Lu Wang1, Yafang Wang1, Xueqing Wang2, Lin Sun1, Zhengzheng Zhou1, Jinjian Lu1, Ying Zheng1. 1. a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , SAR , China ; 2. b State Key Laboratory of Natural and Biomimetic Drugs , School of Pharmaceutical Sciences, Peking University , Beijing , China.
Abstract
CONTEXT: PLGA nanoparticles have been widely utilised to encapsulate lipophilic drugs for sustained release. OBJECTIVE: This study was to enhance encapsulation efficiency and drug loading for the poorly lipophilic drug dihydroartemisinin (DHA) in PLGA nanoparticles, where amphiphilic phospholipid was employed as the intermediate. MATERIALS AND METHODS: DHA-phospholipid complex formulation was optimised using the response surface method. DHA-phospholipid complex-nanoparticles (DHA-PLC-NPs) were prepared using the solvent evaporation method. RESULTS: The particle size, zeta potential, entrapment efficiency and drug loading of the nanoparticles were 265.3 ± 7.9 nm, -21.4 ± 6.3 mV, 74.2 ± 6.5% and 2.80 ± 0.35%, respectively. Compared with the rapidly released free form, DHA underwent sustained release from the nanoparticles. DHA-PLC-NPs presented stronger cell proliferative inhibition than DHA treatment alone and apoptosis was obviously induced after DHA-PLC-NPs treatment. CONCLUSION: Phospholipid complexes are useful intermediate to improve the lipophilicity of drugs, the interaction with the hydrophobic core of PLGA and the encapsulation efficiency of poorly lipophilic drugs in polymeric nanoparticles.
CONTEXT: PLGA nanoparticles have been widely utilised to encapsulate lipophilic drugs for sustained release. OBJECTIVE: This study was to enhance encapsulation efficiency and drug loading for the poorly lipophilic drug dihydroartemisinin (DHA) in PLGA nanoparticles, where amphiphilic phospholipid was employed as the intermediate. MATERIALS AND METHODS:DHA-phospholipid complex formulation was optimised using the response surface method. DHA-phospholipid complex-nanoparticles (DHA-PLC-NPs) were prepared using the solvent evaporation method. RESULTS: The particle size, zeta potential, entrapment efficiency and drug loading of the nanoparticles were 265.3 ± 7.9 nm, -21.4 ± 6.3 mV, 74.2 ± 6.5% and 2.80 ± 0.35%, respectively. Compared with the rapidly released free form, DHA underwent sustained release from the nanoparticles. DHA-PLC-NPs presented stronger cell proliferative inhibition than DHA treatment alone and apoptosis was obviously induced after DHA-PLC-NPs treatment. CONCLUSION:Phospholipid complexes are useful intermediate to improve the lipophilicity of drugs, the interaction with the hydrophobic core of PLGA and the encapsulation efficiency of poorly lipophilic drugs in polymeric nanoparticles.