Cyclodextrin Inclusion Complexes for Improved Drug Bioavailability and Activity: Synthetic and Analytical Aspects

Pharmaceutics · 5 authors, 2 centres

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TL;DR

This narrative review discusses how forming inclusion complexes with cyclodextrins is a tool to improve the oral bioavailability and stability of various drugs and nutraceuticals.

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This is a narrative review covering synthetic, analytical, and pharmaceutical aspects of cyclodextrin inclusion complexes. It describes how cyclodextrins, as cyclic oligosaccharides, can form complexes with active pharmaceutical ingredients and nutraceuticals to improve properties like dissolution rate, bioavailability, and stability. The review discusses the use of cyclodextrin-based polymers, nanosponges, and nanofibers for drug delivery and stabilization, with examples for labile drugs and poorly soluble compounds classified as BCS class IV. It also reviews synthetic routes for chemically modified cyclodextrins and analytical techniques (e.g., spectroscopic methods) to verify complex formation in solution and solid state. The review concludes that cyclodextrins and their derivatives offer possibilities for personalized medicine and sustained drug delivery.

STUDY TYPE

narrative_review

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biomedical research

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ORIGINAL PAPER

PMC10534465

Cyclodextrin Inclusion Complexes for Improved Drug Bioavailability and Activity: Synthetic and Analytical Aspects

Pharmaceutics

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ABSTRACT

Many active pharmaceutical ingredients show low oral bioavailability due to factors such as poor solubility and physical and chemical instability. The formation of inclusion complexes with cyclodextrins, as well as cyclodextrin-based polymers, nanosponges, and nanofibers, is a valuable tool to improve the oral bioavailability of many drugs. The microencapsulation process modifies key properties of the included drugs including volatility, dissolution rate, bioavailability, and bioactivity. In this context, we present relevant examples of the stabilization of labile drugs through the encapsulation in cyclodextrins. The formation of inclusion complexes with drugs belonging to class IV in the biopharmaceutical classification system as an effective solution to increase their bioavailability is also discussed. The stabilization and improvement in nutraceuticals used as food supplements, which often have low intestinal absorption due to their poor solubility, is also considered. Cyclodextrin-based nanofibers, which are polymer-free and can be generated using environmentally friendly technologies, lead to dramatic bioavailability enhancements. The synthesis of chemically modified cyclodextrins, polymers, and nanosponges based on cyclodextrins is discussed. Analytical techniques that allow the characterization and verification of the formation of true inclusion complexes are also considered, taking into account the differences in the procedures for the formation of inclusion complexes in solution and in the solid state.

CITATION EXPORT

Álvaro Sarabia-Vallejo, María del Mar Caja, Ana I. Olives et al.. Cyclodextrin Inclusion Complexes for Improved Drug Bioavailability and Activity: Synthetic and Analytical Aspects. Pharmaceutics. (2023). https://doi.org/10.3390/pharmaceutics15092345

AUTHORS

5 · 2 CENTRES

Álvaro Sarabia-Vallejo, María del Mar Caja, Ana I. Olives, M. Antonia Martín, J. Carlos Menéndez

1Unidad de Química Orgánica y Farmacéutica, Departamento de Química en Ciencias Farmacéuticas, Facultad de Farmacia, Universidad Complutense, 28040 Madrid, Spain; [email protected]
2Unidad de Química Analítica, Departamento de Química en Ciencias Farmacéuticas, Facultad de Farmacia, Universidad Complutense, 28040 Madrid, Spain; [email protected]

EDITOR / REVIEWER

Magdalena Paczkowska-Walendowska