Abstract:
: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.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Jannin V,Chevrier S,Michenaud M,Dumont C,Belotti S,Chavant Y,Demarne Fdoi
10.1016/j.ijpharm.2015.09.009subject
Has Abstractpub_date
2015-11-10 00:00:00pages
385-392issue
1eissn
0378-5173issn
1873-3476pii
S0378-5173(15)30207-6journal_volume
495pub_type
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