Hydrotropic Solubilization: An Emerging Approach

Abstract

Drug development plays an important role in patient safety and effectiveness. The therapeutic suitability of a new drug depends on the solubility. The solubility of the sparingly soluble drug remains a problem in identifying new active compounds. Solubility plays an important role in achieving optimal drug concentration. Low solubility is not only a concern for the production of formulations, but also an obstacle from the outset when identifying active chemicals for therapeutic purposes. Due to its simplicity in terms of ease of administration and economy, the oral route is the preferred route of drug administration over other routes. Effective aqueous solubility is the first prerequisite for oral medication, since low solubility has poor absorption and bioavailability and unpredictable toxicity of the gastrointestinal mucosa. To avoid these crises, different methodologies are used to improve the solubility and bioavailability of poorly soluble drugs, and hydrotropic solubilization is one of them. Hydrotropic agents have the potential to improve the solubility of water-insoluble drugs. In this review, we try to address hydrotropic solubilization methodologies.
 Keywords: Hydrotropy, Micelles, Solubility, Formulation.

Solubility Enhancement of a Poorly Water-Soluble Drug Using Hydrotropy and Mixed Hydrotropy-Based Solid Dispersion Techniques

“…In order to maximize drug release and, by extension, bioavailability, this approach formulates solid dispersions of medications with low water solubility. Compared to existing formulations that employ costly excipients, the newly created formulations are more affordable [ 5 ]. Drug: hydrotropic agents' ratio of 1 : 4 was used to prepare hydrotropic solid dispersion by a solvent evaporation method.…”

“…The mix of hydrophobic and hydrophilic components determines the success of hydrotrope solubilization. The hydrotropic potency of a molecule increases as the hydrophobic component increases and the load on the hydrophilic part decreases [ 5 ]. Hydrotropes use an amphiphilic chemical structure to increase the solubility of sparingly soluble organic compounds in water.…”

“…Combining two hydrotropic compounds has a significant synergistic impact on improving the solubility of medicines with low water solubility. Mixed hydrotropy will also be employed in the development of aqueous formulations for medicines with low aqueous solubility [ 5 ]. Hydrotropic agents can be anionic, cationic, neutral, organic, inorganic, or liquids or solids in the natural world.…”

“…Hydrotropic solid dispersions are commercially viable because they are easy to make on a large scale and the technology is simple. They improve the therapeutic potential of solid oral medications that do not dissolve well in water [ 5 ].…”

“…(a) Te hypothesis of self-aggregation (b) Te hypothesis of water structure (c) Solute hydrotrope hypothesis Hydrotrope assemblies are distinguished from other solubilizers by their distinct geometrical properties and various association patterns [5]. Many drugs that do not dissolve well in water are easier to dissolve in hydrotropic solutions of sodium benzoate, sodium aciculate, urea, nicotinamide, sodium citrate, and sodium acetate.…”