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用于抗生素控释的二氧化硅溶胶-凝胶。I. 合成、表征及体外释放

Silica sol-gel for the controlled release of antibiotics. I. Synthesis, characterization, and in vitro release.

作者信息

Radin S, Ducheyne P, Kamplain T, Tan B H

机构信息

University of Pennsylvania, Department of Bioengineering, Center for Biomaterials and Tissue Engineering, 3320 Smith Walk, Philadelphia, Pennsylvania 19104, USA.

出版信息

J Biomed Mater Res. 2001 Nov;57(2):313-20. doi: 10.1002/1097-4636(200111)57:2<313::aid-jbm1173>3.0.co;2-e.

Abstract

Room temperature processed silica sol-gel (xerogel) was investigated as a novel controlled release carrier of antibiotics (vancomycin). Xerogel characteristics, in vitro release properties, and bactericidal efficacy of the released antibiotic were determined. The xerogel/vancomycin composite showed a long-term sustained release (up to 6 weeks). In addition, bactericidal efficacy of released vancomycin was retained. The kinetics of release and the amount released were dose dependent. The initial, first-order release was followed by a near-zero-order release. The time to transition from the first- to zero-order release increased with vancomycin load (from 2 to 3 weeks with load increase from 2.2 to 11.1 mg/g). Regardless of the load, about 70% of the original vancomycin content was released by the transitional point, and the cumulative release after 6 weeks of immersion was about 90%. This study, combined with other reports documenting biocompatibility and controlled resorbability of the xerogel/drug composite in vivo, suggests that silica xerogel is a promising controlled release material for the treatment of bone infections.

摘要

研究了室温处理的硅溶胶 - 凝胶(干凝胶)作为抗生素(万古霉素)的新型控释载体。测定了干凝胶的特性、体外释放特性以及释放抗生素的杀菌效果。干凝胶/万古霉素复合物显示出长期持续释放(长达6周)。此外,释放的万古霉素保留了杀菌效果。释放动力学和释放量呈剂量依赖性。初始的一级释放之后是接近零级的释放。从一级释放转变为零级释放的时间随着万古霉素负载量的增加而增加(负载量从2.2 mg/g增加到11.1 mg/g时,时间从2周增加到3周)。无论负载量如何,在转变点时约70%的原始万古霉素含量已释放,浸泡6周后的累积释放量约为90%。这项研究与其他记录干凝胶/药物复合物在体内生物相容性和可控吸收性的报告相结合,表明硅干凝胶是一种用于治疗骨感染的有前景的控释材料。

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