Advances of nanosystems containing cyclodextrins and their applications in pharmaceuticals.

For many years, researchers have worked with supramolecular structures involving inclusion complexes with cyclodextrins. These studies have resulted in new commercially available drugs which have been of great benefit. More recently, studies using nanoparticles, including nanosystems containing cyclodextrins, have become a focus of academic research due to the versatility of the systems and their remarkable therapeutic potential. This review focuses on studies published between 2002 and 2018 involving nanosystems containing cyclodextrins. We consider the type of nanosystems, their importance in a health context, the physicochemical techniques used to show the quality of these systems and their potential for the development of novel pharmaceutical formulations. These have been developed in recent studies which have mainly been focusing on basic science with no clinical trials as yet being performed. This is important to note because it means that the studies do not include any toxicity tests. Despite this limitation, the characterization assays performed suggest that these new formulations may have therapeutic potential. However, more research is required to assess the efficacy and safety of these nanosystems.

Physicochemical Characterization and Antinociceptive Effect of ß-cyclodextrin/Lippia pedunculosa Essential Oil in Mice.

BACKGROUND: Some research studies have shown that Lippia pedunculosa essential oil (EOLP) has interesting biological activities. However, its low water solubility is the main challenge to achieve its therapeutic potential. In this context, Cyclodextrins (CDs) have been widely used in order to overcome this problem due to your capability to improve the physicochemical properties of drugs. OBJECTIVE: In this perspective, the main goal of this study was to investigate how the improvement of the physicochemical properties of inclusion complexes (EOLP and ß-CD) enhance the antinociceptive effect in mice. METHODS: To achieve that, we prepared samples by Physical Mixture (PM), Paste Complexation (PC) and Slurry Complexation (SC) methods, followed by their physicochemical characterization. In addition, it was evaluated if the use of ß-CD enhances the antinociceptive effect of EOLP in mice. RESULTS: The analysis showed that rotundifolone (72.02%) was the major compound of EOLP and we found out based on DSC results that ß-CD protected it from oxidation. In addition, TG techniques demonstrated that the best inclusion methods were PC and SC, due to their greater weight loss (10.8 and 11.6%, respectively) in the second stage (171-312°C), indicating that more complexed oil was released at the higher temperature than oil free. Other characteristics, such as changes in the typical crystalline form, and reduced particle size were observed by SEM and laser diffraction, respectively. The SC was the most effective complexation method, once the presence of rotundifolone was detected by FTIR. Based on that, SC method was used in all mice tests. In this regard, the number of paw licks was reduced for both compounds (all doses), but EOLP was more effective in reducing the nociceptive behavior. CONCLUSION: Therefore, CDs seem not to be a good tool to enhance the pharmacological properties of EOs rich in peroxide compounds such as rotundifolone.