Tamoxifen Citrate

Author(s):  
Mark G. Papich
Keyword(s):  
2011 ◽  
Vol 83 (11) ◽  
pp. 2027-2040 ◽  
Author(s):  
Neralakere Ramanna Ravikumara ◽  
Basavaraj Madhusudhan

In this study, tamoxifen citrate-loaded chitosan nanoparticles (tamoxcL-ChtNPs) and tamoxifen citrate-free chitosan nanoparticles (tamoxcF-ChtNPs) were prepared by an ionic gelation (IG) method. The physicochemical properties of the nanoparticles were analyzed for particle size, zeta (ζ) potential, and other characteristics using photon correlation spectroscopy (PCS), zeta phase analysis light scattering (PALS), scanning electron microscopy (SEM), Fourier transform infrared (FTIR), and differential scanning calorimetry (DSC). The variation in particle size was assessed by changing the concentration of chitosan, pentasodium tripolyphosphate (TPP), and the pH of the solution. The optimized tamoxcL-ChtNPs showed mean diameter of 187 nm, polydispersity of 0.125, and ζ-potential of +19.1 mV. The encapsulation efficiency (EE) of tamoxifen citrate (tamoxc) increased at higher concentrations, and release of tamoxc from the chitosan matrix displayed controlled biphasic behavior. Those tamoxcL-ChtNPs tested for chemosensitivity showed dose- and time-dependent antiproliferative activity of tamoxc. Further, tamoxcL-ChtNPs were found to be hemocompatible with human red blood cells (RBCs) and safe by in vitro cytotoxicity tests, suggesting that they offer promise as drug delivery systems in therapy.


Oncology ◽  
1983 ◽  
Vol 40 (4) ◽  
pp. 296-300
Author(s):  
Phyllis D. Williams ◽  
James P. Karr ◽  
Gerald P. Murphy
Keyword(s):  

1989 ◽  
Vol 7 (6) ◽  
pp. 803-815 ◽  
Author(s):  
R R Love

Since its introduction into clinical use in the early 1970s, the synthetic antiestrogen tamoxifen citrate has been shown to contribute to the control of human breast cancer in increasingly significant ways. While its mechanisms of action and pharmacology are incompletely understood, tamoxifen appears to act predominantly by blocking the action of estrogen by binding to the estrogen receptor. Clinical trials of tamoxifen for 1 to 2 years in primary breast cancer demonstrate consistent beneficial effects on disease-free survival, but only suggested beneficial effects on survival. Routine use of adjuvant tamoxifen for 5 years or more will depend on the results of ongoing large clinical trials of efficacy and detailed studies of unknown biological effects on other tissues.


2020 ◽  
Vol 21 (8) ◽  
Author(s):  
Mohamed Nasr ◽  
Fahima Hashem ◽  
Raghda Abdelmoniem ◽  
Norhan Tantawy ◽  
Mohamed Teiama

Author(s):  
Hayder Hussein Abduljabbar ◽  
Shaimaa Nazar Abd Alhammid

Objective: The aim of the present study was the enhancement in the solubility of tamoxifen citrate using solid dispersion which is considered as a great solution to overcome the poor water solubility behavior of tamoxifen citrate (TMX) by solvent evaporation technique using Soluplus® as a novel carrier then formulate it as an orodispersible tablet.Method: A total of 24 formulas were prepared as a solid dispersion by solvent evaporation method using Soluplus® as a polymeric solubilizer in the ratio of 1:1, 1:3, 1:5, 1:7, and 1:10 then formulated as orodispersible tablets by incorporating three types of superdisintegrants; croscarmellose, crospovidone, and sodium starch glycolate (SSG) with the solid dispersion. Characterization of the formulation was done using differential scanning colorimetry, Fourier transforms infrared spectroscopy, X-ray diffraction, and scanning electron microscope and the best formula was selected according to the disintegration and dissolution tests.Results and Discussion: Formula 22 were selected as the best formula which contains mixed types of superdisintegrants; croscarmellose and SSG with the fastest complete disintegration of 6.5 s and complete dissolution with <2 min.Conclusion: Accordingly, TMX was successfully enhanced its water solubility by converting its crystalline structure into the amorphous state through solid dispersion with Soluplus® and formulated as an orodispersible tablet to improve its oral absorption.


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