Core-crosslinked polymeric micelles: principles, preparation, biomedical applications and clinical translation

M. Talelli, M. Barz, C.J.F. Rijcken, F. Kiessling, W.E. Hennink, Twan Gerardus Gertudis Maria Lammers

Research output: Contribution to journalArticleAcademicpeer-review

199 Citations (Scopus)

Abstract

Polymeric micelles (PM) are extensively used to improve the delivery of hydrophobic drugs. Many different PM have been designed and evaluated over the years, and some of them have steadily progressed through clinical trials. Increasing evidence suggests, however, that for prolonged circulation times and for efficient EPR-mediated drug targeting to tumors and to sites of inflammation, PM need to be stabilized, to prevent premature disintegration. Core-crosslinking is among the most popular methods to improve the in vivo stability of PM, and a number of core-crosslinked polymeric micelles (CCPM) have demonstrated promising efficacy in animal models. The latter is particularly true for CCPM in which (pro-) drugs are covalently entrapped. This ensures proper drug retention in the micelles during systemic circulation, efficient drug delivery to pathological sites via EPR, and tailorable drug release kinetics at the target site. We here summarize recent advances in the CCPM field, addressing the chemistry involved in preparing them, their in vitro and in vivo performance, potential biomedical applications, and guidelines for efficient clinical translation.
Original languageEnglish
Pages (from-to)93-117
JournalNano today
Volume10
Issue number1
DOIs
Publication statusPublished - 2015

Fingerprint

Micelles
Paramagnetic resonance
Pharmaceutical Preparations
Disintegration
Prodrugs
Drug Delivery Systems
Drug delivery
Crosslinking
Tumors
Animals
Animal Models
Pharmacokinetics
Clinical Trials
Guidelines
Inflammation
Kinetics

Keywords

  • METIS-315279
  • IR-99653

Cite this

Talelli, M. ; Barz, M. ; Rijcken, C.J.F. ; Kiessling, F. ; Hennink, W.E. ; Lammers, Twan Gerardus Gertudis Maria. / Core-crosslinked polymeric micelles: principles, preparation, biomedical applications and clinical translation. In: Nano today. 2015 ; Vol. 10, No. 1. pp. 93-117.
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Core-crosslinked polymeric micelles: principles, preparation, biomedical applications and clinical translation. / Talelli, M.; Barz, M.; Rijcken, C.J.F.; Kiessling, F.; Hennink, W.E.; Lammers, Twan Gerardus Gertudis Maria.

In: Nano today, Vol. 10, No. 1, 2015, p. 93-117.

Research output: Contribution to journalArticleAcademicpeer-review

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AU - Barz, M.

AU - Rijcken, C.J.F.

AU - Kiessling, F.

AU - Hennink, W.E.

AU - Lammers, Twan Gerardus Gertudis Maria

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