Improved biological performance of ketoprofen using novel modified halloysite clay nanotubes

In the present work, elegant modification of halloysite (Hal) by citric acid (CA) was realized. The corresponding novel bio-composite (Hal-CA) was then used as drug carrier. To validate this concept, ketoprofen (KET), a known non-steroidal anti-inflammatory agent, was chosen as drug model. KET has low solubility and a short biological half-life, which can cause some limitations in its therapeutic use. In addition, its use is limited due to gastrointestinal side effects. All Hal, Hal-CA, Hal-KET and Hal-CA-KET samples were characterized using several techniques such as X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, transmission electron microscopy (TEM), N2 adsorption-desorption, thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). The release of KET from the prepared formulations was investigated at pH 1 and 6.8 by means of UV-Visible spectroscopy. In addition, kinetics of the release of KET from inclusion complexes were determined by fitting the release profiles to the first order, Korsmeyer-Peppas and Higuchi models. In order to assess these novel bio-composites, anti-inflammatory and anti-nociceptive activities were also evaluated in vivo. Finally, the ulcerogenic activity and the histopathological effects of all formulations were compared to that of pure KET. This work showed the increase of the anti-inflammatory and antinociceptive potentials of KET loaded in Hal-CA, as well as a maximum protection against ulcers. This suggests that Hal-CA can be considered as a new carrier for pharmaceutical formulations.

Automated summary

In this study, halloysite was elegantly modified with citric acid and used as a drug carrier for ketoprofen. The inclusion complexes of Hal-CA with KET showed increased anti-inflammatory and antinociceptive potentials, as well as maximum protection against ulcers. These findings suggest that Hal-CA could be a promising carrier for pharmaceutical formulations.