Cyclosporine a-nanosuspension: formulation, characterization and in vivo comparison with a marketed formulation.
Cyclosporine a-nanosuspension: formulation, characterization and in vivo comparison with a marketed formulation.
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DOI：
10.3797/scipharm.0908-12
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发表时间：
2010-04
影响因子：
2.5
通讯作者：
Vaghani SS
中科院分区：
文献类型：
--
作者：
Nakarani M;Patel P;Patel J;Patel P;Murthy RS;Vaghani SS
使用珍珠研磨技术，使用氧化锆珠作为研磨介质、泊洛沙姆407作为稳定剂和蒸馏水作为水性介质制备环孢霉素A纳米混悬剂。从粒度分布、表面形态、药物-表面活性剂相互作用、药物含量、饱和溶解度、渗透压和稳定性等方面对优化的处方进行了表征。由泊洛沙姆结合的环孢菌素A组成的平均直径为213 nm的纳米颗粒显示出球形形状，与母体药物相比，饱和溶解度增加了5.69倍。发现该制剂与血液等渗并且在2-8°C下稳定长达3个月。在白化病大鼠中进行了体内研究，并将药代动力学参数与市售制剂进行了比较，结果表明制备的制剂的结果优于市售制剂。
Cyclosporine A-nanosuspensions were prepared using zirconium oxide beads as a milling media, Poloxamer 407 as a stabilizer and distilled water as an aqueous medium using the Pearl Milling technique. The optimized formulation was characterized in terms of particle size distribution, surface morphology, drug-surfactant interaction, drug content, saturation solubility, osmolarity, and stability. The nanoparticles consisting of Poloxamer-bound cyclosporin A with a mean diameter of 213 nm revealed a spherical shape and 5.69 fold increased saturation solubility as compared to the parent drug. The formulation was found to be iso-osmolar with blood and stable up to 3 months at 2–8°C. In-vivo studies were carried out in albino rats and the pharmacokinetic parameters were compared with a marketed formulation, which indicated better results of the prepared formulation than the marketed one.