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脂质体和非离子表面活性剂囊泡增强非那雄胺的卵泡递送 1. 使用仓鼠胁腹和耳部模型的体外渗透和体内沉积研究。

Enhancement of follicular delivery of finasteride by liposomes and niosomes 1. In vitro permeation and in vivo deposition studies using hamster flank and ear models.

作者信息

Tabbakhian Majid, Tavakoli Naser, Jaafari Mahmoud Reza, Daneshamouz Saeid

机构信息

Department of Pharmaceutics, School of Pharmacy and Isfahan Pharmaceutical Sciences Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.

出版信息

Int J Pharm. 2006 Oct 12;323(1-2):1-10. doi: 10.1016/j.ijpharm.2006.05.041. Epub 2006 May 26.

Abstract

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.

摘要

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。

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