 containing OA and palmitic acid (PA) respectively and a commercial gel. Materials and methods: The vesicles were made using ceramide 2, cholesterol (Chol), cholesteryl sulfate (CS) and OA or PA, respectively, using film hydration method. The vesicles were characterized for physicochemical properties, ex vivo permeation using human skin and pharmacokinetic parameters and anti-inflammatory activity in rats. Results: The vesicles showed size at 102-125nm while PDI was 0.11-0.13 and negative zeta potential. OV-3 showed highest entrapment efficiency. The drug fluxes were 92.02 and 8.920μg/cm2/h, respectively, for OV-3 and PV-1. The Cmax were 7.91 and 4.01μg/ml at 4 and 6h for OV-3 (2.5mg) and PV-1 (10mg), respectively. OV-3 and PV-1 showed 98.8% and 77.36% edema inhibition, respectively, at 3h. Discussion: Both formulations showed similar physical parameters and different permeation since OA get incorporated in vesicles and increases its permeability and ceramide makes sure that vesicles can rapidly traverse the stratum corneum. Conclusion: OV-3 containing 3% OA showed optimum physical parameters and good permeation with maximum anti-inflammatory activity. © 2014 Informa Healthcare USA, Inc. All rights reserved: reproduction in whole or part not permitted.

Gaur P.K.,Its Paramedical Pharmacy College | Gaur P.K.,Jodhpur National University | Purohit S.,IMS BHU | Kumar Y.,Its Paramedical Pharmacy College | Bhandari A.,Jodhpur National University
Artificial Cells, Nanomedicine and Biotechnology | Year: 2014

Lipid vesicles are an important drug carrier which can serve for controlled delivery of drugs; however, these vesicles are quite unstable at ambient temperature and require stringent storage condition. Present work was done to develop a stable vesicular system for drug delivery. Vesicles of ceramide-2, cholesterol, cholesterol sulfate, and palmitic acid were prepared and compared with phosphatidylcholine vesicles for physicochemical parameters and accelerated stability. Diclofenac sodium was used as a model drug. Based on physicochemical parameter and in vitro release PCV-3 and CV-3 were selected for further studies in three different accelerated stability conditions. PCV-3 showed moderate changes at 4°C but was severely affected at 25°C and 40°C. CV-3 showed stable characteristics at 4°C and 25°C whereas at 40°C, CV-3 showed signs of slight modification owing to moisture absorption. Based on the study, CV-3 containing highest content of palmitic acid was found to be most stable. © 2014 Informa Healthcare USA, Inc.

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