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用于眼部给药的托吡卡胺脂质体制剂的制备与评价。

Preparation and evaluation of liposomal formulations of tropicamide for ocular delivery.

作者信息

Nagarsenker M S, Londhe V Y, Nadkarni G D

机构信息

Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Mumbai, India.

出版信息

Int J Pharm. 1999 Nov 10;190(1):63-71. doi: 10.1016/s0378-5173(99)00265-3.

Abstract

Tropicamide, a mydriatic, cycloplegic drug was entrapped in liposomes. Liposomes were investigated by laser counting studies, transmission electron microscopy and differential scanning calorimetry for characterization. The precorneal clearance of liposomes was compared with solution by gamma-scintigraphy in the rabbit. The neutral liposomes failed to demonstrate significant enhancement in precorneal retention in comparison with aqueous solution. The potential of liposomes as an ophthalmic drug delivery system was investigated by comparing pupil dilatory effect of tropicamide by topical instillation, in the rabbit eye, of the solution and various drug-loaded liposomal forms, i.e. neutral liposomes, positively charged liposomes and neutral liposomes dispersed in 0.25% (w/v) polycarbophil gel. The positively charged liposomal formulation and liposomes dispersed in polycarbophil gel were found to be more effective than neutral liposomal dispersion when data were statistically treated at the 5% level of significance.

摘要

托吡卡胺,一种散瞳、睫状肌麻痹药物,被包裹于脂质体中。通过激光计数研究、透射电子显微镜和差示扫描量热法对脂质体进行表征研究。在兔眼中,通过γ闪烁扫描法比较脂质体与溶液的角膜前清除率。与水溶液相比,中性脂质体在角膜前滞留方面未显示出显著增强。通过比较在兔眼中局部滴入溶液和各种载药脂质体形式(即中性脂质体、带正电荷脂质体以及分散于0.25%(w/v)聚卡波非凝胶中的中性脂质体)时托吡卡胺的散瞳效果,研究了脂质体作为眼科药物递送系统的潜力。当在5%显著性水平进行统计学处理时,发现带正电荷脂质体制剂以及分散于聚卡波非凝胶中的脂质体比中性脂质体分散体更有效。

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