Physical and Pharmacokinetic Characterizations of trans-Resveratrol (t-Rev) Encapsulated with Self-Assembling Lecithin-based Mixed Polymeric Micelles (saLMPMs)

Tzu Pin Li, Wan Ping Wong, Ling Chun Chen, Chia Yu Su, Lih Geeng Chen, Der Zen Liu, Hsiu O. Ho, Ming Thau Sheu

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

This study involved physical and pharmacokinetic characterizations of trans-resveratrol (t-Rev)-loaded saLMPMs which attempted to improve t-Rev's pharmacokinetic profiles and bioavailability resolving hurdles limiting its potential health benefits. The optimal formulation consisted of t-Rev, lecithin, and Pluronic® P123 at 5:2:20 (t-Rev-loaded PP123 saLMPMs) provided mean particle size <200 nm, encapsulation efficiency >90%, and drug loading >15%. Compared to t-Rev solubilized with HP-β-CD, t-Rev-loaded PP123 saLMPMs enhanced t-Rev's stability in PBS at RT, 4 °C, and 37 °C and in FBS at 37 °C, and retarded the in vitro release. Intravenous administration of t-Rev-loaded PP123 saLMPMs was able to enhance 40% absolute bioavailability and a greater portion of t-Rev was found to preferably distribute into peripheral compartment potentially establishing a therapeutic level at the targeted site. With oral administration, t-Rev-loaded LMPMs increases 2.17-fold absolute bioavailability and furnished a 3-h period of time in which the plasma concentration maintained above the desirable concentration for chemoprevention and accomplished a higher value of the dose-normalized area under the curve for potentially establishing an effective level at the target site. Therefore, intravenous and oral pharmacokinetic characteristics of t-Rev encapsulated with PP123 saLMPMs indicate that t-Rev can be translated into a clinically useful therapeutic agent.

Original languageEnglish
Article number10674
JournalScientific Reports
Volume7
Issue number1
DOIs
Publication statusPublished - Dec 1 2017

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Lecithins
Micelles
Pharmacokinetics
Biological Availability
resveratrol
Chemoprevention
Insurance Benefits
Particle Size
Intravenous Administration
Area Under Curve
Oral Administration

ASJC Scopus subject areas

  • General

Cite this

Physical and Pharmacokinetic Characterizations of trans-Resveratrol (t-Rev) Encapsulated with Self-Assembling Lecithin-based Mixed Polymeric Micelles (saLMPMs). / Li, Tzu Pin; Wong, Wan Ping; Chen, Ling Chun; Su, Chia Yu; Chen, Lih Geeng; Liu, Der Zen; Ho, Hsiu O.; Sheu, Ming Thau.

In: Scientific Reports, Vol. 7, No. 1, 10674, 01.12.2017.

Research output: Contribution to journalArticle

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