de Oliveira Mariana Carla, Balbinot Rodolfo Bento, Villa Nova Mônica, Gonçalves Renato Sonchini, Bidóia Danielle Lazarin, Caetano Wilker, Nakamura Celso Vataru, Bruschi Marcos Luciano
Postgraduate Program in Pharmaceutical Sciences, Laboratory of Research and Development of Drug Delivery Systems, Department of Pharmacy, State University of Maringa, Av. Colombo 5790, Maringa 87020-900, PR, Brazil.
Postgraduate Program in Biological Sciences, Laboratory of Technological Innovation in the Development of Pharmaceuticals and Cosmetics, Department of Health Basic Sciences, State University of Maringa, Av. Colombo 5790, Maringa 87020-900, PR, Brazil.
Pharmaceutics. 2023 Aug 12;15(8):2127. doi: 10.3390/pharmaceutics15082127.
Leishmaniasis is a disease caused by protozoa species of the genus, and the current treatments face several difficulties and obstacles. Most anti-leishmanial drugs are administered intravenously, showing many side effects and drug resistance. The discovery of new anti-leishmanial compounds and the development of new pharmaceutical systems for more efficient and safer treatments are necessary. Copaiba oil-resin (CO) has been shown to be a promising natural compound against leishmaniasis. However, CO displays poor aqueous solubility and bioavailability. Self-emulsifying drug delivery systems (SEDDS) can provide platforms for release of hydrophobic compounds in the gastrointestinal tract, improving their aqueous solubilization, absorption and bioavailability. Therefore, the present work aimed to develop SEDDS containing CO and Soluplus surfactant for the oral treatment of leishmaniasis. The design of the systems was accomplished using ternary phase diagrams. Emulsification and dispersion time tests were used to investigate the emulsification process in gastric and intestinal environments. The formulations were nanostructured and improved the CO solubilization. Their in vitro antiproliferative activity against promastigote forms of and , and low in vitro cytotoxicity against macrophages were also observed. More studies are necessary to determine effectiveness of SOL in these systems, which can be candidates for further pharmacokinetics and in vivo investigations.
利什曼病是由利什曼原虫属的原生动物引起的疾病，目前的治疗面临诸多困难和障碍。大多数抗利什曼病药物通过静脉给药，存在许多副作用和耐药性问题。发现新的抗利什曼病化合物并开发更高效、更安全治疗方法的新型药物系统很有必要。巴西香脂油树脂（CO）已被证明是一种有前景的抗利什曼病天然化合物。然而，CO的水溶性和生物利用度较差。自乳化药物递送系统（SEDDS）可为胃肠道中疏水性化合物的释放提供平台，提高其水溶性、吸收和生物利用度。因此，本研究旨在开发含CO和固体分散体增溶剂的SEDDS用于口服治疗利什曼病。利用三元相图完成了系统设计。通过乳化和分散时间测试来研究在胃和肠道环境中的乳化过程。这些制剂具有纳米结构，提高了CO的溶解度。还观察到它们对前鞭毛体形式的利什曼原虫具有体外抗增殖活性，并且对巨噬细胞的体外细胞毒性较低。需要更多研究来确定这些系统中固体分散体增溶剂的有效性，它们可作为进一步药代动力学和体内研究的候选物。
