Preparation and characterization of irinotecan hydrochloride loaded PEO-PPO-PEO micelles and its mechanism of decreasing drug intestinal toxicity / 药学学报
Acta Pharmaceutica Sinica
; (12): 1534-1540, 2012.
Article
ي Zh
| WPRIM
| ID: wpr-274626
المكتبة المسؤولة:
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.
النص الكامل:
1
الفهرس:
WPRIM
الموضوع الرئيسي:
Polyethylene Glycols
/
Propylene Glycols
/
Bile
/
Biological Transport
/
Camptothecin
/
Drug Carriers
/
Pharmacokinetics
/
Cells, Cultured
/
Chemistry
/
Rats, Sprague-Dawley
المحددات:
Animals
اللغة:
Zh
مجلة:
Acta Pharmaceutica Sinica
السنة:
2012
نوع:
Article