Faculty of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung City 80708, Taiwan.
Int J Pharm. 2010 Mar 30;388(1-2):257-62. doi: 10.1016/j.ijpharm.2009.12.051. Epub 2010 Jan 7.
Hesperetin is one of the flavonoids and possess anti-inflammatory, UV-protecting and antioxidant effects. Permeation issues for topical delivery systems of such effects are occasionally problematic, and in view of the fact that microemulsions are potential carriers for transdermal delivery system, the objective of this study was to design an optimal microemulsion formulation by in vitro permeation study for hesperetin topical dosage form and determine its topical photoprotective effect and skin irritation by in vivo study. The hesperetin-loaded microemulsion showed an enhanced in vitro permeation compared to the aqueous and isopropyl myristate (IPM) suspension dosage form of hesperetin. In comparison, the effect of co-surfactant on the drug permeation capacity, propylene glycol showed highest permeation rate, followed by ethanol, glycerol and polyethylene glycol (PEG 400). Sunscreen agent padimate O, as a transdermal enhancer could increase the permeation rate of hesperetin. In case of in vivo study, the hesperetin-loaded microemulsion showed significant topical whitening effect and diminished skin irritation when compared with the non-treatment group, indicating that the hesperetin microemulsion could be used as an effective whitening agent.
橙皮素是一种类黄酮，具有抗炎、防晒和抗氧化作用。对于具有此类功效的局部给药系统，渗透问题偶尔会成为问题，并且鉴于微乳液是经皮传递系统的潜在载体，本研究的目的是通过体外渗透研究设计橙皮素局部剂型的最佳微乳液配方，并通过体内研究确定其局部防晒效果和皮肤刺激性。与橙皮素的水性和肉豆蔻异丙酯（IPM）混悬剂剂型相比，橙皮素负载的微乳液显示出增强的体外渗透。相比之下，助表面活性剂对药物渗透能力的影响，丙二醇显示出最高的渗透速率，其次是乙醇、甘油和聚乙二醇（PEG 400）。防晒剂对氨基苯甲酸辛酯作为透皮促进剂可以增加橙皮素的渗透速率。在体内研究中，与未治疗组相比，负载橙皮素的微乳液显示出显著的局部美白效果和减轻的皮肤刺激性，表明橙皮素微乳液可用作有效的美白剂。
