Laboratoire Des Substances Bioactives, Centre de Biotechnologie de Borj-Cedria (CBBC), BP-901, 2050, Hammam-lif, Tunisia.
Faculté Des Sciences de Bizerte, Université de Carthage, Tunis, Tunisia.
Appl Biochem Biotechnol. 2021 Nov;193(11):3732-3752. doi: 10.1007/s12010-021-03621-w. Epub 2021 Aug 16.
Cyclic lipopeptides produced by Bacillus species exhibit interesting therapeutic potential. However, their clinical use remains limited due to their low stability, undesirable interactions with host macromolecules, and their potential toxicity to mammalian cells. The present work aims to develop suitable lipopeptide-loaded chitosan nanoparticles with improved biological properties and reduced toxicity. Surfactin and bacillomycin D lipopeptides produced by Bacillus amyloliquefaciens B84 strain were loaded onto chitosan nanoparticles by ionotropic gelation process. Nanoformulated lipopeptides exhibit an average size of 569 nm, a zeta potential range of 38.8 mV, and encapsulation efficiency (EE) of 85.58%. Treatment of Candida (C.) albicans cells with encapsulated lipopeptides induced anti-adhesive activity of 81.17% and decreased cell surface hydrophobicity (CSH) by 25.53% at 2000 µg/mL. Nanoformulated lipopeptides also induced antileishmanial activity against Leishmania (L.) major promastigote and amastigote forms at respective IC values of 14.37 µg/mL and 22.45 µg/mL. Nanoencapsulated lipopeptides exerted low cytotoxicity towards human erythrocytes and Raw 264.7 macrophage cell line with respective HC and LC values of 770 µg/mL and 234.56 µg/mL. Nanoencapsulated lipopeptides could be used as a potential delivery system of lipopeptides to improve their anti-adhesive effect against C. albicans cells colonizing medical devices and their anti-infectious activity against leishmania.
由芽孢杆菌属产生的环状脂肽表现出有趣的治疗潜力。然而,由于其稳定性低、与宿主大分子的不理想相互作用以及对哺乳动物细胞的潜在毒性,它们的临床应用仍然受到限制。本工作旨在开发具有改善的生物学性质和降低毒性的合适的载脂肽壳聚糖纳米粒子。通过离子凝胶化过程将由解淀粉芽孢杆菌 B84 菌株产生的表面活性素和杆菌霉素 D 脂肽载入壳聚糖纳米粒子中。纳米配方的脂肽表现出平均粒径为 569nm、zeta 电位范围为 38.8mV 和包封效率(EE)为 85.58%。用包封的脂肽处理白色念珠菌(C.)细胞诱导 81.17%的抗粘附活性和 25.53%的细胞表面疏水性(CSH)降低,在 2000µg/mL 时。纳米配方的脂肽还对利什曼原虫(L.)主要前鞭毛体和无鞭毛体形式表现出抗利什曼原虫活性,各自的 IC 值为 14.37µg/mL 和 22.45µg/mL。纳米包封的脂肽对人红细胞和 Raw 264.7 巨噬细胞系的细胞毒性低,各自的 HC 和 LC 值为 770µg/mL 和 234.56µg/mL。纳米包封的脂肽可用作脂肽的潜在递药系统,以改善其对定植于医疗器械的白色念珠菌细胞的抗粘附作用及其对利什曼原虫的抗感染活性。