Mouhram Nadein Abdelsalam, Mosallam Shaimaa, Hassan Mariam, El-Gazar Amira A, El-Nabarawi Mohamed A, Fayez Sahar M
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza, Egypt.
Int J Pharm. 2025 Feb 10;670:125115. doi: 10.1016/j.ijpharm.2024.125115. Epub 2024 Dec 20.
Oleic acid liposomes (OALs) are novel vesicular carriers ofunsaturated fatty acids and their corresponding ionized species, arranged within an enclosed lipid bilayer. This study aimed to encapsulate moxifloxacin HCl (MOX), a broad-spectrum antibacterial drug into OALs for effective treatment of Methicillin-resistant Staphylococcus aureus (MRSA) infection through topical application. Various OALs were formulatedby combining varied quantities of phosphatidylcholine (PC), oleic acid (OA), and cholesterol (CH) with 50 mg of MOX. The OALs were produced utilizing varying sonication durations. MOX-loaded OALs were formulated using the thin film hydration method by applying (2) a full factorial design utilizing the Design-Expert® software. The formula for MOX-loaded OALs was OAL13, which consisted of 200 mg of PC and 20 mg of OA. The mixture was sonicated for 5 min. The OAL13 exhibited spherical vesicles with a small diameter and a smooth outer surface. Additionally, the entrapment efficiency was measured to be 75.00 ± 1.41 %, the particle size was 234.65 ± 4.74 nm, the polydispersity index was 0.53 ± 0.01, and the zeta potential was -38.50 ± 0.42 mV. The OAL13 formula exhibited an extended release profile. Moreover, the antibiofilm activity of OAL13 gel and MOX-loaded liposomes gel against MRSA infection demonstrates greater activity than the MOX gel at the maximum concentration used (MIC/2). Furthermore, the in-vivo study showed that OAL13 improved MOX's antimicrobial and immunomodulatory effects against MRSA infection by increasing TLR-2 and IL-1β, as well as their downstream molecules NF-κB and TNF-α. Moreover, the histopathological examination conducted by a skin irritation test has verified the safety of OAL13. Overall, the results demonstrated the significant efficacy of MOX-loaded OALs in the treatment of MRSA infected wounds when applied topically.
油酸脂质体(OALs)是不饱和脂肪酸及其相应离子化形式的新型囊泡载体,排列在封闭的脂质双层内。本研究旨在将广谱抗菌药物盐酸莫西沙星(MOX)包封到OALs中,通过局部应用有效治疗耐甲氧西林金黄色葡萄球菌(MRSA)感染。通过将不同量的磷脂酰胆碱(PC)、油酸(OA)和胆固醇(CH)与50mg MOX混合来制备各种OALs。利用不同的超声处理时间制备OALs。采用薄膜水化法,通过使用Design-Expert®软件进行全因子设计来制备载MOX的OALs。载MOX的OALs的配方为OAL13,由200mg PC和20mg OA组成。将混合物超声处理5分钟。OAL13呈现出小直径且外表面光滑的球形囊泡。此外,测得包封率为75.00±1.41%,粒径为234.65±4.74nm,多分散指数为0.53±0.01,ζ电位为-38.50±0.42mV。OAL13配方呈现出缓释特性。此外,OAL13凝胶和载MOX脂质体凝胶对MRSA感染的抗生物膜活性在所用最大浓度(MIC/2)下比MOX凝胶表现出更大的活性。此外,体内研究表明,OAL13通过增加TLR-2和IL-1β及其下游分子NF-κB和TNF-α,改善了MOX对MRSA感染的抗菌和免疫调节作用。此外,皮肤刺激性试验进行的组织病理学检查证实了OAL13的安全性。总体而言,结果表明局部应用载MOX的OALs在治疗MRSA感染伤口方面具有显著疗效。