Encapsulation of Clofazimine by Cyclodextran: Preparation, Characterization, and In Vitro Release Properties

This study aimed to evaluate and compare the efficacy of cyclodextrans (CIs) and cyclodextrins (CDs) in improving the water solubility of a poorly water-soluble drug, clofazimine (CFZ). Among the evaluated CIs and CDs, CI-9 exhibited the highest percentage of drug inclusion and the highest solubility. Additionally, CI-9 showed the highest encapsulation efficiency, with a CFZ:CI-9 molar ratio of 0.2:1. SEM analysis indicated successful formation of inclusion complexes CFZ/CI and CFZ/CD, accounting for the rapid dissolution rate of the inclusion complex. Moreover, CFZ in CFZ/CI-9 demonstrated the highest drug release ratio, reaching up to 97%. CFZ/CI complexes were found to be an effective means of protecting the activity of CFZ against various environmental stresses, particularly UV irradiation, compared to free CFZ and CFZ/CD complexes. Overall, the findings provide valuable insights into designing novel drug delivery systems based on the inclusion complexes of CIs and CDs. However, further studies are needed to investigate the effects of these factors on the release properties and pharmacokinetics of encapsulated drugs in vivo, in order to ensure the safety and efficacy of these inclusion complexes. In conclusion, CI-9 is a promising candidate for drug delivery systems, and CFZ/CI complexes could be a potential formulation strategy for the development of stable and effective drug products.

Automated summary

This study evaluated and compared the effectiveness of CIs and CDs in enhancing the water solubility of the poorly water-soluble drug CFZ. Among all the evaluated CIs and CDs, CI-9 showed the highest drug inclusion percentage and solubility, as well as the highest encapsulation efficiency. SEM analysis confirmed the successful formation of inclusion complexes CFZ/CI and CFZ/CD, which accounted for the rapid dissolution rate. CFZ/CI-9 exhibited the highest drug release ratio and better protection against environmental stresses compared to free CFZ and CFZ/CD complexes. These findings provide valuable insights for designing drug delivery systems based on CIs and CDs, but further studies are needed to ensure their safety and efficacy in vivo.