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Background <p>Emtricitabine (FTC) is a popular antiretroviral drug, but its clinical efficacy may be restricted by rapid release of the drug and poor retention in the site of delivery. </p> Objective <p>The objective of the current research was to prepare and test a fatty acid based liposomal nanoformulation of FTC with palmitic acid to obtain sustained and regulated in vitro drug delivery. </p> Method <p>The palmitic acid, soy lecithin, and cholesterol were used to make FTC-loaded liposomes by thin film hydration method, which were then optimized in order to get nanosized and stable vesicles that had ameliorated release properties. </p> Results <p>The mean size of the particle of the optimized palmitic acid-based FTC liposomes was 108.9&#xa0;nm and the size distribution was narrow (PDI = 0.2402), which indicating a relatively narrow size distribution and good homogeneity of the liposomal population. The zeta potential was found to be negative, that is, -17.2 mV, which showed that there was adequate surface charge, which helped in the electrostatic stabilization as well as decreased aggregation of the vesicles. In vitro drug release experimental studies have reported a biphasic and sustained rate of release, where the first release was 23.19% and a long release rate with a cumulative drug release of 86.78% after 72&#xa0;h. This permanence of release was associated with the presence of palmitic acid-enriched hydrophobic lipid bilayer that increases the rigidity of membrane and inhibits the diffusion of the drug. Kinetics of drug release were compared based on zero-order, first-order, Higuchi, and Korsmeyer-Peppas models. The Korsmeyer-Peppas model had the largest correlation coefficient (R<sup>2</sup> = 0.9647 ), meaning that anomalous (non-Fickian) transport is determined by a mixture of lipid matrix relaxation and diffusion. The Higuchi and first-order models showed moderate correlation, indicating that diffusion-controlled and concentration-dependent mechanisms contribute to drug release, while the poor fit of the zero-order model suggests the absence of constant release behavior. </p> Conclusion <p>Altogether, the results indicate that FTC delivered as a palmitic acid-based liposomal nanoformulation offers better physicochemical stability and extended in vitro release of the drug, which might be utilized as a promising nanocarrier system with prolonged drug delivery use.</p> Graphical Abstract <p></p>

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Design, Development and In Vitro Evaluation of a Palmitic Acid–Based Liposomal Nanoformulation of Emtricitabine with Improved Release Kinetics

  • 期刊论文

  • 发表日期：

    2026年6月16日

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  • Ratan Lal Vishwakarma,
  • Shubhrat Maheshwari,
  • Aditya Singh,
  • Amita Verma

摘要

Background

Emtricitabine (FTC) is a popular antiretroviral drug, but its clinical efficacy may be restricted by rapid release of the drug and poor retention in the site of delivery.

Objective

The objective of the current research was to prepare and test a fatty acid based liposomal nanoformulation of FTC with palmitic acid to obtain sustained and regulated in vitro drug delivery.

Method

The palmitic acid, soy lecithin, and cholesterol were used to make FTC-loaded liposomes by thin film hydration method, which were then optimized in order to get nanosized and stable vesicles that had ameliorated release properties.

Results

The mean size of the particle of the optimized palmitic acid-based FTC liposomes was 108.9 nm and the size distribution was narrow (PDI = 0.2402), which indicating a relatively narrow size distribution and good homogeneity of the liposomal population. The zeta potential was found to be negative, that is, -17.2 mV, which showed that there was adequate surface charge, which helped in the electrostatic stabilization as well as decreased aggregation of the vesicles. In vitro drug release experimental studies have reported a biphasic and sustained rate of release, where the first release was 23.19% and a long release rate with a cumulative drug release of 86.78% after 72 h. This permanence of release was associated with the presence of palmitic acid-enriched hydrophobic lipid bilayer that increases the rigidity of membrane and inhibits the diffusion of the drug. Kinetics of drug release were compared based on zero-order, first-order, Higuchi, and Korsmeyer-Peppas models. The Korsmeyer-Peppas model had the largest correlation coefficient (R2 = 0.9647 ), meaning that anomalous (non-Fickian) transport is determined by a mixture of lipid matrix relaxation and diffusion. The Higuchi and first-order models showed moderate correlation, indicating that diffusion-controlled and concentration-dependent mechanisms contribute to drug release, while the poor fit of the zero-order model suggests the absence of constant release behavior.

Conclusion

Altogether, the results indicate that FTC delivered as a palmitic acid-based liposomal nanoformulation offers better physicochemical stability and extended in vitro release of the drug, which might be utilized as a promising nanocarrier system with prolonged drug delivery use.

Graphical Abstract