Lipid nano/submicron emulsions as vehicles for topical flurbiprofen delivery.
The application of lipid nano/submicron emulsions as topical drug carrier systems for the percutaneous absorption of flurbiprofen was investigated. The lipid emulsions were made up of isopropyl myristate (IPM), soybean oil, or coconut oil as the oil phase, egg lecithin as the predominant emulsifier, and double-distilled water as the external phase. Stearylamine (SA) and deoxycholic acid (DA) also were used to produce positively and negatively charged emulsions. To evaluate the physicochemical properties of the lipid emulsions, particle size by laser light scattering, the image of atomic force microscopy, and relaxation time values by Nuclear Magnetic Resonance (NMR) were determined. The in vitro permeation data showed that incorporation of SA significantly reduced the topical delivery of flurbiprofen. On the other hand, incorporation of DA exhibited no or a negligible effect on drug permeation. Enhancement of drug absorption was observed when adding oleic acid as part of the oil phase. The in vivo topical application of flurbiprofen from selected lipid emulsions showed a similar trend to the in vitro status. Furthermore, the intersubject variability was considerably reduced by lipid emulsions than by aqueous suspensions in both the in vitro and in vivo experiments. The irritant profiles of lipid emulsions showed that IPM elicited higher irritation than soybean oil. The incorporation of oleic acid also produced skin disruption. The results in the present study suggest the feasibility of lipid emulsions for the topical delivery of flurbiprofen.
Fang
Jia-You
JY
Graduate Institute of Natural Products, Chang Gung University, Tao-Yuan, Taiwan. fajy@mail.cgu.edu.tw
Leu
Yann-Lii
YL
Chang
Chia-Chun
CC
Lin
Chia-Hsuan
CH
Tsai
Yi-Hung
YH
D000287:Administration, Topical; D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods*; D004655:Emulsions; D005260:Female; D005480:Flurbiprofen / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008055:Lipids / Q000008:administration & dosage* / Q000493:pharmacokinetics; D036103:Nanotechnology / Q000379:methods*; D014677:Pharmaceutical Vehicles; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects* / Q000378:metabolism
D004655:Emulsions; D008055:Lipids; D014677:Pharmaceutical Vehicles; D005480:Flurbiprofen