Tabbakhian Majid, Tavakoli Naser, Jaafari Mahmoud Reza, Daneshamouz Saeid
Department of Pharmaceutics, School of Pharmacy and Isfahan Pharmaceutical Sciences Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.
Int J Pharm. 2006 Oct 12;323(1-2):1-10. doi: 10.1016/j.ijpharm.2006.05.041. Epub 2006 May 26.
Finasteride is indicated orally in the treatment of androgenetic alopecia and some other pilosebaceous unit (PSU) disorders. We wished to investigate whether topical application of finasteride-containing vesicles (liposomes and niosomes) could enhance drug concentration at the PSU, as compared to finasteride hydroalcoholic solution (HA). Liposomes consisted of phospholipid (dimyristoyl phosphatidylcholine (DMPC) or egg lecithin):cholesterol:dicetylphosphate (8:2:1, mole ratio). Niosomes were comprising non-ionic surfactant (polyoxyethylene alkyl ethers (Brij series) or sorbitan monopalmitate):cholesterol:dicetylphosphate (7:3:1, mole ratio). Vesicles were prepared by the film hydration technique and characterized with regard to the size, drug entrapment efficiency and gel-liquid transition temperature (T(c)). In vitro permeation of (3)H-finasteride through hamster flank skin was faster from hydroalcoholic solution (0.13 microg/cm(2)h) compared to vesicles (0.025-0.058 microg/cm(2)h). In vivo deposition of (3)H-finasteride vesicles in hamster ear showed that liquid-state vesicle, i.e. those made of DMPC or Brij97:Brij76 (1:1), were able to deposit 2.1 or 2.3% of the applied dose to the PSU, respectively. This was significantly higher than drug deposition by gel-state vesicles (0.35-0.51%) or HA (0.76%). Both in vitro permeation and in vivo deposition studies, demonstrated the potentials of liquid-state liposomes and niosomes for successful delivery of finasteride to the PSU.
非那雄胺口服可用于治疗雄激素性脱发和其他一些毛囊皮脂腺单位(PSU)疾病。我们希望研究与非那雄胺水醇溶液(HA)相比,局部应用含非那雄胺的囊泡(脂质体和非离子脂质体)是否能提高PSU处的药物浓度。脂质体由磷脂(二肉豆蔻酰磷脂酰胆碱(DMPC)或卵磷脂):胆固醇:磷酸二鲸蜡酯(摩尔比8:2:1)组成。非离子脂质体由非离子表面活性剂(聚氧乙烯烷基醚(Brij系列)或脱水山梨醇单棕榈酸酯):胆固醇:磷酸二鲸蜡酯(摩尔比7:3:1)组成。通过薄膜水化技术制备囊泡,并对其大小、药物包封率和凝胶 - 液晶转变温度(T(c))进行表征。与囊泡(0.025 - 0.058 μg/cm²h)相比,(³H) - 非那雄胺通过仓鼠侧腹皮肤的体外渗透在水醇溶液中更快(0.13 μg/cm²h)。(³H) - 非那雄胺囊泡在仓鼠耳部的体内沉积表明,液态囊泡,即由DMPC或Brij97:Brij76(1:1)制成的囊泡,能够分别将给药剂量的2.1%或2.3%沉积到PSU。这显著高于凝胶态囊泡(0.35 - 0.51%)或HA(0.76%)的药物沉积。体外渗透和体内沉积研究均表明,液态脂质体和非离子脂质体有将非那雄胺成功递送至PSU的潜力。