Preparation and in vitro activity of liposome encapsulated opioids.
Four opiate molecules: morphine, naloxone, meperidine and codeine have been encapsulated in liposomes. The encapsulation efficiency has been studied as a function of the following parameters: liposome preparation method, lipid composition and opioid molecule hydrophobicity. The most important parameter as far as the entrapment efficiency is concerned is the liposome preparation method. The opioid activity of these molecules in vitro (Guinea Pig Ileum preparation) has been determined. No differences in the IC50 values could be found between encapsulated and free drug molecules.
Reig
F
F
Laboratory of Peptides, CID, CSIC, Barcelona, Spain.
Alsina
M A
MA
Busquets
M A
MA
Valencia
G
G
Garcia Anton
J M
JM
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D002784:Cholesterol / Q000032:analysis; D003061:Codeine / Q000032:analysis / Q000494:pharmacology*; D004337:Drug Carriers; D004339:Drug Compounding / Q000379:methods; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008081:Liposomes; D008614:Meperidine / Q000032:analysis / Q000494:pharmacology*; D009020:Morphine / Q000032:analysis / Q000494:pharmacology*; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009270:Naloxone / Q000032:analysis / Q000494:pharmacology*; D010713:Phosphatidylcholines / Q000032:analysis; D010718:Phosphatidylserines / Q000032:analysis
D004337:Drug Carriers; D008081:Liposomes; D010713:Phosphatidylcholines; D010718:Phosphatidylserines; D009270:Naloxone; D009020:Morphine; D002784:Cholesterol; D008614:Meperidine; D003061:Codeine