Preparation and drug release characteristics of pingyangmycin-loaded dextran cross-linked gelatin microspheres for embolization therapy

• Published in: Journal of biomedical materials research. Part B, Applied biomaterials Applied biomaterials, 2006-07, Vol.78B (1), p.56-62
• Main Authors: Wu, Hong, Zhang, Zhenxi, Wu, Daocheng, Zhao, Hongping, Yu, Kaitao, Hou, Zhenqing
• Format: Article
• Language: English
• Subjects: Animals; Bleomycin - administration & dosage; Bleomycin - analogs & derivatives; dextran; Dextrans; Drug Delivery Systems; embolization; Embolization, Therapeutic; Female; Gelatin; gelatin microspheres; Male; Microspheres; pingyangmycin; Rabbits; sustained release
• ISSN: 1552-4973; 1552-4981
• DOI: 10.1002/jbm.b.30458

Gelatin microspheres (GMs) containing Pingyangmycin hydrochloride were prepared for the interventional embolization by a double‐phase emulsified thermal gelation method using oxidized dextran (ox‐dex) as the cross‐linking agent. The average diameter of the microspheres was 82 μm with 74% ranging from 50–200 μm. Drug content and the characteristics of drug release in vitro and in vivo were evaluated using UV‐spectroscopy and HPLC, respectively. The prepared microspheres showed a rather high percentage of encapsulation ranging from 85 to 88% and drug content at 7.2%. The results of in vitro experiments showed that about 65.5% of the total amount of the encapsulated drug was released after 6 h at 37°C. Experiments conducted through artery perfusion and artery embolization in rabbits revealed that the local drug concentration was significantly higher than the systemic blood–drug concentration, with a high level of local drug concentration maintained for more than 120 min after artery embolization with the Pingyangmycin‐loaded ox‐dex‐GMs. The results indicated that the external carotid artery embolization with Pingyangmycin‐loaded ox‐dex‐GMs at reduced dosages prolonged the local drug concentration at a higher level, and could achieve the purpose of a localized targeting tumor therapy. Compared with other embolization materials, ox‐dex‐GMs are an excellent alternative interventional embolization material for the treatment of head and neck tumors. © 2005 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2006