MICRODROPLET-BASED SUSTAINED DELIVERY OF AZIDOTHYMIDINE

描述：(改编自申请人的摘要)。形成了一种 药物的微滴制剂，改善组织的手段 配伍并提供缓释，涉及制备 含药油相的微球(0.1微米直径)和 用一层磷脂将它们包裹起来。一种大鼠模型将是 用于测试基于微滴技术的缓释 打算提供长达一周的治疗的齐多夫定 艾滋病病毒感染的治疗方案。一系列微滴制剂 含有不同浓度的叠氮胸苷将在 至少三种组织相容的FDA批准的合成油。 含有AZT的微滴的释放动力学将在 体外模型以及皮内和肌肉内注射 老鼠。提供可接受的(零级)释放的配方 将在一周内确定动力学，以供进一步 在第二阶段SBIR提案中进行开发。

DESCRIPTION: (Adapted from the Applicant's Abstract). The formation of microdroplet formulations of a drug, means of improving tissue compatibility and providing sustained release, involves the preparation of microspheres (O.1 micron diameter) of a drug-containing oil phase and encapsulation of them with a layer of phospholipid. A rat model will be used to test the microdroplet technology-based sustained delivery of azidothymidine which is intended to provide up to one week treatment regimen for HIV infection. A series of microdroplet formulations containing different concentrations of azidothymidine will be prepared in at least three tissue-compatible and FDA approved synthetic oils.The drug release kinetics of the AZT-containing microdroplets will be tested in an in vitro model as well as by intradermal and intramuscular injections into rats. A formulation which provides acceptable (zero order) release kinetics over a period of one week will be identified for further development in a Phase II SBIR proposal.