Lecithin vesicles for topical delivery of diclofenac.
Skin penetration of topically applied diclofenac is important for the treatment of rheumatic diseases and actinic keratoses. We have studied the permeation of diclofenac across human cadaver epidermis in-vitro from four lecithin vesicle formulations and a few marketed semi-solid preparations. The lecithin vesicle formulations were prepared by dissolving the lipid contents (lecithin and sodium cholate) in a 1:1 mixture of methanol-chloroform, evaporating the solvents under vacuum, and hydrating the lipid layer with the drug solution in water or 10% ethanol. The vesicles were sonicated for 5 min to reduce the vesicle size and their size and Zeta potential were characterized. The cumulative amount and maximum flux of diclofenac was 69.7+/-40.3 micrograms and 4.77+/-3.16 micrograms/hcm(2) from lecithin vesicles containing sodium cholate and 10% ethanol, and is the highest of all formulations studied. The cumulative amount and mean maximum flux obtained from other formulations were in the range of 2.46+/-1.98-29.9+/-10.1 micrograms and 0.53+/-0.46-3.61+/-0.86 micrograms/hcm(2). Based on the results, lecithin vesicles of diclofenac appear to be advantageous for the topical delivery of diclofenac.
Karmanos Cancer Institute, Wayne State University, Detroit, MI, USA. boinpall@karmanos.org
Ramesh R
RR
Boinpally
Sen Lin
SL
Zhou
Srinivasu
S
Poondru
Gopinath
G
Devraj
Bhaskara R
BR
Jasti
D000287:Administration, Topical; D004008:Diclofenac / Q000008:administration & dosage* / Q000493:pharmacokinetics; D015194:Diffusion Chambers, Culture; D016503:Drug Delivery Systems / Q000379:methods*; D004817:Epidermis / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D010713:Phosphatidylcholines / Q000008:administration & dosage* / Q000493:pharmacokinetics
D010713:Phosphatidylcholines; D004008:Diclofenac