Nanogel-based natural polymers as smart carriers for the controlled delivery of Timolol Maleate through the cornea for glaucoma

Int J Biol Macromol. 2018 Apr 1:109:955-962. doi: 10.1016/j.ijbiomac.2017.11.090. Epub 2017 Nov 14.

Abstract

Despite frequent scientific efforts, efficient ocular drug delivery is a major challenge for pharmaceutical scientists. Poor bioavailability of ophthalmic solutions can be overcome by using smart ophthalmic drug-delivery systems. In this research, loading and delivery of Timolol Maleate (TM) through the cornea by synthesized nanoparticles based on biopolymers (chitosan-alginate) were studied. The physico-chemical properties of these nanoparticles were characterized using scanning electron microscopy (SEM), transmission electron microscopy (TEM) and dynamic light scattering (DLS). Loading and release were evaluated by a UV-vis spectrometer and the ex vivo permeation study was carried out using the Franz Diffusion Cell and fluorescent microscopy studies. The results indicated that morphology and size of nanoparticles were spherical and in the range of 80-100nm. The loading capacity and encapsulation efficiency were about 42% and 94% respectively. They illustrated a burst release in the first hour followed by a slower and more sustained drug release during the next 24h. Also, the results indicated that the cornea penetration of TM loaded in nanoparticles was twice than that of TM. Hence, this nanocarrier can be considered as a suitable candidate for controlled TM delivery and release through the cornea.

Keywords: Glaucoma; Nanoparticles; Timolol maleate.

MeSH terms

  • Biological Products / chemistry*
  • Cornea / drug effects*
  • Drug Carriers / chemistry*
  • Drug Delivery Systems*
  • Drug Liberation
  • Drug Stability
  • Gels / chemistry*
  • Glaucoma
  • Nanocomposites / chemistry*
  • Nanocomposites / ultrastructure
  • Nanoparticles / chemistry
  • Nanoparticles / ultrastructure
  • Particle Size
  • Permeability
  • Polymers / chemistry*
  • Spectroscopy, Fourier Transform Infrared
  • Timolol / administration & dosage*
  • Timolol / pharmacokinetics
  • Viscosity

Substances

  • Biological Products
  • Drug Carriers
  • Gels
  • Polymers
  • Timolol