| ID | JOS-pharmaceutics14040785 |
| 著者：名前 | |
| 著者：別形式 | Okada, Akie / Niki, Rina / Inoue, Yutaka / Tomita, Junki / Todo, Hiroaki / Itakura, Shoko / Sugibayashi, Kenji |
| 著者：カナ | |
| 著者：所属 | 城西大学薬学部 / 城西大学薬学部 / 城西大学機器分析センター / 城西大学薬学部 / 城西大学薬学部 / 城西大学薬学部 |
| 著者：所属(別形式） | Josai University, Faculty of Pharmacy and Pharmaceutical Sciences / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences / Josai University, Research Analysis Center / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences |
| 著者版フラグ | publisher |
| 出版地 | Basel |
| 出版者 | MDPI |
| 電子ISSN | 19994923 |
| 掲載誌名 | |
| 巻 | 14 |
| 号 | 4 |
| 刊行年月 | 2022-04 |
| 開始ページ | 1 |
| 終了ページ | 14 |
| コンテンツ作成日 | 2022-02-18 |
| コンテンツ修正日 | 2022-04-01 |
| コンテンツ登録日 | 2022-06-16 |
| 識別番号：DOI | info:doi/10.3390/pharmaceutics14040785 |
| 識別番号：DOI（リンク） | |
| PubMed番号 | 35456619 |
| 抄録 | In recent years, the development of self-injectable formulations has attracted much attention, and the development of formulations to control pharmacokinetics, as well as drug release and migration in the skin, has become an active research area. In the present study, the development of a lipid-based depot formulation containing leuprorelin acetate (LA) as an easily metabolizable drug in the skin was prepared with a novel non-lamellar liquid-crystal-forming lipid of mono-O-(5,9,13-trimethyl-4-tetradecenyl) glycerol ester (MGE). Small-angle X-ray scattering, cryo-transmission electron microscopy, and nuclear magnetic resonance observations showed that the MGE-containing formulations had a face-centered cubic packed micellar structure. In addition, the bioavailability (BA) of LA after subcutaneous injection was significantly improved with the MGE-containing formulation compared with the administration of LA solution. Notably, higher Cmax and faster Tmax were obtained with the MGE-containing formulation, and the BA increased with increasing MGE content in the formulation, suggesting that LA migration into the systemic circulation and its stability might be enhanced by MGE. These results may support the development of self-administered formulations of peptide drugs as well as nucleic acids, which are easily metabolized in the skin. |
| キーワード | |
| 注記 | Article number: 785, This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited |
| 言語 | eng |
| 資源タイプ | text |
| ジャンル | |
| フォーマット | application/pdf |
| 権利 | Copyright © 2022 by the authors. |
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| このアイテムを表示する：URI | |
