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Updated: Aug 9, 2025
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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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Transcellular Transport Behavior of the Intact Polymeric Mixed Micelles with Different Polymeric Ratios
Wenting Wu1, Quan Ding2, Zhiwei Zhou2
1Institute of Modern Chinese Medicine Pharmaceutical Industry, Jiangxi University of Chinese Medicine, Nanchang, Jiangxi, China.
AAPS Pharmscitech
|February 15, 2023
Summary
Polymeric mixed micelles (PMMs) with high Solutol HS15 content enhance oral drug absorption by utilizing receptor-mediated endocytosis. Adjusting polymeric ratios in PMMs effectively modulates drug delivery and pharmacokinetic profiles.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Biopharmaceutics
Background:
- Polymeric mixed micelles (PMMs) show promise for oral drug delivery, but understanding their absorption characteristics is crucial.
- Investigating the influence of polymer composition on PMMs' cellular transport and in vivo performance is necessary for optimizing oral formulations.
Purpose of the Study:
- To evaluate the transcellular transport and pharmacokinetic behavior of Pluronic F127 and Solutol HS15 based PMMs (FS/PMMs) across Caco-2 cells.
- To determine how varying polymeric ratios (FS) affect the absorption pathways and in vivo outcomes of drug-loaded FS/PMMs.
Main Methods:
- Encapsulation of an environment-responsive probe with aggregation-caused quenching (ACQ) ability to track intact FS/PMMs.
- Utilizing Caco-2 cell transport assays and single-pass intestinal perfusion (SPIP) experiments.
- Analyzing pharmacokinetic parameters and comparing FS/PMM formulations with a drug suspension.
Main Results:
- Polymeric ratios influenced the proportion of endocytosis pathways but not the fundamental pathways or intracellular itinerary.
- FS/PMMs with higher Solutol HS15 content (System-I) favored receptor-mediated endocytosis, reduced lysosomal degradation, and improved Cmax and AUC.
- FS/PMMs with higher Pluronic F127 content (System-II) did not enhance plasma concentration but prolonged in vivo retention time.
Conclusions:
- The ratio of Pluronic F127 to Solutol HS15 in PMMs is a critical factor in modulating transcellular absorption and pharmacokinetic parameters.
- Optimizing FS ratios can enhance oral drug delivery by controlling cellular uptake mechanisms and in vivo drug disposition.
- These findings provide a basis for designing advanced PMM formulations for improved oral drug delivery systems.
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