醋氯芬酸niosomal给药系统的研制及体外评价。

Samreen Sulthana, M. Aruna, S. Rasheed
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引用次数: 1

摘要

在过去的几十年里,新型给药系统(NDDS)的开发受到了广泛的关注。理想情况下,NDDS应该满足两个先决条件。首先,它应该在治疗期间以人体需要的速度输送药物。其次,它应该引导活动实体到行动地点。包括缓释剂型在内的常规剂型无法满足这些要求。目前,还没有一种理想的药物传递系统,但人们已经通过各种新的药物传递方法进行了真诚的尝试。本研究的目的是开发一种醋氯芬酸的乳质体给药系统。为了进行药物-聚合物相容性,进行了傅里叶变换红外研究,观察到APl与辅料之间没有相互作用。采用薄膜水合法以胆固醇为磷脂制备了8种膜质体制剂。通过囊泡大小、形状、表面电荷、包封效率、药物含量和体外药物释放研究对制备的乳质体制剂进行了表征。优化后的配方(F5)的囊泡大小、粒径分布和zeta电位为65.6 nm, zeta电位为-1.5mV。大小分布曲线证实了囊泡的正常大小分布。乳质体囊泡制剂的包封率为54.18±0.59 ~ 92.71±0.56,优化制剂的包封率为92.71±0.56,乳质体制剂(f1 ~ F8)的含药量为94.6 ~ 97.8%。所有外用乳质体凝胶的pH值均在7.4±0.02 ~ 7.4±0.08之间。所有制剂的零级释放量均符合Korsemeyer peppas方程,具有较高的相关性(r2> 0.99),说明乙酰氯芬酸从脂质双分子层囊泡中释放是由扩散引起的。进行了稳定性研究,在配方中没有发现明显的变化。
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Formulation and in-vitro evaluation of niosomal drug delivery system for aceclofenac.
In the past few decades, considerable attention has been focused on the development of new drug delivery system (NDDS). The NDDS should ideally fulfill two prerequisites. Firstly, it should deliver the drug at a rate directed by the needs of the body, over the period of treatment. Secondly, it should channel the active entity to the site of action. Conventional dosage forms including prolonged release dosage forms are unable to meet none of these. At present, no available drug delivery system behaves ideally, but sincere attempts have been made to achieve them through various novel approaches in drug delivery. The aim of present work is to develop a niosomal drug delivery system of aceclofenac. To perform drug-polymer compatibility FT-IR studies were carried out and observed that there was no interaction between the APl and excipients. 8 niosomal formulations are prepared by the thin film hydration method using the cholesterol as the phospholipid. Prepared niosomal formulations were characterized by vesicle size, shape, surface charge, entrapment efficiency, drug content and invitro drug release studies. The vesicle size, size distribution and zeta potential of the optimized formulation (F5) was found to be 65.6 nm and zeta potential was found to be -1.5mV. Size distribution curve confirms the normal size distribution of the vesicles. The % entrapment efficiency of niosomal vesicles formulations were found to be in the range of 54.18±0.59 to 92.71±0.56 and optimized formulation was found to be 92.71±0.56 and drug content of niosomes formulations (F1to F8) were determined to be in the range of 94.6 -97.8%. The pH of all topical niosomal gels were found to be in the range of 7.4±0.02 to 7.4±0.08.The best fit with higher correlation (r2> 0.99) was found with the Zero Order Release and follows Korsemeyer peppas equation for all the formulations, which means that release of Aceclofenac from the lipid bilayer vesicles were due to diffusion. The stability studies were carried out and there was no significant change found in the formulations.
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