title: Encapsulation of low lipophilic and slightly water-soluble dihydroartemisinin in PLGA nanoparticles with phospholipid to enhance encapsulation efficiency and in vitro bioactivity.
abstract: BACKGROUND
  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.
  
  
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , SAR , China ;
authors.forename: Lu
authors.initials: L
authors.lastname: Wang
authors.affiliation: a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , SAR , China ;
authors.forename: Yafang
authors.initials: Y
authors.lastname: Wang
authors.affiliation: b State Key Laboratory of Natural and Biomimetic Drugs , School of Pharmaceutical Sciences, Peking University , Beijing , China.
authors.forename: Xueqing
authors.initials: X
authors.lastname: Wang
authors.affiliation: a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , SAR , China ;
authors.forename: Lin
authors.initials: L
authors.lastname: Sun
authors.affiliation: a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , SAR , China ;
authors.forename: Zhengzheng
authors.initials: Z
authors.lastname: Zhou
authors.affiliation: a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , SAR , China ;
authors.forename: Jinjian
authors.initials: J
authors.lastname: Lu
authors.affiliation: a State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , SAR , China ;
authors.forename: Ying
authors.initials: Y
authors.lastname: Zheng
mesh_terms: D037621:Artemisinins / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010743:Phospholipids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011100:Polyglycolic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D037621:Artemisinins; D004337:Drug Carriers; D010743:Phospholipids; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C039060:artenimol
keywords: PLGA; Phospholipids; cancer; encapsulation; nanoparticle