To study the impact of different surfactants on the supersaturation of nifedipine stabilized with HPMC and PVP-VA.
Different kinds of surfactants, including one cationic surfactant, two anionic surfactants, and three nonionic surfactants, were used to evaluate their impacts on the supersaturation of nifedipine stabilized with HPMC and PVP-VA. Polymer-surfactant interaction was studied by nuclear magnetic resonance (NMR) and fluorescent method. Solubility of nifedipine in solutions containing different amounts of polymers and surfactants was measured. Drug-polymer affinity was evaluated by measuring the percentage of polymer coprecipitated together with the drug from supersaturated solutions.
Different polymer-surfactant combinations had different impacts on the supersaturation of nifedipine. Some combinations, such as PVP-VA/SLS and PVP-VA/NaTC under higher surfactant concentrations, showed improved drug supersaturation, due to increased drug solubility or polymer-surfactant synergy; while other combinations, such as HPMC/SLS and HPMC/Tween 20 under lower surfactant concentrations, showed reduced drug supersaturation, which could result from competitive surfactant-polymer or drug-surfactant interaction that disrupted pre-existent drug-polymer interaction.
The ultimate impacts of various surfactants on polymer stabilized nifedipine supersaturation could be attributed to the interplay between different factors, including solubility enhancement of the drug, drug-polymer-surfactant interactions, and polymer-surfactant synergy.
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Area under the curve
Critical aggregation concentration CMC
Critical micelle concentration DMSO
Dodecyl trimethyl ammonium bromide
Evaporative light scattering detector
High performance liquid chromatography
Nuclear magnetic resonance
Phosphatic buffer solution
Polymer coprecipitation percentage
Powder x-ray diffraction
Supersaturating drug delivery systems
Sodium lauryl sulfate
D-α-Tocopherol polyethylene glycol succinate
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This research is supported by China National Nature Science Foundation (Project Number 81573355), and by Janssen Pharmaceuticals, Inc., a pharmaceutical company of Johnson & Johnson.
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Wang, S., Liu, C., Chen, H. et al. Impact of Surfactants on Polymer Maintained Nifedipine Supersaturation in Aqueous Solution. Pharm Res 37, 113 (2020). https://doi.org/10.1007/s11095-020-02837-5