萘普生钠局部给药血管内舒的处方与评价

A. Shailaja, Uzma Afreen
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引用次数: 1

摘要

萘普生钠是一种非甾体抗炎药,用于治疗类风湿关节炎、强直性脊柱炎,减轻疼痛和炎症。它主要通过抑制COX1和COX2受体起作用。它通过抑制COX1受体引起严重的胃出血和消化性溃疡,通过抑制COX2受体引起心血管副作用。为了避免萘普生的不良反应,需要开发新的给药系统。因此侵入体由于它的囊泡结构它们能够深入到体循环中它们既能局部作用也能全身作用。本研究试图制备并表征萘普生钠负载侵入体。以大豆卵磷脂为脂质,span60为表面活性剂,柠檬烯为萜烯,甲醇、乙醇和氯仿为有机溶剂,采用薄膜水合技术制备了萘普生钠负载侵入体。共制备了12种侵入体制剂(inv1 ~ inv12),其中4种为变药脂比制剂,8种为变药脂比制剂。对各制剂进行药物含量、包封效率、粒径、zeta电位和体外药物释放度评价。12个制剂中,以含40mg药物与40mg表面活性剂(span60)比例为1:1的inv2制剂为最佳制剂,其药物含量为96.62%,包封效率为90.9%,zeta电位为-68.5mV,平均粒径为572.4 nm, 12 h的体外释药率为91.6%,符合零级动力学,具有非动力学扩散机制。本研究成功制备了萘普生钠负载侵入体并对其进行了评价。
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Formulation and Evaluation of Naproxen Sodium Loaded Invasomes for Topical Delivery
Naproxen sodium is a Non-steroidal anti-inflammatory agent used in treatment of rheumatoid arthritis, ankylosing spondylitis to relieve pain and inflammation. It is mainly act by inhibiting COX1 and COX2 receptors. By inhibiting COX1 receptor it causes severe gastric bleeding and peptic ulcer and by inhibiting COX2 receptor it causes cardiovascular side effects.In order to avoid the adverse effects of naproxen there is need to develop novel drug delivery system. So that invasomes because of its vesicular structure they are capable of penetrating more into the systemic circulation and they will be acting locally as well as systemically. In this study attempts have been made to prepare and characterize Naproxen sodium loaded invasomes. Naproxen sodium loaded invasomes were prepared by thin film hydration technique by using soya lecithin as lipid, span60 as surfactant, limonene as terpene and methanol, ethanol and chloroform as organic solvents. Total twelve formulations (INV1-INV12) of invasomes were prepared, in which four formulations were prepared by varying drug to surfactant ratio and eight formulations were prepared by varying drug to lipid ratio. All the formulations were evaluated for drug content, entrapment efficiency, particle size, zeta potential and invitro drug release. Among the twelve formulations of invasomestheINV2 formulation (1:1) ratio containing 40mg drug and 40mg surfactant (span60) was found to be the best formulation with drug content of 96.62%, entrapment efficiency of 90.9%, zeta potential of -68.5mV, mean particle diameter of 572.4 nm and invitro drug release of 91.6% in a time period of 12 hrs and followed the zero order kinetics with non fickian diffusion mechanism. In this present study naproxen sodium loaded invasomes were successfully prepared and evaluated.
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来源期刊
Current Nanomedicine
Current Nanomedicine Medicine-Medicine (miscellaneous)
CiteScore
2.00
自引率
0.00%
发文量
15
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