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Preparation, in vitro and in vivo evaluation of mPEG-PLGA nanoparticles co-loaded with syringopicroside and hydroxytyrosol

  • Qingxia Guan
  • Shuang Sun
  • Xiuyan Li
  • Shaowa Lv
  • Ting Xu
  • Jialin Sun
  • Wenjing Feng
  • Liang Zhang
  • Yongji Li
Delivery Systems Original Research
Part of the following topical collections:
  1. Delivery Systems

Abstract

This study investigated the therapeutic efficiency of monomethoxy polyethylene glycol-poly(lactic-co-glycolic acid) (mPEG-PLGA) co-loaded with syringopicroside and hydroxytyrosol as a drug with effective targeting and loading capacity as well as persistent circulation in vivo. The nanoparticles were prepared using a nanoprecipitation method with mPEG-PLGA as nano-carrier co-loaded with syringopicroside and hydroxytyrosol (SH-NPs). The parameters like in vivo pharmacokinetics, biodistribution in vivo, fluorescence in vivo endomicroscopy, and cellular uptake of SH-NPs were investigated. Results showed that the total encapsulation efficiency was 32.38 ± 2.76 %. Total drug loading was 12.01 ± 0.42 %, particle size was 91.70 ± 2.11 nm, polydispersity index was 0.22 ± 0.01, and zeta potential was −24.5 ± 1.16 mV for the optimized SH-NPs. The nanoparticle morphology was characterized using transmission electron microscopy, which indicated that the particles of SH-NPs were in uniformity within the nanosize range and of spherical core shell morphology. Drug release followed Higuchi kinetics. Compared with syringopicroside and hydroxytyrosol mixture (SH), SH-NPs produced drug concentrations that persisted for a significantly longer time in plasma following second-order kinetics. The nanoparticles moved gradually into the cell, thereby increasing the quantity. ALT, AST, and MDA levels were significantly lower on exposure to SH-NPs than in controls. SH-NPs could inhibit the proliferation of HepG2.2.15 cells and could be taken up by HepG2.2.15 cells. The results confirmed that syringopicroside and hydroxytyrosol can be loaded simultaneously into mPEG-PLGA nanoparticles. Using mPEG-PLGA as nano-carrier, sustained release, high distribution in the liver, and protective effects against hepatic injury were observed in comparison to SH.

Keywords

Drug Release Zeta Potential Cellular Uptake Drug Loading Entrapment Efficiency 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Abbreviation

SYR

Syringopicroside

HT

Hydroxytyrosol

SH

Syringopicroside and hydroxytyrosol

SH-NPs

Nanoparticles co-loaded with syringopicroside and hydroxytyrosol

t1/2 α

Alpha elimination half-life

t1/2 β

Beta elimination half-life

CL

Clearance

AUC

Area under the concentration–time curve

Notes

Acknowledgments

We acknowledge Specialized Research Fund for the Doctoral Program of Higher Education (20112327110009) and the National Natural Science Foundation of China (81274091) for the Grants received in support of this research.

Compliance with ethical standards

Disclosure

The authors report no conflicts of interest in this work.

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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  • Qingxia Guan
    • 1
  • Shuang Sun
    • 1
  • Xiuyan Li
    • 1
  • Shaowa Lv
    • 1
  • Ting Xu
    • 1
  • Jialin Sun
    • 1
  • Wenjing Feng
    • 1
  • Liang Zhang
    • 1
  • Yongji Li
    • 1
  1. 1.College of PharmacyHeilongjiang University of Chinese MedicineHarbinChina

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