Comparing water solubility of β-cyclodextrin derivatives with dendrimers modified with β-cyclodextrin units, how significant is the change in water solubility?

Nowadays, β-cyclodextrin (βCD) is considered a molecule of great interest for the pharmaceutical industry since it is widely used as a component in different formulations. Its properties as a complexing agent allow increasing the aqueous solubility of poorly soluble drugs, thereby improving their stability and bioavailability. βCD molecules exhibit moderate solubility in water. This phenomenon is caused by the high symmetry of its 3D structure, which limits its interaction with water molecules. When this symmetry is disrupted by the addition of adequate substituents in its structure, βCD becomes a molecule with significantly increased aqueous solubility. In this work, we compared the water solubility values for βCD and their improved derivatives and performed measurements of the quantitative water solubility for novel PAMAM-βCD and EDTA-βCD dendrimers in order to demonstrate that significant improvement in water solubility is possible using this new class of platforms, which are at least 27 times more soluble than βCD. Graphical abstract