Liposome-Encapsulated Tamoxifen Citrate: A Breakthrough Approach to Enhance Therapeutic Effectiveness

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This study aimed to create a brand-new liposomal tamoxifen citrate formulation with an enhanced therapeutic index. The thin film hydration process was used to create the liposomes, and several formulations with different lipid compositions (lecithin and cholesterol), drug-to-lipid ratios, and amounts of amine-bearing lipids (stearyl amine) were investigated. The hydration temperature and time were also studied to optimize the liposome properties. The size and encapsulation effectiveness of the liposomes were evaluated using optical microscopy, scanning electron microscopy (SEM), Fourier transform infrared absorption (FTIR), and surface morphology analysis. In vitro, drug release parameters were investigated in 0.9% w/v saline medium, and the effect of stearylamine concentration on the release rate of tamoxifen citrate was examined.

The results showed that tamoxifen citrate was encapsulated with lipid and amine-bearing lipid into the liposomes with an entrapment efficiency of 77.54% and 81%, respectively. The stability of the liposomes was assessed for 3 weeks under defined storage conditions, and the release kinetics of the tamoxifen citrate liposomes were studied. In vitro release studies indicated that the maximum drug release was up to 18 hours, demonstrating the potential of this liposomal formulation as a novel, prolonged delivery system with reasonable drug loading and desirable liposome properties. In conclusion, a liposomal tamoxifen citrate formulation with desired attributes was successfully prepared and showed promising results as a novel drug delivery system.