Issue 8, 2017

Clinical application of polymeric micelles for the treatment of cancer

Abstract

The in vivo administration of chemotherapeutic drugs is a challenge due to their poor pharmacokinetic (PK) and biodistribution profiles. For this reason, the development of delivery systems capable of targeting these compounds to pathological sites is of great importance. Polymeric micelles (PMs) are good systems for the encapsulation of hydrophobic compounds because their hydrophobic core can accommodate these types of drugs whereas their hydrophilic corona, usually poly(ethylene glycol), enables PMs to circulate for an extended period of time in the bloodstream which allows them to reach tumour tissues by means of the enhanced permeability and retention (EPR) effect. The first generation of PMs was rather unstable and essentially used to solubilize hydrophobic drugs for intravenous (i.v.) administration. More recently, the next-generation of PMs has been developed to achieve high encapsulation and retention of drugs while maintaining prolonged circulation after i.v. administration. These systems are suitable for both passive and active drug targeting. Different approaches have been employed to achieve the abovementioned goals: both non-covalent (hydrophobic and π–π interactions) and chemical (covalent binding of the drug to the polymer backbone and/or crosslinking of the core/shell) strategies have been used to improve the stability in the circulation and to retain the loaded drug in the PM. This will result in the accumulation of the drug at the target site to a greater extent than in healthy tissues and will, in principle, lead to improved therapeutic outcome. Several PM-based formulations are currently being evaluated in clinical trials. In this review, the pre-clinical and clinical outcomes of these PMs are summarized along with the strategies to translate PMs to patients.

Graphical abstract: Clinical application of polymeric micelles for the treatment of cancer

Article information

Article type
Review Article
Submitted
01 ноя 2016
Accepted
10 фев 2017
First published
13 фев 2017

Mater. Chem. Front., 2017,1, 1485-1501

Clinical application of polymeric micelles for the treatment of cancer

A. Varela-Moreira, Y. Shi, M. H. A. M. Fens, T. Lammers, W. E. Hennink and R. M. Schiffelers, Mater. Chem. Front., 2017, 1, 1485 DOI: 10.1039/C6QM00289G

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements