A more efficient ocular delivery system of triamcinolone acetonide as eye drop to the posterior segment of the eye

Drug Deliv. 2019 Dec;26(1):188-198. doi: 10.1080/10717544.2019.1571122.

Abstract

As a leading cause of vision impairment of the retina, macular edema (ME) has one of the highest clinical demands for treatment. Current treatment of ME relies heavily on invasive techniques resulting in complications and poor patient compliance. To enhance the efficiency of triamcinolone acetonide as eye drop to the posterior segment of the eye, we developed and characterized a novel formulation, namely, triamcinolone acetonide chitosan-coated liposomes (TA-CHL), prepared by the calcium acetate gradient method with some modifications. TA-CHL provided the mean particle size of 135.46 ± 4.49 nm and high entrapment efficiency (90.66 ± 3.21%), exhibited a sustained release profile, excellent physical stability, and no significant toxicity on cornea, conjunctiva, and retina. Optical coherence tomography system (OCT) was used to detect pharmacokinetics of CHL in vivo, indicating that CHL had good potency for drug delivery. Cellular uptake experiments showed CHL had the higher transduction efficiency into HCEC and ARPE-19 than liposomes. TA-CHL was shown to be potentially effective eye drop to contribute to the posterior segment of the eye.

Keywords: Chitosan; liposome; posterior segment; topical administration; triamcinolone acetonide.

MeSH terms

  • Administration, Ophthalmic*
  • Animals
  • Anti-Inflammatory Agents / administration & dosage*
  • Anti-Inflammatory Agents / metabolism
  • Cells, Cultured
  • Drug Delivery Systems / methods*
  • Mice
  • Mice, Inbred C57BL
  • Ophthalmic Solutions / administration & dosage*
  • Ophthalmic Solutions / metabolism
  • Random Allocation
  • Retinal Pigment Epithelium / drug effects*
  • Retinal Pigment Epithelium / metabolism
  • Triamcinolone Acetonide / administration & dosage*
  • Triamcinolone Acetonide / metabolism

Substances

  • Anti-Inflammatory Agents
  • Ophthalmic Solutions
  • Triamcinolone Acetonide

Grants and funding

This study was partly supported by National Natural Science Foundation of China (31570789), and Fundamental Research Funds of Shandong University (2017JC034). The funder had no role in study design, data collection, and analysis, decision to publish, or preparation of the manuscript.