Abstract
Cannabidiol (CBD) is one specific kind of the cannabinoid in Cannabis sativa L with a wide range of pharmacological activities. However, the poor water solubility and specificity of CBD limits its application in pharmaceutical field. For solving these problems, in this work, we successfully prepared a targeted carrier by grafting biotin (BIO) onto ethylenediamine-β-Cyclodextrin (EN-CD) in a single step to generate a functionalized supramolecule, named BIO-CD. Subsequently, an amantadine-conjugated cannabinoids (AD-CBD) was prepared and self-assembled with the BIO-CD. A series of methods were used to characterize the inclusion behavior and physicochemical properties of AD-CBD and BIO-CD. The results showed that AD-CBD entered the cavity of BIO-CD and formed a 1:1 host-guest inclusion complex. MTT assay and confocal laser scanning microscopy (CLSM) revealed that the targeting effect and anticancer activity of AD-CBD/BIO-CD inclusion complex against three human cancer cell lines were higher than BIO-CD, AD-CBD and free CBD. Moreover, the inclusion complex could release drugs under weakly acidic conditions. These results demonstrated that AD-CBD/BIO-CD inclusion complex possess excellent targeted and anticancer activity, which is hopeful to be applied in clinic as a new therapeutic approach.
Highlights
Cannabaceae, an annual herbaceous crop, has been widely cultivated for fiber, food, and medicine for thousands of years (Pain, 2015; Guo et al, 2018)
AD-CBD/BIO-CD inclusion complex was obtained on NMR spectrometer after stirring for 1 h, and water solubility was calculated through integral ratio
The results indicated that AD-CBD entered the cavity of BIO-CD completely or partially, which limited the vibration of the corresponding functional groups
Summary
Cannabaceae, an annual herbaceous crop, has been widely cultivated for fiber, food, and medicine for thousands of years (Pain, 2015; Guo et al, 2018). AD-CBD/BIO-CD inclusion complex was obtained on NMR spectrometer after stirring for 1 h, and water solubility was calculated through integral ratio. The crystal form information of AD-CBD/BIO-CD inclusion complex could be obtained by powder X-ray diffraction analysis.
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