Calcipotriol delivery into the skin with PEGylated liposomes

Research output: Contribution to journalJournal articlepeer-review

Standard

Calcipotriol delivery into the skin with PEGylated liposomes. / Knudsen, Nina Østergaard; Rønholt, Stine; Salte, Ragnhild Djønne; Jorgensen, Lene; Thormann, Thorsten; Basse, Line Hollesen; Hansen, Jens; Frokjaer, Sven; Foged, Camilla.

In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 81, No. 3, 2012, p. 532-9.

Research output: Contribution to journalJournal articlepeer-review

Harvard

Knudsen, NØ, Rønholt, S, Salte, RD, Jorgensen, L, Thormann, T, Basse, LH, Hansen, J, Frokjaer, S & Foged, C 2012, 'Calcipotriol delivery into the skin with PEGylated liposomes', European Journal of Pharmaceutics and Biopharmaceutics, vol. 81, no. 3, pp. 532-9. https://doi.org/10.1016/j.ejpb.2012.04.005

APA

Knudsen, N. Ø., Rønholt, S., Salte, R. D., Jorgensen, L., Thormann, T., Basse, L. H., Hansen, J., Frokjaer, S., & Foged, C. (2012). Calcipotriol delivery into the skin with PEGylated liposomes. European Journal of Pharmaceutics and Biopharmaceutics, 81(3), 532-9. https://doi.org/10.1016/j.ejpb.2012.04.005

Vancouver

Knudsen NØ, Rønholt S, Salte RD, Jorgensen L, Thormann T, Basse LH et al. Calcipotriol delivery into the skin with PEGylated liposomes. European Journal of Pharmaceutics and Biopharmaceutics. 2012;81(3):532-9. https://doi.org/10.1016/j.ejpb.2012.04.005

Author

Knudsen, Nina Østergaard ; Rønholt, Stine ; Salte, Ragnhild Djønne ; Jorgensen, Lene ; Thormann, Thorsten ; Basse, Line Hollesen ; Hansen, Jens ; Frokjaer, Sven ; Foged, Camilla. / Calcipotriol delivery into the skin with PEGylated liposomes. In: European Journal of Pharmaceutics and Biopharmaceutics. 2012 ; Vol. 81, No. 3. pp. 532-9.

Bibtex

@article{14f106c34f8d483e90a69414aa889786,
title = "Calcipotriol delivery into the skin with PEGylated liposomes",
abstract = "The d-vitamin analogue calcipotriol is commonly used for topical treatment of psoriasis, but skin penetration is required for calcipotriol to reach its pharmacological target: the keratinocytes in the lower epidermis. Liposomes can enhance the delivery of drugs into the skin, but a major challenge for the development of dosage forms containing liposomes is to maintain the colloidal stability in the formulation. The purpose of this study was to investigate the effect of stabilising liposomes with the lipopolymer poly(ethylene glycol)-distearoylphosphoethanolamine (PEG-DSPE) on the physicochemical properties of the liposomes and the ability to deliver membrane-intercalated calcipotriol into the skin. Inclusion of 0.5, l and 5mol% PEG-DSPE in the membrane enhanced the colloidal stability of the liposomes without compromising the delivery of calcipotriol from the vehicle into excised pig skin. Calcipotriol-loaded liposomes with 1mol% PEG-DSPE did even provide for a significantly increased deposition of calcipotriol into the stratum corneum. The size of the liposomes affected the penetration of calcipotriol into the stratum corneum since small unilamellar vesicles enhanced calcipotriol penetration as compared to large multilamellar vesicles, indicating that the liposomes to some extent migrate as intact vesicles into the stratum corneum. However, calcipotriol penetrated the skin better than the lipid component of the liposomes, suggesting that at least a fraction of the drug is released from the liposomes during skin migration. In conclusion, PEGylation is therefore a promising approach for stabilising calcipotriol-containing liposomal dispersions without compromising their favourable skin accumulation properties.",
author = "Knudsen, {Nina {\O}stergaard} and Stine R{\o}nholt and Salte, {Ragnhild Dj{\o}nne} and Lene Jorgensen and Thorsten Thormann and Basse, {Line Hollesen} and Jens Hansen and Sven Frokjaer and Camilla Foged",
note = "Copyright {\textcopyright} 2012 Elsevier B.V. All rights reserved.",
year = "2012",
doi = "10.1016/j.ejpb.2012.04.005",
language = "English",
volume = "81",
pages = "532--9",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
issn = "0939-6411",
publisher = "Elsevier",
number = "3",

}

RIS

TY - JOUR

T1 - Calcipotriol delivery into the skin with PEGylated liposomes

AU - Knudsen, Nina Østergaard

AU - Rønholt, Stine

AU - Salte, Ragnhild Djønne

AU - Jorgensen, Lene

AU - Thormann, Thorsten

AU - Basse, Line Hollesen

AU - Hansen, Jens

AU - Frokjaer, Sven

AU - Foged, Camilla

N1 - Copyright © 2012 Elsevier B.V. All rights reserved.

PY - 2012

Y1 - 2012

N2 - The d-vitamin analogue calcipotriol is commonly used for topical treatment of psoriasis, but skin penetration is required for calcipotriol to reach its pharmacological target: the keratinocytes in the lower epidermis. Liposomes can enhance the delivery of drugs into the skin, but a major challenge for the development of dosage forms containing liposomes is to maintain the colloidal stability in the formulation. The purpose of this study was to investigate the effect of stabilising liposomes with the lipopolymer poly(ethylene glycol)-distearoylphosphoethanolamine (PEG-DSPE) on the physicochemical properties of the liposomes and the ability to deliver membrane-intercalated calcipotriol into the skin. Inclusion of 0.5, l and 5mol% PEG-DSPE in the membrane enhanced the colloidal stability of the liposomes without compromising the delivery of calcipotriol from the vehicle into excised pig skin. Calcipotriol-loaded liposomes with 1mol% PEG-DSPE did even provide for a significantly increased deposition of calcipotriol into the stratum corneum. The size of the liposomes affected the penetration of calcipotriol into the stratum corneum since small unilamellar vesicles enhanced calcipotriol penetration as compared to large multilamellar vesicles, indicating that the liposomes to some extent migrate as intact vesicles into the stratum corneum. However, calcipotriol penetrated the skin better than the lipid component of the liposomes, suggesting that at least a fraction of the drug is released from the liposomes during skin migration. In conclusion, PEGylation is therefore a promising approach for stabilising calcipotriol-containing liposomal dispersions without compromising their favourable skin accumulation properties.

AB - The d-vitamin analogue calcipotriol is commonly used for topical treatment of psoriasis, but skin penetration is required for calcipotriol to reach its pharmacological target: the keratinocytes in the lower epidermis. Liposomes can enhance the delivery of drugs into the skin, but a major challenge for the development of dosage forms containing liposomes is to maintain the colloidal stability in the formulation. The purpose of this study was to investigate the effect of stabilising liposomes with the lipopolymer poly(ethylene glycol)-distearoylphosphoethanolamine (PEG-DSPE) on the physicochemical properties of the liposomes and the ability to deliver membrane-intercalated calcipotriol into the skin. Inclusion of 0.5, l and 5mol% PEG-DSPE in the membrane enhanced the colloidal stability of the liposomes without compromising the delivery of calcipotriol from the vehicle into excised pig skin. Calcipotriol-loaded liposomes with 1mol% PEG-DSPE did even provide for a significantly increased deposition of calcipotriol into the stratum corneum. The size of the liposomes affected the penetration of calcipotriol into the stratum corneum since small unilamellar vesicles enhanced calcipotriol penetration as compared to large multilamellar vesicles, indicating that the liposomes to some extent migrate as intact vesicles into the stratum corneum. However, calcipotriol penetrated the skin better than the lipid component of the liposomes, suggesting that at least a fraction of the drug is released from the liposomes during skin migration. In conclusion, PEGylation is therefore a promising approach for stabilising calcipotriol-containing liposomal dispersions without compromising their favourable skin accumulation properties.

U2 - 10.1016/j.ejpb.2012.04.005

DO - 10.1016/j.ejpb.2012.04.005

M3 - Journal article

C2 - 22538098

VL - 81

SP - 532

EP - 539

JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

SN - 0939-6411

IS - 3

ER -

ID: 40370263