Bioavailability enhanced clopidogrel -loaded solid SNEDDS: Development and in-vitro/in-vivo characterization
| Autor: | Eman Abd-Elhakeem, Mahmoud Hm. Teaima, Ghada A. Abdelbary, Galal M. El Mahrouk |
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| Rok vydání: | 2019 |
| Předmět: |
Drug
Chromatography Chemistry media_common.quotation_subject Dispersity Pharmaceutical Science 02 engineering and technology bacterial infections and mycoses 021001 nanoscience & nanotechnology Clopidogrel 030226 pharmacology & pharmacy Bioavailability stomatognathic diseases 03 medical and health sciences 0302 clinical medicine Differential scanning calorimetry Oral administration Drug delivery medicine 0210 nano-technology Drug metabolism medicine.drug media_common |
| Zdroj: | Journal of Drug Delivery Science and Technology. 49:603-614 |
| ISSN: | 1773-2247 |
| Popis: | The purpose of this study is to develop solid self-nanoemulsifying drug delivery systems (S-SNEDDS) for oral bioavailability enhancement of Clopidogrel (CLP). CLP is an anti-platelet drug used to prevent heart strokes. It suffers from low bioavailability due to extensive hepatic metabolism. Two pseudo-ternary phase diagrams were constructed using different oils, bioenhancing surfactants and co-surfactants. SNEDDS were evaluated for their globule size, polydispersity index and in-vitro drug release. The optimum SNEDDS were adsorbed onto Aeroperl®300 to produce S-SNEDDS. Results showed that SNEDDS-8 (SII8) consisting of 10% Capryol™90, 10% Cremophore®EL and 80% Transcutol®HP possessed the smallest globule size and high % drug release. Furthermore, the optimum S-SNEDDS formula was characterized using differential scanning calorimetry and Fourier Transform Infra-Red which indicated that CLP was molecularly dispersed within the solid nano-system without any signs of interactions. CLP bioavailability in male albino rabbits after oral administration of the optimum CLP-loaded S-SNEDDS formulation compared to the commercially CLP tablets (Plavix®) was investigated. Results revealed that the optimum prepared system exhibited nine folds increment in CLP bioavailability compared to the conventional Plavix® tablets. In conclusion, CLP-loaded S-SNEDDS formulations containing bioenhancing surfactants proved to be a promising approach to improve the oral bioavailability of CLP. |
| Databáze: | OpenAIRE |
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