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已发表论文
虎杖苷的新型纳米脂质体给药系统： 制备、表征和体内评价
Authors Wang X, Guan Q, Chen W, Hu X, Li L
Published Date March 2015 Volume 2015:9 Pages 1805—1813
DOI http://dx.doi.org/10.2147/DDDT.S77615
Received 16 November 2014, Accepted 11 February 2015, Published 30 March 2015
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
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
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