制备新型载庆大霉素固体脂质微球及其体内外评价。
Preparation of novel solid lipid microparticles loaded with gentamicin and its evaluation in vitro and in vivo.
机构信息
School of Pharmacy, University of Nigeria, Nsukka 410001, Nigeria.
出版信息
J Microencapsul. 2012;29(3):296-307. doi: 10.3109/02652048.2011.651495. Epub 2012 Jan 27.
OBJECTIVE
To formulate and evaluate solid-reversed-micellar-solution (SRMS)-based solid lipid microparticles (SLMs) for intramuscular administration of gentamicin.
METHODS
SRMS formulated with Phospholipon® 90G and Softisan® 154 were used to prepare gentamicin-loaded SLMs. Characterizations based on size and morphology, stability and encapsulation efficiency (EE%) were carried out on the SLMs. In vitro release of gentamicin from the SLMs was performed in phosphate buffer while in vivo release studies were conducted in rats.
RESULTS
Maximum EE% of 90.0, 91.6 and 83.0% were obtained for SLMs formed with SRMS 1:1, 1:2 and 2:1, respectively. Stable, spherical and smooth SLMs of size range 9.80 ± 1.46 µm to 33.30 ± 6.42 µm were produced. The release of gentamicin in phosphate buffer varied widely with the lipid contents. Moreover, significant (p < 0.05) amount of gentamicin was released in vivo from the SLMs.
CONCLUSION
SRMS-based SLMs would likely offer a reliable means of delivering gentamicin intramuscularly.
目的
制备并评价基于固相反胶束溶液（SRMS）的硫酸庆大霉素固体脂质微球（SLMs），用于肌肉内给药。
方法
采用 Phospholipon® 90G 和 Softisan® 154 制备 SRMS，用于制备硫酸庆大霉素载药 SLMs。对 SLMs 进行粒径和形态、稳定性以及包封效率（EE%）的特征分析。在磷酸盐缓冲液中进行硫酸庆大霉素的体外释放研究，在大鼠体内进行释放研究。
结果
采用 SRMS 1:1、1:2 和 2:1 制备的 SLMs 的最大 EE%分别为 90.0%、91.6%和 83.0%。制得的 SLMs 稳定、呈球形且表面光滑，粒径范围为 9.80±1.46μm 至 33.30±6.42μm。在磷酸盐缓冲液中，硫酸庆大霉素的释放情况因脂质含量而异。此外，SLMs 体内显著（p<0.05）释放了硫酸庆大霉素。
结论
基于 SRMS 的 SLMs 可能为肌肉内给予硫酸庆大霉素提供一种可靠的方法。
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