Department of Pharmaceutics, Parul Institute of Pharmacy, Faculty of Pharmacy, Parul University, Vadodara, Gujarat, India.
Department of Pharmaceutics, Srinath College of Pharmacy, Aurangabad, Maharashtra, India.
J Dermatolog Treat. 2022 Mar;33(2):885-896. doi: 10.1080/09546634.2020.1789043. Epub 2020 Jul 8.
Present investigation was aimed to develop aspasomal gel of Mometasone Furoate for the treatment of Psoriasis that are biologically active and deliver drug at controlled rate and decrease dosing frequency.
The vesicles were fabricated using film hydration method and optimized using 32 factorial Design. Prepared formulations were evaluated for percent drug loading, vesicle size, Zeta potential, polydispersity index and morphological studies. Gel was prepared using carbopol by loading optimized drug loaded asposomes and was evaluated for drug content, pH, viscosity and spreadability. The drug release study from the gel was done using dialysis membrane and goat skin. Anti- oxidant potency of the prepared aspasomal gel was determined by Ferric Reducing Assay whereas, in-vivo performance for inflammation and skin irritation was carried out using Wistar rats.
Optimized aspasomes demonstrated desired properties for entrapment efficiency (74.72 ± 1.8), vesicle size (282.9 ± 1.7), polydispersity index (0.2), zeta potential (-20.2 mV) with spherical shape. The results recorded for drug release from the optimized aspasomal gel exhibited sustained release (24h) compared to the marketed cream (5h). Depot formation of Mometasone furoate loaded aspasomal gel in the epidermis was confirmed by ex vivo skin penetration study by using fluorescent marker. In-vivo study revealed no any irritation and inflammation to the skin promoting drug delivery system to treat psoriasis.
In conclusion, Mometasone furoate loaded aspasomal gel releases the drug for longer duration of time and reduce dosing frequency, providing the new dimension for the treatment of psoriasis.
本研究旨在开发莫米松糠酸的无定形凝胶，用于治疗银屑病，这种凝胶具有生物活性，能够控制药物释放速度，减少给药频率。
采用薄膜水化法制备囊泡，并采用 32 因子设计进行优化。对制备的制剂进行药物载量、囊泡粒径、Zeta 电位、多分散指数和形态学研究。采用卡波姆制备凝胶，将优化的载药无定形囊泡负载，并对载药量、pH 值、黏度和铺展性进行评价。采用透析膜和山羊皮进行凝胶的体外释放研究。采用铁还原法测定制备的无定形囊泡凝胶的抗氧化能力，采用 Wistar 大鼠进行体内抗炎和皮肤刺激性试验。
优化后的无定形囊泡表现出良好的包封效率（74.72±1.8）、囊泡粒径（282.9±1.7）、多分散指数（0.2）和 Zeta 电位（-20.2mV），呈球形。与市售乳膏（5h）相比，优化后的无定形囊泡凝胶的药物释放呈现出持续释放（24h）的特点。荧光标记的离体皮肤渗透研究证实，莫米松糠酸负载的无定形囊泡凝胶在表皮中形成了储库。体内研究表明，该载药系统无皮肤刺激性和炎症反应，可用于治疗银屑病。
总之，莫米松糠酸负载的无定形囊泡凝胶可以延长药物释放时间，减少给药频率，为治疗银屑病提供了新的维度。
