皮内给药氟西诺酮凝胶脂质体的制备及评价

G. Rao, R. Murthy
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引用次数: 1

摘要

制备了羟丙基甲基纤维素(HPMC) K4M凝胶,其中含有游离氟西洛酮丙酮、脂质体包封氟西洛酮丙酮以及药物与脂质的物理混合物,并在大鼠皮肤上进行了体外药物释放研究,以确定扩散参数。对数据进行分析,计算药物在皮肤(Qm)和血液(Csf)中的残留量以及Qm与Csf的比值。用这些制剂在人体志愿者身上进行的体内皮肤漂白试验显示,脂质体凝胶制剂的漂白分数很低,这表明脂质体包裹的药物在血液中的吸收很低,导致药物在皮肤中的积累。这一结果与体外实验中获得的高Qm/Csf比率一致。以药物与磷脂酰胆碱、胆固醇按4:8:1的比例配制的脂质体包封氟西奈酮凝胶,Qm/Csf比值最高,漂烫评分最低。结果表明含有脂质体包封药物的外用制剂在皮肤中选择性积累药物的潜力。
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Preparation and Evaluation of Liposomal Flucinolone Acetonide Gel for Intradermal Delivery
Hydroxypropyl methylcellulose (HPMC) K4M gels containing free flucinolone acetonide, liposomal-encapsulated flucinolone acetonide and physical mixture of the drug and lipids were prepared and evaluated in in-vitro drug release studies using rat skin to determine diffusion parameters. Data were analysed to calculate the quantity of the drug remaining in the skin (Qm) and in the blood (Csf) and the ratio of Qm to Csf. The in-vivo skin blanching assay performed with these formulations in human volunteers showed low blanching scores for liposomal gel formulations indicating low absorption of the liposomal-encapsulated drug into the blood stream and leading to the accumulation of the drug in the skin. This result is in agreement with the high Qm/Csf ratios obtained in the in-vitro experiments. Of all the formulations, gels containing liposomal-encapsulated flucinolone acetonide, prepared with drug, phosphatidyl choline and cholesterol in the ratio of 4:8:1, had the highest Qm/Csf ratio and minimum blanching score. The results indicate the potential of topical preparations containing liposomal-encapsulated drugs for selective accumulation of the drug in the skin.
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