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shaped block copolymer (methoxypoly( ethylene glycol))(2)-b-poly(L-glutamic acid): preparation, self-assembly, and use as drug carriers

机译：嵌段共聚物（甲氧基聚（乙二醇））（2）-b-聚（L-谷氨酸）：制备，自组装和用作药物载体

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摘要

Y-shaped amphiphilic block copolymers, (methoxy-poly(ethylene glycol))(2)-block-poly(L-glutamic acid) ((mPEG)(2)-PGA) and its precursor (methoxy-poly(ethylene glycol)(2)-block-poly(gamma-benzyl-L-glutamate) ((mPEG)(2)-PBG), were prepared in three steps: (1) macroinitiator (methoxy-poly(ethylene glycol))(2)-NH2 ((mPEG)(2)-NH2) was synthesized by coupling two methoxy-poly(ethylene glycol)s with serinol and diisocyanate. (2) (mPEG)(2)-PBG was synthesized by ring opening polymerization of gamma-benzyl-l-glutamate-N-carboxyanhydride initiated with the macroinitiator ((mPEG)(2)-NH2); (3) the protective benzyl groups in (mPEG)(2)-PBG were removed to obtain (mPEG)(2)-PGA. The properties of both (mPEG)(2)-PBG and (mPEG)(2)-PGA were characterized by H-1 NMR, FT-IR, GPC, and DLS. In aqueous solution (mPEG)(2)-PBG tends to form more stable micelles compared to linear mPEG-PBG copolymer. The size of (mPEG)(2)-PBG decreases with increasing length of hydrophobic PBG in (mPEG)(2)-PBG. Paclitaxel and cisplatin were grafted onto (mPEG)(2)-PGA to form (mPEG)(2)-PGA-PTX (MPTX) with a grafting ratio of near 90% and (mPEG)(2)-PGA-Pt (MPt) conjugates with a loading efficacy of 15% (w/w). MPTX can greatly improve the solubility of PTX. Both conjugates can self-assemble into micelles with a mean diameter of about 50 nm and show enhanced anti-cancer activity against MCF-7, HeLa, and SMMC cell lines. The in vivo anticancer evaluation in mice shows MPt showed a desirable antitumor activity and allowed us to deduce the system toxicity. Therefore, both MPTX and MPt have a great potential as a polymer drug in cancer chemotherapy.
机译：Y形两亲嵌段共聚物，（甲氧基-聚（乙二醇））（2）-嵌段-聚（L-谷氨酸）（（mPEG）（2）-PGA）及其前体（甲氧基-聚（乙二醇） （2）-嵌段-聚（γ-苄基-L-谷氨酸）（（mPEG）（2）-PBG）分三步制备：（1）大分子引发剂（甲氧基-聚（乙二醇））（2）- NH2（（mPEG）（2）-NH2）通过将两个甲氧基-聚（乙二醇）与丝氨醇和二异氰酸酯偶联而合成。（2）（mPEG）（2）-PBG通过γ-苄基的开环聚合反应合成用大分子引发剂（（mPEG）（2）-NH2）引发的-1-谷氨酸-N-羧基酐;（3）除去（mPEG）（2）-PBG中的保护性苄基，得到（mPEG）（2）- （mPEG）（2）-PBG和（mPEG）（2）-PGA的性质均通过H-1 NMR，FT-IR，GPC和DLS表征。在水溶液（mPEG）（2）-与线性mPEG-PBG共聚物相比，PBG倾向于形成更稳定的胶束，（mPEG）（2）-PBG的尺寸随着（mPEG）（2）-PBG中疏水性PBG长度的增加而减小。将异铂接枝到（mPEG）（2）-PGA上以形成接枝率接近90％的（mPEG）（2）-PGA-PTX（MPTX）和（mPEG）（2）-PGA-Pt（MPt）缀合物负载效率为15％（w / w）。 MPTX可以大大提高PTX的溶解度。两种结合物都可以自组装成平均直径约为50 nm的胶束，并显示出针对MCF-7，HeLa和SMMC细胞系的增强的抗癌活性。小鼠体内抗癌评估显示MPt显示出理想的抗肿瘤活性，并允许我们推断系统毒性。因此，MPTX和MPt在癌症化疗中作为高分子药物具有巨大的潜力。

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