Preparation, characterization and biocompatibility studies of thermoresponsive eyedrops based on the combination of nanostructured lipid carriers (NLC) and the polymer Pluronic F-127 for controlled delivery of ibuprofen

• Type: Article in International Scientific Journal
• Date: 2017

Authors

Almeida, H (Author) Other; Paulo Lobão (Author) FFUP; Frigerio, C (Author) Other; Fonseca, J (Author) Other; Silva, R (Author) Other; Sousa Lobo JM (Author) FFUP; Maria Helena Amaral (Author) FFUP

Journal

Title: Pharmaceutical Development and Technology

Vol. 22

Pages: 336-349

ISSN: 1083-7450

Publisher: Taylor & Francis

Indexing

ISI Web of Knowledge - 38 Citations

Scopus - 44 Citations

Other information

Authenticus ID: P-00M-JJT

DOI: 10.3109/10837450.2015.1125922

Abstract (EN): Context: Nanostructured lipid carrier (NLC) dispersions present low viscosity and poor mucoadhesive properties, which reduce the pre-corneal residence time and consequently, the bioavailability of ocular drugs. Objective: The aim of this study was to prepare thermoresponsive eyedrops based on the combination of lipid nanoparticles and a thermoresponsive polymer with mucomimetic properties (Pluronic (R) F-127). Materials and methods: NLCi dispersions were prepared based on the melt-emulsification and ultrasonication technique. Physicochemical and morphological characteristics of the colloidal dispersions were evaluated. The formulation was also investigated for potential cytotoxicity in Y-79 human retinoblastoma cells and the in vitro drug release profile of the ibuprofen was determined. Results: NLCi showed a Z-average below 200 nm, a highly positive zeta potential and an efficiency of encapsulation (EE) of similar to 90%. The gelification of the NLCi dispersion with 15% (w/w) Pluronic (R) F-127 did not cause significant changes to the physicochemical properties. The potential NLC-induced cytotoxicity was evaluated by the Alamar Blue reduction assay in Y-79 cells, and no relevant cytotoxicity was observed after exposure to 0-100 mu g/mL NLC for up to 72 hours. The optimized formulations showed a sustained release of ibuprofen over several hours. Discussion and conclusion: The strategy proposed in this work can be successfully used to increase the bioavailability and the therapeutic efficacy of conventional eyedrops.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 14