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

作者 ： Renata Bem dos Santos ^a ， Kelly Ayumi Nakama ^a ， Camila Oliveira Pacheco ^a ， Marcelo Gomesde Gomes ^a ， Jaqueline Ferreirade Souza ^b ， Ana Claudiade Souza Pinto ^c ， Fernanda Alicede Oliveira ^c ， Amanda Luisada Fonseca ^c ， Fernando Varotti ^c ， André Ricardo Fajardo ^b ， Sandra Elisa Haas ^a

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

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

^c Núcleo de Pesquisa em Química Biológica, Universidade Federal de São João Del Rei, Campus Centro Oeste, 400 Sebastião Gonçalves Coelho, Divinópolis, MG 35501-296, Brazil

摘要： 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.

关键词： Nanocapsules， Polysorbate 80 ， PEG ， Chitosan ， Eudragit RS100® ， Antimalarial ， Nanomaterials