Optimization and Evaluation of the Thermosensitive In Situ and Adhesive Gel for Rectal Delivery of Budesonide
| Autor: | Yujie Liu, Xingliang Xie, Qing Su, Lin Chen, Sheng Yanmei, Quan Zhang, Yingchun Zeng, Xu Xiaohong, Xue Han |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Budesonide
In situ Male Pharmacology toxicology Anti-Inflammatory Agents Drug Evaluation Preclinical Pharmaceutical Science Biological Availability 02 engineering and technology Poloxamer Aquatic Science 030226 pharmacology & pharmacy Rats Sprague-Dawley 03 medical and health sciences 0302 clinical medicine Drug Delivery Systems In vivo Administration Rectal Adhesives Drug Discovery medicine Animals Ecology Evolution Behavior and Systematics Chromatography Ecology Chemistry Rectum General Medicine 021001 nanoscience & nanotechnology Bioavailability Rats Rectal administration Female Adhesive 0210 nano-technology Agronomy and Crop Science Gels medicine.drug |
| Zdroj: | AAPS PharmSciTech. 21(3) |
| ISSN: | 1530-9932 |
| Popis: | Budesonide is a glucocorticoid for the treatment of ulcerative colitis (UC). The current study aims to develop a thermosensitive in situ and adhesive gel for rectal delivery of budesonide. HPMC K4M was selected as the adhesive agent based on the adhesive force and the effect on gel performance. The formulation of gel was optimized by using the central composite design-response surface methodology (CCD-RSM); a mathematical model was successfully developed to predict desired formulations as well as to analyze relationships between the amount of Pluronic F-127, Pluronic F-68, and HPMC K4M and the performances of gel. Based on CCD-RSM, a thermosensitive in situ and adhesive gel consisting of 0.002% budesonide, 0.74% HPMC, 4.87% F-68, and 19.0% F-127 was developed. Furthermore, the in vivo behavior of gel was evaluated in Sprague-Dawley rats. In comparison with budesonide solution, rectal administration of budesonide gel at 0.1 mg/kg in rats showed relative bioavailability of 230% with significant increase in rectum uptake. |
| Databáze: | OpenAIRE |
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