Fabrication and Release Kinetics of Liposomes Containing Leuprolide Acetate

Sudipta Das, A. Samanta, Koushik Bankura, D. Roy, A. Nayak
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引用次数: 1

Abstract

The present work is focused on the preparation and in vitro release kinetics of liposomal formulation of Leuprolide Acetate. In this work, “Thin Lipid Film Hydration Method” was used for preparation of Leuprolide Acetate loaded liposomes. Prepared liposomal formulations of Leuprolide acetate was evaluated by drug entrapment study, in-vitro drug release kinetics and stability studies. The percentage drug entrapment of Leuprolide acetate for F1 and F2 formulations were found to be 78.14 ± 0.67 and 66.70 ± 0.81% respectively. In-vitro drug release study of liposomal formulations had shown zero order release pattern. Regression co-efficient (R2) value of Zero order kinetics for F1 and F2 formulations were 0.9912 and 0.9676 respectively. After storing formulations for 1 month, stability testing was done at 40C.It was found that all batches were stable. These liposomal formulations of Leuprolide acetate can be formulated for parenteral application to treat prostate cancer and in women, to treat symptoms of endometriosis (overgrowth of uterine lining outside of the uterus) or uterine fibroids.
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含醋酸Leuprolide脂质体的制备及释放动力学
本文研究了醋酸左连翘酯脂质体制剂的制备及其体外释放动力学。本研究采用“薄脂膜水合法”制备醋酸Leuprolide负载脂质体。通过药物包埋研究、体外释药动力学和稳定性研究对制备的醋酸Leuprolide脂质体制剂进行了评价。F1和F2制剂的药物包封率分别为78.14±0.67和66.70±0.81%。脂质体制剂体外释药研究呈零级释放模式。F1和F2配方的零级动力学回归系数(R2)分别为0.9912和0.9676。贮存1个月后,在40℃下进行稳定性试验。发现所有批次都是稳定的。醋酸Leuprolide的这些脂质体制剂可配制用于肠外应用治疗前列腺癌和妇女,用于治疗子宫内膜异位症(子宫外子宫内膜过度生长)或子宫肌瘤的症状。
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