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Purpose <p>The aim of the present study was to develop nanoparticles of acyclovir using chitosan as a natural polysaccharide for improving its poor oral bioavailability, dosing frequency and to reduce side effects and to assess the pharmacokinetic profile using PK-Sim software.</p> Methods <p>The ionic gelation method was used to synthesize acyclovir loaded chitosan nanoparticles using STPP (sodium tripolyphosphate) as crosslinking agent. For formulations (F1-F9), a constant ratio of polymer (chitosan) and crosslinking agent (STPP) was maintained. The prepared formulations were characterized by determining particle size using DLS, surface morphology using SEM, percentage of yield, entrapment efficiency, drug- excipient compatibility by Fourier transform infrared Spectroscopy(FT-IR), in-vitro release study and in-silico study using PK- Sim software.</p> Results <p>The particle size of prepared nanoparticles were reported to be within 100&#xa0;nm with a moderate polydispersity index. The SEM study indicated oval shape with microscopic pores. Higher encapsulation efficiency (⁓98%) demonstrated the potential of chitosan as a drug carrier. FT-IR study has confirmed the compatibility between acyclovir and other excipients. The prepared F3 formulation showed 23.8% drug release over 3&#xa0;h indicating a slow release of acyclovir that may reduce dosing frequency and improve patient compliance. The drug release was found to follow Korsemeyer-Peppas kinetics with diffusion-controlled release of acyclovir. Additionally, in-silico study predicted improved plasma profile compared to the conventional oral dosage form.</p> Conclusion <p>The study findings suggested F3 as the optimized formulation with controlled release ability of incorporated drug, acyclovir and potential of reducing dosing frequency while minimizing side effects.</p> Graphical Abstract <p></p>

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Fabrication and Characterization of Polymeric Nanoparticles for Efficient and Sustained delivery of Acyclovir for Antiviral Therapy and In-silico Study Using PK-Sim Software

  • 期刊论文

  • 发表日期：

    2026年3月10日

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  • Sudipta Das,
  • Arnab Samanta,
  • Sourish Sarkar,
  • Baishali Ghosh,
  • Sawan Das,
  • Rimi Dey,
  • Sreejan Manna,
  • Trishna Das

摘要

Purpose

The aim of the present study was to develop nanoparticles of acyclovir using chitosan as a natural polysaccharide for improving its poor oral bioavailability, dosing frequency and to reduce side effects and to assess the pharmacokinetic profile using PK-Sim software.

Methods

The ionic gelation method was used to synthesize acyclovir loaded chitosan nanoparticles using STPP (sodium tripolyphosphate) as crosslinking agent. For formulations (F1-F9), a constant ratio of polymer (chitosan) and crosslinking agent (STPP) was maintained. The prepared formulations were characterized by determining particle size using DLS, surface morphology using SEM, percentage of yield, entrapment efficiency, drug- excipient compatibility by Fourier transform infrared Spectroscopy(FT-IR), in-vitro release study and in-silico study using PK- Sim software.

Results

The particle size of prepared nanoparticles were reported to be within 100 nm with a moderate polydispersity index. The SEM study indicated oval shape with microscopic pores. Higher encapsulation efficiency (⁓98%) demonstrated the potential of chitosan as a drug carrier. FT-IR study has confirmed the compatibility between acyclovir and other excipients. The prepared F3 formulation showed 23.8% drug release over 3 h indicating a slow release of acyclovir that may reduce dosing frequency and improve patient compliance. The drug release was found to follow Korsemeyer-Peppas kinetics with diffusion-controlled release of acyclovir. Additionally, in-silico study predicted improved plasma profile compared to the conventional oral dosage form.

Conclusion

The study findings suggested F3 as the optimized formulation with controlled release ability of incorporated drug, acyclovir and potential of reducing dosing frequency while minimizing side effects.

Graphical Abstract