Guarnieri Michael, Tyler Betty M, Detolla Louis, Zhao Ming, Kobrin Barry
Department of Neurological Surgery, Johns Hopkins School of Medicine, Baltimore, Maryland, USA.
Department of Pathology and Medicine, School of Medicine, Division of Infectious Diseases and Public Health, The Program of Comparative Medicine, University of Maryland, Baltimore, Maryland, USA.
J Pharm Bioallied Sci. 2014 Jan;6(1):38-42. doi: 10.4103/0975-7406.124315.
Long-acting therapy in laboratory animals offers advantages over the current practice of 2-3 daily drug injections. Yet little is known about the disintegration of biodegradable drug implants in rodents.
Compare bioavailability of buprenorphine with the biodegradation of lipid-encapsulated subcutaneous drug pellets.
Pharmacokinetic and histopathology studies were conducted in BALB/c female mice implanted with cholesterol-buprenorphine drug pellets.
Drug levels are below the level of detection (0.5 ng/mL plasma) within 4-5 days of implant. However, necroscopy revealed that interstitial tissues begin to seal implants within a week. Visual inspection of the implant site revealed no evidence of inflammation or edema associated with the cholesterol-drug residue. Chemical analyses demonstrated that the residues contained 10-13% of the initial opiate dose for at least two weeks post implant.
The results demonstrate that biodegradable scaffolds can become sequestered in the subcutaneous space.
Drug implants can retain significant and unintended reservoirs of drugs.
在实验动物中，长效治疗相较于当前每日2至3次注射药物的做法具有优势。然而，关于可生物降解药物植入物在啮齿动物体内的降解情况，人们了解甚少。
比较丁丙诺啡的生物利用度与脂质包裹皮下药物微丸的生物降解情况。
对植入胆固醇 - 丁丙诺啡药物微丸的BALB/c雌性小鼠进行药代动力学和组织病理学研究。
植入后4至5天内，药物水平低于检测限（血浆0.5 ng/mL）。然而，尸检显示间质组织在一周内开始封闭植入物。对植入部位的目视检查未发现与胆固醇 - 药物残留相关的炎症或水肿迹象。化学分析表明，植入后至少两周，残留物含有初始阿片类药物剂量的10 - 13%。
结果表明可生物降解支架可在皮下空间被隔离。
药物植入物可保留大量意外的药物储存库。
