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スチレン- マレイン酸コポリマー結合アンフォテリシンB の合成及び評価
https://fukuyama-u.repo.nii.ac.jp/records/9075
https://fukuyama-u.repo.nii.ac.jp/records/90754a1f6884-ec3d-467f-ab2c-f5413fc34155
名前 / ファイル | ライセンス | アクション |
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53 福山大学薬学部研究年報第38号 (695.2 kB)
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Copyright(c)2020 by Fukuyama University
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Item type | 紀要論文 / Departmental Bulletin Paper(1) | |||||
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公開日 | 2021-04-14 | |||||
タイトル | ||||||
タイトル | スチレン- マレイン酸コポリマー結合アンフォテリシンB の合成及び評価 | |||||
タイトル | ||||||
言語 | en | |||||
タイトル | Synthesis and evaluation of styrene-maleic acid copolymer conjugated amphotericin B. | |||||
言語 | ||||||
言語 | jpn | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Amphotericin B | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Animals | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Antifungal Agents | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Drug Liberation | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Erythrocytes | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Hemolysis | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Lethal Dose 50 | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Male | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Maleates | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Mice | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Micelles | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Saccharomyces cerevisiae | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Solubility | |||||
キーワード | ||||||
言語 | en | |||||
主題Scheme | Other | |||||
主題 | Styrene | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | departmental bulletin paper | |||||
著者 |
番匠谷, 研吾
× 番匠谷, 研吾× 金尾, 義治× 田中, 哲郎× 山本, 繁史× 前田, 浩 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Amphotericin B (AmB), which plays a central role in the treatment of systemic fungal infections, is difficult to formulate because it's sparingly soluble in water and organic solvents. We previously prepared AmB-loaded micelles using styrene-maleic acid copolymer (SMA). Although solubilization was achieved by this formulation, stability in the blood circulation was as insufficient as that of Fungizone®, which is a conventional formulation of AmB. Meanwhile, it is well known that polymer-drug conjugates are more stable in circulation than drug-loaded micelles. Therefore, in this study, we developed covalently conjugated SMA-AmB (SMA-AmB conjugate). The SMA-AmB conjugate was found to be soluble and present as micelles in aqueous solution. Furthermore, it was revealed that this micelle behaves as a larger molecule by forming a complex with albumin. The circulation in the blood increased significantly compared to that of Fungizone®, which was suggested to be due to this complex-forming ability. Although in vitro and in vivo antifungal activity of the SMA-AmB conjugate against Saccharomyces cerevisiae was reduced by 1/3 compared to that of Fungizone®, hemolysis decreased to 1/40 or less, and the LD | |||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | decreased to 1/10. In conclusion, it is expected that the SMA-AmB conjugate can be a polymer-therapeutic agent with high antifungal selectivity. | |||||
内容記述 | ||||||
内容記述タイプ | Other | |||||
内容記述 | Amphotericin B (AmB), which plays a central role in the treatment of systemic fungal infections, is difficult to formulate because it's sparingly soluble in water and organic solvents. We previously prepared AmB-loaded micelles using styrene-maleic acid copolymer (SMA). Although solubilization was achieved by this formulation, stability in the blood circulation was as insufficient as that of Fungizone®, which is a conventional formulation of AmB. Meanwhile, it is well known that polymer-drug conjugates are more stable in circulation than drug-loaded micelles. Therefore, in this study, we developed covalently conjugated SMA-AmB (SMA-AmB conjugate). The SMA-AmB conjugate was found to be soluble and present as micelles in aqueous solution. Furthermore, it was revealed that this micelle behaves as a larger molecule by forming a complex with albumin. The circulation in the blood increased significantly compared to that of Fungizone®, which was suggested to be due to this complex-forming ability. Although in vitro and in vivo antifungal activity of the SMA-AmB conjugate against Saccharomyces cerevisiae was reduced by 1/3 compared to that of Fungizone®, hemolysis decreased to 1/40 or less, and the LD | |||||
内容記述 | ||||||
内容記述タイプ | Other | |||||
内容記述 | decreased to 1/10. In conclusion, it is expected that the SMA-AmB conjugate can be a polymer-therapeutic agent with high antifungal selectivity. | |||||
書誌情報 |
福山大学薬学部研究年報 en : Annual report of the Faculty of Pharmacy & Pharmaceutical Sciences, Fukuyama University 号 38, p. 53-53, 発行日 2020-12-25 |
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出版者 | ||||||
出版者 | 福山大学薬学部 | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0288724X | |||||
書誌レコードID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AN10064550 | |||||
著者版フラグ | ||||||
出版タイプ | VoR | |||||
出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 |