Fatty acids in Botryococcus braunii accelerate topical delivery of flurbiprofen into and across skin.
To improve the drug absorption into and across the skin, fatty acids extracted from Botryococcus braunii were evaluated using in vitro and in vivo techniques with Wistar rats as the animal model. Palmitic acid (C16:0), oleic acid (C18:1), linoleic acid (C18:2), and linolenic acid (C18:3) were the major components in the B. braunii extract. Topical delivery of flurbiprofen was significantly enhanced after pretreatment with 3% B. braunii extract for 30min in an in vitro Franz cell and in vivo pharmacokinetic studies. Pure unsaturated fatty acids were more-effective enhancers than the B. braunii extract. However, a greater irritant potential was also observed with those fatty acids than with the B. braunii extract according to the skin tolerance study as determined by transepidermal water loss (TEWL). Both human keratinocytes and skin fibroblasts showed a 1.5-2-fold increase in prostaglandin E(2) (PGE(2)) release as compared to the control. The findings in this study indicate that the fatty acids in B. braunii may be useful enhancers for flurbiprofen delivery via the skin.
Fang
Jia-You
JY
Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, 259 Wen-Hwa 1st Road, Kweishan, Taoyuan 333, Taiwan. fajy@mail.cgu.edu.tw
Chiu
Hsien-Chih
HC
Wu
Jiunn-Tzong
JT
Chiang
Yin-Ru
YR
Hsu
Shu-Hui
SH
D000287:Administration, Topical; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002478:Cells, Cultured; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems / Q000379:methods*; D005227:Fatty Acids / Q000032:analysis / Q000302:isolation & purification / Q000494:pharmacology*; D005347:Fibroblasts / Q000187:drug effects / Q000378:metabolism; D005480:Flurbiprofen / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006801:Humans; D008297:Male; D010936:Plant Extracts / Q000032:analysis / Q000302:isolation & purification / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption / Q000187:drug effects*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005227:Fatty Acids; D010936:Plant Extracts; D005480:Flurbiprofen