Abstract
Background:Conventional and PEGylated liposomes were developed, aimed at improving the pain-killing effect of opiorphin.Methods:The antinociceptive action of the formulations was investigated on rats (tail-flick test), and compared with that of opiorphin and morphine aqueous solutions (all at 5 mg/kg).Results:Opiorphin loading in conventional liposomes enabled a 28% AUC increase with respect to free peptide. PEGylated liposomes provided AUC values 80, 60 and 40% higher than free peptide, morphine and opiorphin-loaded conventional liposomes, respectively. Moreover, opiorphin entrapment in PEGylated liposomes increased analgesic effect duration by more than 50%. These results were attributed to the greater effectiveness of PEGylated liposomes in protecting the drug and prolonging its circulation time.Conclusion:Opiorphin-loaded PEGylated-liposomes can represent a valid alternative to morphine in pain management.
Highlights
Conventional and PEGylated liposomes were developed, aimed at improving the pain-killing effect of opiorphin
Opiorphin is a natural peptide secreted into the human saliva, endowed with a strong analgesic effect, even superior to that of morphine, and without the several side effects typical of morphine and morphine-like drugs
Conventional and PEGylated liposomes, aimed at protecting the drug from rapid metabolization and improving its therapeutic efficacy, were developed, and both allowed the entrapment of large amounts of the peptide
Summary
Conventional and PEGylated liposomes were developed, aimed at improving the pain-killing effect of opiorphin. Methods:The antinociceptive action of the formulations was investigated on rats (tail-flick test), and compared with that of opiorphin and morphine aqueous solutions (all at 5 mg/kg). Results: Opiorphin loading in conventional liposomes enabled a 28% AUC increase with respect to free peptide. PEGylated liposomes provided AUC values 80, 60 and 40% higher than free peptide, morphine and opiorphin-loaded conventional liposomes, respectively. Opiorphin entrapment in PEGylated liposomes increased analgesic effect duration by more than 50%. These results were attributed to the greater effectiveness of PEGylated liposomes in protecting the drug and prolonging its circulation time. Conclusion: Opiorphin-loaded PEGylated-liposomes can represent a valid alternative to morphine in pain management
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