Controlled initial surge despite high drug fraction and high solubility
| Autor: | Jiwen Zheng, Dinesh V. Patwardhan, Anne D. Lucas, Srilekha Sarkar Das, Alan S. Carlin, David M. Saylor |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
Evaporation
Pharmaceutical Science 02 engineering and technology 030226 pharmacology & pharmacy 03 medical and health sciences Tetracycline Hydrochloride chemistry.chemical_compound 0302 clinical medicine Polylactic Acid-Polyglycolic Acid Copolymer Lactic Acid Solubility Chromatography Volatilisation Chemistry technology industry and agriculture General Medicine Tetracycline 021001 nanoscience & nanotechnology Microstructure Controlled release Anti-Bacterial Agents Lactic acid Drug Liberation PLGA Delayed-Action Preparations Solvents Volatilization 0210 nano-technology Polyglycolic Acid Nuclear chemistry |
| Zdroj: | Pharmaceutical Development and Technology. 22:35-44 |
| ISSN: | 1097-9867 1083-7450 |
| Popis: | Potential connections between release profiles and solvent evaporation rates alongside polymer chemistry were elucidated for the release of tetracycline hydrochloride from two different poly (d, l-lactide-co-glycolide) (PLGA) film matrices containing high drug fractions (50%, 30%, and 15%), and prepared at two distinct solvent evaporation rates. At highest tetracycline concentrations (50%), (i) the early release rates were ≤0.5 μg/min in all cases; (ii) release was linear from systems fabricated with lower lactic content and slower solvent evaporation rate and bimodal from systems fabricated with higher lactic content and faster evaporation rate; (iii) surface fractions covered by the drug were similar at both evaporation rates for 85:15 PLGA but very different for 50:50 PLGA, leading to unexpectedly reduced early release from 50:50 PLGA than from 85:15 PLGA when both the matrices were fabricated using a slower evaporation rate. These features remained unaffected in case of low drug concentration. Results suggested that during the formation of the drug-polymer microstructure, the combined effect of polymer chemistry and solvent evaporation rate sets apart the surface characteristics and the initial release profiles of systems containing high drug fraction, and an appropriate combination of these parameters may be utilized to control the early stage of drug release. |
| Databáze: | OpenAIRE |
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