Tailoring the physicochemical properties of core-crosslinked polymeric micelles for pharmaceutical applications

Qizhi Hu; Cristianne J.F Rijcken; Ethlinn van Gaal; Paul Brundel; Hana Kostkova; Tomas Etrych; Benjamin Weber; Matthias Barz; Fabian Kiessling; Jai Prakash; Gerrit Storm; Wim E. Hennink; Twan Lammers

doi:10.1016/j.jconrel.2016.07.012

Tailoring the physicochemical properties of core-crosslinked polymeric micelles for pharmaceutical applications

Qizhi Hu, Cristianne J.F Rijcken, Ethlinn van Gaal, Paul Brundel, Hana Kostkova, Tomas Etrych, Benjamin Weber, Matthias Barz, Fabian Kiessling, Jai Prakash, Gerrit Storm, Wim E. Hennink, Twan Lammers

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Abstract

To optimally exploit the potential of (tumor-) targeted nanomedicines, platform technologies are needed in which physicochemical and pharmaceutical properties can be tailored according to specific medical needs and applications. We here systematically customized the properties of core-crosslinked polymeric micelles (CCPM). The micelles were based on mPEG-b-pHPMAmLacn (i.e. methoxy poly(ethylene glycol)-b-poly[N-(2-hydroxypropyl) methacrylamide-lactate]), similar to the block copolymer composition employed in CriPec® docetaxel, which is currently in phase I clinical trials. The CCPM platform was tailored with regard to size (30 to 100 nm), nanocarrier degradation (1 month to 1 year) and drug release kinetics (10 to 90% in 1 week). This was achieved by modulating the molecular weight of the block copolymer, the type and density of the crosslinking agent, and the hydrolytic sensitivity of the drug linkage, respectively. The high flexibility of CCPM facilitates the development of nanomedicinal products for specific therapeutic applications.

Original language	English
Pages (from-to)	314-325
Journal	Journal of controlled release
Volume	244
Issue number	Part B
DOIs	https://doi.org/10.1016/j.jconrel.2016.07.012
Publication status	Published - 2016
Event	14th European Symposium on Controlled Drug Delivery, ESCDD 2016 - Egmond aan Zee, Netherlands Duration: 13 Apr 2015 → 15 Apr 2016 Conference number: 14

Keywords

2023 OA procedure

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10.1016/j.jconrel.2016.07.012

ArticleFinal published version, 1.28 MBLicence: Taverne

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Hu, Q., Rijcken, C. J. F., van Gaal, E., Brundel, P., Kostkova, H., Etrych, T., Weber, B., Barz, M., Kiessling, F., Prakash, J., Storm, G., Hennink, W. E., & Lammers, T. (2016). Tailoring the physicochemical properties of core-crosslinked polymeric micelles for pharmaceutical applications. Journal of controlled release, 244(Part B), 314-325. https://doi.org/10.1016/j.jconrel.2016.07.012

@article{ae45afe7e1064f218e219289c4ce3597,

title = "Tailoring the physicochemical properties of core-crosslinked polymeric micelles for pharmaceutical applications",

abstract = "To optimally exploit the potential of (tumor-) targeted nanomedicines, platform technologies are needed in which physicochemical and pharmaceutical properties can be tailored according to specific medical needs and applications. We here systematically customized the properties of core-crosslinked polymeric micelles (CCPM). The micelles were based on mPEG-b-pHPMAmLacn (i.e. methoxy poly(ethylene glycol)-b-poly[N-(2-hydroxypropyl) methacrylamide-lactate]), similar to the block copolymer composition employed in CriPec{\textregistered} docetaxel, which is currently in phase I clinical trials. The CCPM platform was tailored with regard to size (30 to 100 nm), nanocarrier degradation (1 month to 1 year) and drug release kinetics (10 to 90% in 1 week). This was achieved by modulating the molecular weight of the block copolymer, the type and density of the crosslinking agent, and the hydrolytic sensitivity of the drug linkage, respectively. The high flexibility of CCPM facilitates the development of nanomedicinal products for specific therapeutic applications.",

keywords = "2023 OA procedure",

author = "Qizhi Hu and Rijcken, {Cristianne J.F} and {van Gaal}, Ethlinn and Paul Brundel and Hana Kostkova and Tomas Etrych and Benjamin Weber and Matthias Barz and Fabian Kiessling and Jai Prakash and Gerrit Storm and Hennink, {Wim E.} and Twan Lammers",

year = "2016",

doi = "10.1016/j.jconrel.2016.07.012",

language = "English",

volume = "244",

pages = "314--325",

journal = "Journal of controlled release",

issn = "0168-3659",

publisher = "Elsevier B.V.",

number = "Part B",

note = "14th European Symposium on Controlled Drug Delivery, ESCDD 2016, ESCDD ; Conference date: 13-04-2015 Through 15-04-2016",

}

Hu, Q, Rijcken, CJF, van Gaal, E, Brundel, P, Kostkova, H, Etrych, T, Weber, B, Barz, M, Kiessling, F, Prakash, J, Storm, G, Hennink, WE & Lammers, T 2016, 'Tailoring the physicochemical properties of core-crosslinked polymeric micelles for pharmaceutical applications', Journal of controlled release, vol. 244, no. Part B, pp. 314-325. https://doi.org/10.1016/j.jconrel.2016.07.012

TY - JOUR

T1 - Tailoring the physicochemical properties of core-crosslinked polymeric micelles for pharmaceutical applications

AU - Hu, Qizhi

AU - Rijcken, Cristianne J.F

AU - van Gaal, Ethlinn

AU - Brundel, Paul

AU - Kostkova, Hana

AU - Etrych, Tomas

AU - Weber, Benjamin

AU - Barz, Matthias

AU - Kiessling, Fabian

AU - Prakash, Jai

AU - Storm, Gerrit

AU - Hennink, Wim E.

AU - Lammers, Twan

N1 - Conference code: 14

PY - 2016

Y1 - 2016

N2 - To optimally exploit the potential of (tumor-) targeted nanomedicines, platform technologies are needed in which physicochemical and pharmaceutical properties can be tailored according to specific medical needs and applications. We here systematically customized the properties of core-crosslinked polymeric micelles (CCPM). The micelles were based on mPEG-b-pHPMAmLacn (i.e. methoxy poly(ethylene glycol)-b-poly[N-(2-hydroxypropyl) methacrylamide-lactate]), similar to the block copolymer composition employed in CriPec® docetaxel, which is currently in phase I clinical trials. The CCPM platform was tailored with regard to size (30 to 100 nm), nanocarrier degradation (1 month to 1 year) and drug release kinetics (10 to 90% in 1 week). This was achieved by modulating the molecular weight of the block copolymer, the type and density of the crosslinking agent, and the hydrolytic sensitivity of the drug linkage, respectively. The high flexibility of CCPM facilitates the development of nanomedicinal products for specific therapeutic applications.

AB - To optimally exploit the potential of (tumor-) targeted nanomedicines, platform technologies are needed in which physicochemical and pharmaceutical properties can be tailored according to specific medical needs and applications. We here systematically customized the properties of core-crosslinked polymeric micelles (CCPM). The micelles were based on mPEG-b-pHPMAmLacn (i.e. methoxy poly(ethylene glycol)-b-poly[N-(2-hydroxypropyl) methacrylamide-lactate]), similar to the block copolymer composition employed in CriPec® docetaxel, which is currently in phase I clinical trials. The CCPM platform was tailored with regard to size (30 to 100 nm), nanocarrier degradation (1 month to 1 year) and drug release kinetics (10 to 90% in 1 week). This was achieved by modulating the molecular weight of the block copolymer, the type and density of the crosslinking agent, and the hydrolytic sensitivity of the drug linkage, respectively. The high flexibility of CCPM facilitates the development of nanomedicinal products for specific therapeutic applications.

KW - 2023 OA procedure

U2 - 10.1016/j.jconrel.2016.07.012

DO - 10.1016/j.jconrel.2016.07.012

M3 - Article

SN - 0168-3659

VL - 244

SP - 314

EP - 325

JO - Journal of controlled release

JF - Journal of controlled release

IS - Part B

T2 - 14th European Symposium on Controlled Drug Delivery, ESCDD 2016

Y2 - 13 April 2015 through 15 April 2016

ER -

Tailoring the physicochemical properties of core-crosslinked polymeric micelles for pharmaceutical applications

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Keywords

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