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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.
Highlights
One of the greatest difficulties confronted today by the pharmaceutical industries lies in empowering the conveyance of inadequately watersoluble drug
The independent variables concentration of methylcellulose (%), PEG 6000, Croscarmellose Sodium (%) and Spheronization Speed of pellet obtained by using melt extrusion and spheronization technique against dependent variables i.e. Theoretical Yield (%), Mean Pellet Size, Sphericity, Friability (%), Porosity (%), Mechanical Crushing Force(N) and dissolution efficiency (DE) was studied
The present study concluded that PEG 6000 and methylcellulose (MC) can effectively improve the dissolution behavior of tamoxifen citrate
Summary
One of the greatest difficulties confronted today by the pharmaceutical industries lies in empowering the conveyance of inadequately watersoluble drug. Tamoxifen citrate (TMC) is BCS class II drug commercially converted to salt form as citrate to increase so as to increase its aqueous solubility and efficacy. It is in the salt form its solubility in water is limited as it has a higher melting point (146 oC) which inhibits its dissolution [1]. HME technique is presently used in pharmaceutical industries for various applications because of its numerous advantages over traditional methods [2]
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