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AAPS PharmSciTech

, 20:98 | Cite as

Preparation and Characterization of Syringic Acid–Loaded TPGS Liposome with Enhanced Oral Bioavailability and In Vivo Antioxidant Efficiency

  • Yingkun Liu
  • Congyong Sun
  • Wenjing Li
  • Michael Adu-Frimpong
  • Qilong Wang
  • Jiangnan YuEmail author
  • Ximing XuEmail author
Research Article
  • 18 Downloads

Abstract

In this study, syringic acid–loaded TPGS liposome (SA-TPGS-Ls) was successfully prepared to improve oral bioavailability of syringic acid (SA). SA is a natural and notable antioxidant activity compound with its limited bioavailability ascribable to its poor aqueous solubility and fast elimination. Recently, TPGS has become a perfect molecular biomaterial in developing several carrier systems with sustained, controlled, and targeted the drug delivery. SA-TPGS-Ls was prepared via thin-film dispersion method and characterized in terms of particle size, stability, morphology, and encapsulation efficiency (EE). The results showed that SA-TPGS-Ls had regular spherical-shaped nanoparticles with EE of 96.48 ± 0.76%. The pharmacokinetic studies demonstrated a delayed MRT and prolonged t1/2, while relative oral bioavailability increased by 2.8 times. Tissue distribution showed that SA-TPGS-Ls maintained liver drug concentration while delayed elimination was also observed in the kidney. In CCl4-induced hepatotoxicity study, the activities of hepatic T-AOC, GSH-Px, CAT, GSH, and SOD were greatly elevated, while serum biological markers ALT, AST, and AKP were reduced after treatment of mice with SA-TPGS-Ls. Histopathological studies confirmed that SA-TPGS-Ls could remarkably improve the status of hepatic tissues. Collectively, SA-TPGS-Ls significantly improved the drug encapsulation efficiency, stability coupled with bioavailability of SA, hence increasing in vivo antioxidant activity of the drug.

KEY WORDS

syringic acid vitamin E d-α-tocopheryl polyethylene glycol succinate liposome tissue distribution antioxidant activity 

Notes

Funding information

This work was supported by the National Natural Science Foundation of China (Grants 81720108030 and 81773695), National “Twelfth Five-Year” Plan for Science and Technology Support (Grant 2013BAD16B07-1).

Compliance with Ethical Standards

The procedure for using the experimental animals in this study was followed in concordance with the protocol on animal experiments issued by the Jiangsu University Ethics Committee.

Conflict of Interests

The authors declare that they have no conflict of interest.

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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  • Yingkun Liu
    • 1
  • Congyong Sun
    • 1
  • Wenjing Li
    • 1
  • Michael Adu-Frimpong
    • 1
  • Qilong Wang
    • 1
  • Jiangnan Yu
    • 1
    • 2
    Email author
  • Ximing Xu
    • 1
    • 2
    Email author
  1. 1.Center for Nano Drug/Gene Delivery and Tissue Engineering, School of PharmacyJiangsu UniversityZhenjiangChina
  2. 2.Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue EngineeringJiangsu UniversityZhenjiang CityChina

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