Enantiomeric PLA–PEG block copolymers and their stereocomplex micelles used as rifampin delivery

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• 作者：Li Chen ; Zhigang Xie ; Junli Hu ; Xuesi Chen and Xiabin Jing
• 关键词：PLLA–PEG ; PDLA–PEG ; stereocomplex ; micelle ; rifampin ; drug delivery ; controlled release ; nanobiomedicine ; nanotechnology
• 刊名：Journal of Nanoparticle Research
• 出版年：2007
• 出版时间：October, 2007
• 年：2007
• 卷：9
• 期：5
• 页码：777-785
• 全文大小：301 KB
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Nanotechnology
  Inorganic Chemistry
  Characterization and Evaluation Materials
  Physical Chemistry
  Applied Optics, Optoelectronics and Optical Devices
  
• 出版者：Springer Netherlands
• ISSN：1572-896X

文摘

A novelty approach to self-assembling stereocomplex micelles by enantiomeric PLA–PEG block copolymers as a drug delivery carrier was described. The particles were encapsulated by enantiomeric PLA–PEG stereocomplex to form nanoscale micelles different from the microspheres or the single micelles by PLLA or PDLA in the reported literatures. First, the block copolymers of enantiomeric poly(l-lactide)–poly(ethylene–glycol) (PLLA–PEG) and poly(D-lactide)–poly(ethylene–glycol) (PDLA–PEG) were synthesized by the ring-opening polymerization of l-lactide and d-lactide in the presence of monomethoxy PEG, respectively. Second, the stereocomplex block copolymer micelles were obtained by the self-assembly of the equimolar mixtures of enantiomeric PLA–PEG copolymers in water. These micelles possessed partially the crystallized hydrophobic cores with the critical micelle concentrations (cmc) in the range of 0.8–4.8 mg/l and the mean hydrodynamic diameters ranging from 40 to 120 nm. The micelle sizes and cmc values obviously depended on the hydrophobic block PLA content in the copolymer. Compared with the single PLLA–PEG or PDLA–PEG micelles, the cmc values of the stereocomplex micelles became lower and the sizes of the stereocomplex micelles formed smaller. And lastly, the stereocomplex micelles encapsulated with rifampin were tested for the controlled release application. The rifampin loading capacity and encapsulation efficiency by the stereocomplex micelles were higher than those by the single polymer micelles, respectively. The drug release time in vitro was depending on the composites of the block copolymers and also could be controlled by the polymer molecular weight and the morphology of the polymer micelles.