In vitro permeation and in vivo whitening effect of topical hesperetin microemulsion delivery system.
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.
Tsai
Yi-Hung
YH
Faculty of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung City 80708, Taiwan.
Lee
Ko-Feng
KF
Huang
Yaw-Bin
YB
Huang
Chi-Te
CT
Wu
Pao-Chu
PC
D010129:4-Aminobenzoic Acid / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D016503:Drug Delivery Systems; D004655:Emulsions; D005079:Excipients / Q000737:chemistry*; D006168:Guinea Pigs; D006569:Hesperidin / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D017495:Hyperpigmentation / Q000188:drug therapy* / Q000209:etiology; D066298:In Vitro Techniques; D008297:Male; D009226:Myristates / Q000737:chemistry; D010539:Permeability; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption; D013501:Surface-Active Agents / Q000737:chemistry; D014466:Ultraviolet Rays / Q000009:adverse effects; D062366:para-Aminobenzoates
D000975:Antioxidants; D004655:Emulsions; D005079:Excipients; D009226:Myristates; D013501:Surface-Active Agents; D062366:para-Aminobenzoates; C008205:isopropyl myristate; D006569:Hesperidin; C013015:hesperetin; D010129:4-Aminobenzoic Acid; C041981:padimate-O