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Formulation and Evaluation of Solid Lipid Nanoparticles of Ramipril

机译:雷米普利固体脂质纳米粒的制备与评价

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摘要

Solid lipid nanoparticles are typically spherical with an average diameter between 1 and 1000 nm. It is an alternative carrier system to tradition colloidal carriers, such as, emulsions, liposomes, and polymeric micro and nanoparticles. Ramipril is an antihypertensive agent used in the treatment of hypertension. Its oral bioavailability is 28% and it is rapidly excreted through the renal route. This drug has many side effects such as, postural hypotension, hyperkalemia, and angioedema, when given as an immediate dosage form. To overcome the side effects and to increase the bioavailability of ramipril, solid lipid nanoparticles of ramipril are prepared by using lipids (glyceryl monostearate and glyceryl monooleate) with stabilizers (tween 80, poloxamer 188, and span 20). The prepared formulations have been evaluated for entrapment efficiency, drug content, in-vitro drug release, particle size analysis, scanning electron spectroscopy, Fourier transform-infrared studies, and stability. A formulation containing glyceryl monooleate, stabilized with span 20 as surfactant showed prolonged drug release, smaller particle size, and narrow particle size distribution, as compared to other formulations with different surfactants and lipids.
机译:固体脂质纳米颗粒通常是球形的,平均直径在1-1000nm之间。它是传统胶体载体(例如乳液,脂质体以及聚合物微粒和纳米颗粒)的替代载体系统。雷米普利是一种用于治疗高血压的降压药。它的口服生物利用度为28%,并通过肾脏途径迅速排泄。当以直接剂型给予时,该药物具有许多副作用,例如姿势性低血压,高钾血症和血管性水肿。为克服副作用并提高雷米普利的生物利用度,雷米普利的固体脂质纳米颗粒通过使用脂质(单硬脂酸甘油酯和单油酸甘油酯)与稳定剂(吐温80,泊洛沙姆188和跨度20)制备。已经评估了所制备的制剂的包封效率,药物含量,体外药物释放,粒度分析,扫描电子光谱,傅立叶变换红外研究和稳定性。与具有不同表面活性剂和脂质的其他制剂相比,含有跨度为20的甘油单油酸酯作为表面活性剂的制剂显示出更长的药物释放,更小的粒度和更窄的粒度分布。

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