Development of Acyclovir-Loaded Albumin Nanoparticles and Improvement of Acyclovir Permeation Across Human Corneal Epithelial T Cells

J Ocul Pharmacol Ther. 2017 Dec;33(10):743-752. doi: 10.1089/jop.2017.0057. Epub 2017 Nov 7.

Abstract

Purpose: The aim of the present study was to develop acyclovir (ACV) ocular drug delivery systems of bovine serum albumin (BSA) nanoparticles as well as to assess their in vitro transcorneal permeation across human corneal epithelial (HCE-T) cell multilayers.

Methods: The ACV-loaded BSA nanoparticles were prepared by desolvation method along with physicochemical characterization, cytotoxicity, as well as in vitro transcorneal permeation studies across HCE-T cell multilayers.

Results: The nanoparticles appeared to be spherical in shape and nearly uniform in size of about 200 nm. The size of nanoparticles became smaller with decreasing BSA concentration, while the ratios of water to ethanol seemed not to affect the size. Increasing the amount of ethanol in desolvation process led to significant reduction of drug entrapment of nanoparticles with smaller size and more uniformity. The ACV-loaded BSA nanoparticles prepared were shown to have no cytotoxic effect on HCE-T cells used in permeation studies. The in vitro transcorneal permeation results revealed that ACV could permeate through the HCE-T cell multilayers significantly higher from BSA nanoparticles than from aqueous ACV solutions.

Conclusion: The ACV-loaded BSA nanoparticles could be prepared by desolvation method without glutaraldehyde in the formulation. ACV could increasingly permeate through the multilayers of HCE-T cells from the ACV-loaded BSA nanoparticles. Therefore, the ACV-loaded BSA nanoparticles could be a highly potential ocular drug delivery system.

Keywords: acyclovir; bovine serum albumin; nanoparticles; ocular drug delivery; transcorneal permeability.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acyclovir / administration & dosage
  • Acyclovir / pharmacokinetics*
  • Animals
  • Antiviral Agents / administration & dosage
  • Antiviral Agents / pharmacokinetics*
  • Drug Delivery Systems*
  • Epithelium, Corneal / metabolism*
  • Humans
  • Nanoparticles / chemistry*
  • Particle Size
  • Serum Albumin, Bovine / chemistry*
  • Solubility

Substances

  • Antiviral Agents
  • Serum Albumin, Bovine
  • Acyclovir