Kenechukwu Franklin C, Momoh Mumuni A, Umeyor Emmanuel C, Uronnachi Emmanuel M, Attama Anthony A
Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Enugu State, Nigeria.
Department of Pharmaceutics and Pharmaceutical Technology, Nnamdi Azikiwe University, Awka, Anambra State, Nigeria.
Int J Pharm Investig. 2016 Jan-Mar;6(1):32-8. doi: 10.4103/2230-973X.176473.
The aim of this study was to formulate solidified reverse micellar solution (SRMS)-based solid lipid microparticles (SLMs) using homolipids from tallow fat (Bos indicus) and evaluate its potential for enhanced delivery of gentamicin.
SLMs were formulated by melt-emulsification using SRMS (15% w/w Phospholipon(®) 90G in 35% w/w Bos indicus), polyethylene glycol 4000 (PEG) and gentamicin (1.0, 2.0, 3.0% w/w), and characterized with respect to size, morphology, encapsulation efficiency % and pH-dependent stability. The in vitro release of gentamicin from the SLMs was performed in phosphate buffer (pH 7.4) while bioevaluation was carried out using clinical isolates of Staphylococcus aureus and Escherichia coli.
Results showed that the lipid matrix accommodated gentamicin in a concentration-dependent manner, and that stable and spherical SLMs with size range of 18.62 ± 1.24-20.59 ± 1.36 μm and 21.35 ± 1.57-50.62 ± 2.37 μm respectively for unloaded and drug-loaded formulations were obtained. The in vitro drug release studies revealed that SRMS-based SLMs could better be used to control the release of gentamicin than gentamicin injection. Results of sensitivity test revealed that the SLMs time-dependently and capacity-limitedly produced greater inhibition zone diameters (IZDs) than the standards, an indication of improved bioactivity against the test organisms, with greater IZDs against S. aureus than E. coli. Overall, SLMs containing 2% w/w SRMS, 3% w/w gentamicin and PEG 4000 entrapped the highest amount of drug, achieved complete drug release and gave highest IZD against the organisms within 420 min, while plain gentamicin gave the least.
This research has shown that SLMs based on Bos indicus and P90G is a potential carrier system for dissolution and bioactivity enhancement of gentamicin.
本研究旨在使用来自瘤牛脂肪（印度牛）的同质性脂质制备基于固化反胶束溶液（SRMS）的固体脂质微粒（SLMs），并评估其增强庆大霉素递送的潜力。
通过熔融乳化法，使用SRMS（35%重量/重量的印度牛中含15%重量/重量的磷脂酰胆碱90G）、聚乙二醇4000（PEG）和庆大霉素（1.0%、2.0%、3.0%重量/重量）制备SLMs，并对其粒径、形态、包封率%和pH依赖性稳定性进行表征。在磷酸盐缓冲液（pH 7.4）中进行庆大霉素从SLMs的体外释放实验，同时使用金黄色葡萄球菌和大肠杆菌的临床分离株进行生物活性评估。
结果表明脂质基质以浓度依赖的方式容纳庆大霉素，未载药和载药制剂分别获得了稳定且呈球形的SLMs，粒径范围分别为18.62±1.24 - 20.59±1.36μm和21.35±1.57 - 50.62±2.37μm。体外药物释放研究表明，基于SRMS的SLMs比庆大霉素注射液能更好地控制庆大霉素的释放。敏感性测试结果显示，SLMs随时间和容量限制产生的抑菌圈直径（IZDs）比标准品更大，表明对测试微生物的生物活性有所提高，对金黄色葡萄球菌的IZDs比对大肠杆菌的更大。总体而言，含有2%重量/重量SRMS、3%重量/重量庆大霉素和PEG 4000的SLMs包封的药物量最高，在420分钟内实现了药物的完全释放，并对受试微生物产生了最高的IZD，而普通庆大霉素产生的IZD最小。
本研究表明基于印度牛和P90G的SLMs是一种用于提高庆大霉素溶解性和生物活性的潜在载体系统。
