Polyelectrolyte-based solid dispersions for enhanced dissolution and pH-Independent controlled release of sildenafil citrate
The aim of this study was to design a novel matrix tablet with enhanced dissolution and pH-independent controlled release of sildenafil citrate (SIL), a drug with pH-dependent solubility, by using solid dispersions (SDs) and polyelectrostatic interactions. SIL-loaded SDs were prepared using various...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2023-12-01
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| Series: | Heliyon |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2405844023102994 |
| _version_ | 1797383871644303360 |
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| author | Ju-Hyeong Woo Hai V. Ngo Hy D. Nguyen Myung-Chul Gil Chulhun Park Jun-Bom Park Jing-Hao Cui Qing-Ri Cao Beom-Jin Lee |
| author_facet | Ju-Hyeong Woo Hai V. Ngo Hy D. Nguyen Myung-Chul Gil Chulhun Park Jun-Bom Park Jing-Hao Cui Qing-Ri Cao Beom-Jin Lee |
| author_sort | Ju-Hyeong Woo |
| collection | DOAJ |
| description | The aim of this study was to design a novel matrix tablet with enhanced dissolution and pH-independent controlled release of sildenafil citrate (SIL), a drug with pH-dependent solubility, by using solid dispersions (SDs) and polyelectrostatic interactions. SIL-loaded SDs were prepared using various polymeric carriers such as poloxamer 188, poloxamer 407, Soluplus®, polyvinylpyrrolidone (PVP) K 12, and PVP K 17 by the solvent evaporation method. Among these polymers, Soluplus® was found to be the most effective in SDs for enhancing the drug dissolution over 6 h in pH 6.8 intestinal fluid. SIL was well dispersed in Soluplus®-based SDs in an amorphous form. When the Soluplus®-based SDs were added in the tablet containing positively charged chitosan and negatively charged Eudragit® L100, the drug release rate was further modulated in a controlled manner. The charge density of the tablet was higher at pH 6.8 than at pH 1.2 due to the polyelectrostatic interaction between chitosan and Eudragit® L100. This interaction could provide a pH-independent controlled release of SIL. Our study demonstrates that a combinatory approach of Soluplus®-based SDs and polyelectrostatic interactions can improve the dissolution and pH-independent release performance of SIL. This approach could be a promising pharmaceutical strategy to design a matrix tablet of poorly water-soluble drugs for the enhanced bioavailability. |
| first_indexed | 2024-03-08T21:27:15Z |
| format | Article |
| id | doaj.art-6dfbc9ecc056445a8391d43e5a9155b3 |
| institution | Directory Open Access Journal |
| issn | 2405-8440 |
| language | English |
| last_indexed | 2024-03-08T21:27:15Z |
| publishDate | 2023-12-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Heliyon |
| spelling | doaj.art-6dfbc9ecc056445a8391d43e5a9155b32023-12-21T07:35:42ZengElsevierHeliyon2405-84402023-12-01912e23091Polyelectrolyte-based solid dispersions for enhanced dissolution and pH-Independent controlled release of sildenafil citrateJu-Hyeong Woo0Hai V. Ngo1Hy D. Nguyen2Myung-Chul Gil3Chulhun Park4Jun-Bom Park5Jing-Hao Cui6Qing-Ri Cao7Beom-Jin Lee8College of Pharmacy, Ajou University, Suwon 16499, Republic of KoreaCollege of Pharmacy, Ajou University, Suwon 16499, Republic of KoreaCollege of Pharmacy, Ajou University, Suwon 16499, Republic of KoreaCollege of Pharmacy, Ajou University, Suwon 16499, Republic of KoreaCollege of Pharmacy, Jeju National University, Jeju 63243, Republic of KoreaCollege of Pharmacy, Sahmyook University, Seoul 01795, Republic of KoreaCollege of Pharmaceutical Sciences, Soochow University, Suzhou 215123, ChinaCollege of Pharmaceutical Sciences, Soochow University, Suzhou 215123, ChinaCollege of Pharmacy, Ajou University, Suwon 16499, Republic of Korea; Institute of Pharmaceutical Science and Technology, Ajou University, Suwon 16499, Republic of Korea; Corresponding author. College of Pharmacy, Ajou University, Suwon 16499, Republic of Korea.The aim of this study was to design a novel matrix tablet with enhanced dissolution and pH-independent controlled release of sildenafil citrate (SIL), a drug with pH-dependent solubility, by using solid dispersions (SDs) and polyelectrostatic interactions. SIL-loaded SDs were prepared using various polymeric carriers such as poloxamer 188, poloxamer 407, Soluplus®, polyvinylpyrrolidone (PVP) K 12, and PVP K 17 by the solvent evaporation method. Among these polymers, Soluplus® was found to be the most effective in SDs for enhancing the drug dissolution over 6 h in pH 6.8 intestinal fluid. SIL was well dispersed in Soluplus®-based SDs in an amorphous form. When the Soluplus®-based SDs were added in the tablet containing positively charged chitosan and negatively charged Eudragit® L100, the drug release rate was further modulated in a controlled manner. The charge density of the tablet was higher at pH 6.8 than at pH 1.2 due to the polyelectrostatic interaction between chitosan and Eudragit® L100. This interaction could provide a pH-independent controlled release of SIL. Our study demonstrates that a combinatory approach of Soluplus®-based SDs and polyelectrostatic interactions can improve the dissolution and pH-independent release performance of SIL. This approach could be a promising pharmaceutical strategy to design a matrix tablet of poorly water-soluble drugs for the enhanced bioavailability.http://www.sciencedirect.com/science/article/pii/S2405844023102994Sildenafil citrateSoluplus®-based solid dispersionEnhanced dissolutionDifferently charged polymersPolyelectrostatic interactionControlled release |
| spellingShingle | Ju-Hyeong Woo Hai V. Ngo Hy D. Nguyen Myung-Chul Gil Chulhun Park Jun-Bom Park Jing-Hao Cui Qing-Ri Cao Beom-Jin Lee Polyelectrolyte-based solid dispersions for enhanced dissolution and pH-Independent controlled release of sildenafil citrate Heliyon Sildenafil citrate Soluplus®-based solid dispersion Enhanced dissolution Differently charged polymers Polyelectrostatic interaction Controlled release |
| title | Polyelectrolyte-based solid dispersions for enhanced dissolution and pH-Independent controlled release of sildenafil citrate |
| title_full | Polyelectrolyte-based solid dispersions for enhanced dissolution and pH-Independent controlled release of sildenafil citrate |
| title_fullStr | Polyelectrolyte-based solid dispersions for enhanced dissolution and pH-Independent controlled release of sildenafil citrate |
| title_full_unstemmed | Polyelectrolyte-based solid dispersions for enhanced dissolution and pH-Independent controlled release of sildenafil citrate |
| title_short | Polyelectrolyte-based solid dispersions for enhanced dissolution and pH-Independent controlled release of sildenafil citrate |
| title_sort | polyelectrolyte based solid dispersions for enhanced dissolution and ph independent controlled release of sildenafil citrate |
| topic | Sildenafil citrate Soluplus®-based solid dispersion Enhanced dissolution Differently charged polymers Polyelectrostatic interaction Controlled release |
| url | http://www.sciencedirect.com/science/article/pii/S2405844023102994 |
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