Drug Delivery Research Unit, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria.
Department of Biochemistry, Faculty of Biological Sciences, University of Nigeria, Nsukka, Nigeria.
Mater Sci Eng C Mater Biol Appl. 2019 Apr;97:245-253. doi: 10.1016/j.msec.2018.12.041. Epub 2018 Dec 13.
Erythromycin-loaded solid lipid microparticles (SLM) based on solidified reverse micellar solution (SRMS) as an oral delivery formulation was studied. Hot homogenization technique was employed to prepare erythromycin stearate-loaded SLMs using blends of Softisan® 154 and Phospholipon® 90H or beeswax in the ratio of 1:2, and characterized in vitro. Antibacterial evaluation of the formulations was carried out by agar diffusion technique against some selected clinical isolates of bacterial. Preliminary pharmacokinetic study was performed after oral administration in male Albino rats. The results of matrix contain Softisan® 154 and phospholipon® 90H (1:2) showed that erythromycin-loaded SLM was smooth; particle size ranged from 10.3 ± 11.24 μm to 18.1 ± 10.11 μm and maximum encapsulation efficiency and loading capacity were 95.11 ± 0.3% and 43.22 ± 0.1 mg, respectively. While that of beeswax- containing matrix showed maximum particle size of 18.9 ± 21.10 μm, maximum encapsulation efficiency of 89.01 ± 0.11% and loading capacity of 39.02 ± 0.12 mg. All the formulations had prolonged release and antibacterial activity. Significantly (p > 0.05), prolonged plasma erythromycin concentration was obtained in the optimized formulation (>14 h) compared with commercial sample of erythromycin tablet (10h). Erythromycin stearate-loaded SLMs formulation could serve as an alternative to conventional oral formulation of erythromycin.
基于固态反胶束溶液（SRMS）的红霉素固体脂质纳米粒（SLM）作为口服递药制剂进行了研究。采用热匀化技术，使用 Softisan® 154 和 Phospholipon® 90H 或蜂蜡以 1:2 的比例制备红霉素硬脂酸酯载药 SLM，并进行体外特性评价。采用琼脂扩散法对部分临床分离菌进行了制剂的抗菌评价。在雄性白化大鼠中进行了口服给药后的初步药代动力学研究。结果表明，含有 Softisan® 154 和 Phospholipon® 90H（1:2）的基质的载药 SLM 呈光滑状；粒径范围为 10.3±11.24μm 至 18.1±10.11μm，最大包封效率和载药量分别为 95.11±0.3%和 43.22±0.1mg。而含有蜂蜡的基质的载药 SLM 的最大粒径为 18.9±21.10μm，最大包封效率为 89.01±0.11%，载药量为 39.02±0.12mg。所有制剂均具有缓释和抗菌活性。与红霉素片剂的商业样品（10h）相比，优化的制剂（>14h）可显著延长（p>0.05）血浆中红霉素的浓度。红霉素硬脂酸酯载药 SLM 制剂可作为红霉素常规口服制剂的替代品。
