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Indomethacin-containing interpolyelectrolyte complexes based on Eudragit® E PO/S 100 copolymers as a novel drug
Rouslan I Moustafine1, Alexander Y Sitenkov1, Alexandra V Bukhovets1
1Department of Pharmaceutical, Analytical and Toxicological Chemistry, Kazan State Medical University, Butlerov Street 49, 420012 Kazan, Russian Federation.
International Journal of Pharmaceutics
|April 4, 2017
Summary
This study developed novel drug delivery systems using Eudragit EPO and S100 copolymers with indomethacin for oral administration. The resulting drug-polyelectrolyte complexes show sustained drug release, with potential for colon-specific delivery.
Area of Science:
- Polymer chemistry and materials science
- Pharmaceutical sciences
- Drug delivery systems
Background:
- Eudragit EPO and S100 are oppositely-charged (meth)acrylate copolymers with potential in oral drug delivery.
- Indomethacin (IND) is a model drug used to evaluate novel delivery systems.
- Drug-polyelectrolyte complexes (DPEC) and drug-interpolyelectrolyte complexes (DIPEC) offer unique properties for drug encapsulation.
Purpose of the Study:
- To evaluate the potential applications of a novel system composed of Eudragit EPO and S100 copolymers loaded with indomethacin (IND) for oral drug delivery.
- To characterize the formation, composition, and solid-state properties of drug-polyelectrolyte complexes (DPC) and drug-interpolyelectrolyte complexes (DIPEC).
- To investigate the drug release profiles and assess the suitability of these systems for sustained and colon-specific delivery.
Main Methods:
- Preparation of DPC and DIPEC particles by mixing aqueous copolymer solutions.
- Characterization using gravimetry, UV-spectrophotometry, capillary viscosity, and elemental analysis.
- Solid-state analysis via FTIR/NIR, Raman spectroscopy, XRPD, and modulated DSC.
- In vitro drug release studies under simulated gastrointestinal tract conditions.
Main Results:
- DIPEC particles ((EPO-IND)/S100) were successfully prepared, forming chemically homogenous materials with a single glass transition temperature (Tg).
- Ionic interactions between copolymers and indomethacin were confirmed through spectroscopic analysis (IR band at 1560cm-1).
- Indomethacin was converted into its amorphous form within the DIPEC formulation, confirmed by XRPD, NIR, and Raman spectroscopy.
- Sustained release of IND from both DPC and DIPEC systems was observed over 7 hours.
- The S100 component in DIPEC slowed the release rate, indicating potential for colon-specific drug delivery.
Conclusions:
- Novel DPC and DIPEC systems incorporating indomethacin were successfully developed using Eudragit EPO and S100.
- These systems demonstrate sustained indomethacin release, with DIPEC showing promise for colon-specific oral drug delivery.
- The prepared DPC and DIPEC can be formulated into tablets for potential oral dosage forms offering controlled drug release profiles.