背景:类风湿性关节炎确实是一个常数,作用于滑膜的进行性自身免疫性疾病,以关节疼痛为特征,肿胀,和温柔。Sulfasala-zine属于具有低溶解度和低渗透性的BCSIV类。为了克服该问题并提供局部效应,选择立方体用于透皮药物递送系统。
目的:本研究的主要目的是将负载柳氮磺吡啶的长方体通过皮肤来治疗类风湿性关节炎。在克服这一问题的方式口服磺胺嘧啶和提供局部效果,选择立方体用于经皮药物递送系统。
方法:通过使用GMO和泊洛沙姆407的自上而下的方法制备负载柳氮磺胺吡啶的立方体。使用32个全因子设计在制剂中使用不同浓度的脂质和表面活性剂。评估制备的制剂的p.s,z,p,%EE,FTIR,SEM,体外释放,离体渗透,和用pH7.4磷酸盐缓冲盐水进行沉积研究。
结果:粒径在65nm至129nm之间变化,而负zeta电位范围为-18.8mV至-24.8mV。包封效率在87%和95%之间。制剂的体外药物释放进行12小时。与柳氮磺胺吡啶混悬液相比,优化的制剂显示出磺胺吡啶的受控释放和更好的离体渗透和沉积性质。
结论:总体研究结果支持应用经皮舒拉嗪负载的立方体减轻类风湿性关节炎的可能性。
BACKGROUND: Rheumatoid arthritis is indeed a constant, progressive autoimmune disease that acts on the synovial membrane, distinguished by joint pain, swelling, and tenderness. Sulfasala- zine belongs to BCS Class IV having low solubility and low permeability. To overcome the issue and provide a localized effect Cubosomes were chosen for the transdermal drug delivery system.
OBJECTIVE: The primary objective of this investigation was to pass on sulfasalazine-loaded cubo- somes over the skin to treat rheumatoid arthritis. On the way to overcome this issue of oral sulfasala- zine and provide localized effect, Cubosomes were chosen for the transdermal drug delivery system.
METHODS: Sulfasalazine-loaded cubosomes were prepared by the top-down method using GMO and Poloxamer 407. Different concentrations of lipid and surfactant were used in the formulation using 32 full factorial designs. The prepared formulations were assessed for p.s, z,p, %EE, FTIR, SEM, in- vitro release, ex-vivo permeation, and deposition studies with pH 7.4 phosphate buffer saline.
RESULTS: The particle size varies between 65 nm to 129 nm, while the negative zeta potential ranged from - 18.8 mV to -24.8 mV. The entrapment efficiency was between 87% and 95%. The formulations\' in-vitro drug release was carried out for 12 hours. The optimized formulation showed a controlled release of sul- fasalazine and better ex-vivo permeation and deposition properties than sulfasalazine suspension.
CONCLUSIONS: Overall study findings support the possibility of applying transdermal sulfasalazine- loaded cubosomes to alleviate rheumatoid arthritis.