Micelle controlled release of 5-fluorouracil: Follow the guideline for good polymer–drug compatibility
Micelle controlled release of 5-fluorouracil: Follow the guideline for good polymer–drug compatibility
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5-氟尿嘧啶的胶束控释：遵循良好聚合物与药物相容性的指南
DOI：
10.1016/j.colsurfa.2014.04.062
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发表时间：
2014-09
期刊：
影响因子：
--
通讯作者：
Meidong Lang
中科院分区：
文献类型：
--
作者：
Chao Wei;Yutong Fu;Jianwen Liu;Meidong Lang
采用Flory-Huggins相互作用参数（χpd）定性评价了亲水性5-氟尿嘧啶（5-FU）与聚[γ-（氨基甲酸苄酯）-ε-己内酯]（PCABCL）和聚（ε-己内酯）（PCL）形成的疏水性核嵌段之间的药物-聚合物相容性。计算结果表明，PCABCL与5-FU的亲和性优于PCL。因此，合成了一系列二嵌段聚合物单甲氧基聚乙二醇-b-聚[γ-氨基甲酸苄酯-ε-己内酯]（mPEG 45-b-PCABCLn），并制备了5-FU胶束。γ-氨基甲酸苄酯（CAB）基团的引入显著降低了共聚物的结晶度，增加了胶束核的亲水性，从而提高了载药量。这些胶束具有高稳定性和球形形态。成核嵌段的长度可以改变药物的释放行为。mPEG 45-b-PCABCL 19制备的胶束具有最高的5-FU载药量和最好的控释性能。这些空白胶束对HCT 116癌细胞显示出非常低的毒性。同时5-FU载药胶束在体外可诱导HCT 116细胞凋亡，并呈浓度依赖性增加细胞死亡率。这些结果表明，这些胶束在癌症治疗中具有很大的潜力。
Flory–Huggins interaction parameter (χpd) was introduced to qualitatively evaluate the drug–polymer compatibility between hydrophilic 5-fluorouracil (5-FU) and hydrophobic core block, which was formed by poly[γ-(carbamic acid benzyl ester)-ɛ-caprolactone] (PCABCL) and poly(ɛ-caprolactone) (PCL). The calculation results indicated that PCABCL had better affinity with 5-FU than PCL. Thus, a series of diblock polymers monomethoxy poly(ethylene glycol)-b-poly[γ-(carbamic acid benzyl ester)-ɛ-caprolactone] (mPEG45-b-PCABCLn) was synthesized, followed by the preparation of 5-FU loaded micelles. The introduction of γ-(carbamic acid benzyl ester) (CAB) group significantly decreased the crystallinity of copolymers and increased the hydrophilicity of the micellar core, leading to an improved drug loading content. These micelles had high stability and spherical morphology. The release behavior could be turned by the length of core-forming block. Moreover, micelles prepared by mPEG45-b-PCABCL19displayed the highest 5-FU loading content and the most controlled release behavior. These blank micelles showed very low toxicity against HCT116 cancer cells. Meanwhile 5-FU loaded micelles exhibited a concentration dependent increase in HCT116 cell death by inducing cell apoptosisin vitro. These results indicated that these micelles have great potential in cancer therapy.
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