透皮药修饰脂质体的制备及评价

Ghule Mm, Bhoyar Gs
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引用次数: 14

摘要

目的:普拉克索被广泛应用于抗帕金森病的治疗,但其存在多种副作用,目的是研究普拉克索的脂质体给药,从而降低其毒副作用,提高其生物利用度、疗效和治疗指标。进一步研究改变给药方式,确定硬脂胺和胆酸钠含量对脂质体特性的影响。方法:采用普拉克索、磷脂酰胆碱、胆固醇、硬脂胺和胆酸钠按不同比例制备改性脂质体。这些脂质体采用薄膜水合法制备,并进行了囊泡大小、药物包裹、体外释放、zeta电位、离体研究等表征。结果:通过研究药物脂质比对药物囊泡包埋的影响,初步制备了载普拉克索脂质体。脂质体的药物承载能力始终取决于脂质体组成中采用的药物脂质比,然后通过添加硬脂胺和胆酸钠来确定渗透增强剂。对优化后的脂质体批次进行了修饰。进一步的修饰脂质体被评估包裹效率,体外释放,zeta电位和囊泡大小。因此,带正电荷的脂质体有望作为普拉克索药物经皮给药系统的载体。结论:硬脂胺的加入使普拉克索的包封率增加,这是由于其对膜填料的硬化作用所致。改性普拉克索脂质体有望成为治疗帕金森病的有效载体。
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Formulation and Evaluation of Modified Liposome for Transdermal Drug
Objective: Pramipexole is widely used in the treatment of anti-Parkinson’s, however it is associated with several side effects so the objective was to develop liposomal drug delivery of Pramipexole and thus reduce its side effect and toxicity and improve bioavaibility, efficacy and therapeutic index. Further study to modify drug delivery and to determine effect of stearylamine and sodium cholate content on the liposomal characteristics was investigated.Methods: In the present study the modified liposomes were prepared by using Pramipexole, phosphotidylcholine, cholesterol, stearylamine and sodium cholate in different ratio. These liposomes were prepared using thin film hydration method and characterized for vesicle size, drug entrapment studies, in-vitro release, and zeta potential, ex-vivo study.Results: The preparation of pramipexole loaded liposome was initiated by studying the influencing of drug lipid ratio on drug entrapment in vesicles. The drug bearing capacity of liposome was found to be invariably dependent on drug lipid ratio employed in liposomal composition, then formulation addition of stearylamine and sodium cholate to determine penetration enhancer. Modified liposome of optimized liposomal batches was formulated. Further modified liposomes were evaluated for entrapment efficiency, in-vitro release, zeta potential, and vesicle size. Thus, positive charged liposome seen to be promising as carrier for pramipexole drug thought transdermal drug delivery system.Conclusion: Incorporation of stearylamine enhanced the percent entrapment of pramipexole owing to rigidizaton effect on the membrane packing. Modified Liposomes of pramipexole can be promising carriers for the effective treatment of Parkinson’s.
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