Cyclodextrins as multifunctional excipients

Cyclodextrins are pharmaceutical excipients which can form inclusion complexes. They are mainly used to increase the solubility of active pharmaceutical ingredients, which causes increased bioavailability. In addition, they can mask the taste and smell, affect the modification of biological properties and increase its chemical stability. The aim of the studies was to determine the possibility of using cyclodextrins as substances modifying chemical stability of model labile active pharmaceutical ingredients for which the susceptibility to degradation in acid-base hydrolysis (meropenem), thermolysis (meropenem), oxidation (cetirizine) or photolysis (rutin) has been previously proven. The extension of the research was a parallel assessment of the effect of cyclodextrin on selected physicochemical and biological properties important due to the possibility of modifying the pharmaceutical properties of selected model labile active pharmaceutical ingredients. In the first stage, preparations of labile systems of active pharmaceutical ingredients with β-cyclodextrin were carried out using kneading and dry mixing methods. Next, the identity of the obtained systems was confirmed using spectral (UV, FT-IR, Raman, XRPD), thermal (DSC) and microscopic (SEM) methods. The analytical methods (UV method for meropenem, HILIC for cetirizine and UHPLC-DAD for rutin) have been developed and validated to assess the changes in the concentration of model labile active pharmaceutical ingredients during stability, solubility and permeability studies through artificial biological membranes. The conducted research confirms the possibility of modifying the chemical stability of labile active pharmaceutical ingredients under acid- -base hydrolysis conditions, thermolysis, oxidation and photolysis. They also confirm the beneficial effect of the presence of inclusion systems based on cyclodextrin systems on parameters for other pharmaceutical properties of active substances, especially such as dissolution dynamics, dissolution rate, permeability and eventually bioavailability.