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Abstract <p>Although numerous, effective antiviral therapies are in clinical use, there is a significant demand for novel, improved drug delivery systems (DDS) to enhance the biological and pharmacokinetic properties of administered drugs. Nanostructured carrier systems are increasingly recognized as promising candidates; however, their development is still in its infancy. Herein, we have developed a biocompatible system composed of polylactide and chitosan, loaded with tenofovir alafenamide (TAF) as an antiretroviral drug. Our nanoparticles (NPs) were able to release TAF for 21&#xa0;days, depending on the chitosan content in their matrix. Moreover, the NPs were not cytotoxic and showed high antiviral activity in an <i>in vitro</i> HIV infection assay. Most importantly, the effectiveness of the selected nanoformulations was comparable to that of free TAF (IC<sub>50</sub> of 56&#xa0;nM <i>versus</i> 62–75&#xa0;nM for NPs), indicating that TAF encapsulation preserved its antiviral effect. The results of this study demonstrate the potential of TAF-loaded NPs and provide a straightforward, effective, and biocompatible strategy for the delivery of anti-HIV drugs.</p> Graphical Abstract <p></p>

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Development of Biocompatible Nanocarriers for Antiretrovirals Based on Polylactide and Chitosan

  • 期刊论文

  • 发表日期：

    2026年3月10日

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  • Vedha Hari B. Narayanan,
  • Artur Lewandowski,
  • Ramya Devi Durai,
  • Paweł Wawrzyniak,
  • Samson Folami,
  • Lisa Weber,
  • Hannah Sabeth Schwarzer-Sperber,
  • Marek Brzeziński,
  • Roland Schwarzer

摘要

Abstract

Although numerous, effective antiviral therapies are in clinical use, there is a significant demand for novel, improved drug delivery systems (DDS) to enhance the biological and pharmacokinetic properties of administered drugs. Nanostructured carrier systems are increasingly recognized as promising candidates; however, their development is still in its infancy. Herein, we have developed a biocompatible system composed of polylactide and chitosan, loaded with tenofovir alafenamide (TAF) as an antiretroviral drug. Our nanoparticles (NPs) were able to release TAF for 21 days, depending on the chitosan content in their matrix. Moreover, the NPs were not cytotoxic and showed high antiviral activity in an in vitro HIV infection assay. Most importantly, the effectiveness of the selected nanoformulations was comparable to that of free TAF (IC50 of 56 nM versus 62–75 nM for NPs), indicating that TAF encapsulation preserved its antiviral effect. The results of this study demonstrate the potential of TAF-loaded NPs and provide a straightforward, effective, and biocompatible strategy for the delivery of anti-HIV drugs.

Graphical Abstract