Wang Changguang, Liu Jie, Gao Qinghong, Bi Yueqi, Gan Liangchun, Wang Xinchun, Hou Shixiang
West China College of Pharmacy, Sichuan University, Chengdu 610041, China.
Int J Pharm. 2007 May 24;336(2):361-6. doi: 10.1016/j.ijpharm.2007.02.013. Epub 2007 Feb 15.
Bovine serum albumin microspheres (BSA-MSs) containing Pingyangmycin hydrochloride (PYM) were prepared for the interventional embolization by an emulsification-crosslinking method. The average diameter of the MSs was 83.6 microm with 80% ranging from 35 to 200 microm. The MSs showed a rather high entrapment efficiency (EE%) of 87.6+/-5.7% and the drug loading efficacy (DL%) was 20.2+/-1.3%. The drug release behaviors were evaluated both in vitro and in vivo, using UV-spectroscopy and HPLC, respectively. The in vitro results showed a significantly delayed release of drug for 10 days. The central auricular artery of rabbit was chosen as an embolization sites to study the in vivo drug release and the pharmacokinetics of the MSs compared with PYM injections. Experiments performed by artery perfusion and embolization in rabbits central auricular artery revealed that the PYM loaded BSA-MSs (PYM-BSA-MSs) could obviously prolong in vivo drug release, extend the mean residence time (MRT) and had equal bioavailability compared with plain PYM injections. These results demonstrated that by embolization of the central auricular artery with PYM-BSA-MSs, the local drug concentration could maintain at a relative high level for a longer time, thus achieve the aim of tumor targeting therapy. PYM-BSA-MSs are excellent potential alternatives of interventional embolization materials for the treatment of maxillofacial region tumors.
采用乳化交联法制备了含盐酸平阳霉素（PYM）的牛血清白蛋白微球（BSA-MSs）用于介入栓塞。微球的平均直径为83.6微米，80%的微球直径在35至200微米之间。微球显示出相当高的包封率（EE%），为87.6±5.7%，载药效率（DL%）为20.2±1.3%。分别使用紫外光谱法和高效液相色谱法在体外和体内评估了药物释放行为。体外结果显示药物释放明显延迟了10天。选择兔耳中央动脉作为栓塞部位，研究微球的体内药物释放和药代动力学，并与PYM注射进行比较。通过兔耳中央动脉的动脉灌注和栓塞实验表明，载PYM的BSA-MSs（PYM-BSA-MSs）可明显延长体内药物释放，延长平均驻留时间（MRT），与普通PYM注射相比具有相同的生物利用度。这些结果表明，通过用PYM-BSA-MSs栓塞耳中央动脉，局部药物浓度可在较长时间内维持在相对较高水平，从而实现肿瘤靶向治疗的目的。PYM-BSA-MSs是治疗颌面部肿瘤的介入栓塞材料的优秀潜在替代品。
