Cyclodextrins: An Overview of the Complexation of Pharmaceutical Proteins

G.H.C.      Varca; N.      Andreo-Filho; P.S.      Lopes; H.G.      Ferraz

Abstract

Cyclodextrins are oligosaccharides, specifically cyclic α-1,4-D-glucose oligomers, that possess a cone-like shape resulting in a hydrophobic inner cavity capable of forming complexes with several guest molecules in a hydrophilic matrix. This capability has led to an extensive investigation into cyclodextrin applications in several different substrates with the purpose of overcoming limitations, such as solubility issues, physical degradation and sensitivity to solvents, in guest substances. Researchers have recently described successful interactions between cyclodextrins and proteins, such as enzymes, peptides and amino acids. These complex biomolecules consist of potent active ingredients and are employed in several industrial biocatalyst processes. However, this group in particular tends to have limited usage in pharmaceuticals due to its natural processes of degradation and instability in unusual environments, frequently requiring accurate procedures and stabilization methods in all stages of production. In several cases, the final product still has a short shelflife and often requires a controlled environment for storage. The formation of a cyclodextrin supramolecular complex could not only prevent such problems, but also enhance the intrinsic characteristics of guest substances, thus allowing for an expansion in their industrial production and application. This work focuses on cyclodextrin interactions with proteinlike structures in order to describe their possible applications in the formulation of pharmaceutical proteins.

Keywords: Cyclodextrin, protein, enzyme, amino acids, peptides, supramolecular complexes, macromolecules