Shear-Thinning Viscous Materials for Subconjunctival Injection of Microparticles

AAPS PharmSciTech. 2020 Nov 25;22(1):8. doi: 10.1208/s12249-020-01877-9.

Abstract

While drug-loaded microparticles (MPs) can serve as drug reservoirs for sustained drug release and therapeutic effects, needle clogging by MPs poses a challenge for ocular drug delivery via injection. Two polymers commonly used in ophthalmic procedures-hyaluronic acid (HA) and methylcellulose (MC)-have been tested for their applicability for ocular injections. HA and MC were physically blended with sunitinib malate (SUN)-loaded PLGA MPs for subconjunctival (SCT) injection into rat eyes. The HA and MC viscous solutions facilitated injection through fine-gauged needles due to their shear-thinning properties as shown by rheological characterizations. The diffusion barrier presented by HA and MC reduced burst drug release and extended overall release from MPs. The significant level of MP retention in the conjunctiva tissue post-operation confirmed the minimal leakage of MPs following injection. The safety of HA and MC for ocular applications was demonstrated histologically.

Keywords: hyaluronic acid; methylcellulose; microparticles; ocular drug delivery; shear-thinning materials.

MeSH terms

  • Administration, Ophthalmic
  • Animals
  • Conjunctiva*
  • Delayed-Action Preparations
  • Drug Delivery Systems
  • Microspheres*
  • Polylactic Acid-Polyglycolic Acid Copolymer / administration & dosage
  • Rats
  • Viscosity*

Substances

  • Delayed-Action Preparations
  • Polylactic Acid-Polyglycolic Acid Copolymer