Bioavailability Improvement Strategies for Poorly Water-Soluble Drugs Based on the Supersaturation Mechanism: An Update

Abstract

-The formulation development for poorly soluble drugs still remains a challenge. Supersaturating drug delivery systems (SDDS) or drug delivery systems based on supersaturating provide a promising way to improve the oral bioavailability of poorly water-soluble drugs. In supersaturable formulations, drug concentration exceeds the equilibrium solubility when exposed to gastrointestinal fluids, and the supersaturation state is maintained long enough to be absorbed, resulting in compromised bioavailability. In this article, the mechanism of generating and maintaining supersaturation and the evaluation methods of supersaturation assays are discussed. Recent advances in different drug delivery systems based on supersaturating are the focus and are discussed in detail.

Investigating the Influence of Aromatic Moieties on the Formulation of Hydrophobic Natural Products and Drugs in Poly(2-oxazoline)-Based Amphiphiles

“…[2] Through high-throughput screening, new chemical entities or lead structures are being identified and evaluated every day, [3] but only a minute fraction ever ripen into an approved drug. Obviously, a large proportion of drug candidates are poorly water-soluble [4,5] which calls for effective formulation strategies. Traditionally used surfactants like Cremophor EL and Tween 80 have drawbacks as they can elicit potentially life-threatening side effects and are limited with respect to their in solubilizing ability.…”

A Mixed Micellar Formulation for the Transdermal Delivery of an Indirubin Analog

“…There are various systems, including solid dispersion, liposomes, polymer micelles, nanoemulsions, and cyclodextrin that are developed for the enhancement of drug solubility [22,23]. Considering the molecular characteristics of KY19382, we selected HP-β-CD as a solubility enhancer from a list of FDA-approved substances.…”

Silodosin oral films: Development, physico-mechanical properties and in vitro dissolution studies in simulated saliva

“…This effect could be attributed to the synergistic effect of the surfactant (TPGS) and the polymer (HPMC), resulting in improved solubility and maintained supersaturation [54,55,56]. Therefore, film formulation F4 appears to have potential for the development of a silodosin film formulation with improved performance and improved oral sublingual absorption as a result of the high degree of supersaturation solubility [57,58].…”