Silk fibroin as an organic polymer for controlled drug delivery

S. Hofmann, S. Foo, F. Rossetti, M. Textor, G. Vunjak-Novakovic, D.L. Kaplan, H.P. Merkle, L. Meinel

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Abstract

The pharmaceutical utility of silk fibroin (SF) materials for drug delivery was investigated. SF films were prepared from aqueous solutions of the fibroin protein polymer and crystallinity was induced and controlled by methanol treatment. Dextrans of different molecular weights, as well as proteins, were physically entrapped into the drug delivery device during processing into films. Drug release kinetics were evaluated as a function of dextran molecular weight, and film crystallinity. Treatment with methanol resulted in an increase in beta-sheet structure, an increase in crystallinity and an increase in film surface hydrophobicity determined by FTIR, X-ray and contact angle techniques, respectively. The increase in crystallinity resulted in the sustained release of dextrans of molecular weights ranging from 4 to 40 kDa, whereas for less crystalline films sustained release was confined to the 40 kDa dextran. Protein release from the films was studied with horseradish peroxidase (HRP) and lysozyme (Lys) as model compounds. Enzyme release from the less crystalline films resulted in a biphasic release pattern, characterized by an initial release within the first 36 h, followed by a lag phase and continuous release between days 3 and 11. No initial burst was observed for films with higher crystallinity and subsequent release patterns followed linear kinetics for HRP, or no substantial release for Lys. In conclusion, SF is an interesting polymer for drug delivery of polysaccharides and bioactive proteins due to the controllable level of crystallinity and the ability to process the biomaterial in biocompatible fashion under ambient conditions to avoid damage to labile compounds to be delivered.
Original languageEnglish
Pages (from-to)219-227
Number of pages8
JournalJournal of Controlled Release
Volume111
Issue number1-2
DOIs
Publication statusPublished - 2006

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Fibroins
Silk
Dextrans
Polymers
Molecular Weight
Horseradish Peroxidase
Muramidase
Pharmaceutical Preparations
Methanol
Proteins
Biocompatible Materials
Fourier Transform Infrared Spectroscopy
Hydrophobic and Hydrophilic Interactions
Polysaccharides
Pharmacokinetics
X-Rays
Equipment and Supplies
Enzymes

Cite this

Hofmann, S., Foo, S., Rossetti, F., Textor, M., Vunjak-Novakovic, G., Kaplan, D. L., ... Meinel, L. (2006). Silk fibroin as an organic polymer for controlled drug delivery. Journal of Controlled Release, 111(1-2), 219-227. https://doi.org/10.1016/j.jconrel.2005.12.009
Hofmann, S. ; Foo, S. ; Rossetti, F. ; Textor, M. ; Vunjak-Novakovic, G. ; Kaplan, D.L. ; Merkle, H.P. ; Meinel, L. / Silk fibroin as an organic polymer for controlled drug delivery. In: Journal of Controlled Release. 2006 ; Vol. 111, No. 1-2. pp. 219-227.
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abstract = "The pharmaceutical utility of silk fibroin (SF) materials for drug delivery was investigated. SF films were prepared from aqueous solutions of the fibroin protein polymer and crystallinity was induced and controlled by methanol treatment. Dextrans of different molecular weights, as well as proteins, were physically entrapped into the drug delivery device during processing into films. Drug release kinetics were evaluated as a function of dextran molecular weight, and film crystallinity. Treatment with methanol resulted in an increase in beta-sheet structure, an increase in crystallinity and an increase in film surface hydrophobicity determined by FTIR, X-ray and contact angle techniques, respectively. The increase in crystallinity resulted in the sustained release of dextrans of molecular weights ranging from 4 to 40 kDa, whereas for less crystalline films sustained release was confined to the 40 kDa dextran. Protein release from the films was studied with horseradish peroxidase (HRP) and lysozyme (Lys) as model compounds. Enzyme release from the less crystalline films resulted in a biphasic release pattern, characterized by an initial release within the first 36 h, followed by a lag phase and continuous release between days 3 and 11. No initial burst was observed for films with higher crystallinity and subsequent release patterns followed linear kinetics for HRP, or no substantial release for Lys. In conclusion, SF is an interesting polymer for drug delivery of polysaccharides and bioactive proteins due to the controllable level of crystallinity and the ability to process the biomaterial in biocompatible fashion under ambient conditions to avoid damage to labile compounds to be delivered.",
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Hofmann, S, Foo, S, Rossetti, F, Textor, M, Vunjak-Novakovic, G, Kaplan, DL, Merkle, HP & Meinel, L 2006, 'Silk fibroin as an organic polymer for controlled drug delivery', Journal of Controlled Release, vol. 111, no. 1-2, pp. 219-227. https://doi.org/10.1016/j.jconrel.2005.12.009

Silk fibroin as an organic polymer for controlled drug delivery. / Hofmann, S.; Foo, S.; Rossetti, F.; Textor, M.; Vunjak-Novakovic, G.; Kaplan, D.L.; Merkle, H.P.; Meinel, L.

In: Journal of Controlled Release, Vol. 111, No. 1-2, 2006, p. 219-227.

Research output: Contribution to journalArticleAcademicpeer-review

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T1 - Silk fibroin as an organic polymer for controlled drug delivery

AU - Hofmann, S.

AU - Foo, S.

AU - Rossetti, F.

AU - Textor, M.

AU - Vunjak-Novakovic, G.

AU - Kaplan, D.L.

AU - Merkle, H.P.

AU - Meinel, L.

PY - 2006

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N2 - The pharmaceutical utility of silk fibroin (SF) materials for drug delivery was investigated. SF films were prepared from aqueous solutions of the fibroin protein polymer and crystallinity was induced and controlled by methanol treatment. Dextrans of different molecular weights, as well as proteins, were physically entrapped into the drug delivery device during processing into films. Drug release kinetics were evaluated as a function of dextran molecular weight, and film crystallinity. Treatment with methanol resulted in an increase in beta-sheet structure, an increase in crystallinity and an increase in film surface hydrophobicity determined by FTIR, X-ray and contact angle techniques, respectively. The increase in crystallinity resulted in the sustained release of dextrans of molecular weights ranging from 4 to 40 kDa, whereas for less crystalline films sustained release was confined to the 40 kDa dextran. Protein release from the films was studied with horseradish peroxidase (HRP) and lysozyme (Lys) as model compounds. Enzyme release from the less crystalline films resulted in a biphasic release pattern, characterized by an initial release within the first 36 h, followed by a lag phase and continuous release between days 3 and 11. No initial burst was observed for films with higher crystallinity and subsequent release patterns followed linear kinetics for HRP, or no substantial release for Lys. In conclusion, SF is an interesting polymer for drug delivery of polysaccharides and bioactive proteins due to the controllable level of crystallinity and the ability to process the biomaterial in biocompatible fashion under ambient conditions to avoid damage to labile compounds to be delivered.

AB - The pharmaceutical utility of silk fibroin (SF) materials for drug delivery was investigated. SF films were prepared from aqueous solutions of the fibroin protein polymer and crystallinity was induced and controlled by methanol treatment. Dextrans of different molecular weights, as well as proteins, were physically entrapped into the drug delivery device during processing into films. Drug release kinetics were evaluated as a function of dextran molecular weight, and film crystallinity. Treatment with methanol resulted in an increase in beta-sheet structure, an increase in crystallinity and an increase in film surface hydrophobicity determined by FTIR, X-ray and contact angle techniques, respectively. The increase in crystallinity resulted in the sustained release of dextrans of molecular weights ranging from 4 to 40 kDa, whereas for less crystalline films sustained release was confined to the 40 kDa dextran. Protein release from the films was studied with horseradish peroxidase (HRP) and lysozyme (Lys) as model compounds. Enzyme release from the less crystalline films resulted in a biphasic release pattern, characterized by an initial release within the first 36 h, followed by a lag phase and continuous release between days 3 and 11. No initial burst was observed for films with higher crystallinity and subsequent release patterns followed linear kinetics for HRP, or no substantial release for Lys. In conclusion, SF is an interesting polymer for drug delivery of polysaccharides and bioactive proteins due to the controllable level of crystallinity and the ability to process the biomaterial in biocompatible fashion under ambient conditions to avoid damage to labile compounds to be delivered.

U2 - 10.1016/j.jconrel.2005.12.009

DO - 10.1016/j.jconrel.2005.12.009

M3 - Article

C2 - 16458987

VL - 111

SP - 219

EP - 227

JO - Journal of Controlled Release

JF - Journal of Controlled Release

SN - 0168-3659

IS - 1-2

ER -