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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

Published on: August 28, 2015

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The biological fate of orally administered mPEG-PDLLA polymeric micelles

Haisheng He1, Luting Wang1, Yuhua Ma2

  • 1Key Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, China.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|September 18, 2020
PubMed

Insights

This study tracked integral polymeric micelles (PMs) after oral administration in rats, finding direct evidence of their absorption into the bloodstream and liver. While some PMs entered the lymphatic system, the total oral absorption amount requires further investigation.

Area of Science:

  • Nanotechnology and Drug Delivery
  • Pharmaceutics and Pharmacokinetics

Background:

  • Understanding the oral absorption of polymeric micelles (PMs) is crucial for developing effective oral drug delivery systems.
  • Integral transport of PMs across the gastrointestinal tract remains a key area for investigation.

Purpose of the Study:

  • To investigate the biological fate of integral polymeric micelles (PMs) following oral administration.
  • To elucidate the contribution of integral PM transport to overall oral absorption.
  • To track the absorption and biodistribution of PMs using near-infrared fluorophores.

Main Methods:

  • Polymeric micelles (PMs) composed of mPEG-PDLLA copolymers and DSPE-PEG were synthesized and characterized for particle size.
  • PMs were labeled with near-infrared fluorophores and administered orally to rats.
  • Confocal laser scanning microscopy and Caco-2 cell line models were used to assess cellular uptake and trans-epithelial transport.

Main Results:

  • Integral PMs were retained in the gastrointestinal tract for at least 4 hours post-administration.
  • Fluorescence in blood and liver confirmed the oral absorption of intact PMs, with approximately 1-2% absorbed via the lymphatic pathway.
  • Cellular uptake efficiency varied, being higher in Caco-2 cells (4-7%) than in mucus-hindered co-culture models (1-3%), with significant transport across multi-layered cell models.

Conclusions:

  • Direct evidence supports the penetration of integral polymeric micelles across the enteric epithelia.
  • The total amount of PMs absorbed systemically following oral administration may be limited.
  • Further studies are needed to fully elucidate the extent of PMs reaching systemic circulation.
Keywords:
Aggregation-caused quenchingBiological fateDrug deliveryOralPolymeric micellesin vivo fate

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