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Acta Pharmaceutica, Vol. 68 No. 3, 2018

Original scientific paper
https://doi.org/10.2478/acph-2018-0032

Effect of surface hydrophobicity of therapeutic protein loaded in polyelectrolyte nanoparticles on transepithelial permeability

ANA MIKLAVŽIN ; Faculty of Pharmacy, University of Ljubljana, SI-1000 Ljubljana, Slovenia; Lek Pharmaceuticals d. d., Sandoz Development Center Slovenia, 1526 Ljubljana, Slovenia
MATEJA CEGNAR ; Faculty of Pharmacy, University of Ljubljana, SI-1000 Ljubljana, Slovenia; Lek Pharmaceuticals d. d., Sandoz Development Center Slovenia, 1526 Ljubljana, Slovenia
JANEZ KERČ ; Faculty of Pharmacy, University of Ljubljana, SI-1000 Ljubljana, Slovenia; Lek Pharmaceuticals d. d., Sandoz Development Center Slovenia, 1526 Ljubljana, Slovenia
JULIJANA KRISTL   ORCID icon orcid.org/0000-0001-9136-6507 ; Faculty of Pharmacy, University of Ljubljana, SI-1000 Ljubljana, Slovenia

Fulltext: english, pdf (872 KB) pages 275-293 downloads: 154* cite
APA 6th Edition
MIKLAVŽIN, A., CEGNAR, M., KERČ, J. & KRISTL, J. (2018). Effect of surface hydrophobicity of therapeutic protein loaded in polyelectrolyte nanoparticles on transepithelial permeability. Acta Pharmaceutica, 68 (3), 275-293. https://doi.org/10.2478/acph-2018-0032
MLA 8th Edition
MIKLAVŽIN, ANA, et al. "Effect of surface hydrophobicity of therapeutic protein loaded in polyelectrolyte nanoparticles on transepithelial permeability." Acta Pharmaceutica, vol. 68, no. 3, 2018, pp. 275-293. https://doi.org/10.2478/acph-2018-0032. Accessed 22 Mar. 2019.
Chicago 17th Edition
MIKLAVŽIN, ANA, MATEJA CEGNAR, JANEZ KERČ and JULIJANA KRISTL. "Effect of surface hydrophobicity of therapeutic protein loaded in polyelectrolyte nanoparticles on transepithelial permeability." Acta Pharmaceutica 68, no. 3 (2018): 275-293. https://doi.org/10.2478/acph-2018-0032
Harvard
MIKLAVŽIN, A., et al. (2018). 'Effect of surface hydrophobicity of therapeutic protein loaded in polyelectrolyte nanoparticles on transepithelial permeability', Acta Pharmaceutica, 68(3), pp. 275-293. doi: https://doi.org/10.2478/acph-2018-0032
Vancouver
MIKLAVŽIN A, CEGNAR M, KERČ J, KRISTL J. Effect of surface hydrophobicity of therapeutic protein loaded in polyelectrolyte nanoparticles on transepithelial permeability. Acta Pharm. [Internet]. 2018 [cited 2019 March 22];68(3):275-293. doi: https://doi.org/10.2478/acph-2018-0032
IEEE
A. MIKLAVŽIN, M. CEGNAR, J. KERČ and J. KRISTL, "Effect of surface hydrophobicity of therapeutic protein loaded in polyelectrolyte nanoparticles on transepithelial permeability", Acta Pharmaceutica, vol.68, no. 3, pp. 275-293, 2018. [Online]. doi: https://doi.org/10.2478/acph-2018-0032

Abstracts
Oral delivery of protein drugs is greatly limited by low hydrophobicity, an important determinant for intestinal epithelial permeation and bioavailability. Herein, surface properties of recombinant erythropoietin were investigated using the fluorescent dye bis-ANS to monitor relative hydrophobicity for correlation with permeabilities with Caco-2 cells. At various pHs, bis-ANS fluorescence intensity indicated different surface hydrophobicities of erythropoietin molecules. Erythropoietin incorporated in chitosan or chitosan-trimethylchitosan (CS-TMC) nanoparticles prepared by polyelectrolyte complexation and ionotropic gelation with tripolyphosphate also showed different surface hydrophobicities. Chitosan nanoparticles with erythropoietin provided the most hydrophobic surface, followed by free erythropoietin (in water) and that loaded into CS-TMC nanoparticles. Chitosan nanoparticles were more effective than CS-TMC nanoparticles for permeation of erythropoietin across Caco-2 cell monolayers; the lowest permeability was shown by erythropoietin itself. Thus, hydrophilic protein molecules complexed with polyelectrolytes can provide more hydrophobic surfaces that enhance transepthelial permeability. This bis-ANS method also provides valuable information for the design of polyelectrolyte nanoparticules for oral delivery of protein drugs.

Keywords
erythropoietin; bis-ANS fluorescence intensity; chitosan; Caco-2 model; membrane permeability; oral drug delivery

Hrčak ID: 202048

URI
https://hrcak.srce.hr/202048

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