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Solubility is the measure of the maximum amount of solute that can be dissolved in a given quantity of solvent at a given temperature and pressure. Solubility is usually measured in molarity (M) or moles per liter (mol/L). A compound is termed soluble if it dissolves in water.
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Solution, Solubility, and Solubility Equilibrium
A solution is a homogeneous mixture composed of a solvent, the major component, and a solute, the minor component. The physical state of a solution—solid, liquid, or gas—is typically the same as that of the solvent. Solute concentrations are often described with qualitative terms such as dilute (of relatively low concentration) and concentrated (of relatively high concentration).
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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
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Structure of Carboxylic Acid Derivatives
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Water-Soluble Nystatin and Derivative.

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Researchers developed a new Nystatin derivative to combat drug-resistant fungal infections. This ethanol amide derivative is water-soluble, retains antifungal potency, and exhibits significantly lower toxicity, offering a promising alternative for treating serious fungal diseases.

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Area of Science:

  • Mycology
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Fungal infections cause significant morbidity and mortality, particularly in immunocompromised individuals.
  • Emerging drug-resistant fungal strains present a growing clinical challenge.
  • Nystatin, a polyene antifungal, has limitations in solubility and high toxicity, restricting its use.

Purpose of the Study:

  • To develop novel Nystatin derivatives and formulations to overcome existing limitations.
  • To enhance the therapeutic potential of Nystatin for broader clinical applications.

Main Methods:

  • Synthesis of Nystatin amide derivatives and a deoxycholate formulation.
  • Antifungal potency testing using USP(81) method and minimum inhibitory concentration (MIC) against Candida albicans and Aspergillus niger.
  • In vitro toxicity and stability assessments of the novel compounds.

Main Results:

  • An ethanol amide derivative of Nystatin was synthesized and found to be fully water-soluble (up to 100 mg/mL).
  • This derivative demonstrated equivalent antifungal potency to Nystatin.
  • The ethanol amide derivative exhibited 13.5 times lower in vitro toxicity compared to Nystatin.

Conclusions:

  • The novel ethanol amide derivative of Nystatin represents a significant advancement.
  • Its improved solubility, retained potency, and reduced toxicity make it a promising candidate for future antifungal drug development.
  • This derivative could offer a safer and more effective treatment option for challenging fungal infections.