Effect of charge and lipid concentration on in-vivo percutaneous absorption of methyl nicotinate from liposomal vesicles.
We have investigated the influence of charge and lipid concentration on the in-vivo percutaneous absorption of a model compound, methyl nicotinate (MN), from liposomal vesicles. MN-loaded liposomes were produced by the reverse-phase evaporation method (REV) using different concentrations of phosphatidyl choline (PC), in association with surfactants such as dioctadecyl dimethyl ammonium bromide (DDAB18) and dicetyl phosphate (DCP), which impart a positive or negative charge to the systems, respectively. The liposomal suspensions were then processed to hydrogels and used to study in-vivo the MN permeation profile. MN was chosen as the model compound since it was capable of causing cutaneous erythema, the intensity and duration of which was proportional to the amount entering the living epidermis over time. The extent of the erythema was monitored by reflectance spectrophotometry, a non-invasive technique. In-vivo findings showed an interesting MN delayed release, which was proportional to the amount of phospholipids in each liposomal formulation. Furthermore, it could be noted that the erythematous effect was more prolonged when MN was delivered from neutral or negatively-charged liposomal forms.
Puglia
Carmelo
C
Department of Pharmaceutical Sciences, School of Pharmacy, University of Catania, Catania, Italy. capuglia@unict.it
Esposito
Elisabetta
E
Menegatti
Enea
E
Nastruzzi
Claudio
C
Rizza
Luisa
L
Cortesi
Rita
R
Bonina
Francesco
F
D000287:Administration, Topical; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004890:Erythema / Q000139:chemically induced; D006801:Humans; D008055:Lipids / Q000737:chemistry* / Q000494:pharmacology; D008081:Liposomes; D009539:Nicotinic Acids / Q000008:administration & dosage / Q000009:adverse effects* / Q000378:metabolism*; D010713:Phosphatidylcholines / Q000737:chemistry / Q000494:pharmacology; D012869:Skin Absorption / Q000187:drug effects* / Q000502:physiology; D013053:Spectrophotometry / Q000379:methods; D013678:Technology, Pharmaceutical / Q000379:methods
D008055:Lipids; D008081:Liposomes; D009539:Nicotinic Acids; D010713:Phosphatidylcholines; C008473:methyl nicotinate