Pharmacy Department, Faculty of Pharmacy, Kalabhavan Campus, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat-390001, India.
Pharmacy Department, Faculty of Pharmacy, Kalabhavan Campus, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat-390001, India.
Int J Pharm. 2022 Aug 25;624:122045. doi: 10.1016/j.ijpharm.2022.122045. Epub 2022 Jul 22.
Omiganan is a novel 12 amino acid synthetic cationic peptide from the cathelicidin family. Omiganan possesses antimicrobial action against a wide range of microbes, including gram-positive and gram-negative bacteria and fungi. Omiganan mainly acts by depolarizing the cytoplasmic membrane, resulting in cellular disruption and death. Apart from its antimicrobial effect, Omiganan also has anti-inflammatory activity. The present investigation aimed to evaluate and compare the efficacy of Omiganan liposomal gel with conventional formulations (Omiganan gel and lotion) in atopic dermatitis (AD) and psoriasis mice animal models. Liposomes encapsulating Omiganan were prepared using the reverse-phase evaporation technique and incorporated into Carbopol 934P gel. The optimized Omiganan liposomes were then characterized for various physicochemical parameters such as vesicle size, shape and surface morphology, zeta-potential, rheological parameters, in-vitro drug release, ex-vivo skin permeation/deposition, in-vitro antimicrobial activity, proteolytic stability, and cellular toxicity and uptake studies. Liposomes exhibited 72 % encapsulation with 7.8 % loading efficacy, a vesicle size, and zeta potential of 120 nm and - 17.2 mv, respectively. Moreover, Omiganan liposomal gel demonstrated controlled release and a better permeation profile than conventional formulations. A substantial reduction in levels of pro-inflammatory cytokines and improvement in AD and psoriatic lesions were achieved by Omiganan liposomal gel compared to Omiganan gel and lotion-based formulations. The present study confirms that Omiganan liposomal formulation can be an effective, safe, and novel alternative treatment approach in atopic dermatitis and psoriasis.
奥米加能是一种新型的 12 个氨基酸合成阳离子肽,来自于抗菌肽家族。奥米加能对多种微生物具有抗菌作用,包括革兰氏阳性和革兰氏阴性细菌和真菌。奥米加能主要通过去极化细胞质膜起作用,导致细胞破裂和死亡。除了其抗菌作用外,奥米加能还具有抗炎活性。本研究旨在评估和比较奥米加能脂质体凝胶与传统制剂(奥米加能凝胶和洗剂)在特应性皮炎(AD)和银屑病小鼠动物模型中的疗效。采用反相蒸发技术制备包封奥米加能的脂质体,并将其掺入卡波姆 934P 凝胶中。然后对优化的奥米加能脂质体进行各种物理化学参数的表征,如囊泡大小、形状和表面形态、Zeta 电位、流变学参数、体外药物释放、体外皮肤渗透/沉积、体外抗菌活性、蛋白水解稳定性以及细胞毒性和摄取研究。脂质体的包封率为 72%,载药量为 7.8%,囊泡大小和 Zeta 电位分别为 120nm 和-17.2mv。此外,奥米加能脂质体凝胶表现出优于传统制剂的控释和更好的渗透特性。与奥米加能凝胶和洗剂制剂相比,奥米加能脂质体凝胶可显著降低促炎细胞因子水平,并改善 AD 和银屑病病变。本研究证实,奥米加能脂质体制剂可作为特应性皮炎和银屑病的一种有效、安全和新型的替代治疗方法。