Drug–Excipient Complexation in Lipid Based Delivery Systems: An Investigation of the Tipranavir-1,3-Dioctanolyglycerol Complex

Maintenance of Supersaturation I: Indomethacin Crystal Growth Kinetic Modeling Using an Online Second-derivative Ultraviolet Spectroscopic Method

“…For poorly water‐soluble drugs, oral bioavailability enhancement may be possible by achieving and maintaining supersaturated drug concentrations in the gastrointestinal (GI) tract 1–6. Salts,7 cyclodextrin complexes,8 , 9 lipid‐based delivery systems,9 , 5 , 10 high‐energy amorphous solid dispersions,3 and nanoparticles6 , 11 are among the types of strategies that may produce high, supersaturated drug concentrations in the GI tract facilitated by the local GI environment, which is constantly changing in pH, food effects, natural surfactant concentrations and so on. However, prolonged maintenance of supersaturation in the GI tract may be difficult to achieve due to the inherent thermodynamic instability of the supersaturated state, which may lead to precipitation or crystallization (nucleation and crystal growth) of poorly water‐soluble drugs and variable, suboptimal oral bioavailability.…”

“…For poorly watersoluble drugs, oral bioavailability enhancement may be possible by achieving and maintaining supersaturated drug concentrations in the gastrointestinal (GI) tract. [1][2][3][4][5][6] Salts, 7 cyclodextrin complexes, 8,9 lipidbased delivery systems, 9,5,10 high-energy amorphous solid dispersions, 3 and nanoparticles 6,11 are among the types of strategies that may produce high, supersaturated drug concentrations in the GI tract facili-to prolong drug supersaturation to varying degrees depending on the properties of the drug and excipient. The effectiveness of such excipients in maintaining supersaturation may be attributable to their ability to inhibit nucleation, crystal growth, or both.…”