Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Study, Panjab University, Chandigarh, India.
Colloids Surf B Biointerfaces. 2013 May 1;105:67-74. doi: 10.1016/j.colsurfb.2012.12.043. Epub 2013 Jan 5.
Isotretinoin (ITR) is a drug of choice in the treatment of all types of acne, including recalcitrant, severe and nodulocystic. The most widely employed route of its administration, i.e., oral intake, is reported to be associated with severe side-effects including teratogenecity, skin dryness and psychological disorders. Topical delivery, though advised for ITR, is marked with several hiccups like irritation, erythema and peeling of skin. The current studies, therefore, were embarked upon to develop "optimized" SLNs of ITR employing formulation by design (FbD) approach. The developed system was characterized and evaluated for skin compliance, skin transport characteristics and anti-acne potential against testosterone-induced acne in male Laca mice. The SLNs were able to transport the drug to various skin layers effectively while formed drug micro-reservoirs. The nano-colloidal systems showed marked anti-acne potential and tolerability on the mouse skin vis-à-vis the marketed product. The optimized SLNs exhibited drug entrapment of 89.49±4.1%, while the size was found to be in the nano-range (i.e., 75.3±2.4 nm). The ITR formulation was found to be stable too as per ICH guidelines. The results vouch immense promise of the optimized SLNs of ITR in reducing dermal irritation and increasing the therapeutic performance, thus resulting in an efficacious and patient-compliant formulation.
异维 A 酸（ITR）是治疗所有类型痤疮，包括难治性、严重和结节囊肿性痤疮的首选药物。其最广泛使用的给药途径，即口服给药，据报道与严重的副作用有关，包括致畸性、皮肤干燥和心理障碍。尽管建议使用局部递送，但 ITN 存在许多问题，如刺激、红斑和皮肤剥落。因此，目前进行了研究，以通过设计配方（FbD）方法开发“优化”的 ITR 固体脂质纳米粒（SLN）。对开发的系统进行了特征描述和评估，以考察其皮肤顺应性、皮肤转运特性和抗雄激素诱导的雄性 Laca 小鼠痤疮的潜力。SLN 能够将药物有效地输送到各种皮肤层，并形成药物微储库。纳米胶体系统在小鼠皮肤上表现出显著的抗痤疮潜力和耐受性，优于市售产品。优化的 SLN 表现出 89.49±4.1%的药物包封率，而粒径被发现处于纳米范围（即 75.3±2.4nm）。根据 ICH 指南，ITR 制剂也被发现是稳定的。结果证明，优化的 ITR SLN 具有减少皮肤刺激和提高治疗效果的巨大潜力，从而产生一种有效且符合患者需求的制剂。
