[Preparation and characterization of irinotecan hydrochloride loaded PEO-PPO-PEO micelles and its mechanism of decreasing drug intestinal toxicity].

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.
Authors	Xin-Xin Zhang, Shi-Yan Guo, Fei-Fei Li, Yong Gan
Journal	Yao xue xue bao = Acta pharmaceutica Sinica (Yao Xue Xue Bao) Vol. 47 Issue 11 Pg. 1534-40 (Nov 2012) ISSN: 0513-4870 [Print] China
PMID	23387089 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	ABCG2 protein, human ATP Binding Cassette Transporter, Subfamily G, Member 2 ATP-Binding Cassette Transporters Antineoplastic Agents, Phytogenic Drug Carriers Micelles Neoplasm Proteins PEO-PPO-PEO Propylene Glycols Polyethylene Glycols Irinotecan Camptothecin
Topics	ATP Binding Cassette Transporter, Subfamily G, Member 2 ATP-Binding Cassette Transporters (metabolism) Animals Antineoplastic Agents, Phytogenic (administration & dosage, adverse effects, pharmacokinetics) Bile (metabolism) Biological Transport Camptothecin (administration & dosage, adverse effects, analogs & derivatives, pharmacokinetics) Cells, Cultured Diarrhea (chemically induced, drug therapy) Dogs Drug Carriers Intestines (drug effects) Irinotecan Madin Darby Canine Kidney Cells Male Micelles Neoplasm Proteins (metabolism) Polyethylene Glycols (administration & dosage, chemistry) Propylene Glycols (administration & dosage, chemistry) Rats Rats, Sprague-Dawley

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