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Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation

Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation


Title: Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation
Author: Lorenzo Veiga, Blanca   orcid.org/0000-0003-1767-9868
Sigurdsson, Hakon Hrafn   orcid.org/0000-0003-4074-9182
Loftsson, Thorsteinn   orcid.org/0000-0002-9439-1553
Date: 2019-01-11
Language: English
Scope: 229
University/Institute: Háskóli Íslands
University of Iceland
School: Heilbrigðisvísindasvið (HÍ)
School of Health Sciences (UI)
Department: Lyfjafræðideild (HÍ)
Faculty of Pharmaceutical Sciences (UI)
Series: Materials;12(2)
ISSN: 1996-1944
DOI: 10.3390/ma12020229
Subject: Aggregate; Complexation; Cyclodextrin; Nepafenac; Ocular drug delivery; Polymer; Self-assemble; Lyfjaefnafræði; Lyf; Augnsjúkdómar; Lyfhrifafræði
URI: https://hdl.handle.net/20.500.11815/1855

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Citation:

Lorenzo-Veiga, B.; Sigurdsson, H.H.; Loftsson, T. Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation. Materials 2019, 12, 229.

Abstract:

The topical administration route is commonly used for targeting therapeutics to the eye; however, improving the bioavailability of drugs applied directly to the eye remains a challenge. Different strategies have been studied to address this challenge. One of them is the use of aggregates that are formed easily by self-assembly of cyclodextrin (CD)/drug complexes in aqueous solution. The aim of this study was to design a new eye drop formulation based on aggregates formed between CD/drug complexes. For this purpose, the physicochemical properties of the aggregates associated with six CDs and selected water-soluble polymers were analysed. Complex formation was studied using differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR) and 1 H nuclear magnetic resonance spectroscopy ( 1 H-NMR). Results showed that HPβCD performed best in terms of solubilization, while γ CD performed best in terms of enhancing nanoaggregate formation. Formation of inclusion complexes was confirmed by DSC, FT-IR and 1 H-NMR studies. A mixture of 15% (w/v) γ CD and 8% (w/v) HPβCD was selected for formulation studies. It was concluded that formulations with aggregate sizes less than 1 μm and viscosity around 10-19 centipoises can be easily prepared using a mixture of CDs. Formulations containing polymeric drug/CD nanoaggregates represent an interesting strategy for enhanced topical delivery of nepafenac.

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited

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