Title: Cyclodextrins in inclusion and non-inclusion complex with drugs: in vitro and in vivo approach

Adley Antonini Neves de Lima

Federal University of Rio Grande do Norte, Brazil


Pharmacist, Master and PhD in Pharmaceutical Sciences at UFPE. He was a professor at the Federal University of Amazonas (UFAM). Member of the Thematic Technical Committee of Excipients and Adjuvants of the Brazilian Pharmacopoeia. Professor of the Pharmacy course at UFRN. Published several articles published in several international journals, published book chapter and several deposited patents. Reviewer of several periodicals and chapter editor of Biomolecules (MDPI) and InTechOpen. He has partnership and R&D projects with several Brazilian pharmaceutical and cosmetic industries. He has international partnerships with universities: Universitá degli Studi di Parma, Genova and Firenze (Italy).


Cyclodextrins (CDs) are cyclic oligaccharides, derived from sugar, which have amphiphilic characteristics, which can form inclusion complexes with various drugs, new synthetic, semi-synthetic molecules, vegetable oils. CDs, are macrocyclic oligosaccharides such as alpha-cyclodextrin (α-CD), beta-cyclodextrin (β-CD) and gamma-cyclodextrin (γ-CD), are composed of 6, 7 or 8 glucose units, and their synthetic derivatives are divided into three groups: hydrophilic, such as 2-hydroxypropyl-β-CD (HP-β-CD); hydrophobic, such as 2,6-di-O-ethyl-β-CD; and ionizable, such as sulfobutyl ether β -CD (SBE-β-CD). Structurally the cyclodextrins have a cavity size which is determined by the number of glucose units. Free hydroxyls on the outside of the CD's impart a more hydrophilic character, whereas the oxygen atoms at the glycosidic bonds and the hydrogen atoms impart a hydrophobic character inside the cavity. The character of a hydrophobic cavity and free hydroxyls on the outside of the molecule allows the "dissolution" in aqueous medium of low solubility compounds. This space inside the molecule allows the cyclodextrins to form inclusion complexes of compounds with low solubility. CD's are widely used in pharmaceuticals, drug delivery systems, cosmetics, and the food and chemical industries and are considered safe. They can be found in commercially available medications, including tablets, eye drops, and ointments. The use of cyclodextrins (CDs) for the development of inclusion complexes (IC) can promote improvements in the chemical and biological properties of the complexed active principles, and may also improve solubility and aqueous stability. Biological assays are required to evaluate and compare the bioactive efficacy of complexed and non-complexed substances. This review highlights studies using in vitro assays to assess their antimicrobial, antichagasic, antitumor, antioxidant and other properties, and in vivo bioassays examining their anti-inflammatory, antinociceptive and anticancer and other properties, as well as their intestinal absorption characteristics. The objective of this presentation is to detail the use of CDs in applied studies, performance tests and biological assays in cells and animals, aimed at the development of new pharmaceutical products using inclusion complexes. Based on this literature review, cyclodextrin inclusion complexes (CDs-IC) have been shown to be effective, adding to the bioavailability, solubility and stability of drugs, and promoting the desired pharmacological effects in both in vivo and in vitro studies. Although the literature shows the importance of (CDs-IC) and their ability to help to produce innovative biotechnological substances, further studies are still required to develop and enlarge their therapeutic properties and use.
Audience take away:
• Students and researchers can apply the knowledge acquired to the development of new drug delivery systems using cyclodextrins with various biological applications
• Teachers and students can use the knowledge in the area of teaching, in the classes of pharmaceutical technology, biopharmacy. In the research area, they will be able to publish high-impact scientific articles, deposit patents and still attract the attention of pharmaceutical industries through the development of new products with physio-chemical and biological characteristics improved with the complexation of drugs with cyclodextrins