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Preparation and characterization of irinotecan hydrochloride loaded PEO-PPO-PEO micelles and its mechanism of decreasing drug intestinal toxicity / 药学学报
Yao Xue Xue Bao ; (12): 1534-1540, 2012.
Article em Zh | WPRIM | ID: wpr-274626
Biblioteca responsável: WPRO
ABSTRACT
In this work, we developed PEO-PPO-PEO micelles loaded with irinotecan hydrochloride (CPT-11) using breast cancer resistance protein (BCRP) inhibitory material PEO20-PPO70-PEO20, and studied its mechanism of decreasing CPT-11 induced delayed diarrhea and intestinal toxicity. BCRP-overexpressing MDCKII (MDCKII/BCRP) cells were used to evaluate the effect of PEO20-PPO70-PEO20 and PEO-PPO-PEO micelles on transmembrane transport of CPT-11 in vitro. The biliary excretion, delayed diarrhea and intestinal damage of CPT-11 loaded PEO-PPO-PEO micelles of rats were investigated. The results showed that the obtained micelles could decrease the biliary excretion of CPT-11, ameliorate delayed diarrhea and intestinal toxicity of rats through inhibiting BCRP-mediated CPT-11 efflux. PEO-PPO-PEO micelles were promising carriers to reduce intestinal toxicity of CPTs.
Assuntos
Texto completo: 1 Base de dados: WPRIM Assunto principal: Polietilenoglicóis / Propilenoglicóis / Bile / Transporte Biológico / Camptotecina / Portadores de Fármacos / Farmacocinética / Células Cultivadas / Química / Ratos Sprague-Dawley Limite: Animals Idioma: Zh Revista: Yao Xue Xue Bao Ano de publicação: 2012 Tipo de documento: Article
Texto completo: 1 Base de dados: WPRIM Assunto principal: Polietilenoglicóis / Propilenoglicóis / Bile / Transporte Biológico / Camptotecina / Portadores de Fármacos / Farmacocinética / Células Cultivadas / Química / Ratos Sprague-Dawley Limite: Animals Idioma: Zh Revista: Yao Xue Xue Bao Ano de publicação: 2012 Tipo de documento: Article