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Enhanced dermal delivery of acyclovir using solid lipid nanoparticles.

Sanyog Jain1, Meghal A Mistry, Nitin K Swarnakar

  • 1Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, SAS Nagar, Mohali, 160062, Punjab, India, sanyogjain@niper.ac.in.

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Solid lipid nanoparticles (SLNs) effectively delivered the hydrophilic drug acyclovir (ACV) for dermal applications. These ACV-SLNs showed significantly enhanced skin accumulation compared to conventional cream.

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Area of Science:

  • Pharmaceutical Nanotechnology
  • Dermal Drug Delivery
  • Antiviral Therapeutics

Background:

  • Hydrophilic drugs like acyclovir (ACV) pose challenges for effective dermal delivery.
  • Solid lipid nanoparticles (SLNs) offer a promising carrier system for improving drug penetration.
  • Optimizing SLN formulation is crucial for enhancing drug encapsulation and release.

Purpose of the Study:

  • To develop and characterize solid lipid nanoparticles (SLNs) for dermal delivery of acyclovir (ACV).
  • To evaluate the potential of ACV-loaded SLNs (ACV-SLNs) as a carrier for topical herpes simplex infection treatment.
  • To investigate the skin permeation and dermal distribution mechanisms of ACV-SLNs.

Main Methods:

  • ACV-SLNs were prepared using an optimized double emulsion process with Compritol 888 ATO.
  • Physicochemical characterization included particle size, polydispersity index, entrapment efficiency, DSC, and XRD.
  • In vitro skin permeation studies were conducted on human cadaver and rat skin, with confocal microscopy for mechanism analysis.

Main Results:

  • Prepared ACV-SLNs exhibited favorable characteristics: smooth, spherical shape, average diameter of 262 nm, PDI of 0.280, and 40.08% entrapment efficiency.
  • ACV was found in an amorphous state within the SLNs, confirmed by DSC and XRD.
  • ACV-SLNs demonstrated significantly higher dermal accumulation (15.17-17.65 times) compared to acyclovir cream after 24 hours.
  • Confocal microscopy indicated SLN penetration via the pilosebaceous route, with minimal skin irritation observed.

Conclusions:

  • ACV-loaded SLNs are a viable and effective system for enhancing the dermal delivery of acyclovir.
  • The developed SLNs show potential for improved treatment of topical herpes simplex infections.
  • The pilosebaceous route facilitates deep dermal penetration of SLNs, offering a novel delivery strategy.