RESUMO
AIM: The present work investigates the efficacy of Polysorbate 80(P80) coated Kokum butter (KB) solid lipid nanoparticles (P80NvKLNs) for the brain targeted delivery of Nevirapine (Nv). METHODS: Solid lipid nanoparticles (SLNs) were prepared by nanoprecipitation technique and evaluated for drug excipient compatibility studies, z- average particle size (nm), zeta potential (mv), percentage drug entrapment efficiency (%EE), surface morphology and in-vitro drug release properties. The in-vivo biodistribution and brain targeting efficiency of nanoparticles were studied in healthy male Wistar rat (150-200 g). RESULTS: P80NvKLNs were found to be smooth surfaced, spherical shaped having average particle size of 177.80 ± 0.82 nm, zeta potential of -8.91 ± 4.36 mv and %EE of 31.32 ± 0.42%. P80NvKLNs remained in blood circulation for 48 h maintaining a sustained release in brain for 24 h (p < 0.05). CONCLUSION: The study proves the efficacy of Polysorbate 80 coated Kokum butter nanoparticles for brain-targeted delivery of drugs providing ample opportunities for further study.
Assuntos
Fármacos Anti-HIV/farmacocinética , Encéfalo/metabolismo , Preparações de Ação Retardada/química , Garcinia/química , Lipídeos/química , Nanopartículas/química , Nevirapina/farmacocinética , Complexo AIDS Demência/tratamento farmacológico , Complexo AIDS Demência/etiologia , Complexo AIDS Demência/metabolismo , Síndrome da Imunodeficiência Adquirida/complicações , Síndrome da Imunodeficiência Adquirida/tratamento farmacológico , Síndrome da Imunodeficiência Adquirida/metabolismo , Animais , Fármacos Anti-HIV/administração & dosagem , Preparações de Ação Retardada/metabolismo , Sistemas de Liberação de Medicamentos , Metabolismo dos Lipídeos , Masculino , Nanopartículas/metabolismo , Transtornos Neurocognitivos/tratamento farmacológico , Transtornos Neurocognitivos/etiologia , Transtornos Neurocognitivos/metabolismo , Nevirapina/administração & dosagem , Polissorbatos/química , Polissorbatos/metabolismo , Ratos Wistar , Propriedades de Superfície , Distribuição TecidualRESUMO
The present work envisages utilisation of biodegradable and biocompatible material from natural sources for the development of controlled release microspheres of metformin hydrochloride (MetH). Natural polysaccharides extracted from Dillenia indica L. (DI), Abelmoschus esculentus L. (AE) and Bora rice flour were used in fabricating controlled release microspheres. The microspheres were prepared by the emulsion solvent diffusion technique with different proportions of natural materials and were studied for entrapment efficiency, particle size, particle shape, surface morphology, drug excipient compatibility, mucoadhesivity and in vitro release properties. The prepared microspheres showed mucoadhesive properties and controlled release of metformin hydrochloride. The study has revealed that natural materials can be used for formulation of controlled release microspheres and will provide ample opportunities for further study.