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.
Texto completo:
1
Base de dados:
WPRIM
Assunto principal:
Polietilenoglicóis
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Propilenoglicóis
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Bile
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Transporte Biológico
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Camptotecina
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Portadores de Fármacos
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Farmacocinética
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Células Cultivadas
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Química
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Ratos Sprague-Dawley
Limite:
Animals
Idioma:
Zh
Revista:
Yao Xue Xue Bao
Ano de publicação:
2012
Tipo de documento:
Article