Novel nanoliposomal delivery system for polydatin: preparation, characterization, and in vivo evaluation

Abstract

Xiaobo Wang,1,* Qigang Guan,2,* Wei Chen,3 Xianming Hu,3 Li Li11Department of Hematology, The Second Hospital of Dalian Medical University, Dalian, 2Department of Cardiology, The First Affiliated Hospital of China Medical University, Shenyang, 3Department of Pharmaceutical, Shenyang Institute of Pharmaceutical Industry, Shenyang, People’s Republic of China *These authors contributed equally to this work 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.Conclusion: PLD-loaded liposomes could significantly prolong the drug circulation time in vivo and increase the oral bioavailability of the drug. Keywords: polydatin, liposome, in vitro release, oral bioavailability, histological change