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Controlled Dissolution of Griseofulvin Solid Dispersions from Electrosprayed Enteric Polymer Micromatrix Particles: Physicochemical Characterization and in Vitro Evaluation.
- Source :
-
Molecular pharmaceutics [Mol Pharm] 2015 Jul 06; Vol. 12 (7), pp. 2254-64. Date of Electronic Publication: 2015 Jun 10. - Publication Year :
- 2015
-
Abstract
- The oral bioavailability of a poorly water-soluble drug is often inadequate for the desired therapeutic effect. The bioavailability can be improved by enhancing the physicochemical properties of the drug (e.g., dissolution rate, permeation across the gastrointestinal tract). Other approach include shielding the drug from the gastric metabolism and targeted drug release to obtain optimal drug absorption. In this study, a poorly water-soluble model drug, griseofulvin, was encapsulated as disordered solid dispersions into Eudragit L 100-55 enteric polymer micromatrix particles, which were produced by electrospraying. Similar micromatrix particles were also produced with griseofulvin-loaded thermally oxidized mesoporous silicon (TOPSi) nanoparticles dispersed to the polymer micromatrices. The in vitro drug dissolution at pH 1.2 and 6.8, and permeation at pH 7.4 across Caco-2/HT29 cell monolayers from the micromatrix particles, were investigated. The micromatrix particles were found to be gastro-resistant, while at pH 6.8 the griseofulvin was released very rapidly in a fast-dissolving form. Compared to free griseofulvin, the permeability of encapsulated griseofulvin across the intestinal cell monolayers was greatly improved, particularly for the TOPSi-doped micromatrix particles. The griseofulvin solid dispersions were stable during storage for 6 months at accelerated conditions. Overall, the method developed here could prove to be a useful oral drug delivery solution for improving the bioavailability of poorly water-soluble or otherwise problematic drugs.
- Subjects :
- Acrylic Resins chemistry
Biological Availability
Caco-2 Cells
Cell Line, Tumor
Drug Carriers chemistry
Griseofulvin pharmacokinetics
HT29 Cells
Humans
Intestinal Absorption drug effects
Nanoparticles chemistry
Permeability
Silicon chemistry
Solubility
Technology, Pharmaceutical methods
Water chemistry
Griseofulvin chemistry
Polymers chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1543-8392
- Volume :
- 12
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Molecular pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 26035734
- Full Text :
- https://doi.org/10.1021/mp500787b