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Tamoxifen Citrate Loaded Solid Lipid Nanoparticles- A Novel Approach In The Treatment of ER+ Breast Cancer


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1 Sharadchandra Pawar College of Pharmacy, Otur, Pune-412409, India
     

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Breast cancer is one of the most frequently occurring cancers in women and the second leading cause of cancer deaths in women. Biodegradable SLNs of Tamoxifen citrate (Tmx) can be used for the targeting of anticancer drugs to the organs, thereby achieving major benefits such as reduction in total dose and avoidance of systemic absorption. Solid lipid nanoparticles (SLNs) were prepared by O/W Microemulsion technique and characterized by various parameters such as particle size analysis, scanning electron microscopy, drug entrapment efficiency and in-vitro release studies. In-vitro release studies were performed in phosphate buffer of pH 7.4 along with 0.5% SLS for increasing the solubility of lipophilic drug in PBS using Franz diffusion cell by dialysis method. The kinetics of release was determined and fitted to an empirical equation. The Tmx-loaded tristearine SLNs shown maximum entrapment efficiency compared to the glycerol monostearate SLN. Percentage of tamoxifen citrate released from SLN formulations up to 8 hrs was in the range of 32.3 to 65.5% with Tristearine and 43.2 to 81.4% with Glycerol monostearate (GMS). Tristearine had shown slow release and maximum entrapment than GMS which can be attributed to the hydrophobic long chain fatty acids of the triglyceride that retain lipophilic drugs and also increased accommodation of lipophilic drugs. Thus the above mentioned solid lipid nanoparticles can be a beneficial system to deliver tamoxifen to cancer tissues through enhanced permeability and retention (EPR) effect.

Keywords

Solid lipid Nanoparticles, Tamoxifen Citrate, Microemulsion Technique, Triglycerides.
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  • Tamoxifen Citrate Loaded Solid Lipid Nanoparticles- A Novel Approach In The Treatment of ER+ Breast Cancer

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Authors

Sudarshan Borkar
Sharadchandra Pawar College of Pharmacy, Otur, Pune-412409, India
Shende Vikas
Sharadchandra Pawar College of Pharmacy, Otur, Pune-412409, India
Chatap Viveknand
Sharadchandra Pawar College of Pharmacy, Otur, Pune-412409, India
Sawant Vilas
Sharadchandra Pawar College of Pharmacy, Otur, Pune-412409, India
R. Suresh
Sharadchandra Pawar College of Pharmacy, Otur, Pune-412409, India
Dama Ganesh
Sharadchandra Pawar College of Pharmacy, Otur, Pune-412409, India

Abstract


Breast cancer is one of the most frequently occurring cancers in women and the second leading cause of cancer deaths in women. Biodegradable SLNs of Tamoxifen citrate (Tmx) can be used for the targeting of anticancer drugs to the organs, thereby achieving major benefits such as reduction in total dose and avoidance of systemic absorption. Solid lipid nanoparticles (SLNs) were prepared by O/W Microemulsion technique and characterized by various parameters such as particle size analysis, scanning electron microscopy, drug entrapment efficiency and in-vitro release studies. In-vitro release studies were performed in phosphate buffer of pH 7.4 along with 0.5% SLS for increasing the solubility of lipophilic drug in PBS using Franz diffusion cell by dialysis method. The kinetics of release was determined and fitted to an empirical equation. The Tmx-loaded tristearine SLNs shown maximum entrapment efficiency compared to the glycerol monostearate SLN. Percentage of tamoxifen citrate released from SLN formulations up to 8 hrs was in the range of 32.3 to 65.5% with Tristearine and 43.2 to 81.4% with Glycerol monostearate (GMS). Tristearine had shown slow release and maximum entrapment than GMS which can be attributed to the hydrophobic long chain fatty acids of the triglyceride that retain lipophilic drugs and also increased accommodation of lipophilic drugs. Thus the above mentioned solid lipid nanoparticles can be a beneficial system to deliver tamoxifen to cancer tissues through enhanced permeability and retention (EPR) effect.

Keywords


Solid lipid Nanoparticles, Tamoxifen Citrate, Microemulsion Technique, Triglycerides.