DEVELOPMENT OF TAMOXIFEN CITRATE PELLETS BY HOT-MELT EXTRUSION FOR IMMEDIATE RELEASE: STUDY OF EFFECT OF VARIABLES

  • VISHAL YADAV Department of Pharmaceutics, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies (VISTAS), Pallavaram, Chennai 600117, India
  • S. SATHESH KUMAR Department of Pharmaceutics, School of Pharmaceutical Sciences, Vels Institute of Science, Technology and Advanced Studies (VISTAS), Pallavaram, Chennai 600117, India

Abstract

Objective: Objective of the study was to develop tamoxifen citrate immediate release pellets by hot-melt extrusion (HME) and to study the effect of various formulation and process variables.


Methods: Pellets were prepared by HME technique. Effect of various parameters such as the concentration of ethylcellulose, PEG 6000, croscarmellose sodium, and spheronization speed were studied by using Central Composite Design. Pellets were evaluated for theoretical yield (%), mean pellet size (mm), sphericity (pellips), friability (%), porosity (%), mechanical crushing force (n), and dissolution efficiency. Optimized formulation was studied for compatibility study using IR, DSC, and XRD, SEM, In vitro drug release. In vitro Cell Cytotoxicity and Viability Assay were carried out using MCF-7 (human breast cancer cells) by MTT assay.


Results: Results showed that a variable such as the amount of Methyl Cellulose, PEG 6000 and Spheronization speed showed positive correlation and amount of Croscarmellose sodium showed a negative correlation with dependent variables. Optimized formulation showed Korsmeyer Peppas model as a mechanism of drug release. Value of n was found to be in between 0.77+0.04, which reveals that, release mechanism of the drug as non-Fickian transport (0.45<n<0.89). MTT results of MCF-7 cells showed that optimized immediate release pellets have maximum cytotoxicity at 80 µg/ml.


Conclusion: Study concluded that HME method and materials i.e. PEG 6000 and methylcellulose can effectively use to get immediate release of tamoxifen citrate so as to increase dissolution rate and cytotoxic effect.

Keywords: Tamoxifen citrate, Pellets, Hot-melt extrusion, Immediate release, Central composite design

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YADAV, V., & KUMAR, S. S. (2019). DEVELOPMENT OF TAMOXIFEN CITRATE PELLETS BY HOT-MELT EXTRUSION FOR IMMEDIATE RELEASE: STUDY OF EFFECT OF VARIABLES. International Journal of Applied Pharmaceutics, 11(5), 111-124. https://doi.org/10.22159/ijap.2019v11i5.33933
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