Rouslan I. Moustafine, Natalia N. Porfiryeva, Shamil F. Nasibullin, Alexander Y. Sitenkov, Aleksandra V. Sitenkova, Venera R. Timergalieva, Vera A. Kemenova
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The binding ratio of a unit molecule of RL with polyanions was found to range between 1.73:1 and 4.19:1 while increasing the percentages of carboxylic groups in their structures from 10% (FS) to 50% (L100-55). As a result of electrostatic interaction between the copolymer chains, the glass transition temperature of the IPEC changed significantly. Considerable pH-sensitive swelling in acidic and neutral media was observed for different type of IPECs. Through evaluation of diffusion-transportation properties of the IPECs, basic mechanisms controlling the delivery of indomethacin were obtained. The results of swelling and release of the model drug from the polycomplex matrices confirm that they have potential to be used in colon-specific drug delivery.</p><h3>Graphical Abstract</h3>\n<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 2","pages":""},"PeriodicalIF":3.4000,"publicationDate":"2025-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Characterization of Interpolyelectrolyte Complexes Based on Eudragit® RL and Oppositely Charged Eudragit® Polyanions as a Novel Matrix System for Colon-specific Drug Delivery\",\"authors\":\"Rouslan I. Moustafine, Natalia N. Porfiryeva, Shamil F. Nasibullin, Alexander Y. Sitenkov, Aleksandra V. Sitenkova, Venera R. Timergalieva, Vera A. Kemenova\",\"doi\":\"10.1208/s12249-024-03025-z\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The design of new interpolyelectrolyte complexes (IPEC) between Eudragit<sup>®</sup> polycation (type RL) and oppositely charged Eudragit<sup>®</sup> polyanions (types L100-55, L100, S100, FS) was investigated. The formation and chemical composition of novel IPECs between countercharged Eudragit<sup>®</sup> copolymers was established by gravimetric and elemental analysis. The structure and solid state properties of the synthesized IPEC were investigated comparatively to correspondent physical mixtures pairs of copolymers in similar molar ratio, using Fourier transform infrared (FTIR) spectroscopy and modulated temperature differential scanning calorimetry (mDSC). The binding ratio of a unit molecule of RL with polyanions was found to range between 1.73:1 and 4.19:1 while increasing the percentages of carboxylic groups in their structures from 10% (FS) to 50% (L100-55). As a result of electrostatic interaction between the copolymer chains, the glass transition temperature of the IPEC changed significantly. Considerable pH-sensitive swelling in acidic and neutral media was observed for different type of IPECs. Through evaluation of diffusion-transportation properties of the IPECs, basic mechanisms controlling the delivery of indomethacin were obtained. 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Characterization of Interpolyelectrolyte Complexes Based on Eudragit® RL and Oppositely Charged Eudragit® Polyanions as a Novel Matrix System for Colon-specific Drug Delivery
The design of new interpolyelectrolyte complexes (IPEC) between Eudragit® polycation (type RL) and oppositely charged Eudragit® polyanions (types L100-55, L100, S100, FS) was investigated. The formation and chemical composition of novel IPECs between countercharged Eudragit® copolymers was established by gravimetric and elemental analysis. The structure and solid state properties of the synthesized IPEC were investigated comparatively to correspondent physical mixtures pairs of copolymers in similar molar ratio, using Fourier transform infrared (FTIR) spectroscopy and modulated temperature differential scanning calorimetry (mDSC). The binding ratio of a unit molecule of RL with polyanions was found to range between 1.73:1 and 4.19:1 while increasing the percentages of carboxylic groups in their structures from 10% (FS) to 50% (L100-55). As a result of electrostatic interaction between the copolymer chains, the glass transition temperature of the IPEC changed significantly. Considerable pH-sensitive swelling in acidic and neutral media was observed for different type of IPECs. Through evaluation of diffusion-transportation properties of the IPECs, basic mechanisms controlling the delivery of indomethacin were obtained. The results of swelling and release of the model drug from the polycomplex matrices confirm that they have potential to be used in colon-specific drug delivery.
期刊介绍：
AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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