Gürbüz Aslı, Özhan Gül, Güngör Sevgi, Erdal M Sedef
Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, Istanbul, Turkey.
Arch Dermatol Res. 2015 Sep;307(7):607-15. doi: 10.1007/s00403-015-1566-y. Epub 2015 Apr 23.
Acne vulgaris is the chronical, multifactorial and complex disease of the pilosebaceous unit in the skin. The main goal of the topical therapy in acne is to target the drug to epidermal and deep dermal regions by minimizing systemic absorption . Isotretinoin, a retinoic acid derivative, is the most effective drug in acne pathogenesis. Because systemic treatment may cause many side effects, topical isotretinoin treatment is an option in the management of acne. However, due to its high lipophilic character, isotretinoin tends to accumulate in the upper stratum corneum, thus its penetration into the lower layers is limited, which restricts the efficiency of topical treatment. Microemulsions are fluid, isotropic, colloidal drug carriers that have been widely studied as drug delivery systems. The percutaneous transport of active agents can be enhanced by microemulsions when compared with their conventional formulations. The purpose of this study was to evaluate microemulsions as alternative topical carriers for isotretinoin with an objective to improve its skin uptake. After in vitro permeation studies, the dermal penetration of isotretinoin from microemulsions was investigated by tape stripping procedure. Confocal laser scanning microscopy provided insight about the localization of the drug in the skin. The interaction between the microemulsion components and stratum corneum lipids is studied by ATR-FTIR spectroscopy. The relative safety of the microemulsions was assessed in mouse embryonic fibroblasts using MTT viability test. The results indicate that microemulsion-based novel colloidal carriers have a potential for enhanced skin delivery and localization of isotretinoin.
寻常痤疮是一种发生于皮肤毛囊皮脂腺单位的慢性、多因素且复杂的疾病。痤疮局部治疗的主要目标是通过最小化全身吸收，使药物靶向作用于表皮和真皮深层区域。异维A酸是一种维甲酸衍生物，是治疗痤疮发病机制最有效的药物。由于全身治疗可能会引起许多副作用，局部使用异维A酸治疗是痤疮管理的一种选择。然而，由于其高亲脂性，异维A酸倾向于在上层角质层中蓄积，因此其渗透到下层的能力有限，这限制了局部治疗的效果。微乳剂是流体、各向同性的胶体药物载体，作为药物递送系统已被广泛研究。与传统制剂相比，微乳剂可增强活性剂的经皮转运。本研究的目的是评估微乳剂作为异维A酸替代局部载体的可能性，以提高其皮肤摄取量。经过体外渗透研究后，采用胶带剥离法研究了异维A酸从微乳剂中的皮肤渗透情况。共聚焦激光扫描显微镜提供了关于药物在皮肤中定位的见解。通过衰减全反射傅里叶变换红外光谱（ATR-FTIR）研究了微乳剂成分与角质层脂质之间的相互作用。使用MTT活力试验在小鼠胚胎成纤维细胞中评估了微乳剂的相对安全性。结果表明，基于微乳剂的新型胶体载体具有增强异维A酸皮肤递送和定位的潜力。
