Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER), Punjab, India.
J Drug Target. 2011 May;19(4):239-50. doi: 10.3109/1061186X.2010.492524. Epub 2010 Jun 14.
Leishmania parasite is an obligate intracellular parasite of the mammalian host and lives inside resident macrophages of liver and spleen. A high dose of paromomycin (PM) is required for the treatment.
Preparation and in vitro evaluation of PM loaded albumin microspheres (MS) (of size ≤ 5 µm) to target macrophages for treatment of visceral leishmaniasis.
PM loaded MS were prepared by spray-drying method using albumin as a polymer matrix and stabilized using heat treatment. These MS were evaluated for product yield, encapsulation efficiency, particle size, size distribution, contact angle, drug-polymer interactions, and for in vitro drug release. Fluorescent labeling and in vitro uptake of these MS was assessed in RAW 264.7 cell line.
PM loaded albumin MS were prepared with a mean particle size ≈3 µm. Free albumin content and contact angle study confirmed the stabilization of these MS. Release studies showed biphasic release pattern. Interaction studies ruled out any possibility of drug-polymer interaction. Uptake study in macrophage confirmed the suitability of prepared MS for macrophage targeting.
The proposed drug-delivery system was found suitable for targeting macrophages in vitro and may serve as an optimum carrier to target macrophages where Leishmania parasite resides.
利什曼原虫是哺乳动物宿主体内的必需内寄生原虫，存在于肝脏和脾脏的常驻巨噬细胞内。治疗需要高剂量的巴龙霉素（PM）。
制备并体外评价载巴龙霉素白蛋白微球（MS）（粒径≤5μm），以靶向巨噬细胞治疗内脏利什曼病。
采用喷雾干燥法，以白蛋白为聚合物基质，采用热稳定化方法制备载巴龙霉素 MS。对产物收率、包封效率、粒径、粒径分布、接触角、药物-聚合物相互作用以及体外药物释放进行评价。在 RAW 264.7 细胞系中评估这些 MS 的荧光标记和体外摄取。
载巴龙霉素白蛋白 MS 的平均粒径约为 3μm。游离白蛋白含量和接触角研究证实了这些 MS 的稳定性。释放研究显示出两相释放模式。相互作用研究排除了药物-聚合物相互作用的任何可能性。巨噬细胞摄取研究证实了所制备 MS 适合靶向巨噬细胞。
该递药系统被发现适合体外靶向巨噬细胞，可能是一种针对利什曼原虫驻留的巨噬细胞的理想载体。
