University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh 160014, India.
Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandar Sindri, Ajmer, Rajasthan 305 817, India.
J Pharm Sci. 2019 Dec;108(12):3879-3889. doi: 10.1016/j.xphs.2019.09.020. Epub 2019 Sep 27.
The cost, side effects, and patient compliance-related issues of topically effective imiquimod have prevented its widespread acceptance. The present work intends to evaluate the feasibility of overcoming the shortcomings of poorly soluble and skin-penetrating immunomodulator by using biocompatible keratolytic agent with drug-loaded hybrid vesicles. Salicylic acid was complexed with phospholipid through simple mixing and incorporated into carbopol 940 gel containing drug-loaded vesicles, prepared by thin-film hydration method. The morphology, physicochemical properties, rheological behavior, release profile, and dermatokinetics of developed gel were compared with control gel (developed gel without keratolytic agent). In ex vivo drug release studies across the rat skin, there was significant increase in the steady-state permeation flux (J) and skin retention of drug from developed gel in comparison with control. There was favorable change in almost every evaluated dermatokinetic parameter. The innocuous nature of control gel had not changed on addition of skin structure-altering agent. The developed gel was found to be stable at room temperature and humidity for 1 year.
局部有效的咪喹莫特在成本、副作用和患者依从性方面存在问题,这阻碍了其广泛应用。本研究旨在通过使用具有生物相容性的角质松解剂和载药混合囊泡来克服免疫调节剂溶解性差和透皮吸收差的缺点。通过简单混合将水杨酸与磷脂复合,并将其掺入含有载药囊泡的卡波姆 940 凝胶中,通过薄膜水化法制备。将所开发的凝胶的形态、理化性质、流变行为、释放曲线和皮肤动力学与对照凝胶(不含角质松解剂的开发凝胶)进行比较。在离体大鼠皮肤的药物释放研究中,与对照相比,开发的凝胶使药物的稳态渗透通量(J)和皮肤滞留显著增加。几乎每个评估的皮肤动力学参数都有良好的变化。在加入改变皮肤结构的试剂后,对照凝胶的无害性质没有改变。研究发现,开发的凝胶在室温湿度下可稳定保存 1 年。