Enhancing the Water Solubility and Efficacy of Anticancer Drugs Using Hydroxypropyl-β-Cyclodextrin

TL;DR

This paper shows how hydroxypropyl-β-cyclodextrin improves the water solubility and effectiveness of anticancer drugs, potentially changing its role from a formulation aid to an active treatment ingredient.

Contribution

The paper highlights the novel role of HP-β-CyD as an active pharmaceutical ingredient in cancer therapy, beyond its traditional use as a solubility enhancer.

Findings

HP-β-CyD improves solubility and biocompatibility of poorly water-soluble anticancer drugs.

Folate-conjugated HP-β-CyD shows higher selectivity and potency against cancer cells.

HP-β-CyD may trigger autophagy and could be used in treating leukemia and breast cancer.

Abstract

Cyclodextrins (CyDs) are cyclic oligosaccharides that form inclusion complexes that allow organic compounds and other substances to be incorporated into their cavities. Hydroxypropyl-β-cyclodextrin (HP-β-CyD) is frequently used to improve the formulation properties of poorly water-soluble drugs because of its aqueous solubility and biocompatibility. Previous studies have demonstrated that the solubility and biocompatibility of poorly water-soluble anti-cancer agents can be improved by complexation with HP-β-CyD, which in some cases enhances their anticancer activity relative to the unmodified drugs. Advances in formulation strategies have enabled more efficient intracellular delivery, improved tissue and cell selectivity, and controlled release. HP-β-CyD has also been investigated as an active pharmaceutical ingredient, with demonstrated efficiency in treating leukemia and breast cancer. For example, folate-conjugated HP-β-CyD exhibits high selectivity for folate receptor-expressing cells and more potent anti-cancer activity than unmodified HP-β-CyD. Autophagy has been suggested to be involved in this mechanism. The continued development of drug-delivery systems that integrate advanced technologies and materials based on HP-β-CyD holds promise for further advances in cancer therapy. These findings indicate a paradigm shift in the role of HP-β-CyD from a formulation additive to an active pharmaceutical ingredient, suggesting broader applications for HP-β-CyD in anticancer treatments.

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