In vivo study of liposomes as drug carriers to oral mucosa using EPR oximetry.
The purpose of this study was to select the best types of liposomes for use as drug carriers for topical treatment of oral mucosal lesions. Electron paramagnetic resonance (EPR) oximetry, using the paramagnetic probe lithium phthalocyanine, was used in vivo to measure the effects of a hyperemic drug, benzyl nicotinate (BN) which was incorporated into liposomes of varying size and composition. The liposomes were made from either hydrogenated or non-hydrogenated soy lecithin and mixed with polymethyl methacrylate ointment for application. EPR oximetry was used to measure the partial pressure of oxygen (pO2) in the oral mucosa before and after application of liposomes. It was found that the most pronounced changes of pO2 in oral mucosa and also the longest action of the drug occurred after the topical application of BN in multi-lamellar liposomes made from hydrogenated soy lecithin (p<0.0001). When these liposomes were applied to oral mucosa over 3 successive days it was found that pO2 increased the most on the first day, the effect gradually decreased following application on the second and third days. The duration of the resulting hyperemia was the longest on the second day (p<0.01). Among the examined carriers, multi-lamellar liposomes made from hydrogenated soy lecithin appear to be the most appropriate for local drug delivery to oral mucosa.
Erjavec
V
V
Clinic for Small Animal Medicine and Surgery, Veterinary Faculty, University of Ljubljana, Gerbiceva 60, 1115 Ljubljana, Slovenia.
Pavlica
Z
Z
Sentjurc
M
M
Petelin
M
M
D000818:Animals; D002784:Cholesterol; D003497:Cyclic N-Oxides; D016503:Drug Delivery Systems; D004578:Electron Spin Resonance Spectroscopy; D005260:Female; D006940:Hyperemia / Q000139:chemically induced / Q000175:diagnosis; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry; D009061:Mouth Mucosa / Q000378:metabolism*; D009539:Nicotinic Acids / Q000008:administration & dosage; D009824:Ointments / Q000008:administration & dosage; D010092:Oximetry / Q000379:methods; D010100:Oxygen / Q000032:analysis / Q000378:metabolism*; D010316:Particle Size; D010713:Phosphatidylcholines; D019904:Polymethyl Methacrylate; D051381:Rats; D017208:Rats, Wistar; D013113:Spin Labels
D003497:Cyclic N-Oxides; D008081:Liposomes; D009539:Nicotinic Acids; D009824:Ointments; D010713:Phosphatidylcholines; D013113:Spin Labels; C051599:4-(N,N,N-trimethylamino)-2,2,6,6-tetramethylpiperidine-1-oxyl; D019904:Polymethyl Methacrylate; D002784:Cholesterol; C025653:nicotinic acid benzyl ester; D010100:Oxygen