Preparation and evaluation of conjugate nanogels of glycyl-prednisolone with natural anionic polysaccharides as anti-arthritic delivery systems
Although prednisolone (PD) is used as an anti-arthritis drug due to its rapid and strong anti-inflammatory potential, its frequent and large dosing often brings about adverse effects. Therefore, targeting therapy has attracted increasing attention to overcome such adverse effects. In the present stu...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2021-01-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/10717544.2020.1865478 |
| _version_ | 1818987111304396800 |
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| author | Kohei Mizuno Yuri Ikeuchi-Takahashi Yoshiyuki Hattori Hiraku Onishi |
| author_facet | Kohei Mizuno Yuri Ikeuchi-Takahashi Yoshiyuki Hattori Hiraku Onishi |
| author_sort | Kohei Mizuno |
| collection | DOAJ |
| description | Although prednisolone (PD) is used as an anti-arthritis drug due to its rapid and strong anti-inflammatory potential, its frequent and large dosing often brings about adverse effects. Therefore, targeting therapy has attracted increasing attention to overcome such adverse effects. In the present study, nanogels (NGs) composed of macromolecule–PD conjugates were developed as a novel targeting delivery system, and their anti-inflammatory potential was examined. Conjugates were prepared by carbodiimide coupling between glycyl-prednisolone (GP) and the natural anionic polysaccharides, alginic acid (AL) and hyaluronic acid (HA). NGs were produced by the evaporation of organic solvent from the conjugate solution. The obtained NGs, named AL-GP-NG and HA-GP-NG, respectively, were examined for particle characteristics, in vitro release, pharmacokinetics, and in vivo efficacy. Both NGs were several hundred nanometers in size, had negative zeta potentials, and several % (w/w) drug contents. They released PD gradually at pH 7.4 and 6. They exhibited fairly good retention in the systemic circulation. In the efficacy examination using rats with adjuvant-induced arthritis, both NGs showed the stronger and more prolonged suppression of paw inflammation than PD alone. These suggested that the present NGs should be possibly useful as anti-arthritis targeting therapeutic systems. |
| first_indexed | 2024-12-20T19:01:29Z |
| format | Article |
| id | doaj.art-a68f031b9cc249b3aa7518a714ca7088 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-20T19:01:29Z |
| publishDate | 2021-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-a68f031b9cc249b3aa7518a714ca70882022-12-21T19:29:22ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642021-01-0128113614410.1080/10717544.2020.18654781865478Preparation and evaluation of conjugate nanogels of glycyl-prednisolone with natural anionic polysaccharides as anti-arthritic delivery systemsKohei Mizuno0Yuri Ikeuchi-Takahashi1Yoshiyuki Hattori2Hiraku Onishi3Department of Drug Delivery Research, Hoshi UniversityDepartment of Drug Delivery Research, Hoshi UniversityDepartment of Drug Delivery Research, Hoshi UniversityDepartment of Drug Delivery Research, Hoshi UniversityAlthough prednisolone (PD) is used as an anti-arthritis drug due to its rapid and strong anti-inflammatory potential, its frequent and large dosing often brings about adverse effects. Therefore, targeting therapy has attracted increasing attention to overcome such adverse effects. In the present study, nanogels (NGs) composed of macromolecule–PD conjugates were developed as a novel targeting delivery system, and their anti-inflammatory potential was examined. Conjugates were prepared by carbodiimide coupling between glycyl-prednisolone (GP) and the natural anionic polysaccharides, alginic acid (AL) and hyaluronic acid (HA). NGs were produced by the evaporation of organic solvent from the conjugate solution. The obtained NGs, named AL-GP-NG and HA-GP-NG, respectively, were examined for particle characteristics, in vitro release, pharmacokinetics, and in vivo efficacy. Both NGs were several hundred nanometers in size, had negative zeta potentials, and several % (w/w) drug contents. They released PD gradually at pH 7.4 and 6. They exhibited fairly good retention in the systemic circulation. In the efficacy examination using rats with adjuvant-induced arthritis, both NGs showed the stronger and more prolonged suppression of paw inflammation than PD alone. These suggested that the present NGs should be possibly useful as anti-arthritis targeting therapeutic systems.http://dx.doi.org/10.1080/10717544.2020.1865478conjugate nanogelprednisolonenatural anionic polysaccharideanti-arthritisefficacy |
| spellingShingle | Kohei Mizuno Yuri Ikeuchi-Takahashi Yoshiyuki Hattori Hiraku Onishi Preparation and evaluation of conjugate nanogels of glycyl-prednisolone with natural anionic polysaccharides as anti-arthritic delivery systems Drug Delivery conjugate nanogel prednisolone natural anionic polysaccharide anti-arthritis efficacy |
| title | Preparation and evaluation of conjugate nanogels of glycyl-prednisolone with natural anionic polysaccharides as anti-arthritic delivery systems |
| title_full | Preparation and evaluation of conjugate nanogels of glycyl-prednisolone with natural anionic polysaccharides as anti-arthritic delivery systems |
| title_fullStr | Preparation and evaluation of conjugate nanogels of glycyl-prednisolone with natural anionic polysaccharides as anti-arthritic delivery systems |
| title_full_unstemmed | Preparation and evaluation of conjugate nanogels of glycyl-prednisolone with natural anionic polysaccharides as anti-arthritic delivery systems |
| title_short | Preparation and evaluation of conjugate nanogels of glycyl-prednisolone with natural anionic polysaccharides as anti-arthritic delivery systems |
| title_sort | preparation and evaluation of conjugate nanogels of glycyl prednisolone with natural anionic polysaccharides as anti arthritic delivery systems |
| topic | conjugate nanogel prednisolone natural anionic polysaccharide anti-arthritis efficacy |
| url | http://dx.doi.org/10.1080/10717544.2020.1865478 |
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