CHEN Jun1, XIAO Han-lu1, SHEN Yuan1, GU Wei1, YANG Tao2, LI Jun2, CAI Bao-chang1,*
1. Department of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China;
2. Nanjing Maternity and Child Health Care Hospital of Nanjing Medical University, Nanjing 210004, China
Abstract��
To enhance the percutaneous absorption of propranolol by modifying the lipid composition of elastic liposomes. METHODS Elastic liposomes composed of both 1,2-dipalmitoyl-sn-glycero-3-phosphacholine(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 alone 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.
CHEN Jun-,
XIAO Han-Lu-,
SHEN Yuan- etc
.Preparation and Pharmacokinetic Investigation of Propranolol-Loaded Elastic Liposomes Composed of DPPC and SPC[J] Chinese Pharmaceutical Journal, 2013,V48(20): 1761-1765
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