Preparation and Characterization of Insulin-Loaded Acrylic Hydrogels Containing Absorption Enhancers.
-
- UCHIDA Takahiro
- Faculty of Pharmaceutical Sciences, Mukogawa Women’s University
-
- TOIDA Yuka
- Faculty of Pharmaceutical Sciences, Mukogawa Women’s University
-
- SAKAKIBARA Sadako
- Faculty of Pharmaceutical Sciences, Mukogawa Women’s University
-
- MIYANAGA Yohko
- Faculty of Pharmaceutical Sciences, Mukogawa Women’s University
-
- TANAKA Hiromi
- Faculty of Pharmaceutical Sciences, Mukogawa Women’s University
-
- NISHIKATA Mayumi
- Faculty of Pharmaceutical Sciences, Mukogawa Women’s University
-
- TAZUYA Keiko
- Faculty of Pharmaceutical Sciences, Mukogawa Women’s University
-
- YASUDA Noriko
- Faculty of Pharmaceutical Sciences, Mukogawa Women’s University
-
- MATSUYAMA Kenji
- Faculty of Pharmaceutical Sciences, Mukogawa Women’s University
この論文をさがす
抄録
The objectives of this study were to prepare insulin-loaded acrylic hydrogel formulations containing various absorption enhancers, to perform in vitro and in vivo characterization of these formulations, and to evaluate the factors which affecting insulin availability on rectal delivery of insulin using this hydrogel system. The acrylic block copolymer of methacrylic acid and methacrylate, Eudispert®, was used to make the hydrogel formulations. As absorption enhancers, 2,6-di-O-methyl-β-cyclodextrin (DM-β-CyD), lauric acid (C12), or the sodium salt of C12 (C12Na), were incorporated into the hydrogels. In an in vitro release test, the release rate of insulin from the hydrogels decreased as the polymer concentration of the hydrogel increased. The addition of C12Na to the hydrogel further increased the insulin release rate, which was greater at higher concentrations of the enhancer. A portion of the C12Na was found to remain bound to the acrylic polymer in dissolution medium. Serum insulin levels were determined at various time points after the administration of insulin solution or insulin-loaded (50 units/kg body weight) Eudispert® hydrogels containing 5% (w/w) of C12, C12Na, or DM-β-CyD to in situ loops in various regions of the rat intestine. The most effective enhancement of insulin release was observed with formulations containing C12Na. The bioavailability of insulin from the hydrogels was lower than that from the insulin solutions. Hydrogel formulations containing 7% or 10% Eudispert® remained in the rectum for 5 h after rectal administration. However, the 5% (w/w) C12Na solution stained with Evan’s-blue had diffused out and the dye had reached the upper intestinal tract within 2 h. Finally, the rectal administration of insulin-loaded hydrogels, containing 4%, 7%, or 10% (w/w) Eudispert® and 5% (w/w) of enhancer (C12, C12Na, or DM-β-CyD) to normal rats was shown to decrease serum glucose concentrations. The greatest effect was found with insulin-loaded 7% (Eudispert®) hydrogel containing C12Na which having cosiderable large insulin release rate and bioadhesive characteristics.
収録刊行物
-
- CHEMICAL & PHARMACEUTICAL BULLETIN
-
CHEMICAL & PHARMACEUTICAL BULLETIN 49 (10), 1261-1266, 2001
公益社団法人 日本薬学会
- Tweet
詳細情報 詳細情報について
-
- CRID
- 1390001204164047872
-
- NII論文ID
- 110003615772
-
- NII書誌ID
- AA00602100
-
- COI
- 1:CAS:528:DC%2BD3MXnt1Cksbk%3D
-
- ISSN
- 13475223
- 00092363
-
- NDL書誌ID
- 5926564
-
- PubMed
- 11605651
-
- 本文言語コード
- en
-
- データソース種別
-
- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可