Cyclodextrin–Drug Inclusion Complexes: In Vivo and In Vitro Approaches

Abstract

This review aims to provide a critical review of the biological performance of natural and synthetic substances complexed with cyclodextrins, highlighting: (i) inclusion complexes with cyclodextrins and their biological studies in vitro and in vivo; (ii) Evaluation and comparison of the bioactive efficacy of complexed and non-complexed substances; (iii) Chemical and biological performance tests of inclusion complexes, aimed at the development of new pharmaceutical products. Based on the evidence presented in the review, it is clear that cyclodextrins play a vital role in the development of inclusion complexes which promote improvements in the chemical and biological properties of the complexed active principles, as well as providing improved solubility and aqueous stability. Although the literature shows the importance of their ability to help produce innovative biotechnological substances, we still need more studies to develop and expand their therapeutic properties. It is, therefore, very important to gather together evidence of the effectiveness of inclusion complexes with cyclodextrins in order to facilitate a better understanding of research on this topic and encourage further studies.

Formation of inclusion complex of enrofloxacin with 2-hydroxypropyl- β -cyclodextrin

“…The problem of the low solubility of many drugs has been overcome by complexation of the active principle ingredient with a-, b-, or c-cyclodextrins, and 2-hydroxypropyl-b-cyclodextrin (HP-b-CD) as well. HP-b-CD, is the most widely used modified cyclodextrin, has excellent inclusion properties for many compounds, is less toxic, safe, and an effective drug carrier (Gould & Scott, 2005;Misiuk & Zalewska, 2009;Folch Cano et al, 2014;Srivalli & Mishra, 2016;Carneiro et al, 2019). Previously, HP-b-CD was used to form the inclusion complex with enrofloxacin to increase its aqueous solubility and stability.…”

Influence of Pomace Matrix and Cyclodextrin Encapsulation on Olive Pomace Polyphenols’ Bioaccessibility and Intestinal Permeability

“…CDs are cyclic oligosaccharides used for the improvement of water-solubility and bioavailability of medicinal products. Their key feature is the hydrophobic internal cavity, that provides the ability to form complexes with a variety of guest molecules resulting with the formation of encapsulation complexes [18]. The encapsulation can influence the stability of nutraceutical in gastrointestinal tract by reducing the rate of hydrolysis, oxidation, stearic rearrangement, racemization, enzymatic decomposition, or formation of complexes with other food components which, all together, can have significant impact on nutraceutical bioaccessibility.…”

Development and Evaluation of Antimicrobial and Modulatory Activity of Inclusion Complex of Euterpe oleracea Mart Oil and β-Cyclodextrin or HP-β-Cyclodextrin

“…CD have been used as a pharmaceutical excipient able to increase the solubility of drugs. These cyclic oligosaccharides also exhibit stable physicochemical characteristics capable of protecting host molecules from degradation in the gastrointestinal tract and against oxidation, provide photo and thermal stability, and reduce physiological effects, undesirable organoleptic characteristics, drug volatility and toxicity [20][21][22][23][24][25].…”