In vitro permeation and in vivo whitening effect of topical hesperetin英文书.pdf

International Journal of Pharmaceutics 388 (2010) 257–262 Contents lists available at ScienceDirect International Journal of Pharmaceutics journal homepage: /locate/ijpharm Pharmaceutical Nanotechnology In vitro permeation and in vivo whitening effect of topical hesperetin microemulsion delivery system Yi-Hung Tsai b, Ko-Feng Lee b, Yaw-Bin Huang a, Chi-Te Huang b, Pao-Chu Wu b,? a Graduate Institute of Clinical Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung City 80708, Taiwan b Faculty of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung City 80708, Taiwan article info Article history: Received 20 August 2009 Received in revised form 1 December 2009 Accepted 27 December 2009 Available online 7 January 2010 Keywords: Hesperetin Microemulsion Transdermal delivery Padimate O Whitening effect abstract Hesperetin is one of the ?avonoids and possess anti-in?ammatory, 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 cosurfactant 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 hesperetinloaded microemulsion showed signi?cant topical whitening effect and diminished skin irritation when compared w