Optimization and charaterization of repaglinide biodegradable polymeric nanoparticle loaded transdermal patchs: In vitro and in vivo studies

• Published in: Colloids and surfaces, B, Biointerfaces Vol. 111; pp. 150 - 155
• Main Authors: Vijayan, V., Reddy, K. Ravindra, Sakthivel, S., Swetha, C.
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01-11-2013
• Subjects: Animals; Bioavailability; Biocompatibility; Biocompatible Materials - chemistry; biodegradability; Biological Availability; Biomedical materials; Blood Glucose - metabolism; Carbamates - pharmacology; chitosan; colloids; drugs; equations; Ex vivo; In vitro release; In Vitro Techniques; In vitro testing; in vivo studies; In vivo testing; In vivo tests; Insulin - blood; Kinetics; Lactic Acid - chemistry; Nanoparticles; Nanoparticles - chemistry; Nanoparticles - ultrastructure; oral administration; Particle Size; Permeability - drug effects; Piperidines - pharmacology; Polyesters; Polymeric nanoparticle; Polymers - chemistry; Rats, Wistar; Repaglinide; Skin Absorption - drug effects; solvents; Spectroscopy, Fourier Transform Infrared; Surgical implants; Transdermal Patch; zeta potential; Polymeric nanoparticle; Repaglinide; In vitro release; Ex vivo
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2013.05.020

•Repaglinide-PLA polymeric nanoparticle prepared by solvent evaporation method.•Optimized nanoparticle formulation was incorporated in Methocel transdermal patch.•Nanopatch was evaluated by physiochemical, in vitro, ex vivo and in vivo studies.•The in vivo hypoglycemic effect was observed in diabetes rats.•The nanopatch may use to control glucose level over a week period.
Biodegradable polymeric nanoparticles loaded Repaglinide were prepared by solvent extraction method. In this method chitosan, PLA and PCL were employed to prepare Repaglinide polymeric nanoparticles. Some of the formulation parameters were optimized to obtain high quality nanoparticles. The particles were spherical shape with sizes of 108.6±3.4nm to 220.6±1.2nm and the poly dispersity indexes were in the range of 0.06 to 0.44. The zeta potential was in the range between – 16.48±2.02 and 30.52±3.20mV. The percentage entrapment efficiency (EE%) was 81.4±1.8% to 92.7±1.4%. The drug release behavior was studied by externally sink method and the release pattern of drug was found to follow zero order, Higuchi and Peppas equations. The optimized PLA-Repaglinide nanoparticles were loaded in Methocel transdermal patches. These transdermal patches were evaluated by physiochemical parameters, in vitro, ex vivo and in vivo studies. Based on in vivo hypoglycemic results, bioavailability parameters like AUC, AUMC, Cmax, Tmax, MRT, t1/2and relative bioavailability were found to be 2218.88μIU/mL/h, 381630.3μIU/mL/h, 41.88μIU/mL, 36h, 83.24h, and 52.79h respectively. The transdermal patch containing Repaglinide nanoparticles showed 76 fold effective than conventional oral administrations.