The effect of component of cream for topical delivery of hesperetin.
The aim of this study was to optimize hesperetin cream formulations by in vitro permeation study and evaluate topical whitening active effect and skin irritation by in vivo study. The results showed that the solubility of lipophilic compound of hesperetin was increased by short-chain alcohol including ethanol, glycerin, propylene glycol and polyethylene glycols 400 (PEG 400). PEG 400 showed strongest solubilized effect by increased 3400-fold. With the addition of 5% enhancers, it was found that menthol showed the most potent enhancing effect, followed by azone and depigmentation agents (linoleic acid and lecithin). Moreover, enhancers could shorten the lag time from 3.7 to 1 h. Combination of menthol, linoleic acid and lecithin of 2.5% had a higher permeation rate of 9.8 microg/cm(2)/h and lower lag time 1 h, therefore the formulation was selected to process the skin whitening and irritation test. The results showed that a significantly topical photoprotective effect with acceptable skin irritation was obtained after hesperetin cream topical application when compared with that of the non-treatment group, indicating that the hesperetin cream may be used as an effective whitening agent.
Huang
Yaw-Bin
YB
Graduate Institute of Clinical Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung 80708, Taiwan.
Lee
Ko-Feng
KF
Huang
Chi-Te
CT
Tsai
Yi-Hung
YH
Wu
Pao-Chu
PC
D000287:Administration, Topical; D000818:Animals; D004304:Dosage Forms; D016503:Drug Delivery Systems; D006168:Guinea Pigs; D006569:Hesperidin / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology*; D008297:Male; D010858:Pigmentation / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000187:drug effects; D012995:Solubility
D004304:Dosage Forms; D006569:Hesperidin; C013015:hesperetin