title: Preparation of sodium cholate-based micelles through non-covalent ıbonding interaction and application as oral delivery systems for paclitaxel.
abstract: In present study, two types of micelles based on sodium cholate (NaC) were prepared through non-covalent bonding interaction and the potential of micelles as oral drug delivery systems for paclitaxel (PTX) was evaluated. Pluronic-chitosan (F127-CS) and Pluronic-poly (acrylic acid) (F127-PAA) copolymers were synthesized. Electrostatic interaction and hydrogen bond were used to prepare F127-CS/NaC micelles and F127-PAA/NaC micelles, respectively. The physicochemical characteristics of micelles were determined. An average diameter of 67.5 nm and unimodal pattern of size distribution were observed for F127-CS/NaC micelles. While for F127-PAA/NaC micelles, an average diameter of 85.89 nm and non-unimodal pattern of size distribution were observed. The results revealed that F127-CS/NaC micelles were more integrated than F127-PAA/NaC micelles. Further experiments showed that the F127-CS/NaC micelles had a higher drug-loading content of 12.8% and a lower critical micelle concentration (CMC) of 2.5 × 10-3mol/L compared with F127-PAA/NaC micelles. In vitro cytotoxicity analysis demonstrated that the PTX-loaded F127-CS/NaC micelles were of great efficiency in inhibiting the growth of drug-resistant breast cancer MCF-7 cells (MCF-7/Adr). The intragastric administration of the PTX-loaded F127-CS/NaC micelles in rats provided a 4.33-fold higher absolute bioavailability compared to commercial Taxol®, indicating an efficient oral absorption of PTX delivered by micelles. These findings signify that F127-CS/NaC micelle may be a promising carrier for the delivery of PTX.
authors: a Department of Pharmaceutics , School of Pharmacy, Shandong University , Jinan , Shandong Province , China.
authors: Yanxiu
authors: Y
authors: Ge
authors: a Department of Pharmaceutics , School of Pharmacy, Shandong University , Jinan , Shandong Province , China.
authors: Yanli
authors: Y
authors: Zhao
authors: a Department of Pharmaceutics , School of Pharmacy, Shandong University , Jinan , Shandong Province , China.
authors: Lingbing
authors: L
authors: Li
mesh_terms: D000179:Acrylates / Q000138:chemical synthesis* / Q000737:chemistry; D000818:Animals; D001682:Biological Availability; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D048271:Chitosan / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D005260:Female; D006801:Humans; D061986:MCF-7 Cells; D008823:Micelles; D017239:Paclitaxel / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D020358:Sodium Cholate / Q000737:chemistry*
chemical_list: D000179:Acrylates; D008823:Micelles; C000615932:Pluronic-poly(acrylic acid); C000615952:pluronic-chitosan; D048271:Chitosan; D020358:Sodium Cholate; D017239:Paclitaxel
keywords: Non-covalent interaction; Pluronic F127; oral absorption; paclitaxel; sodium cholate