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可吸收微珠实现抗真菌药物的缓释：体外和体内分析

Resorbable Beads Provide Extended Release of Antifungal Medication: In Vitro and In Vivo Analyses.

作者信息

Hsu Yung-Heng, Chen Huang-Yu, Chen Jin-Chung, Yu Yi-Hsun, Chou Ying-Chao, Ueng Steve Wen-Neng, Liu Shih-Jung

机构信息

Department of Orthopedic Surgery, Chang Gung Memorial Hospital-Linkou, Tao-Yuan 33305, Taiwan.

Department of Mechanical Engineering, Chang Gung University, Tao-Yuan 33302, Taiwan.

出版信息

Pharmaceutics. 2019 Oct 24;11(11):550. doi: 10.3390/pharmaceutics11110550.

DOI:10.3390/pharmaceutics11110550
PMID:31652891
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6920839/
Abstract

Fungal osteomyelitis has been difficult to treat, with first-line treatments consisting of implant excision, radical debridement, and local release of high-dose antifungal agents. Locally impregnated antifungal beads are another popular treatment option. This study aimed to develop biodegradable antifungal-agent-loaded Poly(d,l-lactide--glycolide) (PLGA) beads and evaluate the in vitro/in vivo release patterns of amphotericin B and fluconazole from the beads. Beads of different sizes were formed using a compression-molding method, and their morphology was evaluated via scanning electron microscopy. Intrabead incorporation of antifungal agents was evaluated via Fourier-transform infrared spectroscopy, and in vitro fluconazole liberation curves of PLGA beads were inspected via high-performance liquid chromatography. When we implanted the drug-incorporated beads into the bone cavity of rabbits, we found that a high level of fluconazole (beyond the minimum therapeutic concentration [MTC]) was released for more than 49 d in vivo. Our results indicate that compression-molded PLGA/fluconazole beads have potential applications in treating bone infections.

摘要

真菌性骨髓炎一直难以治疗，一线治疗方法包括植入物切除、彻底清创以及局部释放高剂量抗真菌药物。局部浸渍抗真菌珠是另一种常用的治疗选择。本研究旨在开发可生物降解的载有抗真菌剂的聚（d，l-丙交酯-乙交酯）（PLGA）珠，并评估两性霉素B和氟康唑从珠中的体外/体内释放模式。使用压缩成型法制备不同尺寸的珠，并通过扫描电子显微镜评估其形态。通过傅里叶变换红外光谱评估抗真菌剂在珠内的掺入情况，并通过高效液相色谱检查PLGA珠的体外氟康唑释放曲线。当我们将载药珠植入兔骨腔时，发现体内氟康唑高水平（超过最低治疗浓度[MTC]）释放超过49天。我们的结果表明，压缩成型的PLGA/氟康唑珠在治疗骨感染方面具有潜在应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826e/6920839/aef39d6d1887/pharmaceutics-11-00550-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826e/6920839/aef39d6d1887/pharmaceutics-11-00550-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826e/6920839/aeed422fec2e/pharmaceutics-11-00550-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826e/6920839/9202f0484bfa/pharmaceutics-11-00550-g002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826e/6920839/9b2f5edceda8/pharmaceutics-11-00550-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826e/6920839/8b438bb0afe6/pharmaceutics-11-00550-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826e/6920839/988d708dde6c/pharmaceutics-11-00550-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826e/6920839/d8dd91a7a685/pharmaceutics-11-00550-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826e/6920839/21ee376e2f5b/pharmaceutics-11-00550-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/826e/6920839/aef39d6d1887/pharmaceutics-11-00550-g011.jpg

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