PLGA nanoparticles in the ocular drug delivery

PLGA nanoparticles in the ocular drug delivery

The topical ocular administration of drugs has two different purposes: to treat superficial eye diseases, such as infections (e.g. conjunctivitis, blepharitis, keratitis sicca) and to provide intraocular treatment through the cornea for diseases such as glaucoma or uveitis.Compared with drug delivery to other parts of the body, ocular drug delivery has met with significant challenges posed by various ocular barriers. Ocular drug delivery efficiency depends on the barriers and the clearance from the choroidal, conjunctival vessels and lymphatic. Traditional drug administration reduces the clinical efficacy especially for poor water soluble molecules and for the posterior segment of the eye. They typically provide low bioavailability (less than 5%) owing to poor pre-corneal retention and penetration. The factors affecting pre-corneal retention include rapid tear turnover, blinking, and solution drainage, which result in the loss of drug after topical administration. Therefore, frequent instillations of eye drops are required to maintain a therapeutic drug level on the pre-corneal surface. Frequent use of concentrated eye drops can induce toxicity, corneal dryness and possible severe systemic side effects[1, 2].

In different studies has been evaluatedthe suitability and feasibility of PLGA nanoparticles (~200 nm) as suitable for ophthalmic administration such as the ocular delivery of Flurbiprofen, Moxifloxacin, Aceclofenac, loteprednol etabonate,Bevacizumab, Tacrolimus,Dexamethasone acetate, Sparfloxacin[3-13].

plga eye


Proprierties of PLGA NPs for ocular delivery:

  • Nanoparticles (NPs) with size range from 10nm to 1000nm improved topical passage of large, poorly water-soluble molecules through the barriers of ocular system[14].
  • Surface modifications of PLGA nanoparticles was done to increase the PLGA nanoparticles propierties for ocular drug delivery. Chitosan-coated PLGA NPs improve the mucoadhesion ability and the drug release properties. Chitosan adheres to mucus layers in vivo, via electrostatic interactions between the positively charged amino groups within chitosan, and the negatively charged sialic groups of mucin [9, 15].PEG-coated PLGA nanoparticles was found to be significantly greater for bioadhesion, bioretention, and susteined/prolonged pharmacologic effect in the rat’s eyes[16].
  • Positive and negatively charged NPs were shown to distribute to the inner ocular tissues such as retina and vitreous humor following application of iontophoresis technique. Positively charged NPs have shown higher penetration than negatively charged NPs [17]. For topical administration, positively charged polymeric materials on the other hand, may allow more prolonged retention on the eye surface. Following intravitreal injection, anionic NPs were shown to distribute to the subretinal space [18].




  1. Gaudana, R., et al., Ocular Drug Delivery. The AAPS Journal, 2010. 12(3): p. 348-360.
  2. Ameeduzzafar, et al., Colloidal drug delivery system: amplify the ocular delivery. Drug delivery, 2016. 23(3): p. 700-716.
  3. Vega, E., et al., PLGA nanospheres for the ocular delivery of flurbiprofen: drug release and interactions. J Pharm Sci, 2008. 97(12): p. 5306-17.
  4. Mudgil, M. and P.K. Pawar, Preparation and In Vitro/Ex Vivo Evaluation of Moxifloxacin-Loaded PLGA Nanosuspensions for Ophthalmic Application. Sci Pharm, 2013. 81(2): p. 591-606.
  5. Canadas, C., et al., In vitro, ex vivo and in vivo characterization of PLGA nanoparticles loading pranoprofen for ocular administration. Int J Pharm, 2016. 511(2): p. 719-27.
  6. Salama, H.A., et al., PLGA Nanoparticles as Subconjunctival Injection for Management of Glaucoma. AAPS PharmSciTech, 2017.
  7. Katara, R., S. Sachdeva, and D.K. Majumdar, Enhancement of ocular efficacy of aceclofenac using biodegradable PLGA nanoparticles: formulation and characterization. Drug Deliv Transl Res, 2017.
  8. Sah, A.K., P.K. Suresh, and V.K. Verma, PLGA nanoparticles for ocular delivery of loteprednol etabonate: a corneal penetration study. Artif Cells Nanomed Biotechnol, 2017. 45(6): p. 1-9.
  9. Pandit, J., Y. Sultana, and M. Aqil, Chitosan-coated PLGA nanoparticles of bevacizumab as novel drug delivery to target retina: optimization, characterization, and in vitro toxicity evaluation. Artif Cells Nanomed Biotechnol, 2017. 45(7): p. 1397-1407.
  10. Varshochian, R., et al., Albuminated PLGA nanoparticles containing bevacizumab intended for ocular neovascularization treatment. J Biomed Mater Res A, 2015. 103(10): p. 3148-56.
  11. Kalam, M.A. and A. Alshamsan, Poly (d, l-lactide-co-glycolide) nanoparticles for sustained release of tacrolimus in rabbit eyes. Biomed Pharmacother, 2017. 94: p. 402-411.
  12. Gao, Y., et al., PLGA-PEG-PLGA hydrogel for ocular drug delivery of dexamethasone acetate. Drug Dev Ind Pharm, 2010. 36(10): p. 1131-8.
  13. Gupta, H., et al., Sparfloxacin-loaded PLGA nanoparticles for sustained ocular drug delivery. Nanomedicine, 2010. 6(2): p. 324-33.
  14. Diebold, Y. and M. Calonge, Applications of nanoparticles in ophthalmology. Progress in retinal and eye research, 2010. 29(6): p. 596-609.
  15. Salama, A.H., A.A. Mahmoud, and R. Kamel, A Novel Method for Preparing Surface-Modified Fluocinolone Acetonide Loaded PLGA Nanoparticles for Ocular Use: In Vitro and In Vivo Evaluations. AAPS PharmSciTech, 2016. 17(5): p. 1159-72.
  16. Pan, C.K., et al., Comparison of long-acting bevacizumab formulations in the treatment of choroidal neovascularization in a rat model. Journal of ocular pharmacology and therapeutics, 2011. 27(3): p. 219-224.
  17. Valls, R., et al., Transcorneal permeation in a corneal device of non-steroidal anti-inflammatory drugs in drug delivery systems. Open Med Chem J, 2008. 2: p. 66-71.
  18. Kim, H., S.B. Robinson, and K.G. Csaky, Investigating the movement of intravitreal human serum albumin nanoparticles in the vitreous and retina. Pharmaceutical research, 2009. 26(2): p. 329-337.