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作为一种潜在的两性霉素 B 输送基质,自组装腰果胶-接枝聚乳酸共聚物纳米粒子。

Self-assembling cashew gum-graft-polylactide copolymer nanoparticles as a potential amphotericin B delivery matrix.

机构信息

Department of Organic and Inorganic Chemistry, UFC - CEP, Caixa Postal 6021 - Humberto Monte s/n, Campus do Pici, 60455-760 Fortaleza, Brazil.

Faculty of Medicine, UFC, CEP 62.042-280 - Comandante Mauro Célio Rocha Pontes, 100 Derby, Sobral, Brazil.

出版信息

Int J Biol Macromol. 2020 Jun 1;152:492-502. doi: 10.1016/j.ijbiomac.2020.02.166. Epub 2020 Feb 22.

Abstract

Amphotericin B is an antibiotic used in the treatment of fungal disease and leishmania; however, it exhibits side effects to patients, hindering its wider application. Therefore, nanocarriers have been investigated as delivery systems for amphotericin B (AMB) in order to decrease its toxicity, besides increase bioavailability and solubility. Amphiphilic copolymers are interesting materials to encapsulate hydrophobic drugs such as AMB, hence copolymers of cashew gum (CG) and l-lactide (LA) were synthesized using two different CG:LA molar ratios (1:1 and 1:10). Data obtained revealed that copolymer nanoparticles present similar figures for particle sizes and zeta potentials; however, particle size of encapsulated AMB increases if compared to unloaded nanoparticles. The 1:10 nanoparticle sample has better stability although higher polydispersity index (PDI) if compared to 1:1 sample. High amphotericin (AMB) encapsulation efficiencies and low hemolysis were obtained. AMB loaded copolymers show lower aggregation pattern than commercial AMB solution. AMB loaded nanoparticles show antifungal activities against four C. albicans strains. It can be inferred that cashew gum/polylactide copolymers have potential as nanocarrier systems for AMB.

摘要

两性霉素 B 是一种用于治疗真菌感染和利什曼病的抗生素;然而,它会对患者产生副作用,限制了其更广泛的应用。因此,纳米载体已被研究作为两性霉素 B(AMB)的递送系统,以降低其毒性,同时提高生物利用度和溶解度。两亲性共聚物是一种有趣的封装疏水性药物(如 AMB)的材料,因此使用两种不同的 CG:LA 摩尔比(1:1 和 1:10)合成了腰果胶(CG)和 L-丙交酯(LA)的共聚物。获得的数据表明,共聚物纳米粒子的粒径和 Zeta 电位相似;然而,如果与未负载的纳米粒子相比,负载 AMB 的纳米粒子的粒径会增加。1:10 的纳米粒子样品具有更好的稳定性,尽管与 1:1 样品相比,其多分散指数(PDI)更高。获得了高的两性霉素(AMB)包封效率和低的溶血率。负载 AMB 的共聚物比商业 AMB 溶液表现出更低的聚集模式。负载 AMB 的纳米粒子对四种 C. albicans 菌株表现出抗真菌活性。可以推断,腰果胶/聚丙交酯共聚物具有作为 AMB 的纳米载体系统的潜力。

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