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<p>Background: Liposomal drug delivery systems offer a promising strategy to enhance the therapeutic potential of antiretroviral agents by improving drug encapsulation, stability, and controlled release. This study aimed to develop and optimize emtricitabine (FTC)-loaded liposomes using a systematic Quality by Design approach. Methods: Liposomes were prepared via the thin-film hydration method, with cholesterol and soya lecithin as lipid components. A Box–Behnken Design was employed to study the influence of formulation variables on entrapment efficiency. The optimized formulation was characterized by dynamic light scattering, zeta potential, Fourier-transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). <i>In-vitro</i> drug release and short-term stability studies were also conducted. Results: Among the 12 experimental formulations, formulation F8 exhibited optimal characteristics, including high entrapment efficiency (~ 83%), narrow polydispersity index (PDI &lt; 0.3)&#xa0;with submicron particle size (475.7 nm), and a stable zeta potential (−19.2&#xa0;mV). TEM analysis confirmed spherical, well-dispersed particles, while FTIR and DSC analyses verified successful drug encapsulation without significant chemical interaction. XRD analysis showed reduced crystallinity of FTC in the liposomal matrix, supporting effective drug loading. In vitro drug release exhibited a biphasic pattern with sustained release up to 24&#xa0;h. Stability studies over 30&#xa0;days at 4 and 25&#xa0;°C confirmed the physical integrity of the formulation. Conclusion: The optimized FTC-loaded liposomes demonstrated favorable physicochemical characteristics, controlled release behavior, and short-term stability. These findings highlight the potential of liposomal carriers in improving the pharmacokinetic profile of emtricitabine, thereby offering a promising approach for enhanced antiretroviral therapy.</p>

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Development, Optimization, and Characterization of Emtricitabine-Loaded Liposomes Using Box–Behnken Design for Enhanced Drug Delivery

  • 期刊论文

  • 发表日期：

    2025年9月9日

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  • Shubhrat Maheshwari,
  • Aditya Singh,
  • Habibullah Khalilullah,
  • Amita Verma

摘要

Background: Liposomal drug delivery systems offer a promising strategy to enhance the therapeutic potential of antiretroviral agents by improving drug encapsulation, stability, and controlled release. This study aimed to develop and optimize emtricitabine (FTC)-loaded liposomes using a systematic Quality by Design approach. Methods: Liposomes were prepared via the thin-film hydration method, with cholesterol and soya lecithin as lipid components. A Box–Behnken Design was employed to study the influence of formulation variables on entrapment efficiency. The optimized formulation was characterized by dynamic light scattering, zeta potential, Fourier-transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). In-vitro drug release and short-term stability studies were also conducted. Results: Among the 12 experimental formulations, formulation F8 exhibited optimal characteristics, including high entrapment efficiency (~ 83%), narrow polydispersity index (PDI < 0.3) with submicron particle size (475.7 nm), and a stable zeta potential (−19.2 mV). TEM analysis confirmed spherical, well-dispersed particles, while FTIR and DSC analyses verified successful drug encapsulation without significant chemical interaction. XRD analysis showed reduced crystallinity of FTC in the liposomal matrix, supporting effective drug loading. In vitro drug release exhibited a biphasic pattern with sustained release up to 24 h. Stability studies over 30 days at 4 and 25 °C confirmed the physical integrity of the formulation. Conclusion: The optimized FTC-loaded liposomes demonstrated favorable physicochemical characteristics, controlled release behavior, and short-term stability. These findings highlight the potential of liposomal carriers in improving the pharmacokinetic profile of emtricitabine, thereby offering a promising approach for enhanced antiretroviral therapy.