Department of Pharmaceutics, Shri D.D. Vispute College of Pharmacy and Research Center, New Panvel, Raigad, Maharashtra, 410206, India.
Recent Adv Drug Deliv Formul. 2023;17(4):300-313. doi: 10.2174/0126673878259437231031114907.
Mometasone Furoate (MF) is a corticosteroid (glucocorticoid) used to treat eczema, psoriasis, allergies, and rash on the skin; also used to reduce itching, redness, and swelling (inflammation). It has been reported that the bioavailability of MF is less than 11% when given via the nasal route. Encapsulating the drug in niosomes can improve the active pharmaceutical ingredient's bioavailability by enhancing both physical and biological stability.
The goal of the study is to develop, a non-ionic surfactant-based vesicular system, by loading mometasone furoate, and introducing it into a gel-based formulation by utilizing an appropriate gelling agent, and performing its evaluation.
The niosome vesicle was prepared by vacuum rotary evaporation method (Thin film hydration method). Gel was prepared using the dispersion method and in-vitro drug diffusion studies using Franz-diffusion cells.
According to the results of the experiments conducted for the study, Mometasone Furoate niosomal gel was prepared utilizing Mometasone Furoate niosomes that were made using the thin film hydration process, Cholesterol, and Span 60, and loaded in various amounts of Carbopol as a geling agent. The niosomes' zeta potential was found to be -24 mV, showing that the formulation is stable. The polydispersity index (PDI) was found to be 0.409 and the average size of niosomes to be 252.7 nm. The performance of the gel of the optimized formulations containing 2% Carbopol showed in vitro diffusion for 7 hours and an increased flux rate as compared to the plain MF.
The experiments carried out during the study led to the conclusion that the thin-film hydration method was suitable for the formation of the MF-niosomes by using Span 60 and Cholesterol (2:1). The gel formulation containing 2% Carbopol indicated better in vitro diffusion following the Higuchi model across all niosomal gel formulations. Niosomal gel can be regarded as the best vesicular carrier for the efficient distribution of mometasone furoate via the transdermal route.
糠酸莫米松（MF）是一种皮质类固醇（糖皮质激素），用于治疗湿疹、银屑病、过敏和皮肤皮疹；也用于减少瘙痒、发红和肿胀（炎症）。据报道，MF 经鼻给药的生物利用度不到 11%。将药物包封在类脂体中可以通过增强物理和生物稳定性来提高活性药物成分的生物利用度。
本研究的目的是开发一种基于非离子表面活性剂的囊泡系统，通过加载糠酸莫米松，并利用适当的成胶剂将其引入凝胶制剂，并对其进行评价。
采用真空旋转蒸发法（薄膜水化法）制备类脂体囊泡。凝胶采用分散法制备，采用 Franz 扩散池进行体外药物扩散研究。
根据该研究进行的实验结果，利用薄膜水化法制备的 MF 类脂体囊泡、胆固醇和司盘 60 制备 MF 载药囊泡，并以不同载药量的卡波姆作为成胶剂载入载药囊泡。囊泡的zeta 电位为-24 mV，表明制剂稳定。多分散指数（PDI）为 0.409，囊泡平均粒径为 252.7nm。含 2%卡波姆的优化配方凝胶的体外扩散性能在 7 小时内表现出较好的扩散性能，通量率高于普通 MF。
研究中进行的实验表明，薄膜水化法适用于使用司盘 60 和胆固醇（2:1）形成 MF-类脂体。含 2%卡波姆的凝胶配方在所有载药囊泡凝胶配方中均表现出更好的体外扩散性能，符合 Higuchi 模型。载药囊泡凝胶可以被认为是通过透皮途径高效递运糠酸莫米松的最佳囊泡载体。
