Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release

Research output: Contribution to journalJournal articleResearchpeer-review

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Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release. / Pedersen, Palle J.; Adolph, Sidsel K.; Subramanian, Arun K.; Arouri, Ahmad; Andresen, Thomas L.; Mouritsen, Ole G.; Madsen, Robert; Madsen, Mogens W.; Peters, Günther H.; Clausen, Mads H.

In: Journal of Medicinal Chemistry, Vol. 53, No. 9, 2010, p. 3782-3792.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Pedersen, PJ, Adolph, SK, Subramanian, AK, Arouri, A, Andresen, TL, Mouritsen, OG, Madsen, R, Madsen, MW, Peters, GH & Clausen, MH 2010, 'Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release', Journal of Medicinal Chemistry, vol. 53, no. 9, pp. 3782-3792. https://doi.org/10.1021/jm100190c

APA

Pedersen, P. J., Adolph, S. K., Subramanian, A. K., Arouri, A., Andresen, T. L., Mouritsen, O. G., ... Clausen, M. H. (2010). Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release. Journal of Medicinal Chemistry, 53(9), 3782-3792. https://doi.org/10.1021/jm100190c

Vancouver

Pedersen PJ, Adolph SK, Subramanian AK, Arouri A, Andresen TL, Mouritsen OG et al. Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release. Journal of Medicinal Chemistry. 2010;53(9):3782-3792. https://doi.org/10.1021/jm100190c

Author

Pedersen, Palle J. ; Adolph, Sidsel K. ; Subramanian, Arun K. ; Arouri, Ahmad ; Andresen, Thomas L. ; Mouritsen, Ole G. ; Madsen, Robert ; Madsen, Mogens W. ; Peters, Günther H. ; Clausen, Mads H. / Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release. In: Journal of Medicinal Chemistry. 2010 ; Vol. 53, No. 9. pp. 3782-3792.

Bibtex

@article{24edb96073234401923e0de1b65719ef,
title = "Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release",
abstract = "The design of retinoid phospholipid prodrugs is described based on molecular dynamics simulations and cytotoxicity studies of synthetic retinoid esters. The prodrugs are degradable by secretory phospholipase A2 IIA and have potential in liposomal drug delivery targeting tumors. We have synthesized four different retinoid phospholipid prodrugs and shown that they form particles in the liposome size region with average diameters of 94-118 nm. Upon subjection to phospholipase A2, the lipid prodrugs were hydrolyzed, releasing cytotoxic retinoids and lysolipids. The formulated lipid prodrugs displayed IC50 values in the range of 3-19 μM toward HT-29 and Colo205 colon cancer cells in the presence of phospholipase A 2, while no significant cell death was observed in the absence of the enzyme.",
author = "Pedersen, {Palle J.} and Adolph, {Sidsel K.} and Subramanian, {Arun K.} and Ahmad Arouri and Andresen, {Thomas L.} and Mouritsen, {Ole G.} and Robert Madsen and Madsen, {Mogens W.} and Peters, {G{\"u}nther H.} and Clausen, {Mads H.}",
year = "2010",
doi = "10.1021/jm100190c",
language = "English",
volume = "53",
pages = "3782--3792",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "9",

}

RIS

TY - JOUR

T1 - Liposomal Formulation of Retinoids Designed for Enzyme Triggered Release

AU - Pedersen, Palle J.

AU - Adolph, Sidsel K.

AU - Subramanian, Arun K.

AU - Arouri, Ahmad

AU - Andresen, Thomas L.

AU - Mouritsen, Ole G.

AU - Madsen, Robert

AU - Madsen, Mogens W.

AU - Peters, Günther H.

AU - Clausen, Mads H.

PY - 2010

Y1 - 2010

N2 - The design of retinoid phospholipid prodrugs is described based on molecular dynamics simulations and cytotoxicity studies of synthetic retinoid esters. The prodrugs are degradable by secretory phospholipase A2 IIA and have potential in liposomal drug delivery targeting tumors. We have synthesized four different retinoid phospholipid prodrugs and shown that they form particles in the liposome size region with average diameters of 94-118 nm. Upon subjection to phospholipase A2, the lipid prodrugs were hydrolyzed, releasing cytotoxic retinoids and lysolipids. The formulated lipid prodrugs displayed IC50 values in the range of 3-19 μM toward HT-29 and Colo205 colon cancer cells in the presence of phospholipase A 2, while no significant cell death was observed in the absence of the enzyme.

AB - The design of retinoid phospholipid prodrugs is described based on molecular dynamics simulations and cytotoxicity studies of synthetic retinoid esters. The prodrugs are degradable by secretory phospholipase A2 IIA and have potential in liposomal drug delivery targeting tumors. We have synthesized four different retinoid phospholipid prodrugs and shown that they form particles in the liposome size region with average diameters of 94-118 nm. Upon subjection to phospholipase A2, the lipid prodrugs were hydrolyzed, releasing cytotoxic retinoids and lysolipids. The formulated lipid prodrugs displayed IC50 values in the range of 3-19 μM toward HT-29 and Colo205 colon cancer cells in the presence of phospholipase A 2, while no significant cell death was observed in the absence of the enzyme.

U2 - 10.1021/jm100190c

DO - 10.1021/jm100190c

M3 - Journal article

C2 - 20405849

AN - SCOPUS:77952020524

VL - 53

SP - 3782

EP - 3792

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 9

ER -

ID: 230976626