Kesharwani Disha, Das Paul Swarnali, Paliwal Rishi, Satapathy Trilochan
Columbia Institute of Pharmacy, Raipur, Chhattisgarh, India.
Shri Shankaracharya College of Pharmaceutical Sciences, Shri Shankaracharya Professional University, Bhilai, Chhattisgarh, India.
Colloids Surf B Biointerfaces. 2023 Mar;223:113160. doi: 10.1016/j.colsurfb.2023.113160. Epub 2023 Jan 20.
Diacerein (DCN) is a chondroprotective agent which shows inadequate oral bioavailability along with gastrointestinal side effects. This study is intended to develop a topical novel DCN delivery system. DCN nanogel was prepared by emulsion solvent diffusion technique. The formulation was optimized by response surface methodology by taking two independent variables, concentration of carbopol 940 and eudragit RSPO and three dependent variables, particle size, % entrapment efficiency (EE) and % drug release at 24 h. The optimized formulation had adequat% EE, % drug release at 24 h and particle size. The particle size for optimized nanogel was 190.3 nm with % EE of 83.51% whereas % drug release at 24 h was found 90.13%. The optimized DCN nanogel was analyzed by differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (DTIR) and transmission electron microscopy (TEM) studies. The drug release kinetic study has shown that the gel followed Higuchi's model and the diffusion was anomalous in nature. The nanogel was characterized for physical examination, viscosity, homogeneity and stability parameters and the results obtained were found upto the mark. The ex-vivo permeation study data was in correlation with results of in-vitro study. In-vivo anti-arthritic study proved the efficacy of developed formulation for arthritis in Freund's Adjuvant Arthritic model. This research work has proved the significant potential of innovated product for arthritis by topical route, as it overcomes the drawbacks of oral route, highly efficient, sustained and targeted the release of drug without any accumulation and toxicity.
双醋瑞因（DCN）是一种具有软骨保护作用的药物，但口服生物利用度较低，且伴有胃肠道副作用。本研究旨在开发一种新型的DCN局部给药系统。通过乳液溶剂扩散技术制备了DCN纳米凝胶。采用响应面法对制剂进行优化，以卡波姆940和丙烯酸树脂RSPO的浓度为两个自变量，粒径、包封率（EE）和24小时药物释放率为三个因变量。优化后的制剂具有足够的包封率、24小时药物释放率和粒径。优化后的纳米凝胶粒径为190.3nm，包封率为83.51%，24小时药物释放率为90.13%。通过差示扫描量热法（DSC）、X射线衍射（XRD）、傅里叶变换红外光谱（DTIR）和透射电子显微镜（TEM）研究对优化后的DCN纳米凝胶进行了分析。药物释放动力学研究表明，该凝胶符合Higuchi模型，扩散性质为非菲克扩散。对纳米凝胶的物理性质、粘度、均匀性和稳定性参数进行了表征，结果令人满意。体外渗透研究数据与体外研究结果相关。体内抗关节炎研究证明了所开发制剂在弗氏佐剂性关节炎模型中对关节炎的疗效。这项研究工作证明了该创新产品通过局部给药途径治疗关节炎的巨大潜力，因为它克服了口服途径的缺点，高效、持续且靶向释放药物，无任何蓄积和毒性。
