School of Pharmacy and Technology Management, SVKM's Narsee Monjee Institute of Management Studies (NMIMS) Deemed-to-University, Green Industrial Park, TSIIC, Jadcherla, Hyderabad 509301, India.
School of Pharmacy and Technology Management, SVKM's Narsee Monjee Institute of Management Studies (NMIMS) Deemed-to-University, Shirpur 425405, India.
Ann Pharm Fr. 2024 Sep;82(5):830-839. doi: 10.1016/j.pharma.2024.04.006. Epub 2024 Apr 22.
.In this study, we investigated the potential of meloxicam (MLX) developed as transferosomal gel as a novel lipidic drug delivery system to address osteoarthritis (OTA), a degenerative joint disease that causes pain and stiffness. By incorporating meloxicam into a transferosomal gel, our aim was to provide a targeted and efficient delivery system capable of alleviating symptoms and slowing down the progression of OTA.
Classical lipid film hydration technique was utilized to formulate different transferosomal formulations. Different transferosomal formulations were prepared by varying the molar ratio of phospholipon-90H (phosphodylcholine) to DSPE (50:50, 60:40, 70:30, 80:20, and 90:10) and per batch, 80mg of total lipid was used. The quality control parameters such as entrapment efficiency, particle size and morphology, polydispersity and surface electric charge, in vitro drug release, ex vivo permeation and stability were measured.
The optimized transferosomal formulations revealed a small vesicle size (121±12nm) and greater MLX entrapment (68.98±2.3%). Transferosomes mediated gel formulation MLX34 displayed pH (6.3±0.2), viscosity (6236±12.3 cps), spreadability (13.77±1.77 gm.cm/sec) and also displayed sustained release pattern of drug release (81.76±7.87% MLX released from Carbopol-934 gel matrix in 24h). MLX34 revealed close to substantial anti-inflammatory response, with ∼81% inhibition of TNF-α in 48h. Physical stability analysis concluded that refrigerator temperature was the preferred temperature to store transferosomal gel.
MLX loaded transferosomes containing gel improved the skin penetration and therefore resulted into increased inhibition of TNF-α level.
。在这项研究中,我们研究了美洛昔康(MLX)作为传递体凝胶的潜力,作为一种新型的脂质药物传递系统,用于治疗骨关节炎(OTA),这是一种导致疼痛和僵硬的退行性关节疾病。通过将美洛昔康纳入传递体凝胶中,我们的目标是提供一种靶向且高效的传递系统,能够缓解症状并减缓 OTA 的进展。
采用经典的脂质薄膜水化技术来配制不同的传递体配方。通过改变磷脂酰胆碱(phosphodylcholine)与二硬脂酰基磷脂酰乙醇胺(DSPE)的摩尔比(50:50、60:40、70:30、80:20 和 90:10)和每批 80mg 的总脂质来制备不同的传递体配方。测量了质量控制参数,如包封效率、粒径和形态、多分散性和表面电荷、体外药物释放、离体渗透和稳定性。
优化的传递体配方显示出较小的囊泡大小(121±12nm)和更高的 MLX 包封率(68.98±2.3%)。传递体介导的凝胶配方 MLX34 显示 pH(6.3±0.2)、粘度(6236±12.3cps)、铺展性(13.77±1.77gm.cm/sec),并且也显示出药物释放的持续释放模式(24 小时内 Carbopol-934 凝胶基质中释放 81.76±7.87%的 MLX)。MLX34 显示出接近实质性的抗炎反应,在 48 小时内 TNF-α的抑制率约为 81%。物理稳定性分析得出结论,冰箱温度是储存传递体凝胶的首选温度。
载有美洛昔康的传递体凝胶提高了皮肤渗透,因此导致 TNF-α水平的抑制增加。