Preparation and in vitro releasing of sirolimus-nanostructured lipid carriers dispension
-
摘要: 目的 优化西罗莫司纳米结构脂质载体(sirolimus nanostructured lipid carriers,SRL-NLC)分散液的处方,并考察其体外释放度。 方法 采用星点设计-效应面法(central composite design-response surface methodology,CCD-RSM)优化SRL-NLC分散液的处方,并以粒径、分布系数、载药量和包封率作为评价指标,采用正相透析袋法考察SRL-NLC分散液在0.4%SDS(十二烷基硫酸钠)溶液中的释放度。 结果 经优化的SAbstract: Objective To optimize the preparation and study in vitro releasing of SRL-NLC dispersion. Methods Central composite design-response surface methodology was used to optimize dispersion formulation,then in vitro releasing in 0.4% SDS(sodium lauryl sulfate) solution was explored by normal phase dialysis bag method. Results The optimal dispersion had PS(particle size):82.54nm,PI(polydisperity index):0.207, Zeta potential: -18.0 mv,DL (drug-loading): 1.829%, and EE(entrapment efficiency): 91.3%; SRL-NLC dispersion had a characterization of 60.1% accumulated releasing in 0.4%SDS solution. Conclusion The optimal formulation had good feasibility and reproducibility, in vitro releasing curve showed SRL-NLC dispersion had a characterization of 60.1% accumulated releasing in 0.4% SDS solution.
-
Key words:
- NLC /
- preparation /
- characterization /
- normal phase dialysis bag method /
- in vitro releasing
-
[1] 梁文权.生物药剂学与药物动力学[M].第3版.北京:人民教育出版社,2007:50. [2] Zhuang CY,Li N,Wang M,et al. Preparation and characterization of vinpocetine loaded nanostructured lipid carriers(NLC) for improved oral bioavailiability[J]. Int J Pharm,2010(394):183. [3] Zhang ZW,Bu HH,Gao ZW,et al. The characteristics and mechanism of simvastatin loaded lipid nanoparticles to increase oral bioavailability in rats[J]. Int J Pharm,2010(394):149. [4] Natalie LT,William NC,Christopher JHP. Lipid-based delivery systems and intestinal lymphatic drug transport:A mechanistic update[J]. Adv Drug Deli Rev,2008(60):712. [5] 王 娟,张 晶,宋洪涛,等. 西罗莫司单层高分子渗透泵控释片的制备及其体外释放特性研究[J]. 中国药房,2010,21(37):3503. [6] David JH.Oral lipid-based formulations[J]. Adv Drug Deli Rev,2007(59):668. -
点击查看大图
计量
- 文章访问数: 5619
- HTML全文浏览量: 254
- PDF下载量: 630
- 被引次数: 0
下载:
