Jain Ashay, Garg Neeraj K, Jain Atul, Kesharwani Prashant, Jain Amit Kumar, Nirbhavane Pradip, Tyagi Rajeev K
a Department of Pharmaceutical Sciences, Pharmaceutics Research Laboratory , Dr. Hari Singh Gour University , Sagar , Madhya Pradesh , India .
b Drug Delivery Research Group , University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University , Chandigarh , India .
Drug Dev Ind Pharm. 2016;42(6):897-905. doi: 10.3109/03639045.2015.1104343. Epub 2015 Nov 17.
The present study documents the fabrication and characterization of a topically applicable gel loaded with nanostructured lipid carriers (NLCs) of adapalene (ADA) and vitamin C (ascorbyl-6-palmitate [AP]). The NLCs were prepared by high pressure homogenization (HPH) method followed by incorporation into AP loaded gel. The fabricated system was characterized for size, poly dispersity index, entrapment efficiency (EE) and in vitro drug release properties, and was further investigated for skin compliance, skin transport characteristics (skin permeation and bio-distribution), rheological behavior, texture profile analysis and anti-acne therapeutic potential against testosterone-induced acne in male Wistar rats. The NLC-based formulation improved targeting of the skin epidermal layer and reducing systemic penetration. The co-administration of vitamin C led to an adjunct effect in acne therapy in physiological conditions. In brief, the present results suggest the potential of NLCs as a novel carrier for the dermal delivery of ADA and also the synergistic effect of vitamin C in topical therapeutics.
本研究记录了一种局部应用凝胶的制备与特性，该凝胶负载了阿达帕林（ADA）和维生素C（抗坏血酸-6-棕榈酸酯[AP]）的纳米结构脂质载体（NLCs）。通过高压均质法（HPH）制备NLCs，随后将其掺入负载AP的凝胶中。对制备的体系进行了粒径、多分散指数、包封率（EE）和体外药物释放特性的表征，并进一步研究了其皮肤顺应性、皮肤转运特性（皮肤渗透和生物分布）、流变行为、质地剖面分析以及对雄性Wistar大鼠睾酮诱导痤疮的抗痤疮治疗潜力。基于NLC的制剂改善了对皮肤表皮层的靶向性并减少了全身渗透。维生素C的共同给药在生理条件下对痤疮治疗产生了辅助作用。简而言之，目前的结果表明NLCs作为ADA皮肤递送新型载体的潜力以及维生素C在局部治疗中的协同作用。
