Recent advances in ocular drug delivery

Drug Dev Ind Pharm. 2013 Nov;39(11):1599-617. doi: 10.3109/03639045.2012.736515. Epub 2012 Nov 16.


Amongst the various routes of drug delivery, the field of ocular drug delivery is one of the most interesting and challenging endeavors facing the pharmaceutical scientist. Recent research has focused on the characteristic advantages and limitations of the various drug delivery systems, and further research will be required before the ideal system can be developed. Administration of drugs to the ocular region with conventional delivery systems leads to short contact time of the formulations on the epithelium and fast elimination of drugs. This transient residence time involves poor bioavailability of drugs which can be explained by the tear production, non-productive absorption and impermeability of corneal epithelium. Anatomy of the eye is shortly presented and is connected with ophthalmic delivery and bioavailability of drugs. In the present update on ocular dosage forms, chemical delivery systems such as prodrugs, the use of cyclodextrins to increase solubility of various drugs, the concept of penetration enhancers and other ocular drug delivery systems such as polymeric gels, bioadhesive hydrogels, in-situ forming gels with temperature-, pH-, or osmotically induced gelation, combination of polymers and colloidal systems such as liposomes, niosomes, cubosomes, microemulsions, nanoemulsions and nanoparticles are discussed. Novel ophthalmic delivery systems propose the use of many excipients to increase the viscosity or the bioadhesion of the product. New formulations like gels or colloidal systems have been tested with numerous active substances by in vitro and in vivo studies. Sustained drug release and increase in drug bioavailability have been obtained, offering the promise of innovation in drug delivery systems for ocular administration. Combining different properties of pharmaceutical formulations appears to offer a genuine synergy in bioavailability and sustained release. Promising results are obtained with colloidal systems which present very comfortable conditions of use and prolonged action.

Publication types

  • Review

MeSH terms

  • Adhesiveness
  • Administration, Ophthalmic
  • Animals
  • Biological Availability
  • Chemical Phenomena
  • Cyclodextrins / adverse effects
  • Cyclodextrins / chemistry
  • Delayed-Action Preparations / administration & dosage
  • Delayed-Action Preparations / adverse effects
  • Delayed-Action Preparations / pharmacokinetics
  • Delayed-Action Preparations / therapeutic use
  • Drug Compounding / methods
  • Drug Compounding / trends
  • Drug Delivery Systems* / adverse effects
  • Drug Delivery Systems* / trends
  • Excipients / adverse effects
  • Excipients / chemistry
  • Eye / anatomy & histology
  • Eye / drug effects
  • Eye / metabolism*
  • Eye / physiopathology
  • Eye Diseases / drug therapy*
  • Eye Diseases / metabolism
  • Eye Diseases / physiopathology
  • Humans
  • Ocular Physiological Phenomena / drug effects
  • Prescription Drugs / administration & dosage*
  • Prescription Drugs / adverse effects
  • Prescription Drugs / pharmacokinetics
  • Prescription Drugs / therapeutic use
  • Prodrugs / administration & dosage
  • Prodrugs / adverse effects
  • Prodrugs / pharmacokinetics
  • Prodrugs / therapeutic use
  • Solubility
  • Viscosity


  • Cyclodextrins
  • Delayed-Action Preparations
  • Excipients
  • Prescription Drugs
  • Prodrugs