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Open AccessArticle

Hollow Microcapsules as Periocular Drug Depot for Sustained Release of Anti-VEGF Protein

1
NTU-Northwestern Institute for Nanomedicine (NNIN), School of Materials Science and Engineering, Nanyang Technological University (NTU), 50, Nanyang Avenue, Singapore 639798, Singapore
2
Tan Tock Seng Hospital, Novena, Singapore 308433, Singapore
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2019, 11(7), 330; https://doi.org/10.3390/pharmaceutics11070330
Received: 6 June 2019 / Revised: 3 July 2019 / Accepted: 6 July 2019 / Published: 11 July 2019
(This article belongs to the Special Issue Nanotechnology-Based Approaches for Chronic Diseases)
Diseases affecting the posterior segment of the eye such as age-related macular degeneration and diabetic retinopathy are leading causes of blindness all over the world. The current treatment regimen for such diseases involves repeated intravitreal injections of anti- Vascular Endothelial Growth Factor (VEGF) proteins. This method is highly invasive and can lead to severe complications. In an attempt to develop less invasive alternatives, we propose the use of a controlled release system consisting of anti-VEGF loaded hollow microcapsules that can be administered periocularly to form drug eluting depots on the episcleral surface. The microcapsules with either positive or negative surface charge were prepared by a layer by layer approach and showed pH responsive permeability switching. An ex vivo experiment using porcine sclera indicated positively charged microcapsules remained on the episcleral surface over four days while the negatively charged microcapsules were washed away. These positively charged microcapsules were then loaded with anti-VEGF protein ranibizumab using pH dependent permeability switching and protein release from the microcapsules were studied using an in vitro setup. An ex vivo experiment utilizing porcine sclera demonstrated sustained release of ranibizumab over seven days with zero-order kinetics. View Full-Text
Keywords: protein delivery; controlled release; anti-VEGF; microparticles; drug delivery; layer by layer microcapsules; age related macular degeneration; back of the eye protein delivery; controlled release; anti-VEGF; microparticles; drug delivery; layer by layer microcapsules; age related macular degeneration; back of the eye
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MDPI and ACS Style

Radhakrishnan, K.; Vincent, A.; Joseph, R.R.; Moreno, M.; Dickescheid, A.; Agrawal, R.; Venkatraman, S. Hollow Microcapsules as Periocular Drug Depot for Sustained Release of Anti-VEGF Protein. Pharmaceutics 2019, 11, 330.

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