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Int J Biol Macromol ; 152: 1224-1232, 2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-31751741

RESUMO

AIM: Brinzolamide (BNZ) is a carbonic anhydrase inhibitor commonly used for the treatment of glaucoma. The aim of this study was to prepare BNZ loaded chitosan-pectin mucoadhesive nanocapsules (CPNCs) by polyelectrolyte complex coacervation method for ocular delivery and evaluated for its anti glaucoma efficacy. METHODS: The prepared CPNCs were characterized for their particle size, polydispersity index, zeta-potential, surface morphology, entrapment efficiency, drug loading efficiency, mucoadhesive strength in-vitro and ex-vivo release. The pharmacodynamic studies were conducted for CPNCs on glaucoma induced rabbit eye model and compared with marketed product. RESULT AND DISCUSSION: All the formulated CPNCs exhibited the size range from 217.01 ± 0.21 to 240.05 ± 0.08 nm and appropriate physico-chemical parameters, and depicted a couple of erosion- diffusion release of BNZ over a time of 8 h. Ex-vivo corneal permeation study concluded that BNZ loaded CPNCs crosses the cornea potentially higher rate as compared to the marketed product. In pharmacodynamic study, greater intraocular pressure lowering effect was achieved by CPNCs as compared to marketed drug product. CONCLUSION: The result concluded that CPNCs are a feasible choice to conventional eye drops because of its ability to improve the bioavailability via its longer precorneal retention time and its ability to sustained release of the drug.


Assuntos
Quitosana/química , Glaucoma/tratamento farmacológico , Nanocápsulas/química , Pectinas/química , Sulfonamidas/química , Sulfonamidas/farmacologia , Tiazinas/química , Tiazinas/farmacologia , Animais , Disponibilidade Biológica , Inibidores da Anidrase Carbônica/química , Inibidores da Anidrase Carbônica/farmacologia , Córnea/efeitos dos fármacos , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Pressão Intraocular/efeitos dos fármacos , Nanopartículas/química , Soluções Oftálmicas/química , Soluções Oftálmicas/farmacologia , Tamanho da Partícula , Polieletrólitos/química , Polieletrólitos/farmacologia , Coelhos
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