Solid lipid particles for oral delivery of peptide and protein drugs I - Elucidating the release mechanism of lysozyme during lipolysis

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Solid lipid particles for oral delivery of peptide and protein drugs I - Elucidating the release mechanism of lysozyme during lipolysis. / Christophersen, Philip Carsten B; Zhang, L.; Yang, M; Nielsen, H Mørck; Müllertz, A; Mu, H.

In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 85, No. 3, part A, 02.08.2013, p. 473-480.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Christophersen, PCB, Zhang, L, Yang, M, Nielsen, HM, Müllertz, A & Mu, H 2013, 'Solid lipid particles for oral delivery of peptide and protein drugs I - Elucidating the release mechanism of lysozyme during lipolysis', European Journal of Pharmaceutics and Biopharmaceutics, vol. 85, no. 3, part A, pp. 473-480. https://doi.org/10.1016/j.ejpb.2013.07.017

APA

Christophersen, P. C. B., Zhang, L., Yang, M., Nielsen, H. M., Müllertz, A., & Mu, H. (2013). Solid lipid particles for oral delivery of peptide and protein drugs I - Elucidating the release mechanism of lysozyme during lipolysis. European Journal of Pharmaceutics and Biopharmaceutics, 85(3, part A), 473-480. https://doi.org/10.1016/j.ejpb.2013.07.017

Vancouver

Christophersen PCB, Zhang L, Yang M, Nielsen HM, Müllertz A, Mu H. Solid lipid particles for oral delivery of peptide and protein drugs I - Elucidating the release mechanism of lysozyme during lipolysis. European Journal of Pharmaceutics and Biopharmaceutics. 2013 Aug 2;85(3, part A):473-480. https://doi.org/10.1016/j.ejpb.2013.07.017

Author

Christophersen, Philip Carsten B ; Zhang, L. ; Yang, M ; Nielsen, H Mørck ; Müllertz, A ; Mu, H. / Solid lipid particles for oral delivery of peptide and protein drugs I - Elucidating the release mechanism of lysozyme during lipolysis. In: European Journal of Pharmaceutics and Biopharmaceutics. 2013 ; Vol. 85, No. 3, part A. pp. 473-480.

Bibtex

@article{dd2c50845e4144bca2c80b7671b2fc34,
title = "Solid lipid particles for oral delivery of peptide and protein drugs I - Elucidating the release mechanism of lysozyme during lipolysis",
abstract = "The mechanism of protein release from solid lipid particles was investigated by a new lipolysis model in a biorelevant medium containing both bile salts and phospholipids. Lysozyme, a model protein, was formulated into solid lipid particles using four different types of lipids, two triglycerides with different chain-length of fatty acyl groups i.e. trimyristin (TG14) and tristearin (TG18), and two lipid blends dominated by diglycerides and monoglycerides, respectively. The release of lysozyme from the solid lipid particles and the lipid hydrolysis process were assessed in the lipolysis model, while the change in particle surface during the lipolysis process was evaluated using scanning electron microscopy. The lysozyme release profiles from TG14 and TG18 as well as diglyceride particles correlated well with the release of free fatty acids from the lipid particles during the lipolysis and therefore exhibited a lipase-mediated degradation-based release mechanism. The release of lysozyme from monoglyceride particles was independent on lipase degradation due to the instability of the lipid matrix in the lipolysis medium. In conclusion, the established lipolysis model is successfully used to elucidate the drug release mechanism from solid lipid particles and can potentially be used in rational selection of lipid excipients for oral delivery of peptide/protein drugs.",
author = "Christophersen, {Philip Carsten B} and L. Zhang and M Yang and Nielsen, {H M{\o}rck} and A M{\"u}llertz and H Mu",
note = "Copyright {\circledC} 2013 Elsevier B.V. All rights reserved.",
year = "2013",
month = "8",
day = "2",
doi = "10.1016/j.ejpb.2013.07.017",
language = "English",
volume = "85",
pages = "473--480",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
issn = "0939-6411",
publisher = "Elsevier",
number = "3, part A",

}

RIS

TY - JOUR

T1 - Solid lipid particles for oral delivery of peptide and protein drugs I - Elucidating the release mechanism of lysozyme during lipolysis

AU - Christophersen, Philip Carsten B

AU - Zhang, L.

AU - Yang, M

AU - Nielsen, H Mørck

AU - Müllertz, A

AU - Mu, H

N1 - Copyright © 2013 Elsevier B.V. All rights reserved.

PY - 2013/8/2

Y1 - 2013/8/2

N2 - The mechanism of protein release from solid lipid particles was investigated by a new lipolysis model in a biorelevant medium containing both bile salts and phospholipids. Lysozyme, a model protein, was formulated into solid lipid particles using four different types of lipids, two triglycerides with different chain-length of fatty acyl groups i.e. trimyristin (TG14) and tristearin (TG18), and two lipid blends dominated by diglycerides and monoglycerides, respectively. The release of lysozyme from the solid lipid particles and the lipid hydrolysis process were assessed in the lipolysis model, while the change in particle surface during the lipolysis process was evaluated using scanning electron microscopy. The lysozyme release profiles from TG14 and TG18 as well as diglyceride particles correlated well with the release of free fatty acids from the lipid particles during the lipolysis and therefore exhibited a lipase-mediated degradation-based release mechanism. The release of lysozyme from monoglyceride particles was independent on lipase degradation due to the instability of the lipid matrix in the lipolysis medium. In conclusion, the established lipolysis model is successfully used to elucidate the drug release mechanism from solid lipid particles and can potentially be used in rational selection of lipid excipients for oral delivery of peptide/protein drugs.

AB - The mechanism of protein release from solid lipid particles was investigated by a new lipolysis model in a biorelevant medium containing both bile salts and phospholipids. Lysozyme, a model protein, was formulated into solid lipid particles using four different types of lipids, two triglycerides with different chain-length of fatty acyl groups i.e. trimyristin (TG14) and tristearin (TG18), and two lipid blends dominated by diglycerides and monoglycerides, respectively. The release of lysozyme from the solid lipid particles and the lipid hydrolysis process were assessed in the lipolysis model, while the change in particle surface during the lipolysis process was evaluated using scanning electron microscopy. The lysozyme release profiles from TG14 and TG18 as well as diglyceride particles correlated well with the release of free fatty acids from the lipid particles during the lipolysis and therefore exhibited a lipase-mediated degradation-based release mechanism. The release of lysozyme from monoglyceride particles was independent on lipase degradation due to the instability of the lipid matrix in the lipolysis medium. In conclusion, the established lipolysis model is successfully used to elucidate the drug release mechanism from solid lipid particles and can potentially be used in rational selection of lipid excipients for oral delivery of peptide/protein drugs.

U2 - 10.1016/j.ejpb.2013.07.017

DO - 10.1016/j.ejpb.2013.07.017

M3 - Journal article

VL - 85

SP - 473

EP - 480

JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

SN - 0939-6411

IS - 3, part A

ER -

ID: 50851123