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首页> 外文期刊>Biomaterials >Folate-targeted supramolecular vesicular aggregates based on polyaspartyl-hydrazide copolymers for the selective delivery of antitumoral drugs.
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Folate-targeted supramolecular vesicular aggregates based on polyaspartyl-hydrazide copolymers for the selective delivery of antitumoral drugs.

机译：基于聚天冬氨酰-酰肼共聚物的叶酸靶向的超分子囊状聚集体，用于选择性递送抗肿瘤药物。

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Supramolecular vesicular aggregates (SVAs) have the advantage of combining the safe and biocompatible properties of colloidal vesicular carriers based on phospholipids with those of polymeric materials, i.e. polyaspartyl-hydrazide (PAHy) copolymers. To provide SVAs with a certain tumour selectivity, folate moieties were chemically conjugated to PAHy copolymers. Physicochemical properties (mean sizes, polydispersity index and zeta potential) of folate-targeted SVAs (FT-SVAs) loaded with gemcitabine were evaluated. The antiproliferative and anticancer activity of gemcitabine-loaded FT-SVAs was evaluated against two cancer cell lines, i.e. MCF-7 cells which over-express the folate receptor and the BxPC-3 cells, which do not over-express this receptor. Gemcitabine-loaded FT-SVAs showed a significantly (p < 0.001) greater and more specific in vitro anticancer activity with respect to both the free drug and the drug-loaded conventional liposomes or untargeted SVAs. Confocal microscopy, flow cytometry analysis and beta-scintillation highlighted that FT-SVAs were able to interact with MCF-7 cells after just 3 h and to increase the amount internalization in cells over-expressing the folate receptor. The in vivo biodistribution and pharmacokinetic experiments showed that gemcitabine-loaded SVAs and FT-SVAs were removed from the circulatory system at a slower rate than the native drug and a prolonged gemcitabine plasma concentration was observed for up to 16 h. SVAs were accumulated mainly in the lungs, spleen and kidneys, while FT-SVAs were also up taken by brain. These interesting and stimulating results suggest the existence of a possible in vivo application of SVAs and encourage the use of folate as a targeting agent in anticancer therapy.
机译：超分子水泡聚集体（SVA）具有将基于磷脂的胶体水泡载体的安全和生物相容性与聚合材料即聚天冬氨酰酰肼（PAHy）的那些相结合的优点。为了使SVA具有一定的肿瘤选择性，将叶酸部分化学偶联到PAHy共聚物上。评估了吉西他滨负载叶酸靶向的SVA（FT-SVA）的理化性质（平均大小，多分散指数和Zeta电位）。评估了吉西他滨负载的FT-SVA对两种癌细胞的过度增殖和抗癌活性，即MCF-7细胞过度表达叶酸受体和BxPC-3细胞过度表达叶酸受体。载有吉西他滨的FT-SVA相对于游离药物和载有药物的常规脂质体或未靶向的SVA均具有显着（p <0.001）更大，更特异性的体外抗癌活性。共聚焦显微镜，流式细胞术分析和β-闪烁表明，FT-SVA能够在短短3小时后与MCF-7细胞相互作用，并增加过表达叶酸受体的细胞内在化的数量。体内生物分布和药代动力学实验表明，载有吉西他滨的SVA和FT-SVA的循环速度要比天然药物慢，并且观察到吉西他滨的血药浓度长达16小时。 SVA主要积累在肺，脾脏和肾脏中，而FT-SVA也被大脑摄取。这些有趣且令人兴奋的结果表明，可能在体内应用SVA，并鼓励在抗癌治疗中使用叶酸作为靶向药物。

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