Mathew Mekha, Patil Anasuya, G Hemanth
Department of Pharmaceutics, KLE College of Pharmacy, Rajajinagar, Bengaluru, India.
Pharm Nanotechnol. 2025;13(2):320-327. doi: 10.2174/0122117385269522231113041029.
Rheumatoid arthritis is indeed a constant, progressive autoimmune disease that acts on the synovial membrane, distinguished by joint pain, swelling, and tenderness. Sulfasalazine 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.
The primary objective of this investigation was to pass on sulfasalazine-loaded cubosomes over the skin to treat rheumatoid arthritis. On the way to overcome this issue of oral sulfasalazine and provide localized effect, Cubosomes were chosen for the transdermal drug delivery system.
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 3 full factorial designs. The prepared formulations were assessed for p.s, z,p, %EE, FTIR, SEM, release, permeation, and deposition studies with pH 7.4 phosphate buffer saline.
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 sulfasalazine and better ex-vivo permeation and deposition properties than sulfasalazine suspension.
Overall study findings support the possibility of applying transdermal sulfasalazineloaded cubosomes to alleviate rheumatoid arthritis.
类风湿性关节炎确实是一种持续进展的自身免疫性疾病,作用于滑膜,其特征为关节疼痛、肿胀和压痛。柳氮磺胺吡啶属于BCS IV类药物,具有低溶解度和低渗透性。为克服这一问题并实现局部作用,选择了立方液晶纳米粒用于透皮给药系统。
本研究的主要目的是将负载柳氮磺胺吡啶的立方液晶纳米粒透过皮肤给药以治疗类风湿性关节炎。为克服口服柳氮磺胺吡啶的这一问题并实现局部作用,选择了立方液晶纳米粒用于透皮给药系统。
采用自上而下的方法,使用转基因大豆油和泊洛沙姆407制备负载柳氮磺胺吡啶的立方液晶纳米粒。在配方中使用不同浓度的脂质和表面活性剂,并采用3因素全因子设计。用pH 7.4的磷酸盐缓冲盐水对制备的制剂进行粒径、ζ电位、包封率、傅里叶变换红外光谱、扫描电子显微镜、释放、渗透和沉积研究。
粒径在65nm至129nm之间,ζ电位为负,范围在-18.8mV至-24.8mV之间。包封率在87%至95%之间。制剂的体外药物释放进行了12小时。优化后的制剂显示柳氮磺胺吡啶具有控释特性,并且与柳氮磺胺吡啶混悬液相比具有更好的体外渗透和沉积性能。
总体研究结果支持应用负载柳氮磺胺吡啶的透皮立方液晶纳米粒缓解类风湿性关节炎的可能性。