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The characterisation, pharmacokinetic and tissue distribution studies of TPGS modified myricetrin mixed micelles in

Chunmei Wei1, Qilong Wang1, Wen Weng1

  • 1a Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering , Jiangsu University , Zhenjiang , China.

Journal of Microencapsulation
|May 24, 2019
PubMed

Insights

This study developed myricetrin-loaded TPGS micelles, enhancing bioavailability and liver targeting. These novel micelles show improved drug release and hepatic accumulation compared to traditional formulations.

Area of Science:

  • Pharmacology
  • Nanotechnology
  • Drug Delivery

Background:

  • Myricetrin, a natural compound, has therapeutic potential but suffers from poor bioavailability.
  • Developing effective drug delivery systems is crucial for maximizing myricetrin's therapeutic benefits.
  • TPGS (d-alpha-tocopheryl polyethylene glycol 1000 succinate) is a known excipient that can enhance drug delivery.

Purpose of the Study:

  • To investigate the bioavailability and liver targeting of myricetrin-loaded ternary micelles.
  • To evaluate the effect of TPGS modification on micelle characteristics and drug release.
  • To compare the in vivo performance of TPGS-modified micelles with unmodified micelles and free myricetrin.

Main Methods:

  • Preparation and characterization of myricetrin-loaded micelles with and without TPGS (particle size, encapsulation efficiency).
  • In vitro drug release studies in various media (pH 6.8, pH 1.2, double distilled water).
  • In vivo bioavailability and tissue distribution studies following oral administration in animal models.

Main Results:

  • TPGS-modified micelles exhibited smaller particle size (26.42 nm) and higher encapsulation efficiency (93.8%) compared to unmodified micelles (30.93 nm, 83.3%).
  • Myricetrin release rate was significantly higher from both micellar systems than from free myricetrin.
  • In vivo studies demonstrated markedly improved bioavailability of myricetrin from TPGS micelles and preferential accumulation in liver tissue.

Conclusions:

  • Myricetrin-loaded TPGS micelles represent a promising nanocarrier system for enhancing oral bioavailability.
  • The TPGS modification facilitates improved liver targeting and increased myricetrin concentration in hepatic tissue.
  • These findings suggest potential for developing TPGS-modified myricetrin micelles as an effective therapeutic strategy for liver-related conditions.
Keywords:
releaseMyricetrin mixed micellesTPGSoral bioavailabilitytissue distribution

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