Background: Bortezomib (BTZ) as an anticancer drug has been used through the injection pathway.
Research design and methods: Two types of Cyclodextrin nanosponges (CDNSs) were synthesized and studied by DLS, TEM, FTIR, and DSC instruments for BTZ delivery. Both carriers were analyzed for loading efficiencies and in-vitro release. Cell studies and intestinal permeability of selected CDNS were determined using MTT and SPIP method, respectively.
Results: Both types of CDNSs, encapsulated BTZ in their nano-porous structure, but better loading was shown in CDNS 1:4. FTIR and DSC results proved considerable encapsulation of BTZ into CDNSs. The slow and prolonged release profile was observed for CDNS 1:4 in comparison with CDNS 1:2. Based on in-vitro results, BTZ-CDNS 1:4 was chosen as a selected nanosystem for further analysis. This nontoxic carrier revealed considerable uptake (93.9% in 3 h) against the MCF-7 cell line but indicated higher IC50 in comparison with the plain drug. This carrier also could improve the rat intestinal permeability of BTZ almost 5.8 times.
Conclusion: CDNS 1:4 has the ability to be introduced as a nontoxic carrier for BTZ delivery with its high loading, controlled release manner, high cellular uptake, and permeability improvement characteristics.
Keywords: in-vitro; Bortezomib; cyclodextrin; nanosponge; permeability.