title: Folate-modified pluronic-polyethylenimine and cholic acid polyion complex micelles as targeted drug delivery system for paclitaxel.
abstract: The aim of the present study is to construct a type of polyion complex micelles made of PF127-PEI copolymer and cholic acid (CA) and to evaluate the potential of this type of micelles as a targeted drug delivery system for paclitaxel (PTX). To further improve the targeting capability of micelles, folate was also incorporated into micelles. The characteristics and anti-tumour activity in vitro were investigated. Enhanced solubility of PTX was achieved by incorporating into the micelles. The capability of the polyion complex micelles containing rhodamine 123 to increase the level of intracellular delivery was also observed using fluorescence microscopy. The cytotoxicity of PTX-loaded micelles against cancer cell in vitro was remarkably higher than that of free drug and was better when folate was incorporated into the micelles. These properties such as specificity towards the folate receptor and the low toxicity render folate-modified polyion complex micelles promising candidate for targeted PTX delivery.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Shandong University , Jinan , China.
authors.forename: Yimu
authors.initials: Y
authors.lastname: Li
authors.forename: Yi
authors.initials: Y
authors.lastname: Zhou
authors.forename: Bai
authors.initials: B
authors.lastname: De
authors.forename: Lingbing
authors.initials: L
authors.lastname: Li
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology; D019826:Cholic Acid / Q000737:chemistry / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods*; D005492:Folic Acid / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D008823:Micelles; D017239:Paclitaxel / Q000737:chemistry / Q000494:pharmacology; D020442:Poloxamer / Q000737:chemistry / Q000494:pharmacology; D011094:Polyethyleneimine / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D008823:Micelles; D020442:Poloxamer; D011094:Polyethyleneimine; D005492:Folic Acid; D019826:Cholic Acid; D017239:Paclitaxel
keywords: Drug delivery system; folate modified; paclitaxel; pluronic-polycationic polymer; polyion complex micelles