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Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
Published on: February 8, 2017
Constructing transferrin receptor targeted drug delivery system by using doxorubicin hydrochloride and vanadocene
Yanxia Zhang1, Junfeng Xiang, Yan Liu
1State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China.
Abstract:
Transferrin has shown potential in the delivery of anticancer drugs into primarily proliferating malignant cells that over-express transferrin receptors. Constructing transferrin receptor targeted drug delivery system has been widespread concerned. In this study, whether transferrin could transport noncovalent binding drugs into cancer cells has been investigated. Two representative compounds, doxorubicin hydrochloride (Dox) and vanadocene dichloride (Cp(2)VCl(2)), have been chosen to study the interactions with h-Tf and apo-Tf, and the influences in the presence of h-Tf and apo-Tf by using fluorescence spectroscopy, circular dichroism (CD) spectroscopy and MTT assay. The results have shown that both doxorubicin and Cp(2)VCl(2) could bind to h-Tf and apo-Tf but with different binding modes. The results of MTT assay demonstrate that the presence of both h-Tf and apo-Tf has enhanced the antiproliferative activity of Cp(2)VCl(2). However, the anticancer activity of the mixture of doxorubicin and h-Tf is basically the same as that of doxorubicin does. Our studies indicate that transferrin plays an important role in the transport and targeted delivery of Cp(2)VCl(2) into cancer cells.
Insights
Transferrin (Tf) facilitates targeted anticancer drug delivery. This study shows Tf enhances the efficacy of vanadocene dichloride (Cp(2)VCl(2)) delivery into cancer cells, but not doxorubicin.
Area of Science:
- Biochemistry
- Pharmacology
- Nanotechnology
Background:
- Transferrin (Tf) is explored for targeted anticancer drug delivery to cancer cells overexpressing Tf receptors.
- Investigating Tf's role in transporting non-covalently bound drugs is crucial for developing advanced drug delivery systems.
Purpose of the Study:
- To investigate if transferrin can transport noncovalently binding anticancer drugs into cancer cells.
- To evaluate the interaction of doxorubicin hydrochloride (Dox) and vanadocene dichloride (Cp(2)VCl(2)) with human Tf (h-Tf) and apotransferrin (apo-Tf).
- To assess the influence of h-Tf and apo-Tf on the anticancer activity of Dox and Cp(2)VCl(2).
Main Methods:
- Fluorescence spectroscopy to study drug-Tf interactions.
- Circular dichroism (CD) spectroscopy to analyze structural changes upon binding.
- MTT assay to determine the antiproliferative effects of drug-Tf combinations.
Main Results:
- Both Dox and Cp(2)VCl(2) bind to h-Tf and apo-Tf via distinct binding modes.
- The presence of h-Tf and apo-Tf significantly enhanced the antiproliferative activity of Cp(2)VCl(2).
- Cp(2)VCl(2) delivery into cancer cells was notably improved by Tf, while Dox activity remained largely unchanged.
Conclusions:
- Transferrin plays a significant role in the transport and targeted delivery of Cp(2)VCl(2) into cancer cells.
- Tf enhances the anticancer efficacy of vanadocene dichloride, suggesting its potential as a drug carrier for this compound.
- The interaction and transport mechanism differ between Dox and Cp(2)VCl(2) when complexed with Tf.
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