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载姜黄素的 pH 响应性 PLGA/壳聚糖纤维的动力学和释放行为及其对 HT-29 细胞的抗肿瘤活性。

The kinetics and release behaviour of curcumin loaded pH-responsive PLGA/chitosan fibers with antitumor activity against HT-29 cells.

机构信息

School of Chemistry and Material Engineering, Chaohu University, 238000, Hefei, Anhui, PR China; School of Chemistry and Chemical Engineering, Hefei University of Technology, 230009, Hefei, Anhui, PR China.

School of Chemistry and Chemical Engineering, Hefei University of Technology, 230009, Hefei, Anhui, PR China.

出版信息

Carbohydr Polym. 2021 Aug 1;265:118077. doi: 10.1016/j.carbpol.2021.118077. Epub 2021 Apr 15.

Abstract

The bioavailability and clinical effect of curcumin (Cur) are greatly restricted due to its physicochemical instability and high hydrophobicity. To overcome the disadvantages, the nanofibers of poly(lactide-glycolide)/chitosan loaded with Cur (PLGA/CS/Cur) was developed here by electrospinning technique for controlled Cur delivery. The incorporated Cur was well-dispersed and maintained crystalline form in PLGA/CS fiber matrix by hydrogen bonding. The incorporation of Cur had no obvious influence on the fiber size and morphology but exerted impacts on thermal stability. At pH 7.4, the release followed Fickian diffusion mechanism; while at pH 2.0, the release followed the coexistence of diffusion and erosion mechanisms. In addition, the amount of Cur released at pH 2.0 was much higher than that at pH 7.4. As a result, the nanofibers demonstrated higher anticancer activity at acidic environment. Therefore, the PLGA/CS/Cur nanofibers may be served as a potential pH responsive vehicle for the controlled drug delivery.

摘要

姜黄素(Cur)由于其理化不稳定性和高疏水性,其生物利用度和临床效果受到极大限制。为了克服这些缺点,本研究采用静电纺丝技术制备了载姜黄素的聚(乳酸-乙醇酸)/壳聚糖纳米纤维(PLGA/CS/Cur),用于控制 Cur 的释放。通过氢键作用,掺入的 Cur 在 PLGA/CS 纤维基质中得到了很好的分散并保持结晶形式。Cur 的掺入对纤维的大小和形态没有明显影响,但对热稳定性有影响。在 pH7.4 时,释放遵循菲克扩散机制;而在 pH2.0 时,释放遵循扩散和侵蚀机制的共存。此外,在 pH2.0 时释放的 Cur 量明显高于在 pH7.4 时。因此,纳米纤维在酸性环境下表现出更高的抗癌活性。因此,PLGA/CS/Cur 纳米纤维可以作为一种潜在的 pH 响应型药物载体,用于控制药物释放。

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