論文 - 詳細
| RRC ID | 58722 |
|---|---|
| 著者 | Matsumoto A, Watanabe C, Murakami M. |
| タイトル | Janus microspheres for enhanced enteral drug delivery: Preparation and orientated attachment to a Caco-2 monolayer. |
| ジャーナル | Drug Discov Ther |
| Abstract |
Conventional oral preparations generally release incorporated drugs omnidirectionally, including into the lumen, leading to a low bioavailability of drugs that are unstable in the gastrointestinal tract. Here, we designed Janus microspheres for efficient mucosal drug delivery as single-sided-release microspheres with the oriented attachment to mucus and evaluated their attachment to and orientation on a Caco-2 (human Caucasian colon adenocarcinoma cell line) monolayer. The microspheres comprised a mucus-oriented hemisphere of an ammonioalkyl methacrylate copolymer and a protective hemisphere of a hard fat. Fluorescein isothiocyanate-dextran with an average molecular weight of 3,000-5,000 Da (FD4) was used as a model hydrophilic drug. A water-in-oil emulsion-type solvent evaporation method was employed for fabrication of the Janus microspheres. The yield of Janus microspheres was found to be dependent on the polymer-to-hard fat ratio, with a maximum yield of over 90% being obtained at a ratio of 1:2, whereas lower and higher ratios resulted in monolithic or star-shaped microspheres. FD4 was specifically localized in the polymeric hemisphere. A cell culture study revealed that the Janus microspheres attached to a Caco-2 monolayer via their polymeric hemispheres with the hard fat hemisphere providing a protective sealing. This may lead to the development of an effective enteral drug delivery system for biomedicines, such as polypeptides and nucleic acids. |
| 巻・号 | 13(6) |
| ページ | 343-353 |
| 公開日 | 2019-1-1 |
| DOI | 10.5582/ddt.2019.01090 |
| PMID | 31956233 |
| MeSH | Caco-2 Cells Calorimetry, Differential Scanning Chemistry, Pharmaceutical / methods* Delayed-Action Preparations Dextrans / pharmacology* Drug Delivery Systems Fluorescein-5-isothiocyanate / analogs & derivatives* Fluorescein-5-isothiocyanate / pharmacology Humans Hydrophobic and Hydrophilic Interactions Microspheres Particle Size |
| 引用数 | 0 |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 3 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | CACO-2(RCB0988) |