PCP 共聚物接枝 RGD 可提高 RGD-PCP 胶束进入细胞的内化速率。

PCP copolymers grafted with RGD enhance the rates of RGD-PCP micelles internalized into cells.

机构信息

Department of Chemical Engineering, National Yunlin University of Science and Technology, Tou-Liu, Yunlin, 640 Taiwan, ROC.

出版信息

J Microencapsul. 2010;27(6):514-20. doi: 10.3109/02652048.2010.484104.

DOI:10.3109/02652048.2010.484104

PMID:20560874

Abstract

RGD-PCP copolymers were fabricated by grafting Arg-Gly-Asp (RGD) peptide to poly(epsilon-caprolactone)-b-chitooligosaccharide-b-poly(ethylene glycol) (PCP) copolymers and the rate of internalization of RGD-PCP micelles by PC 12 cells were examined. Increasing intensity of the absorbance of amine groups in FT-IR spectra of RGD-PCP copolymers compared with those of PCP copolymers indicated the presence of RGD in new copolymers. Moreover, the grafting efficiency and molar ratio of RGD peptides to PCP copolymers were 88.2% and 0.45, respectively, analysed with HPLC. The RGD-PCP copolymers self-assemble to micelles at the critical micelle concentration (CMC) of 0.018 wt% (178 mg L(-1)) and with a mean diameter of 90 nm using a dynamic light-scattering (DLS) analyser. Interestingly, the internalization of DPH-loaded RGD-PCP micelles into PC 12 cells is much faster (e.g. within 5 min) than that of PCP micelles. The new RGD-PCP micelles may potentially be used in cellular drug delivery.

摘要

RGD-PCP 共聚物是通过将 Arg-Gly-Asp（RGD）肽接枝到聚（ε-己内酯）-b-壳寡糖-b-聚（乙二醇）（PCP）共聚物上制备的，研究了 RGD-PCP 胶束被 PC12 细胞内化的速率。与 PCP 共聚物相比，RGD-PCP 共聚物的傅里叶变换红外（FT-IR）光谱中胺基团的吸光度强度增加，表明新共聚物中存在 RGD。此外，采用高效液相色谱（HPLC）分析，接枝效率和 RGD 肽与 PCP 共聚物的摩尔比分别为 88.2%和 0.45。RGD-PCP 共聚物在临界胶束浓度（CMC）为 0.018wt%（178mg/L）下自组装成胶束，使用动态光散射（DLS）分析仪，平均粒径为 90nm。有趣的是，DPH 负载的 RGD-PCP 胶束进入 PC12 细胞的内化速度比 PCP 胶束快得多（例如在 5 分钟内）。新型 RGD-PCP 胶束可能有望用于细胞药物递送。