ABSTRACT
OBJECTIVE: To enhance the percutaneous absorption of propranolol by modifying the lipid composition of elastic liposomes. METHODS: Elastic liposomes composed of both 1, 2-dipalmitoyl-m-glycero-3-phosphacholme(DPPC) and soy phosphatidylcholine (SPC) were prepared and propranolol was encapsulated into liposomes by ammonium sulfate gradient loading method. Then the pharmaceutical and pharmacokinetic properties of propranolol-loaded elastic liposomes (PEL) with different lipid compositions were compared. RESULTS: The highest deformability was obtained with PEL composed of binary mixtures of DPPC and SPC (6:4, molar ratio). The encapsulation efficiency(EE) values of PEL composed of binary mixtures of DPPC and SPC(6:4, molar ratio) and SPC a-lone were 78.97 ± 2.94% and 68.67 ± 0.58%, respectively. And the drug release values were (23.23 ± 0.90)% and (39.84 ± 0.51)%, respectively. Following transdermal administration, the bioavailability of PEL composed of binary mixtures of DPPC and SPC (6:4, molar ratio) was significantly increased(14.73-fold) compared with that of PEL composed of SPC alone. CONCLUSION: The membrane stability and percutaneous absorption of PEL can be significantly improved by the application of binary mixtures of DPPC and SPC.