Micelles based on HPMA copolymers

• Published in: Advanced drug delivery reviews 2010-02, Vol.62 (2), p.231-239
• Main Authors: Talelli, M., Rijcken, C.J.F., van Nostrum, C.F., Storm, G., Hennink, W.E.
• Format: Article
• Language: English
• Subjects: Acrylamides - chemistry; Animals; Drug delivery; Drug Delivery Systems - methods; Drug Delivery Systems - trends; Drug targeting; EPR effect; HEMAm; HPMA; Humans; Micelle core; Micelle corona; Micelles; N-(2-hydroxylpropyl) methacrylamide; Nanomedicine - methods; Nanomedicine - trends; Polymeric micelles; Polymers - chemistry
• ISSN: 0169-409X; 1872-8294
• DOI: 10.1016/j.addr.2009.11.029

Polymeric micelles have been under extensive investigation during the past years as drug delivery systems, particularly for anticancer drugs. They are formed by the self-assembly of amphiphilic block copolymers in aqueous solutions and have a spherical shape and a size in the nano-range (< 200 nm). Tumor accumulation of polymeric micelles upon intravenous administration can occur as a result of the leaky vasculature of tumor tissue (called the enhanced permeation and retention (EPR) effect).To benefit from the EPR effect, polymeric micelles need to have prolonged circulation times as well as high and stable drug loadings. Poly[N-(2-hydroxypropyl) methacrylamide] (pHPMA) is a hydrophilic polymer currently under investigation for its use in polymer–drug conjugates. Its biocompatibility, non-immunogenicity and the possibility for functionalization are properties that resulted in broad pharmaceutical and biomedical applications, also in the micelle technology research. Being hydrophilic, it can serve as a micellar stealth corona, while it can also be modified with hydrophobic moieties to serve as a micellar core in which hydrophobic drugs can be solubilized and retained. HPMA-based polymeric micelles have been showing very promising in vitro and in vivo results. This review summarizes the applications of pHPMA in the field of polymeric micelles, either serving as a micellar stealth corona, or, if hydrophobically rendered by derivatization, as a micellar core.