Development of budesonide microparticles using spray-drying technology for pulmonary administration: design, characterization, in vitro evaluation, and in vivo efficacy study
| Autor: | Sonali R. Naikwade, Amrita Bajaj, Pritam Singh Soni, Prashant Gurav, Madhumanjiri M. Gatne |
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| Rok vydání: | 2008 |
| Předmět: |
Cell Survival
Chemistry Pharmaceutical Cmax Anti-Inflammatory Agents Pharmaceutical Science Nanotechnology Aquatic Science Polyethylene Glycols Chitosan Excipients chemistry.chemical_compound Pharmacokinetics X-Ray Diffraction In vivo Drug Discovery Administration Inhalation Spectroscopy Fourier Transform Infrared Animals Humans Anti-Asthmatic Agents Desiccation Particle Size Budesonide Radionuclide Imaging Lung Ecology Evolution Behavior and Systematics Aerosols Chromatography Ecology Inhalation Reproducibility of Results General Medicine Microspheres Bioavailability Rats chemistry Spray drying Delayed-Action Preparations Microscopy Electron Scanning Nanoparticles Particle size Agronomy and Crop Science Bronchoalveolar Lavage Fluid Research Article |
| Zdroj: | AAPS PharmSciTech. 10(3) |
| ISSN: | 1530-9932 |
| Popis: | The purpose of this research was to generate, characterize, and investigate the in vivo efficacy of budesonide (BUD) microparticles prepared by spray-drying technology with a potential application as carriers for pulmonary administration with sustained-release profile and improved respirable fraction. Microspheres and porous particles of chitosan (drug/chitosan, 1:2) were prepared by spray drying using optimized process parameters and were characterized for different physicochemical parameters. Mass median aerodynamic diameter and geometric standard deviation for conventional, microspheres, and porous particles formulations were 2.75, 4.60, and 4.30 microm and 2.56, 1.75, and 2.54, respectively. Pharmacokinetic study was performed in rats by intratracheal administration of either placebo or developed dry powder inhalation (DPI) formulation. Pharmacokinetic parameters were calculated (Ka, Ke, T(max), C(max), AUC, and Vd) and these results indicated that developed formulations extended half life compared to conventional formulation with onefold to fourfold improved local and systemic bioavailability. Estimates of relative bioavailability suggested that developed formulations have excellent lung deposition characteristics with extended T(1/2) from 9.4 to 14 h compared to conventional formulation. Anti-inflammatory activity of BUD and developed formulations was compared and found to be similar. Cytotoxicity was determined in A549 alveolar epithelial cell line and found to be not toxic. In vivo pulmonary deposition of developed conventional formulation was studied using gamma scintigraphy and results indicated potential in vitro-in vivo correlation in performance of conventional BUD DPI formulation. From the DPI formulation prepared with porous particles, the concentration of BUD increased fourfold in the lungs, indicating pulmonary targeting potential of developed formulations. |
| Databáze: | OpenAIRE |
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