两亲性无规聚合物P（MMA-co-MAA）胶束包覆紫杉醇及体外释放

Encapsulation and Release of Paclitaxel with Amphiphilic Random Polymer P（MMA-co-MAA） Micelles

摘要:

运用双亲性无规聚合物P（MMA-co-MAA）透析法制备了紫杉醇载药胶束。用芘荧光探针法测定双亲性聚合物的CMC值；对载药、空白的聚合物胶束的粒径、Zeta电位进行了比较；考察紫杉醇加入量对包覆率和载药量的影响；并在磷酸缓冲溶液（pH 7.4）中进行紫杉醇载药胶束模拟药物缓释研究。研究结果表明：两亲性无规聚合物P（MMA-coo-MAA）单体摩尔比7∶3的聚合物的CMC为0.050 mg/mL；载药胶束的粒径比空白胶束增大近两倍，Zeta电位变得更负；当紫杉醇加入量为21%时，包封率和载药量可分别达到85.2%、18.0%；载药胶束在pH 7.4磷酸缓冲液中140 h内可稳定释放，具有良好的缓释效果。

Abstract:

The amphiphilic random polymer P(MMA-co-MAA) micelle was firstly applied to encapsulate paclitaxel with dialysis method. Critical micelle concentration(CMC) of amphiphilic random polymer P(MMA-co-MAA) was measured using the fluorescent probe method. The Zeta potential and the size of polymeric micelles were measured to compare loading micelle with blank micelle. The influences of the amounts of paclitaxel on encapsulation efficiency and loading content were investigated. Drug release was also studied in a phosphate buffer solution (pH 7.4). The result showed CMC of P(MMA-co-MAA) was 0.050 mg/mL as the monomer ratio of the hydrophobic monomer MMA to the hydrophilic monomer MAA was 7∶3. The encapsulation efficiency and loading content were 85.2% and 18.0%, respectively, as the content of paclitaxel added in polymeric micelle was 21%. Once loading paclitaxel, polymeric micelle became about twice as big as the blank micelle; and Zeta potential became more negative. The loading micelles release paclitaxel stably in 140 hours in phosphate buffer, which revealed that the paclitaxel loading micelles had an effective sustained-release effect.