Development of self emulsifying lipid formulations of BCS class II drugs with low to medium lipophilicity
| Autor: | Camille Dumont, Stéphanie Chevrier, Yann Chavant, Vincent Jannin, Frédéric Demarne, Silvia Belotti, Matthieu Michenaud |
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| Rok vydání: | 2015 |
| Předmět: |
Drug
Curcumin Nifedipine media_common.quotation_subject Chemistry Pharmaceutical Pharmaceutical Science Administration Oral Piroxicam Dosage form Glycerides Excipients Surface-Active Agents Drug Delivery Systems Pulmonary surfactant medicine Solubility media_common Chromatography Chemistry Lipids Bioavailability Drug delivery Lipophilicity Solvents Hydrophobic and Hydrophilic Interactions medicine.drug |
| Zdroj: | International journal of pharmaceutics. 495(1) |
| ISSN: | 1873-3476 |
| Popis: | Lipid-based formulations can be effective drug delivery systems for poorly water-soluble chemical entities, provided they are designed with careful selection of the excipients, based on their role in the delivery system and in relation to drug properties. The primary factor leading to increased bioavailability is the administration of the drug in a pre-dissolved state thereby avoiding the dissolution limiting step. All model drugs tested (piroxicam, curcumin and nifedipine) belong to the same chemical space--small BCS class II molecules with logP ranging from 2 to 3. These drugs, exhibiting low to medium logP, are not soluble in lipophilic lipid-based excipients (e.g., vegetable oils). Water-soluble and water-dispersible surfactants are able to dissolve the target dose of each drug in the dosage form and efficiently keep it in solution during dispersion. In vitro digestion testing was necessary to discriminate formulations and enable selection of the most robust one. For each molecule, the system with the best performance during dispersion/digestion tests did not comprise the surfactant which delivered the highest solvent capacity for the drug. This study demonstrates the potential of surfactant-based formulations - i.e., Type IV systems from the lipid formulation classification system - for this type of hydrophobic drug. |
| Databáze: | OpenAIRE |
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