Preparation and pharmacokinetic investigation of propranolol-loaded elastic liposomes composed of DP-PC and SPC / 中国药学杂志

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 (64, molar ratio). The encapsulation efficiency(EE) values of PEL composed of binary mixtures of DPPC and SPC(64, 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 (64, 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.