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Tamoxifen-2-hydroxylpropyl-beta-cyclodextrin-aggregated nanoassembly for nonbreast estrogen-receptor-positive cancer
Jaya Shukla1, Uma Sharma, Rajarshi Kar
1Department of Nuclear Medicine, All India Institute of Medical Sciences, New Delhi 110029, India.
Background:
Tamoxifen (Tam) is used for the treatment and prevention of estrogen-receptor-positive human breast and other cancers. Its use in ovarian cancer has not been well studied.
Method:
We formulated and characterized a water-soluble Tam-2-hydroxylpropyl-beta-cyclodextrin (HPbetaCD; 1:2 M) complex.
Results:
The differential scanning calorimetery of Tam-HPbetaCD indicated the transition of Tam from crystalline to amorphous form on addition of HPbetaCD. (1)H-nuclear magnetic resonance nuclear overhauser effect cross-peaks between phenyl moieties of Tam and HPbetaCD, and downfield shifts in H-3 (0.26) and H-5 (0.29) protons of HPbetaCD suggested the inclusion of Tam in HPbetaCD cavity. Transmission-electron microscopy studies of HPbetaCD and the Tam-HPbetaCD complex revealed the formation of aggregated nanoassembly at 60-180 nm. Dimethyl thiazol diphenyltetrazolium bromide assay demonstrated 7.37 +/- 2.32% cell survival of OAW-42 cells with 3 microg/ml Tam concentration.
Conclusion:
The Tam-HPbetaCD nanoassembly entered the cell owing to enhanced permeability and retention property of tumor cell and antiestrogenic Tam and, therefore, resulted in excellent anticancer efficacy in the ovarian cancer cell line.
Insights
A novel nanoassembly of tamoxifen (Tam) and hydroxylpropyl-beta-cyclodextrin (HPbetaCD) shows promise for ovarian cancer treatment. This formulation enhances Tam
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Oncology
Background:
- Tamoxifen (Tam) is a key drug for estrogen-receptor-positive breast cancers.
- Its efficacy and application in ovarian cancer remain less explored.
Purpose of the Study:
- To develop and characterize a water-soluble nanoassembly of Tamoxifen.
- To evaluate its potential as an anticancer agent for ovarian cancer.
Main Methods:
- Formulation of a water-soluble Tamoxifen-2-hydroxylpropyl-beta-cyclodextrin (HPbetaCD) complex (1:2 M ratio).
- Characterization using differential scanning calorimetry, NMR spectroscopy, and transmission electron microscopy.
- In vitro cytotoxicity assessment using the dimethyl thiazol diphenyltetrazolium bromide assay on OAW-42 ovarian cancer cells.
Main Results:
- Tamoxifen transitioned from crystalline to amorphous form within the HPbetaCD complex.
- NMR studies confirmed the inclusion of Tamoxifen within the HPbetaCD cavity.
- Transmission electron microscopy revealed nanoassembly formation (60-180 nm).
- The Tam-HPbetaCD complex demonstrated significant cytotoxicity against OAW-42 cells (7.37% cell survival at 3 μg/ml Tam).
Conclusions:
- The Tam-HPbetaCD nanoassembly exhibits enhanced permeability and retention in tumor cells.
- This formulation demonstrates excellent anticancer efficacy in an ovarian cancer cell line.
- The study highlights the potential of HPbetaCD complexation for improving Tamoxifen delivery and efficacy in ovarian cancer.
