April 2014
Volume 55, Issue 13
Free
ARVO Annual Meeting Abstract  |   April 2014
Polyesteramide Microspheres As Carriers In Ophthalmology. In Vitro Toxicity In Macrophages, ARPE-19 Cells And An Organotypic Culture Of Retina
Author Affiliations & Notes
  • Vanessa Andres-Guerrero
    Pharmaceutical Technology, Faculty of Pharmacy, Complutense University of Madrid, Madrid, Spain
  • Blanca Arango-Gonzalez
    Centre for Ophthalmology, Institute for Ophthalmic Research, University of Tuebingen, Tuebingen, Germany
  • Eva Ramsay
    Center for Drug Research, University of Helsinki, Helsinki, Finland
  • Mengmeng Zong
    DSM, Geleen, Netherlands
  • Beatriz de las Heras
    Pharmacology, Faculty of Pharmacy, Complutense University of Madrid, Madrid, Spain
  • George Mihov
    DSM, Geleen, Netherlands
  • Aylvin Dias
    DSM, Geleen, Netherlands
  • Arto Urtti
    Center for Drug Research, University of Helsinki, Helsinki, Finland
  • Marius Ueffing
    Centre for Ophthalmology, Institute for Ophthalmic Research, University of Tuebingen, Tuebingen, Germany
  • Rocio Herrero-Vanrell
    Pharmaceutical Technology, Faculty of Pharmacy, Complutense University of Madrid, Madrid, Spain
  • Footnotes
    Commercial Relationships Vanessa Andres-Guerrero, None; Blanca Arango-Gonzalez, None; Eva Ramsay, None; Mengmeng Zong, DSM (E); Beatriz de las Heras, None; George Mihov, DSM (E); Aylvin Dias, DSM (E); Arto Urtti, None; Marius Ueffing, None; Rocio Herrero-Vanrell, None
  • Footnotes
    Support None
Investigative Ophthalmology & Visual Science April 2014, Vol.55, 4900. doi:https://doi.org/
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      Vanessa Andres-Guerrero, Blanca Arango-Gonzalez, Eva Ramsay, Mengmeng Zong, Beatriz de las Heras, George Mihov, Aylvin Dias, Arto Urtti, Marius Ueffing, Rocio Herrero-Vanrell; Polyesteramide Microspheres As Carriers In Ophthalmology. In Vitro Toxicity In Macrophages, ARPE-19 Cells And An Organotypic Culture Of Retina. Invest. Ophthalmol. Vis. Sci. 2014;55(13):4900. doi: https://doi.org/.

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      © ARVO (1962-2015); The Authors (2016-present)

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Abstract

Purpose: Amino acid based polyesteramides (PEAs) are a new family of synthetic biodegradable polymers based on α-amino acids, aliphatic dicarboxylic acids and aliphatic α-ω diols. The aim of this study was to evaluate the suitability of PEA microspheres (Ms), in terms of toxicity, to be used as carriers in ophthalmology.

Methods: PEA Ms were prepared following an emulsion-solvent evaporation technique. Ms were characterized by morphology, mean particle size, particle size distribution and molar mass. In vitro tolerance was performed with two techniques: (1) MTT in a peritoneal macrophages cell line (RAW 264.7) and a retinal pigment epithelial cell line (ARPE-19), in which cells were exposed to PEA Ms (0.001-2 mg/ml) for 20 hours and 5 hours, respectively, and (2) TUNEL assay, combined with conventional histology, in short and a long term organotypic cultures (7 and 20 days, respectively) of rats’ retinas (0.125-1 mg Ms). PLGA Ms were used as control.

Results: Spherical PEA Ms with no pores and smooth surface were produced (mean particle size= 14.96 ± 6.4 µm; Mn= 48.3 ± 3.7 kDa). PEA microparticles showed no signs of toxicity in the MTT assay (cell viability > 80%), using both macrophages and ARPE-19 cells. Retinas in organotypic cultures treated with 0.125 and 0.625 mg/ml PEA Ms and PLGA Ms in short and long term cultures did not show signs of toxicity. The TUNEL values were similar to the observed in untreated cultures. On the other hand, retinas treated with a high concentration of PEA Ms (1mg/ml), in long term cultures, showed cellular disorganization and internalization of particles. Similar histologic changes were observed in control retinas treated with PLGA Ms.

Conclusions: Biodegradable PEA Ms are potentially useful to develop new controlled drug delivery systems for treating ophthalmic diseases affecting the back of the eye.

Keywords: 694 retinal culture • 701 retinal pigment epithelium  
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