Nanodelivery of Resveratrol-Loaded PLGA Nanoparticles for Age-Related Macular Degeneration

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Research Article Theme: Formulation and Delivery of Natural Products Guest Editors: Harsh Chauhan, Abhijit Date and Sonali Dhindwal

Nanodelivery of Resveratrol-Loaded PLGA Nanoparticles for Age-Related Macular Degeneration Priyanka Bhatt,1 Gulimirerouzi Fnu,1 Deepak Bhatia,2 Amna Shahid,1 and Vijaykumar Sutariya1,3

Received 2 June 2020; accepted 29 September 2020 Abstract.

Age-related macular degeneration, precisely neovascular form, is the leading cause of vision loss and the key treatment includes intravitreal injections of anti-vascular endothelial growth factor (anti-VEGF) agents. A method to increase local concentration of drug at posterior segment of the eye and to reduce the frequency of intravitreal injections is an unmet need. Resveratrol, a naturally occurring antioxidant and anti-inflammatory polyphenol, was loaded in PLGA polymeric nanoparticles to study their sustained release property and effectiveness in reducing expression of VEGF protein in vitro. Nanoparticles were characterized using FTIR, DSC, size, encapsulation efficiency, TEM, and in vitro drug release studies. Using MTT assay, the cytotoxicity of formulation was evaluated on ARPE-19 cells. The cellular uptake and VEGF expression levels were also evaluated in in vitro settings. The optimized formulation had a particle size of 102.7 nm with − 47.30 mVof zeta potential. Entrapment efficiency was found to be 65.21%. The cell viability results suggested compatibility of developed formulation. Cellular uptake and VEGF expression levels for the formulated nanoparticles specified that the developed formulation showed potential cellular uptake and had displayed anti-angiogenic property by inhibiting VEGF expression in vitro. The results showed successful development of resveratrol-loaded nanoparticles which may be used for neovascular AMD treatment alone or in combination with anti-VEGF agents.

KEY WORDS: resveratrol; PLGA nanoparticles; sustained release; intravitreal ocular delivery; antiVEGF.

INTRODUCTION Age-related macular degeneration (AMD), an ocular medical condition, is one of the utmost prevalent reasons of loss of vision among the geriatrics in developed countries. Statistically, it is the third most predominant eye disease leading to loss of vision with a blindness occurrence of 8.7% (1–3). In the USA, about two million AMD patients have an advanced form of AMD while more than eight million have an intermediate form of AMD (4). Initially, the disease develops as dry AMD and almost 85–90% of cases are of dry AMD, whereas with time it progresses to wet/neovascular AMD accounting around 10% of cases. Dry AMD is developed by the presence of small Guest Editors: Harsh Chauhan, Abhijit Date and Sonali Dhindwal 1

Department of Pharmaceutical Sciences, Taneja College of Pharmacy, University of South Florida, 12901 Bruce B. Downs Blvd., MDC30, Tampa, Florida 33612, USA. 2 Department of Pharmacogenomics, Bernard J Dunn School of Pharmacy, 8095 Innovation Park Drive, Fairfax, Virginia 220314868, USA. 3 To whom correspondence should be addressed. (