Polymeric micelles for ocular drug delivery: From structural frameworks to recent preclinical studies

J Control Release. 2017 Feb 28:248:96-116. doi: 10.1016/j.jconrel.2017.01.012. Epub 2017 Jan 11.

Abstract

Effective intraocular drug delivery poses a major challenge due to the presence of various elimination mechanisms and physiological barriers that result in low ocular bioavailability after topical application. Over the past decades, polymeric micelles have emerged as one of the most promising drug delivery platforms for the management of ocular diseases affecting the anterior (dry eye syndrome) and posterior (age-related macular degeneration, diabetic retinopathy and glaucoma) segments of the eye. Promising preclinical efficacy results from both in-vitro and in-vivo animal studies have led to their steady progression through clinical trials. The mucoadhesive nature of these polymeric micelles results in enhanced contact with the ocular surface while their small size allows better tissue penetration. Most importantly, being highly water soluble, these polymeric micelles generate clear aqueous solutions which allows easy application in the form of eye drops without any vision interference. Enhanced stability, larger cargo capacity, non-toxicity, ease of surface modification and controlled drug release are additional advantages with polymeric micelles. Finally, simple and cost effective fabrication techniques render their industrial acceptance relatively high. This review summarizes structural frameworks, methods of preparation, physicochemical properties, patented inventions and recent advances of these micelles as effective carriers for ocular drug delivery highlighting their performance in preclinical studies.

Keywords: Bioavailability; Drug delivery; Dry eye syndrome; Ocular barriers; Ocular drug delivery; Polymeric micelles.

Publication types

  • Review
  • Research Support, N.I.H., Extramural

MeSH terms

  • Administration, Ophthalmic
  • Animals
  • Biological Availability
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemistry*
  • Drug Delivery Systems / methods
  • Dry Eye Syndromes / drug therapy
  • Eye / metabolism
  • Eye Diseases / drug therapy
  • Humans
  • Micelles*
  • Ophthalmic Solutions / administration & dosage
  • Ophthalmic Solutions / chemistry
  • Pharmaceutical Preparations / administration & dosage*
  • Pharmaceutical Preparations / chemistry
  • Polymers / administration & dosage
  • Polymers / chemistry*
  • Solubility

Substances

  • Drug Carriers
  • Micelles
  • Ophthalmic Solutions
  • Pharmaceutical Preparations
  • Polymers