Shamma Rehab Nabil, Aburahma Mona Hassan
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Int J Nanomedicine. 2014 Nov 26;9:5449-60. doi: 10.2147/IJN.S73010. eCollection 2014.
Spironolactone (SL) is a US Food and Drug Administration-approved drug for the treatment of hypertension and various edematous conditions. SL has gained a lot of attention for treating androgenic alopecia due to its potent antiandrogenic properties. Recently, there has been growing interest for follicular targeting of drug molecules for treatment of hair and scalp disorders using nanocolloidal lipid-based delivery systems to minimize unnecessary systemic side effects associated with oral drug administration. Accordingly, the objective of this study is to improve SL efficiency and safety in treating alopecia through the preparation of colloidal nanostructured lipid carriers (NLCs) for follicular drug delivery. SL-loaded NLCs were prepared by an emulsion solvent diffusion and evaporation method using 23 full factorial design. All of the prepared formulations were spherical in shape with nanometric size range (215.6-834.3 nm) and entrapment efficiency >74%. Differential scanning calorimetry thermograms and X-ray diffractograms revealed that SL exists in amorphous form within the NLC matrices. The drug release behavior from the NLCs displayed an initial burst release phase followed by sustained release of SL. Confocal laser scanning microscopy confirmed the potential of delivering the fluorolabeled NLCs within the follicles, suggesting the possibility of using SL-loaded NLCs for localized delivery of SL into the scalp hair follicles.
螺内酯（SL）是一种经美国食品药品监督管理局批准用于治疗高血压和各种水肿病症的药物。由于其强大的抗雄激素特性，SL在治疗雄激素性脱发方面备受关注。最近，人们越来越有兴趣利用基于纳米胶体脂质的递送系统将药物分子靶向毛囊，以治疗毛发和头皮疾病，从而尽量减少与口服给药相关的不必要的全身副作用。因此，本研究的目的是通过制备用于毛囊药物递送的胶体纳米结构脂质载体（NLCs）来提高SL治疗脱发的效率和安全性。采用23全因子设计，通过乳液溶剂扩散和蒸发法制备了载有SL的NLCs。所有制备的制剂均呈球形，粒径在纳米范围内（215.6 - 834.3 nm），包封率>74%。差示扫描量热法热谱图和X射线衍射图显示，SL以无定形形式存在于NLC基质中。NLCs的药物释放行为表现为初始突释阶段，随后是SL的持续释放。共聚焦激光扫描显微镜证实了将荧光标记的NLCs递送至毛囊内的可能性，这表明使用载有SL的NLCs将SL局部递送至头皮毛囊的可能性。
