Biodegradable Porous Starch Spheres as a Novel Carrier for Enhancement of Dissolution Rate and Oral Bioavailability of Itraconazole
| Autor: | Madhavsingh Seervi, Purnima D. Amin, Ritesh Fule, Meer Tarique Ali, Sadhana Sathaye, Kailas K. Moravkar, Jaywant N. Pawar |
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| Rok vydání: | 2017 |
| Předmět: |
Male
Antifungal Agents Starch Antifungal drug Administration Oral Biological Availability Pharmaceutical Science 02 engineering and technology urologic and male genital diseases 01 natural sciences Crystallinity chemistry.chemical_compound Adsorption X-Ray Diffraction Spectroscopy Fourier Transform Infrared 0103 physical sciences Animals Rats Wistar Solubility Dissolution Drug Carriers Chromatography Calorimetry Differential Scanning 010304 chemical physics 021001 nanoscience & nanotechnology Bioavailability Solvent Drug Liberation chemistry Microscopy Electron Scanning Itraconazole 0210 nano-technology Porosity Powder Diffraction hormones hormone substitutes and hormone antagonists Nuclear chemistry |
| Zdroj: | Current Drug Delivery. 14 |
| ISSN: | 1567-2018 |
| DOI: | 10.2174/1567201813666160920154209 |
| Popis: | Background: A biodegradable porous starch (BPS) was developed in order to improve dissolution and oral bioavailability of Itraconazole as a poorly water-soluble antifungal drug. Methods: BPS was developed by converting native starch from hydrogel to alcogel by solvent exchange method. The developed BPS carrier was characterized by SEM and nitrogen adsorption/desorption analysis to understand surface morphology and porosity distribution respectively. Itraconazole (ITR) was loaded on BPS by adsorption mediated solvent evaporation method, which provides a hydrophilic matrix powder. This causes drug distribution within hydrophilic matrix of porous starch. Results: Solid-state characterization of optimized batch (ITR/BPS-3) was performed using DSC, PXRD, FTIR, SEM and FTIR chemical imaging. In vitro dissolution and in vivo pharmacokinetic studies were performed to evaluate therapeutic potential of ITR/BPS-3 system. In vitro studies of ITR: BPS-3 system revealed a burst effect in drug release (93%) compared to marketed product, which showed 90% drug release at the end of 60 min compared to 84% of marketed. Moreover, ITR/BPS-3 system showed improved oral bioavailability up to 3.93 fold and marketed product shows 3.12 fold compared to ITR. Conclusion: This effect is due to high surface area, improved wettability and reduced crystallinity of ITR due to its adsorption into BPS. A successful methodology was reported to prepare BPS from raw starch. |
| Databáze: | OpenAIRE |
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