Tamoxifen-2-hydroxylpropyl-beta-cyclodextrin-aggregated nanoassembly for nonbreast estrogen-receptor-positive cancer therapy

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.

Medienart:

E-Artikel

Erscheinungsjahr:

2009

Erschienen:

2009

Enthalten in:

Zur Gesamtaufnahme - volume:4

Enthalten in:

Nanomedicine (London, England) - 4(2009), 8 vom: 15. Dez., Seite 895-902

Sprache:

Englisch

Beteiligte Personen:

Shukla, Jaya [VerfasserIn]
Sharma, Uma [VerfasserIn]
Kar, Rajarshi [VerfasserIn]
Varma, Indira Kumari [VerfasserIn]
Juyal, Sanjay [VerfasserIn]
Jagannathan, Naranamangalam R [VerfasserIn]
Bandopadhyaya, Guru P [VerfasserIn]

Links:

Volltext

Themen:

094ZI81Y45
Antineoplastic Agents, Hormonal
Beta-Cyclodextrins
Betadex
JV039JZZ3A
Journal Article
Receptors, Estrogen
Research Support, Non-U.S. Gov't
Tamoxifen

Anmerkungen:

Date Completed 03.03.2010

Date Revised 21.11.2013

published: Print

Citation Status MEDLINE

doi:

10.2217/nnm.09.69

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM193247178