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Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
Published on: October 10, 2016
Monoglyceride-based self-assembling copolymers as carriers for poorly water-soluble drugs
L Rouxhet1, M Dinguizli, J P Latere Dwan'isa
1Johnson & Johnson Pharmaceutical Research and Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
International Journal of Pharmaceutics
|August 12, 2009
Summary
New biodegradable polymers self-assemble into micelles to significantly enhance the solubility of poorly soluble drugs. These self-assembling polymers show promise for improving oral drug delivery and biopharmaceutical performance.
Area of Science:
- Polymer Chemistry
- Materials Science
- Pharmaceutical Sciences
Background:
- Poorly soluble drugs present significant challenges in oral drug delivery.
- Developing effective drug delivery systems is crucial for enhancing therapeutic efficacy.
- Self-assembling polymeric micelles offer a promising strategy for solubilizing hydrophobic compounds.
Purpose of the Study:
- To design and synthesize novel amphiphilic biodegradable copolymers for self-assembly into polymeric micelles.
- To enhance the aqueous solubility of poorly water-soluble drug candidates.
- To evaluate the potential of these polymers for improving oral biopharmaceutical performance.
Main Methods:
- Synthesis of biodegradable copolymers via polycondensation of polyethylene glycol (PEG), monooleylglyceride (MOG), and succinic anhydride (SA).
- Characterization of polymer self-assembly, critical micellar concentration, cloud point, and flocculation point.
- Assessment of drug solubility enhancement and in vitro drug release from HPMC capsules.
- Evaluation of polymer cytotoxicity using MTT assay on Caco-2 cells.
Main Results:
- Amphiphilic copolymers self-assembled into micelles with a diameter of approximately 10 nm.
- Polymers increased the solubility of poorly water-soluble drugs up to 500-fold at a 1% concentration.
- Drug solubility enhancement was concentration-dependent.
- Polymers demonstrated rapid drug release from HPMC capsules and showed lower cytotoxicity with longer PEG chains.
- The PEG1000/MOG/SA (45/5/50) copolymer exhibited favorable properties.
Conclusions:
- The designed biodegradable amphiphilic polymers effectively form self-assembling micelles.
- These polymeric micelles significantly improve the solubility and oral biopharmaceutical performance of poorly soluble drugs.
- The developed polymers, particularly PEG1000/MOG/SA, represent promising candidates for advanced drug delivery systems.
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