PSG College of Pharmacy, Department of Pharmaceutics , Peelamedu, Coimbatore - 641004, Tamil Nadu , India.
Expert Opin Drug Deliv. 2014 Sep;11(9):1351-65. doi: 10.1517/17425247.2014.915310. Epub 2014 May 21.
The major objective is to target diethylcarbamazine citrate (DEC) to the lymphatics and to increase its retention time. The effect of various excipients on the physicochemical characteristics of the nanoparticles was also studied.
Solid lipid nanoparticles (SLNs) of DEC were prepared by ultrasonication by varying the concentrations of compritol 888 ATO, poloxamer 188 and soya lecithin. The SLNs were evaluated for size, shape, texture, surface charge, physical nature of the entrapped drug, entrapment efficiency and in vitro drug release. In vivo animal studies were carried out to estimate the pharmacokinetic parameters in blood and drug concentration in lymph after oral administration.
The size of the spherical particles was in the range of 27.25 ± 3.43 nm to 179 ± 3.08 nm and a maximum entrapment efficiency of 68.63 ± 1.53% was observed. In vitro release studies in pH 7.4 PBS displayed a rapid release and the maximum time taken for the complete drug to release was 150 min. In vivo studies indicated an enhancement in the amount of drug that reached lymphatics when administered via SLNs.
Targeting of DEC to the lymphatics is possible through SLNs and the retention time in the lymphatics can also be enhanced.
主要目标是将柠檬酸双羟萘酸噻嘧啶（DEC）靶向至淋巴管，并延长其在其中的驻留时间。还研究了各种赋形剂对纳米粒理化特性的影响。
通过超声处理，用不同浓度的 Compritol 888 ATO、泊洛沙姆 188 和大豆卵磷脂来制备 DEC 的固体脂质纳米粒（SLN）。对 SLN 进行了粒径、形态、质地、表面电荷、包封药物的物理性质、包封效率和体外药物释放的评估。进行了体内动物研究，以估计口服给药后血液中的药代动力学参数和淋巴中的药物浓度。
球形颗粒的粒径范围为 27.25±3.43nm 至 179±3.08nm，观察到最大包封效率为 68.63±1.53%。在 pH7.4 PBS 中的体外释放研究显示出快速释放，完全释放药物所需的最大时间为 150min。体内研究表明，通过 SLN 给药时，到达淋巴管的药物量增加。
通过 SLN 可以将 DEC 靶向至淋巴管，并且可以延长其在淋巴管中的驻留时间。
