Alnasser Sulaiman Mohammed, Azam Faizul, Alqarni Mohammed H, Aodah Alhussain H, Hashmi Sana, Kamal Mehnaz, Meshal Alotaibi, Alam Aftab
Department of Pharmacology and Toxicology, Unaizah College of Pharmacy, Qassim University, Unaizah 51911, Saudi Arabia.
Department of Pharmaceutical Chemistry and Pharmacognosy, Unaizah College of Pharmacy, Qassim University, Unaizah 51911, Saudi Arabia.
Gels. 2023 Mar 15;9(3):228. doi: 10.3390/gels9030228.
In recent years, methicillin-resistant (MRSA) bacteria have seriously threatened the health and safety of the world's population. This challenge demands the development of alternative therapies based on plant origin. This molecular docking study ascertained the orientation and intermolecular interactions of isoeugenol within penicillin-binding protein 2a. In this present work, isoeugenol as an anti-MRSA therapy was selected by encapsulating it into a liposomal carrier system. After encapsulation into the liposomal carrier, it was evaluated for encapsulation efficiency (%), particle size, zeta potential, and morphology. The percentage entrapment efficiency (% EE) was observed to be 57.8 ± 2.89% with a particle size of 143.31 ± 7.165 nm, a zeta potential of (-)25 mV, and morphology was found to be spherical and smooth. After this evaluation, it was incorporated into a 0.5% Carbopol gel for a smooth and uniform distribution on the skin. Notably, the isoeugenol-liposomal gel was smooth on the surface with a pH of 6.4, suitable viscosity, and spreadability. Interestingly, the developed isoeugenol-liposomal gel was safe for human use, with more than 80% cell viability. The in vitro drug release study shows promising results with 75.95 ± 3.79% of drug release after 24 h. The minimum inhibitory concentration (MIC) was 8.236 µg/mL. Based on this, it can be concluded that encapsulating isoeugenol into the liposomal gel is a potential carrier for MRSA treatment.
近年来，耐甲氧西林金黄色葡萄球菌（MRSA）严重威胁着全球人口的健康与安全。这一挑战需要开发基于植物来源的替代疗法。这项分子对接研究确定了异丁香酚在青霉素结合蛋白2a内的取向和分子间相互作用。在本研究中，选择异丁香酚作为抗MRSA疗法，并将其封装到脂质体载体系统中。封装到脂质体载体后，对其包封率（%）、粒径、zeta电位和形态进行了评估。观察到包封率（%EE）为57.8±2.89%，粒径为143.31±7.165nm，zeta电位为（-）25mV，形态为球形且表面光滑。评估后，将其掺入0.5%的卡波姆凝胶中，以便在皮肤上均匀分布。值得注意的是，异丁香酚脂质体凝胶表面光滑，pH值为6.4，具有合适的粘度和铺展性。有趣的是，所开发的异丁香酚脂质体凝胶对人体使用安全，细胞活力超过80%。体外药物释放研究显示出有前景的结果，24小时后药物释放率为75.95±3.79%。最低抑菌浓度（MIC）为8.236µg/mL。基于此，可以得出结论，将异丁香酚封装到脂质体凝胶中是治疗MRSA的一种潜在载体。
