Hani Umme, Paramshetti Sharanya, Angolkar Mohit, Alqathanin Wajan Khalid, Alghaseb Reema Saeed, Al Asmari Saja Mohammed, Alsaab Alhanouf A, Fatima Farhat, Osmani Riyaz Ali M, Gundawar Ravi
Department of Pharmaceutics, College of Pharmacy, King Khalid University, Abha 62529, Saudi Arabia.
Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research (JSS AHER), Mysuru 570015, Karnataka, India.
Pharmaceuticals (Basel). 2024 Nov 27;17(12):1598. doi: 10.3390/ph17121598.
Psoriatic arthritis (PsA), a chronic inflammatory disease, mainly affects the joints, with approximately 30% of psoriasis patients eventually developing PsA. Characterized by both innate and adaptive immune responses, PsA poses significant challenges for effective treatment. Recent advances in drug delivery systems have sparked interest in developing novel formulations to improve therapeutic outcomes. The current research focuses on the development and evaluation of a nanosponge-loaded, cyclo-oxygenase-2 (COX-2) inhibitor-based topical gel for the treatment of PsA. Nanosponges (NSs) were prepared by using beta-cyclodextrin as a polymer and dimethyl carbonate (DMC) as a crosslinker by melting, and gels were prepared by employing carbopol and badam gum as polymers. Solubility studies confirmed that the prepared nanosponges were highly soluble. FT-IR studies confirmed the formation of hydrogen bonds between lumiracoxib and beta-cyclodextrin. SEM confirmed that the prepared formulations were roughly spherical and porous in nature. The average particle size was 190.5 ± 0.02 nm, with a zeta potential of -18.9 mv. XRD studies showed that the crystallinity of lumiracoxib decreased after encapsulation, which helped to increase its solubility. The optimized nanosponges (NS2) were incorporated in an optimized gel (FG10) to formulate a nanosponge-loaded topical gel. The optimized gel formulation exhibited a homogeneous consistency, with a pH of 6.8 and a viscosity of 1.15 PaS, indicating its suitability for topical application and stability. The diffusion studies for the topical gel showed drug release of 82.32% in 24 h. The optimized formulation demonstrated significant antipsoriatic activity, as confirmed through cytotoxicity studies conducted on HaCaT cells. On the basis of the findings, it can be concluded that the prepared nanosponge-loaded topical gel formulation presents a promising solution for the effective management of PsA, offering enhanced drug solubility, sustained release, and improved therapeutic potential.
银屑病关节炎（PsA）是一种慢性炎症性疾病，主要影响关节，约30%的银屑病患者最终会发展为PsA。PsA具有先天性和适应性免疫反应的特征，对有效治疗构成了重大挑战。药物递送系统的最新进展引发了人们对开发新型制剂以改善治疗效果的兴趣。目前的研究重点是开发和评估一种负载纳米海绵的、基于环氧合酶-2（COX-2）抑制剂的局部用凝胶，用于治疗PsA。通过使用β-环糊精作为聚合物和碳酸二甲酯（DMC）作为交联剂，采用熔融法制备纳米海绵（NSs），并使用卡波姆和巴旦木胶作为聚合物制备凝胶。溶解度研究证实所制备的纳米海绵具有高溶解性。傅里叶变换红外光谱（FT-IR）研究证实了氯美昔布与β-环糊精之间形成了氢键。扫描电子显微镜（SEM）证实所制备的制剂本质上大致呈球形且多孔。平均粒径为190.5±0.02 nm，zeta电位为-18.9 mV。X射线衍射（XRD）研究表明，氯美昔布包封后结晶度降低，这有助于提高其溶解度。将优化后的纳米海绵（NS2）掺入优化后的凝胶（FG10）中，制成负载纳米海绵的局部用凝胶。优化后的凝胶制剂呈现均匀的稠度，pH值为6.8，粘度为1.15 Pa·s，表明其适合局部应用且具有稳定性。局部用凝胶的扩散研究表明，24小时内药物释放率为82.32%。通过对HaCaT细胞进行的细胞毒性研究证实，优化后的制剂具有显著的抗银屑病活性。基于这些发现，可以得出结论，所制备的负载纳米海绵的局部用凝胶制剂为有效管理PsA提供了一种有前景的解决方案，具有增强的药物溶解度、持续释放和改善的治疗潜力。
