Lala S, Nandy A K, Mahato S B, Basu M K
Dept. of Chemistry, School of Tropical Medicine, Kolkata 700 073, India.
Indian J Biochem Biophys. 2003 Jun;40(3):169-74.
An antileishmanial compound, 14-deoxy-11-oxo-andrographolide, a derivative of andrographlide, isolated from the Indian medicinal plant Andrographis paniculata was evaluated for efficacy in free form and in different vesicular delivery modes on hamster model of Leishmaniasis. The subcutaneous injection of free drug reduced the spleen parasite load by 39%, whereas for drug incorporated in liposomes, niosomes and microspheres, reductions in the parasite load were 78%, 91% and 59%, respectively. Moreover, the drug in various delivery modes, particularly in liposomal and niosomal forms, showed no apparent immediate toxicity. Although an inverse linear relationship between the size of carriers and per cent efficacy in reduction of spleen parasite load was established, involvement of other factors such as drug release profiles or rates remains an open question. Because of greater efficacy and lesser toxicity, liposomal, niosomal and possibly microsphere-incorporated 14-deoxy-11-oxo-andrographolide might have clinical application to combat visceral Leishmaniasis.
从印度药用植物穿心莲中分离出的一种抗利什曼原虫化合物——14-脱氧-11-氧代穿心莲内酯,是穿心莲内酯的衍生物,对其游离形式以及不同囊泡递送模式在利什曼病仓鼠模型中的疗效进行了评估。皮下注射游离药物可使脾脏寄生虫负荷降低39%,而对于包裹在脂质体、非离子表面活性剂泡囊和微球中的药物,寄生虫负荷的降低率分别为78%、91%和59%。此外,各种递送模式下的药物,特别是脂质体和非离子表面活性剂泡囊形式的药物,未显示出明显的即时毒性。虽然在载体大小与脾脏寄生虫负荷降低百分比之间建立了反向线性关系,但药物释放曲线或速率等其他因素的影响仍是一个悬而未决的问题。由于疗效更高且毒性更小,脂质体、非离子表面活性剂泡囊以及可能包裹有14-脱氧-11-氧代穿心莲内酯的微球可能具有对抗内脏利什曼病的临床应用价值。