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Title: Optimization, biopharmaceutical profile and therapeutic efficacy of pioglitazone-loaded PLGA-PEG nanospheres as a novel strategy for ocular inflammatory disorders.
Author: Silva Abreu, Marcelle
Calpena Campmany, Ana Cristina
Espina García, Marta
Silva, Amelia M.
Gimeno, Alavaro
Egea Gras, Ma. Antonia
García López, María Luisa
Keywords: Sistemes d'alliberament de medicaments
Agents antiinflamatoris
Drug delivery systems
Antiinflammatory agents
Issue Date: 3-Jan-2018
Publisher: Springer Science + Business Media
Abstract: PURPOSE: The main goal of this study was to encapsulate Pioglitazone (PGZ), in biodegradable polymeric nanoparticles as a new strategy for the treatment of ocular inflammatory processes. METHODS: To improve their biopharmaceutical profile for the treatment of ocular inflammatory disorders, nanospheres (NSs) of PGZ were formulated by factorial design with poly (lactic-co-glycolic acid) polyethylene glycol (PLGA-PEG). Interactions drug-polymer have been carried out by spectroscopic (X-ray spectroscopy, FTIR) and thermal methods (DSC). The PGZ-NSs were tested for their in vitro release profile, cytotoxicity, and ocular tolerance (HET-CAM® test); ex vivo corneal permeation, and in vivo inflammatory prevention and bioavailability. RESULTS: The optimized system showed a negative surface charge of -13.9 mV, an average particle size (Zav) of around 160 nm, a polydispersity index (PI) below 0.1, and a high encapsulation efficiency (EE) of around 92%. According to the DSC results, the drug was incorporated into the NSs polymeric matrix. The drug release was sustained for up to 14 h. PGZ-NSs up to 10 μg/ml exhibited no retinoblastoma cell toxicity. The ex vivo corneal and scleral permeation profiles of PGZ-NSs showed that retention and permeation through the sclera were higher than through the cornea. Ocular tolerance in vitro and in vivo demonstrated the non-irritant character of the formulation. CONCLUSION: The in vivo anti-inflammatory efficacy of developed PGZ-NSs indicates this colloidal system could constitute a new approach to prevent ocular inflammation. KEYWORDS: PLGA-PEG; drug delivery; nanospheres; ocular anti-inflammatory efficacy; pioglitazone
Note: Versió postprint del document publicat a:
It is part of: Pharmaceutical Research, 2018, vol. 35, num. 1, p. 11
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ISSN: 0724-8741
Appears in Collections:Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
Articles publicats en revistes (Institut de Nanociència i Nanotecnologia (IN2UB))

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