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Poly(N-isopropylacrylamide) copolymers for constant temperature controlled drug delivery
F Eeckman1, A J Moës, K Amighi
1Laboratoire de Pharmacie Galénique et de Biopharmacie, Université Libre de Bruxelles, Campus Plaine, CP 207, Boulevard du Triomphe, 1050 Bruxelles, Belgium.
International Journal of Pharmaceutics
|March 11, 2004
Summary
Researchers developed thermosensitive poly(N-isopropylacrylamide) (PNIPAAm) copolymers for controlled drug delivery. Incorporating sodium sulfate (Na2SO4) into tablets significantly increased drug release lag times by up to 90%.
Area of Science:
- Polymer Chemistry
- Materials Science
- Pharmaceutical Sciences
Background:
- Development of novel drug delivery systems is crucial for improving therapeutic efficacy.
- Thermosensitive polymers offer potential for time-controlled drug release.
- Poly(N-isopropylacrylamide) (PNIPAAm) exhibits a lower critical solution temperature near physiological conditions.
Purpose of the Study:
- To synthesize and evaluate thermosensitive PNIPAAm-based copolymers for time-controlled drug delivery.
- To investigate the effect of sodium sulfate (Na2SO4) on drug release kinetics from coated tablets.
- To optimize lag time for drug release using a salting-out effect.
Main Methods:
- Synthesis of four thermosensitive PNIPAAm copolymers with phase transition temperatures slightly above 37°C.
- Preparation of compression-coated tablets incorporating Na2SO4 and coated with thermosensitive copolymers.
- In vitro dissolution testing at a constant physiological temperature to measure drug release profiles.
Main Results:
- Thermosensitive copolymers were successfully synthesized for drug delivery applications.
- The incorporation of Na2SO4 into the tablets significantly increased the lag time before drug release.
- A lag time increase of 80-90% was observed for tablets coated with PNIPAAm-co-NVA and PNIPAAm-co-MVA due to the salting out effect.
Conclusions:
- Thermosensitive PNIPAAm copolymers are effective for developing time-controlled drug delivery systems.
- Sodium sulfate incorporation enhances the time-controlled release by modulating polymer swelling and drug diffusion.
- This approach offers a promising strategy for precise control over drug release timing in pharmaceutical formulations.