The invention relates to
dithiolane modified beta-
cyclodextrin, a preparation method thereof and application of the
dithiolane modified beta-
cyclodextrin as a
drug carrier. The method comprises the following steps: carrying out
acylation reaction on beta-
cyclodextrin and
lipoic acid, and modifying different numbers of
dithiolane on the beta-cyclodextrin by changing a feeding ratio; the beta-cyclodextrin has a plurality of hydroxyl groups, and the activity of the hydroxyl groups at the C6 position is relatively high. The hydrophobic cavity of the dithiolane-modified beta-cyclodextrin can be loaded with a hydrophobic small-molecule
drug, and the hydrophobic small-molecule
drug can be loaded into the dithiolane-modified beta-cyclodextrin under the condition of heating
reflux to form a nano-drug. The
disulfide bond on the surface of the nano-drug and sulfydryl on
protein or lipid on the outer side of a
cell membrane are subjected to dynamic covalent
thiol exchange, so that the nano-drug enters cells through a
thiol-mediated cellular uptake way, endosomes and lysosomes can be avoided, the drug is quickly and directly delivered to the
cytoplasm, degradation of the drug in the lysosomes is reduced, and the
drug delivery efficiency is improved. The
utilization rate of small-molecule drugs is improved, side effects are reduced, and better curative effects are achieved.