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载抗菌肽 BF-30 的聚(丙交酯-共聚- 乙交酯)微球的制备、表征及生物学活性。

Preparation, Characterization and Biological Activity of Cathelicidin-BF-30-Loaded Poly(LA-co-MA) Microspheres.

机构信息

Department of Engineering Research Center of Biopolymer Functional Materials of Yunnan, Yunnan Minzu University, Kunming 650500, China.

Department of Yunnan Rural Leader College, Yunnan Agricultural University, Heilongtan 650201 Kunming, China.

出版信息

J Nanosci Nanotechnol. 2019 Apr 1;19(4):2435-2442. doi: 10.1166/jnn.2019.16422.

DOI:10.1166/jnn.2019.16422
PMID:30487016
Abstract

Antimicrobial peptides have a great potential to replace antibiotics in the treatment of bacterial infections. In order to improve the its stability, the antimicrobial peptides were incorporated in poly(L-lactic acid-co-D,L-mandelic acid) (LA-co-MA) microspheres prepared by a double emulsion solvent evaporation method. In this study, the microspheres obtained had a mean particle size of 2.75±0.2 m, Encapsulation Efficiency (EE) of 92.47±1.21% and drug loading of 8.44±0.11%. The peptides were released from poly(LA-co-MA) microspheres at a constant speed and no significant initial burst effect was observed. The secondary structure and antibacterial activity of the released peptide were retained, which were compared with those of the native peptides. In addition, these BF-30-loaded microspheres presented <5% hemolysis and no toxicity for HEK293 cells even at the highest tested concentration (150 g/mL), indicating that the poly(LA-co-MA) microspheres are promising carriers for peptides.

摘要

抗菌肽在治疗细菌感染方面具有很大的潜力,可以替代抗生素。为了提高其稳定性,抗菌肽被包封在聚(L-乳酸-co-D,L-扁桃酸)(LA-co-MA)微球中,该微球是通过双乳液溶剂蒸发法制备的。在本研究中,得到的微球平均粒径为 2.75±0.2 m,包封效率(EE)为 92.47±1.21%,载药量为 8.44±0.11%。抗菌肽以恒定的速度从聚(LA-co-MA)微球中释放出来,没有观察到明显的初始突释效应。释放的肽的二级结构和抗菌活性得以保留,并与天然肽进行了比较。此外,这些负载 BF-30 的微球的溶血率<5%,即使在最高测试浓度(150 g/mL)下对 HEK293 细胞也没有毒性,表明聚(LA-co-MA)微球是肽的有前途的载体。

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