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. 2020 Jun 30;12(7):1459.
doi: 10.3390/polym12071459.

Interpolymer Complexes of Eudragit® Copolymers as Novel Carriers for Colon-Specific Drug Delivery

Aleksandra V Bukhovets  1 , Nikoletta Fotaki  2 , Vitaliy V Khutoryanskiy  1   3 , Rouslan I Moustafine  1
Affiliations

Interpolymer Complexes of Eudragit® Copolymers as Novel Carriers for Colon-Specific Drug Delivery

Aleksandra V Bukhovets et al. Polymers (Basel). .

Abstract

Interpolymer complexes (IPC) based on Eudragit® EPO and Eudragit® S100 were investigated as potential carriers for oral controlled drug delivery to the colon. IPC samples were prepared by mixing copolymer solutions in organic solvents (ethanol, isopropanol:acetone mixture (60:40, % v/v) and tetrahydrofuran). According to the data of elemental analysis, FTIR-spectroscopy, X-ray photoelectron spectroscopy and thermal analysis these IPCs have excess of anionic copolymer (Eudragit® S100) in their structure; they are stabilized by hydrogen and ionic intermacromolecular bonds and do not include free copolymer domains. IPC have pH-independent swelling properties in the media mimicking gastrointestinal tract (GIT) conditions and provide colon-specific delivery of indomethacin in buffer solutions (pH 1.2; 5.8; 6.8; 7.4) and in biorelevant media (fasted state simulated gastric fluid, fasted state simulated intestinal fluid-version 2 and fasted stated simulated colonic fluid).

Keywords: Eudragit®, indomethacin; biorelevant media; controlled drug delivery; drug delivery systems; interpolymer complexes; oral drug delivery.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
FTIR spectra of the IPC.
Figure 2
Figure 2
N1s spectra of interpolymer complexes. (a) IPC-1; (b) IPC-2; (c) IPC-3; (d) IPC-4; (e) IPC-5; (f) IPC-6.
Figure 3
Figure 3
Exemplar differential scanning calorimetry (DSC) thermograms of interpolymer complexes and Eudragit® copolymers: (a) Eudragit® S100; (b) Eudragit® EPO and (c) IPCs.
Figure 4
Figure 4
External appearance of IPC compacts during the swelling test.
Figure 5
Figure 5
Swelling profiles of IPC compacts in buffer solutions mimicking the pH values in different parts of gastrointestinal tract.
Figure 6
Figure 6
FTIR-spectra of polycomplex compacts (prepared from IPC-1), after swelling in buffer solutions mimicking the pH values in different parts of gastrointestinal tract.
Figure 7
Figure 7
Release profiles of indomethacin from IPC compacts in the buffer solutions mimicking the environment of gastrointestinal tract (USP IV apparatus).
Figure 8
Figure 8
Release profiles of indomethacin from IPC compacts in the biorelevant media (USP IV apparatus).
Figure 9
Figure 9
Release profiles of indomethacin from IPC compacts in the buffer solutions mimicking the environment of gastrointestinal tract (USP III apparatus).
Figure 10
Figure 10
Release profiles of indomethacin from IPC compacts in the biorelevant media (USP III apparatus).
See this image and copyright information in PMC

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