Preparation and drug release characteristics of Pingyangmycin-loaded dextran cross-linked gelatin microspheres for embolization therapy.
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 microm with 74% ranging from 50-200 microm. 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 degrees 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.
Wu
Hong
H
The Key Laboratory of Biomedical Information Engineering of Ministry of Education, School of Life Science and Technology, Xi'an Jiaotong University, Xi'an 710049, People's Republic of China.
Zhang
Zhenxi
Z
Wu
Daocheng
D
Zhao
Hongping
H
Yu
Kaitao
K
Hou
Zhenqing
Z
D000818:Animals; D001761:Bleomycin / Q000008:administration & dosage / Q000031:analogs & derivatives*; D003911:Dextrans; D016503:Drug Delivery Systems; D004621:Embolization, Therapeutic; D005260:Female; D005780:Gelatin; D008297:Male; D008863:Microspheres; D011817:Rabbits
D003911:Dextrans; D001761:Bleomycin; C025703:bleomycetin; D005780:Gelatin