School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou 510640, People's Republic of China.
School of Bioscience and Bioengineering, South China University of Technology, Guangzhou 510640, People's Republic of China.
Nanoscale Res Lett. 2014 May 18;9(1):243. doi: 10.1186/1556-276X-9-243. eCollection 2014.
Amphiphilic A2(BC)2 miktoarm star polymers [poly(ϵ-caprolactone)]2-[poly(2-(diethylamino)ethyl methacrylate)-b- poly(poly(ethylene glycol) methyl ether methacrylate)]2 [(PCL)2(PDEA-b-PPEGMA)2] were developed by a combination of ring opening polymerization (ROP) and continuous activators regenerated by electron transfer atom transfer radical polymerization (ARGET ATRP). The critical micelle concentration (CMC) values were extremely low (0.0024 to 0.0043 mg/mL), depending on the architecture of the polymers. The self-assembled empty and doxorubicin (DOX)-loaded micelles were spherical in morphologies, and the average sizes were about 63 and 110 nm. The release of DOX at pH 5.0 was much faster than that at pH 6.5 and pH 7.4. Moreover, DOX-loaded micelles could effectively inhibit the growth of cancer cells HepG2 with IC50 of 2.0 μg/mL. Intracellular uptake demonstrated that DOX was delivered into the cells effectively after the cells were incubated with DOX-loaded micelles. Therefore, the pH-sensitive (PCL)2(PDEA-b-PPEGMA)2 micelles could be a prospective candidate as anticancer drug carrier for hydrophobic drugs with sustained release behavior.
两亲性 A2(BC)2 型星型嵌段聚合物 [聚(ε-己内酯)]2-[聚(2-(二乙氨基)乙基甲基丙烯酸酯)-b-聚(聚乙二醇甲醚甲基丙烯酸酯)]2 [(PCL)2(PDEA-b-PPEGMA)2] 是通过开环聚合 (ROP) 和连续引发剂再生电子转移原子转移自由基聚合 (ARGET ATRP) 的组合制备的。临界胶束浓度 (CMC) 值非常低 (0.0024 至 0.0043 mg/mL)，这取决于聚合物的结构。自组装的空和阿霉素 (DOX) 负载胶束呈球形，平均粒径约为 63 和 110 nm。在 pH 5.0 下，DOX 的释放速度比在 pH 6.5 和 pH 7.4 下快得多。此外，载 DOX 胶束能够有效抑制肝癌细胞 HepG2 的生长，IC50 为 2.0 μg/mL。细胞内摄取表明，细胞与载 DOX 胶束孵育后，DOX 被有效递送到细胞内。因此，具有 pH 敏感性的 (PCL)2(PDEA-b-PPEGMA)2 胶束可以作为具有持续释放行为的疏水性药物的潜在候选抗癌药物载体。
