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Int. J. Mol. Sci. 2018, 19(8), 2304; https://doi.org/10.3390/ijms19082304

Intra-Articular Formulation of GE11-PLGA Conjugate-Based NPs for Dexamethasone Selective Targeting—In Vitro Evaluation

1
Department of Drug Sciences, University of Pavia, V.le Taramelli 12, 27100 Pavia (PV), Italy
2
Laboratory of General Biochemistry and Physical Pharmacy, Ghent University, Ottergemsesteenweg 460, 9000 Gent, Belgium
*
Author to whom correspondence should be addressed.
Received: 2 July 2018 / Revised: 31 July 2018 / Accepted: 3 August 2018 / Published: 6 August 2018
(This article belongs to the Special Issue Smart Polymers for Biomedical Applications)
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Abstract

Selectively targeted nanoscale drug delivery systems have recently emerged as promising intravenously therapeutic option for most chronic joint diseases. Here, a newly synthetized dodecapeptide (GE11)-polylactide-co-glycolide (PLGA)-based conjugate was used to prepare smart nanoparticles (NPs) intended for intra-articular administration and for selectively targeting Epidermal Growth Factor Receptor (EGFR). GE11-PLGA conjugate-based NPs are specifically uptaken by EGFR-overexpressed fibroblast; such as synoviocytes; which are the primarily cellular component involved in the development of destructive joint inflammation. The selective uptake could help to tune drug effectiveness in joints and to decrease local and systemic side effects. Dexamethasone (DXM) is a glucorticoid drug commonly used in joint disease treatment for both systemic and local administration route. In the present research; DXM was efficiently loaded into GE11-PLGA conjugate-based NPs through an eco-friendly nanoprecipitation method set up for this purpose. DXM loaded GE11-PLGA conjugate-based NPs revealed satisfactory ex vivo cytocompatibility; with proper size (≤150 nm) and good dimensional stability in synovial fluid. Intra-articular formulation was developed embedding DXM loaded GE11-PLGA conjugate-based NPs into thermosetting chitosan-based hydrogel; forming a biocompatible composite hydrogel able to quickly turn from liquid state into gel state at physiological temperature; within 15 min. Moreover; the use of thermosetting chitosan-based hydrogel extends the local release of active agent; DXM. View Full-Text
Keywords: EGFR targeting; GE11 peptide; PLGA-PEG nanoparticles; chitosan thermosetting hydrogel; intra-articular injection EGFR targeting; GE11 peptide; PLGA-PEG nanoparticles; chitosan thermosetting hydrogel; intra-articular injection
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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 (CC BY 4.0).
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Chiesa, E.; Pisani, S.; Colzani, B.; Dorati, R.; Conti, B.; Modena, T.; Braeckmans, K.; Genta, I. Intra-Articular Formulation of GE11-PLGA Conjugate-Based NPs for Dexamethasone Selective Targeting—In Vitro Evaluation. Int. J. Mol. Sci. 2018, 19, 2304.

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