Jamal Mahvish, Imam Syed Sarim, Aqil Mohd, Amir Mohd, Mir Shaukat R, Mujeeb Mohd
Faculty of Pharmacy, Jamia Hamdard University, New Delhi, India.
Glocal School of Pharmacy, Glocal University, Saharanpur, Uttar Pradesh, India.
Int Immunopharmacol. 2015 Dec;29(2):361-369. doi: 10.1016/j.intimp.2015.10.029. Epub 2015 Nov 3.
The aim of the present study was to optimize niosomes by experimental design for enhanced transdermal delivery of ursolic acid for the effective treatment of arthritis. The experimental design (3 factor 3 levels, Box-Behnken design) was used to study individual and combined effects of different formulation variables. The variables cholesterol (X1), span 60 (X2) and phospholipid (X3) were taken as independent factors and their effect was observed on size (Y1) entrapment efficiency (Y2), and transflux (Y3). The formulation composition with span 60 (85mg), cholesterol (12.3mg), and phospholipid (65mg) was found to fulfil requisites of optimized ursolic acid niosome formulation (URNF). URNF had shown vesicle size of 665.45nm, entrapment efficiency of 92.74% with transflux of 17.25μg/cm(2)/h. The in vivo bioactivity showed that the prepared URNF-gel was able to provide good anti-arthritic activity due to enhanced permeation of UA through the skin and results were found to be comparable to standard gel (Omni gel). The radiographical image confirmed that, the developed URNF-gel was found to be effective to treat arthritis. Thus niosomal gel of ursolic acid would be a promising alternative to conventional therapy for safe and efficient treatment of arthritis and musculoskeletal disorders.
本研究的目的是通过实验设计优化非离子表面活性剂囊泡，以增强熊果酸的透皮递送，从而有效治疗关节炎。采用实验设计（3因素3水平，Box-Behnken设计）来研究不同制剂变量的单独和联合作用。将变量胆固醇（X1）、司盘60（X2）和磷脂（X3）作为独立因素，并观察它们对粒径（Y1）、包封率（Y2）和通量（Y3）的影响。发现含有司盘60（85mg）、胆固醇（12.3mg）和磷脂（65mg）的制剂组成满足优化的熊果酸非离子表面活性剂囊泡制剂（URNF）的要求。URNF的囊泡粒径为665.45nm，包封率为92.74%，通量为17.25μg/cm²/h。体内生物活性表明，制备的URNF凝胶能够提供良好的抗关节炎活性，这是由于熊果酸经皮渗透增强，结果发现与标准凝胶（全效凝胶）相当。影像学图像证实，所开发的URNF凝胶被发现对治疗关节炎有效。因此，熊果酸非离子表面活性剂囊泡凝胶将是传统疗法的一个有前途的替代方案，用于安全有效地治疗关节炎和肌肉骨骼疾病。
