High loading of lipophilic compounds in mesoporous silica for improved solubility and dissolution performance.

Loading poorly soluble active pharmaceutical ingredients (API) into mesoporous silica can enable API stabilization in non-crystalline form, which leads to improved dissolution. This is particularly beneficial for highly lipophilic APIs (log D > 8) as these drugs often exhibit limited solubility in dispersion forming carrier polymers, resulting in low drug load and reduced solid state stability. To overcome this challenge, we loaded the highly lipophilic natural products coenzyme Q10 (CoQ10) and astaxanthin (ASX), as well as the synthetic APIs probucol (PB) and lumefantrine (LU) into the mesoporous silica carriers Syloid® XDP 3050 and Silsol® 6035.

Novel Biphasic Dissolution Method Correctly Predicts the Oral Bioavailability of Curcumin in Humans.

dissolution methods correctly predicting bioavailability of compounds from complex mixtures are lacking. We therefore used data on the performance of bioavailability-improved curcumin formulations to implement an predictive dissolution method (BiPHa+). BiPHa+ was applied for the characterization of eight curcumin formulations previously studied in a strictly controlled pharmacokinetic human trial.