Topical Versus Systemic Ocular Drug Delivery

  • Lunawati Bennett


The eye is a very complex sensory organ consists of numerous structures function to coordinate sight properly. Several diseases related to eye include: (a) common inflammation and allergic reactions due to bacterial, viral, fungal or chemicals such as cytomegalovirus (CMV) retinitis and allergic rhinitis; (b) inflammatory and autoimmune disease such as scleritis and uveitis; (c) ocular neovascularization such as age-related macular degeneration (AMD), diabetic retinopathy (DR); and (d) retinal vein occlusion that can cause blindness if untreated or treated improperly. For years, ophthalmic formulations have been one of the most important, widely developed and challenging as pharmaceutical companies try to develop innovative drugs. Due to the complicated anatomical structure and a small absorptive surface of the eye, it is difficult to reach the eye compartment properly. Ophthalmologists still face challenges in treating different diseases of the anterior and posterior segments. Systemic, intraocular, and other methods of drug delivery are explained below with major emphasis on topical deliveries.


Topical delivery Systemic delivery Diseases of the eye Intraocular delivery 


  1. Aburahma MH, Mahmoud AA (2011) Biodegradable ocular inserts for sustained delivery of brimonidine tartrate: preparation and in vitro/in vivo evaluation. AAPS Pharm Sci Tech 12(4):1335–1347CrossRefGoogle Scholar
  2. Ako-Adounvo AM, Nagarwal RC, Oliveira L et al (2014) Recent patents on ophthalmic nanoformulations and therapeutic implications. Recent Pat Drug Deliv Formul 8(3):193–201CrossRefGoogle Scholar
  3. Arepalli S, Kaliki S, Shields CL (2015) Choroidal metastases: origin, features, and therapy. Indian J Opthalmology 63:122–127CrossRefGoogle Scholar
  4. Avisar I, Weinberger D, Kremer I (2010) Effect of subconjunctival and intraocular bevacizumab injections on corneal neovascularization in a mouse model. Curr Eye Res 35:108–115CrossRefGoogle Scholar
  5. Baranowski P, Karolewicz B, Gajda M, Pluta J (2014) Ophthalmic drug dosage forms: characterization and research methods. Sci World J doi: 10.1155/2014/861904CrossRefGoogle Scholar
  6. Bell STD, Chu T, He Q, Potter DE (2004) Intraocular delivery compositions and methods. WO2004050065A1Google Scholar
  7. Bernards DA, Bhisitkul RB, Desai T (2014) Zero-order sustained drug delivery to the retina from a nanoporous film device. Drug Deliv 48:20–21Google Scholar
  8. Chauhan A, Gulsen D (2012) Ophthalmic drug delivery system. US8273366Google Scholar
  9. Chaurasia SS, Lim RR, Lakshminarayanan R, Mohan RR (2015) Nanomedicine approaches for cornea diseases. J Funct Biomater 6:277–298CrossRefGoogle Scholar
  10. Chemuturi NV, Yanez JA (2013) The role of xenobiotic transporters in ophthalmic drug delivery. J Pharm Sci 16:683–707Google Scholar
  11. Cholkar K, Patel SP, Vadlapudi AD, Mitra AK (2013) Novel strategies for anterior segment ocular drug delivery. J Ocu Pharm Ther 29(2):106–123CrossRefGoogle Scholar
  12. Donovan S (2004) Intravitreal botulinum toxin implant. US200475871Google Scholar
  13. Gaudana RJ, Jwala J, Boddu SHS, Mitra AK (2009) A Recent perspective in ocular drug delivery. Pharm Res 26(5):1197–1216CrossRefGoogle Scholar
  14. Gaudana RJ, Gokulgandhi MR, Boddu SHS, Mitra AK (2012) Recent overview of ocular patents. Recent Pat Drug Deliv Formul 6(2):95–106CrossRefGoogle Scholar
  15. Gong X, Peng S, Wen W et al (2009) Design and fabrication of magnetically functionalized core/shellmicrospheres for smart drug delivery. Adv Funct Mater 19:292–297CrossRefGoogle Scholar
  16. Hofland H, Bongianni J, Wheeler T (2004) Ophthalmic liposome compositions and uses thereof. US20040224010Google Scholar
  17. Jarvinen T, Jarvinen K (1996) Prodrugs for improved ocular drug delivery. Adv Drug Del Rev 19(2):203–224CrossRefGoogle Scholar
  18. Jiang J, Moore JS, Edelhauser HF, Prausnitz MR (2009) Intrascleral drug delivery to the eye using hollow microneedles. Pharm Res 26:395–403CrossRefGoogle Scholar
  19. Jin J, Zhou KK, Oark K et al (2011) Anti-inflammatory and anti-angiogenic effects of nanoparticles mediated delivery of a natural angiogenic inhibitor. Invest Opthalmol Vis Sci 52:6230–6237CrossRefGoogle Scholar
  20. Kaur IP, Kakkar S (2014) Nanotherapy for posterior eye diseases. J Control Rel 193:100–112CrossRefGoogle Scholar
  21. Kim YC, Chiang B, Wu X, Prausnitz MR (2014) Ocular delivery of macromolecules. J Controlled Release 190:172–181CrossRefGoogle Scholar
  22. Kompella UB, Amrite AC, Ravi RP, Durazo SA (2013) Nanomedicines for back of the eye drug delivery, gene delivery, and imaging. Prog Retin Eye Res 36:172–198CrossRefGoogle Scholar
  23. Lallemand F, Daull P, Benita S et al (2012) Successfully improving ocular drug delivery using the cationic nanoemulsion. Novasorb J Drug Deliv 604204Google Scholar
  24. Lo R, Li PY, Saati S et al (2009) A passive MEMS drug delivery pump for treatment of ocular diseases. Biomed Microdevices 11:959–970CrossRefGoogle Scholar
  25. Malik AS, Chaudhary S, Garg G, Tomar A (2012) Dendrimers: a tool for drug delivery. Adv Biological Res 6(4):165–169Google Scholar
  26. Martin DF, Maguire MG, Fine GS et al (2012) Ranibizumab and bevacizumab for treatment of neovascular age-related macular degeneration: two-year results. Opthalmology 119:1388–1398CrossRefGoogle Scholar
  27. Molokhia SA, Sant H, Simonis J et al (2010) The capsule drug device: novel approach for drug delivery to the eye. Vis Res 50:680–685CrossRefGoogle Scholar
  28. Morrison PWJ, Khutoryanskiy VV (2014) Advances in ophthalmic drug delivery. Ther Deliv 5(12):1297–1315CrossRefGoogle Scholar
  29. Nisha S, Deepak K (2012) An insight to ophthalmic drug delivery system. Inter J Pharma Studies Res 3(2):9–13Google Scholar
  30. Patel SR, Lin AS, Edelhauser HF, Prausnitz MR (2011) Suprachoroidal drug delivery to the back of the eye using hollow microneedles. Pharm Res 28:166–176CrossRefGoogle Scholar
  31. Rajasekaran A, Kumaran KSGA, Preetha JP, Karthika K (2010) A comparative review on conventional and advanced ocular drug delivery formulations. Int J Pharm Tech Res 2(1):668–674Google Scholar
  32. Rathore KS, Nema RK (2009) An insight into ophthalmic drug delivery system. Int J Pharm Sci Drug Res 1(1):1–5Google Scholar
  33. Silva NP, Menacho FP, Chorilli M (2012) Dendrimers as potential platform in nanotechnology-based drug delivery systems. IOSR J Pharm 2(5):23–30Google Scholar
  34. Souza JG, Dias K, Pereira TA et al (2013) Topical delivery of ocular therapeutics: carrier systems and physical methods. J Pharm Pharmacol 66:507–530CrossRefGoogle Scholar
  35. Storobinsky DO, Lubin BC, Hasanreisoglu M, Goldenberg-Cohen N (2009) Effect of subconjunctival and intraocular bevacizumab injection on angiogenic gene expression levels in mouse model of corneal neovascularization. Mol Vis 15:2326–2338Google Scholar
  36. Tangri P, Khurana S (2011) Basics of ocular drug delivery system. Int J Res Pharm Biomed Sci 2(4):1541–1552Google Scholar
  37. Velagaleti PR, Anglade E, Khan IJ et al (2010) Topical delivery of hydrophobic drugs using a novel mixed nanomicelles technology to treat diseases of the anterior and posterior segments of the eye. Drug Deliv Technol 10(4):42–47Google Scholar
  38. Yasin MN, Svirskis D, Seyfoddin A, Rupenthal ID (2014) Implants for drug delivery to the posterior segment of the eye: A focus on stimuli-responsive and tunable release systems. J Controlled Release 196:208–221CrossRefGoogle Scholar
  39. Yavuz B, Pehlivan SB, Unlu N (2013) Dendrimeric system and their applications in ocular drug delivery. Sci World J. doi: 10.1155/2013/732340CrossRefGoogle Scholar

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© Springer International Publishing AG 2016

Open Access This chapter is distributed under the terms of the Creative Commons Attribution Noncommercial License, which permits any noncommercial use, distribution, and reproduction in any medium, provided the original author(s) and source are credited.

Authors and Affiliations

  1. 1.School of PharmacyUnion UniversityJacksonUSA

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