紫杉醇两亲性共聚物纳米胶束体外释药动力学

采用低分子量PEG-PCL-PEG、mPEG-PLLA、mPEG-PDLLA等两亲性嵌段共聚物作载体包载紫杉醇形成纳米胶束.研究了不同载药率胶束在磷酸缓冲液中释放的动力学，发现紫杉醇PEG-PCL-PEG胶束和mPEG-PLLA胶束的体外释药遵从一级释放动力学；紫杉醇mPEG-PDLLA纳米胶束的体外释放多呈现出两段零级释放动力学；低载药率胶束表现出高释药率；体外释药过程中磷酸缓冲液的更新量越大，紫杉醇的释放率越高.

IN VITRO RELEASE KINETICS OF AMPHIPHILIC BLOCK COPOLYMER NANO-MICELLES LOADED WITH PACLITAXEL

Different kinds of amphiphilic block copolymers, PEG-PCL-PEG(PECL), mPEG-PLLA(PELLA) and mPEG-PDLLA(PEDLLA)，were used to encapsulate paclitaxel to prepare nano-micelle formulation. The nano-micelles had a core-shell structure,in which paclitaxel was enveloped in the core, and the PEG shell made the micelles loaded with paclitaxel lyotropic in water. The kinetics of paclitaxel release from the micelles in phosphate buffer solution(PBS) was studied.The results showed that the diameter of the micelles affected apparently drug release rate, and micelles with low drug loaded content(DLC) would release more paclitaxel; enhancing the refresh volume of PBS facilitated drugDK]’s release; both PECL micelle and PELLA micelle released paclitaxel in PBS under the rule of first order equation; PEDLLA micelles loaded with paclitaxel prepared by solid dispersion technology obeyed zero-order release in two stage.