title: Novel nanoliposomal delivery system for polydatin: preparation, characterization, and in vivo evaluation.
abstract: BACKGROUND
  The objective of this study was to develop a novel polydatin (PLD)-loaded liposome system using the thin film hydration technique.
  
  
  METHODS
  The delivery system was characterized in terms of morphology, size, zeta potential, encapsulation efficiency, and in vitro release. In addition, a pharmacokinetic study was carried out in rats after oral administration of PLD-loaded liposomes in vivo.
  
  
  RESULTS
  Transmission electron microscopy revealed that the PLD-loaded liposomes had a homogeneous size and spherical shape. Dynamic light scattering showed that the PLD-loaded liposomes had a smaller size with a mean value of 80.2±3.7 nm and a polydispersity index of 0.12±0.06. The encapsulation efficiency of the prepared liposomes was 88.4%±3.7%. During the release process, liposome showed two distinct phases. The first was characterized by rapid release during the first 2 hours, which could be related to the release of the drug adsorbed on the surface of liposomes. In the second phase, the release rate slowed down, demonstrating a typical sustained and prolonged drug-release behavior. The release kinetic model for the PLD-loaded liposomes fitted well with the Weibull distribution equation. In vivo, relative oral bioavailability of the encapsulated PLD was 282.9%, ie, significantly enhanced (P<0.05) compared with the free drug. No histological changes occurred in the organs after administration of PLD-loaded liposomes.
  
  
  CONCLUSIONS
  PLD-loaded liposomes could significantly prolong the drug circulation time in vivo and increase the oral bioavailability of the drug.
authors.affiliation: Department of Hematology, The Second Hospital of Dalian Medical University, Dalian, People's Republic of China.
authors.forename: Xiaobo
authors.initials: X
authors.lastname: Wang
authors.affiliation: Department of Cardiology, The First Affiliated Hospital of China Medical University, Shenyang, People's Republic of China.
authors.forename: Qigang
authors.initials: Q
authors.lastname: Guan
authors.affiliation: Department of Pharmaceutical, Shenyang Institute of Pharmaceutical Industry, Shenyang, People's Republic of China.
authors.forename: Wei
authors.initials: W
authors.lastname: Chen
authors.affiliation: Department of Pharmaceutical, Shenyang Institute of Pharmaceutical Industry, Shenyang, People's Republic of China.
authors.forename: Xianming
authors.initials: X
authors.lastname: Hu
authors.affiliation: Department of Hematology, The Second Hospital of Dalian Medical University, Dalian, People's Republic of China.
authors.forename: Li
authors.initials: L
authors.lastname: Li
mesh_terms: D000284:Administration, Oral; D000818:Animals; D016503:Drug Delivery Systems; D005960:Glucosides / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D008081:Liposomes; D008297:Male; D015394:Molecular Structure; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D013267:Stilbenes / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D005960:Glucosides; D008081:Liposomes; D013267:Stilbenes; C058229:polydatin
keywords: histological change; in vitro release; liposome; oral bioavailability; polydatin
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