AUTHOR=Zhu Panyong , Lv Pin , Zhang Yazhou , Liao Rongqiang , Liu Jing , Guo Rong , Chen Xuan , Liao Xiali , Gao Chuanzhu , Zhang Kun , Yang Ming , Yang Bo 

TITLE=Self-Assembly System Based on Cyclodextrin for Targeted Delivery of Cannabidiol

JOURNAL=Frontiers in Chemistry

VOLUME=Volume 9 - 2021

YEAR=2021

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2021.754832

DOI=10.3389/fchem.2021.754832

ISSN=2296-2646

ABSTRACT=Cannabidiol (CBD) is one peculiar kind of the cannabinoid in Cannabis sativa L with wide pharmacological activities. However, the poor water solubility and specificity of CBD limiting 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 supramolecular biopolymer, named BIO-CD. Amantadine-conjugated cannabinoids (AD-CBD) was prepared and self-assembled with BIO-CD. At the same time, a series of methods were used to characterize the inclusion behavior and physicochemical properties of AD-CBD and BIO-CD. The results shown that AD-CBD entered the cavity of BIO-CD and formed a 1 : 1 host-guest inclusion complex. The possible inclusion mode of them was also speculated. MTT assay revealed that the targeting effect and confocal laser scanning microscopy (CLSM), 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 convincingly results demonstrated that AD-CBD/BIO-CD inclusion complex possess excellent targeted and anticancer activity, which is hopeful to be applied to clinically as a new therapeutic approach.