Abstract
Cholic acid and galactose or lactose dual conjugated chitosan derivatives were designed and synthesized as potential anti liver cancer drug carriers, their structures were characterized through proton NMR spectra, elemental analysis, size distribution, zeta potential, and scanning electron microscope image studies. The ability of the dual conjugates to enhance the aqueous solubility of the cancer drug sorafenib was evaluated. The entrapment efficiency (EE%) and drug content (DC%) of sorafenib in the inclusion complexes were measured. The chitosan dual conjugate with cholic acid and galactose was found to be best in enhancing the aqueous solubility of sorafenib. The solubility of sorafenib in water has increased from 1.7 µg/mL to 1900 µg/mL which is equal to 1117-fold increase in its solubility due to the inclusion complex with chitosan conjugate.
Highlights
Many of the existing cancer drugs with low water-solubility, non-specific targeting of cancer cells, and lower stability face a barrier for the drugs to reach the tumor area with maximum efficacy
The chemical modification of chitosan through conjugating with hydrophobic moiety imparts amphiphilicity, which enables it in the formation of self-assembled nanoparticles [7], and the resulting hydrophobic cores of nanoparticles could act as reservoirs or microcontainers for various bioactive substances
Stability in comparison with monofunctionalized chitosan conjugates. In this communicawe report preliminary resultsresults on theon design and synthesis of dual chitosan tion, we report preliminary the design and synthesis of functionalized dual functionalized chiderivatives, and their evaluation in increasing the liver cancer drug’s water solubility
Summary
Many of the existing cancer drugs with low water-solubility, non-specific targeting of cancer cells, and lower stability face a barrier for the drugs to reach the tumor area with maximum efficacy. Of liver cancer interest in employing biomolecules as drug carriers for dual targeting [23] of liver cancer cells, cells, we we anticipate anticipate that that the thebifunctionalized bifunctionalized chitosan chitosan compounds compounds can can alsobe beemployed employed as drug carriers for targeting liver cancer cells, and these chitosan-linked molecules as drug carriers for targeting liver cancer cells, and these chitosan-linked molecules may may increase apart from improving drug’s water solubility and and staincreasethe thedrug’s drug’stargeting targetingefficacy, efficacy, apart from improving drug’s water solubility bility in comparison with monofunctionalized chitosan conjugates. Used technique to increase the water solubility of drugs is by supramolecular complexaThe results of employing the above chitosan conjugates 1, 2, and 3 as the dual liver cell tion [28]. Will be described as part of a demonstration of the usefulness of the described chitosan conjugates
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