Self-emulsifying preconcentrates of daidzein–phospholipid complex: design, in vitro and in vivo appraisal
| Autor: | Eman Mm. Shehata, Sally Galal, Ossama Y. Abdallah, Yosra S.R. Elnaggar |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Biomedical Engineering
Administration Oral Biological Availability Medicine (miscellaneous) Bioengineering 02 engineering and technology Absorption (skin) Development Pharmacology medicine.disease_cause 030226 pharmacology & pharmacy Surface-Active Agents 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Pharmacokinetics Pulmonary surfactant In vivo medicine Animals Humans General Materials Science Particle Size Phospholipids Chromatography Chemistry Daidzein 021001 nanoscience & nanotechnology Isoflavones Rats Bioavailability Drug Liberation Solubility Lipophilicity Emulsions Irritation 0210 nano-technology |
| Zdroj: | Nanomedicine. 12:893-910 |
| ISSN: | 1748-6963 1743-5889 |
| DOI: | 10.2217/nnm-2016-0387 |
| Popis: | Aim: Self-emulsifying phospholipid-complex preconcentrates (SEPPs) were fabricated to improve oral bioavailability of daidzein (DAI), an anticancer drug with challenging amphiphobic nature and extensive presystemic metabolism. Methods: DAI–phosphatidylcholine complex was prepared to enhance DAI lipophilicity and loading in SEPPs. The physicochemical characteristics and the pharmacokinetic behavior in rats were studied. Results: Surfactant-free SEPP (plain DAI:Phosal® 53MCT complex) was monodisperse upon aqueous dilution with nanorange globule size (485 ± 15 nm). Compared with drug suspension, it showed enhanced drug release and 2.38-fold enhanced oral bioavailability with minimized drug-induced intestinal irritation. Addition of 30% surfactant/co-surfactant mixture did not show any significant difference in drug release rate or absorption profile. Conclusion: The highly safe surfactant-free SEPP could be an effective approach to improve DAI oral bioavailability. |
| Databáze: | OpenAIRE |
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