Elsewedy Heba S, Shehata Tamer M, Soliman Wafaa E
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Alhofuf 36362, Al-Ahsa, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, Zagazig University, Ash Sharqiyah, Zagazig 44519, Egypt.
Polymers (Basel). 2022 Jun 16;14(12):2436. doi: 10.3390/polym14122436.
Fusidic acid (FA) is an efficient anti-bacterial drug proven to be efficient against a wide range of bacteria. Nevertheless, the main restriction in its formulation is the limited solubility. To avoid such an obstacle, the drug is incorporated into the lipid core of the nanolipid formulation. Consequently, the present study was an attempt to formulate nanolipid preparation, mainly, solid lipid nanoparticle (SLN) integrating FA. FA-SLN was prepared using shea butter as a lipid phase owing to its reported anti-bacterial activity. Different FA-SLNs were fabricated using the central composite design (CCD) approach. The optimized formula was selected and integrated into a hydrogel base to be efficiently used topically. FA-SLN-hydrogel was evaluated for its character, morphology, in vitro release and stability. The formula was examined for irritation reaction and finally evaluated for its anti-bacterial performance. The optimized formula showed particle size 283.83 nm and entrapment 73.057%. The formulated FA-SLN-hydrogel displayed pH 6.2, viscosity 15,610 cP, spreadability 51.1 mm and in vitro release 64.6% following 180 min. FA-SLN-hydrogel showed good stability for three months at different conditions (room temperature and refrigerator). It exhibited no irritation reaction on the treated rats. Eventually, shea butter displayed a noteworthy effect against bacterial growth that improved the effect of FA. This would indicate prospective anti-bacterial activity of FA when combined with shea butter in SLN formulation as a promising nanocarrier.
夫西地酸（FA）是一种有效的抗菌药物，已被证明对多种细菌有效。然而，其制剂的主要限制是溶解度有限。为了避免这一障碍，该药物被纳入纳米脂质制剂的脂质核心中。因此，本研究试图制备纳米脂质制剂，主要是将FA整合到固体脂质纳米粒（SLN）中。由于乳木果油具有抗菌活性的报道，因此使用乳木果油作为脂质相来制备FA-SLN。采用中心复合设计（CCD）方法制备了不同的FA-SLN。选择优化后的配方并将其整合到水凝胶基质中以便局部有效使用。对FA-SLN水凝胶的特性、形态、体外释放和稳定性进行了评估。检测该配方的刺激反应，最后评估其抗菌性能。优化后的配方显示粒径为283.83nm，包封率为73.057%。所制备的FA-SLN水凝胶的pH值为6.2，粘度为15610cP，铺展性为51.1mm，180分钟后的体外释放率为64.6%。FA-SLN水凝胶在不同条件（室温及冰箱）下三个月内显示出良好的稳定性。它在受试大鼠上未表现出刺激反应。最终，乳木果油对细菌生长显示出显著作用，增强了FA的效果。这表明当FA与乳木果油在SLN制剂中作为一种有前景的纳米载体结合时，具有潜在的抗菌活性。
