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脂质体复合多孔 β-TCP 支架的制备、表征及抗生物膜活性

Liposome combined porous beta-TCP scaffold: preparation, characterization, and anti-biofilm activity.

机构信息

Orthopedic Center, Kunming General Hospital of Chengdu Military Command, Kunming, 650032, PR China.

出版信息

Drug Deliv. 2010 Aug;17(6):391-8. doi: 10.3109/10717541003762870.

Abstract

The objective of this study was to design a novel artificial bone scaffold for therapy and prevention of refractory bacterial infection. Porous beta-tricalcium phosphate (beta-TCP) scaffold was combined with liposomal gentamicin (GS) to form a novel complex drug carrier. The liposome combined beta-TCP scaffold (LCS) was characterized for its liposome binding rate, drug loading, and micromorphology. The anti-biofilm activity of LCS was evaluated by Staphylococcus aureus biofilm in vitro. The drug release from LCS was recognized as an initial high dose of liposomal GS released from the matrix and a further sustained release of free GS from the liposome, respectively, and it is an ideal release pattern for treatment and prevention of post-operative osteomyelitis. The release kinetics was influenced by variation of particle size of liposome. LCS displayed a potential anti-biofilm activity even in the lowest GS concentration (2.5 microg/mL), and the regrowth time was extended from 5.0 h to 9.5 h. At a higher dosage range, the highest anti-biofilm activity was achieved by LCS with liposomal particle size of 800 nm. In conclusion, the development of LCS showed a new pathway for controlled delivery of liposomal antibiotics for treatment of osteomyelitis caused by persistent bacterial infection.

摘要

本研究旨在设计一种新型人工骨支架,用于治疗和预防难治性细菌感染。将多孔β-磷酸三钙(β-TCP)支架与脂质体庆大霉素(GS)结合,形成一种新型的复合药物载体。对脂质体结合β-TCP 支架(LCS)的脂质体结合率、载药量和微观形貌进行了表征。通过体外金黄色葡萄球菌生物膜评估了 LCS 的抗生物膜活性。LCS 的药物释放被认为是脂质体 GS 从基质中初始高剂量释放和脂质体中游离 GS 的进一步持续释放,这是治疗和预防术后骨髓炎的理想释放模式。释放动力学受脂质体粒径变化的影响。即使在最低 GS 浓度(2.5μg/mL)下,LCS 也显示出潜在的抗生物膜活性,再生时间从 5.0 h 延长至 9.5 h。在较高的剂量范围内,脂质体粒径为 800nm 的 LCS 达到了最高的抗生物膜活性。总之,LCS 的开发为治疗持续性细菌感染引起的骨髓炎提供了一种新的控制释放脂质体抗生素的途径。

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