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载姜黄素纳米胶囊:表面特性对工艺参数及潜在抗疟活性的影响

Curcumin-loaded nanocapsules: Influence of surface characteristics on technological parameters and potential antimalarial activity.

作者信息

Santos Renata Bem Dos, Nakama Kelly Ayumi, Pacheco Camila Oliveira, de Gomes Marcelo Gomes, de Souza Jaqueline Ferreira, de Souza Pinto Ana Claudia, de Oliveira Fernanda Alice, da Fonseca Amanda Luisa, Varotti Fernando, Fajardo André Ricardo, Haas Sandra Elisa

机构信息

Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Pampa, Campus Uruguaiana BR 472, Km 7, 97500-970 Uruguaiana, RS, Brazil.

Laboratório de Tecnologia e Desenvolvimento de Materiais Poliméricos e Compósitos (LaCoPol), Universidade Federal de Pelotas (UFPel), 96010-900 Pelotas, RS, Brazil.

出版信息

Mater Sci Eng C Mater Biol Appl. 2021 Jan;118:111356. doi: 10.1016/j.msec.2020.111356. Epub 2020 Aug 11.

Abstract

The present study aimed to develop nanocapsules (NCs) loaded with curcumin (CCM) using different coatings, comparing the effect of these coatings on physicochemical properties of NCs. NCs were prepared by interfacial deposition of performed polymer, using different polymers as coatings (P80, PEG, Chitosan and Eudragit RS100®) and then, characterized in detail by different techniques (AFM, FTIR, DSC, XRD, among others). In vitro studies were performed, evaluating the release profile, cytotoxicity and antimalarial activity of CCM-loaded NCs. Overall, all CCM-loaded NCs samples exhibited typical characteristics as nanometric size, coating-dependent zeta potential, acidic pH value, span values below 2, homogeneous morphology and CCM-distribution in pseudophases of type VI (for all of coatings). Experimental results showed that CCM remains stable in lipid-core of NCs, maintaining its physicochemical and biological properties after nanoencapsulation process. In vitro release assays showed that nanoencapsulation was an efficient strategy to controlled release of CCM and P80-coated NCs presented slowest CCM-release considering all nanoformulations tested. Still, CCM-loaded NCs presented no cytotoxic effect. Also, all CCM-loaded NCs showed a perceptible antimalarial activity independently of their coatings (anionic and cationic), with more expressive results for CS-coated NCs. In conclusion, findings for CCM-loaded NCs and their different coatings seem to be a promising strategy to improve your biological activity.

摘要

本研究旨在使用不同的包衣材料制备负载姜黄素(CCM)的纳米胶囊(NCs),比较这些包衣材料对NCs理化性质的影响。通过已制备聚合物的界面沉积法制备NCs,使用不同的聚合物作为包衣材料(聚山梨酯80、聚乙二醇、壳聚糖和丙烯酸树脂RS100®),然后采用不同技术(原子力显微镜、傅里叶变换红外光谱、差示扫描量热法、X射线衍射等)对其进行详细表征。进行了体外研究,评估负载CCM的NCs的释放曲线、细胞毒性和抗疟活性。总体而言,所有负载CCM的NCs样品均表现出纳米尺寸、包衣依赖性zeta电位、酸性pH值、跨度值低于2、形态均匀以及CCM在VI型假相中的分布等典型特征(对于所有包衣材料)。实验结果表明,CCM在NCs的脂质核中保持稳定,在纳米包封过程后保持其理化和生物学性质。体外释放试验表明,纳米包封是控制CCM释放的有效策略,考虑到所有测试的纳米制剂,聚山梨酯80包衣的NCs的CCM释放最慢。此外,负载CCM的NCs没有细胞毒性作用。而且,所有负载CCM的NCs均表现出明显的抗疟活性,与它们的包衣材料(阴离子和阳离子)无关,壳聚糖包衣的NCs的结果更显著。总之,负载CCM的NCs及其不同包衣材料的研究结果似乎是提高其生物活性的一种有前景的策略。

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