What Is the Mechanism Behind Increased Permeation Rate of a Poorly Soluble Drug from Aqueous Dispersions of an Amorphous Solid Dispersion?

A simple and effective method to improve bioavailability of glimepiride by utilizing hydrotropy technique

“…Dahan and Miller (2012) and Miller et al (2012) mentioned that the solubilitypermeability interplay cannot be ignored when using solubility-enabling formulations, looking solely at the solubility enhancement that the formulation enables may be misleading with regards to predicting the resulting absorption, and hence, the solubility-permeability interplay must be taken into account to strike the optimal solubility-permeability balance, in order to maximize the overall absorption. Moreover, the paper (Frank et al, 2012b(Frank et al, , 2014 reported the mechanism behind increased permeation rate of a poorly soluble drug (ABT-102) from aqueous dispersion of an ASDs, the results showed that permeation rate enhancement in aqueous dispersion of ASDs is due to enhanced concentration of molecularly dissolved ABT-102 (''true'' supersaturation) rather than enhanced apparent solubility in the presence of surfactants.…”

Drug Delivery Approaches in Addressing Clinical Pharmacology-Related Issues: Opportunities and Challenges

“…As the toxicity of a surfactant is directly related to its concentration, the surfactant toxicity has to be taken into consideration during drug development. In self-micellizing solid dispersion (SMSD) systems, surfactants or amphiphilic block copolymers have been used to form micelles in aqueous media to solubilize drugs with poor water solubility and to prevent drug precipitation during dissolution process (25,26). Many drugs with poor water solubility have been successfully developed and commercialized using micellar solubilization, such as paclitaxel injection and cyclosporine injection, as well as griseofulvin-PEG-dispersion.…”

Using Environment-Sensitive Fluorescent Probes to Characterize Liquid-Liquid Phase Separation in Supersaturated Solutions of Poorly Water Soluble Compounds

“…The solution remains supersaturated until crystallization occurs, even though a visible precipitate is present. It has been postulated that such two phase systems may be beneficial to drug delivery and bioavailability as the drug-rich phase serves as a reservoir to maintain the supersaturation (14,18).…”