Targeted polymeric micelles for delivery of poorly soluble drugs

Abstract

Polymeric micelles (micelles formed by amphiphilic block copolymers) demonstrate a series of attractive properties as drug carriers, such as high stability both in vitro and in vivo and good biocompatibility, and can be successfully used for the solubilization of various poorly soluble pharmaceuticals. These micelles can also be used as targeted drug delivery systems. The targeting can be achieved via the enhanced permeability and retention effect (into the areas with the compromised vasculature), by making micelles of stimuli-responsive amphiphilic block copolymers, or by attaching specific targeting ligand molecules to the micelle surface. Immunomicelles prepared by coupling monoclonal antibody molecules to p-nitrophenylcarbonyl groups on the water-exposed termini of the micelle corona-forming blocks demonstrate high binding specificity and targetability. Immunomicelles prepared with cancer-specific monoclonal antibody 2C5 specifically bind to different cancer cells in vitro and demonstrate increased therapeutic activity in vivo. This new family of pharmaceutical carriers can be used for the solubilization and targeted delivery of poorly soluble drugs to various pathological sites in the body.

Tumor pH-responsive flower-like micelles of poly(l-lactic acid)-b-poly(ethylene glycol)-b-poly(l-histidine)

“…In tumor treatment the micelles system has proven effective in regression of tumor size while minimizing damage to the healthy tissues [4] and is being actively investigated in conjunction with hyperthermia [5], ultrasound [6], specific enzyme-induced cleavable bonds [7][8][9], and specific ligands or antibodies [10][11][12][13] for active targeting purposes.…”

Hydroxypropyl-β-Cyclodextrin Copolymers and Their Nanoparticles as Doxorubicin Delivery System

“…1,2 The size of micelles permits their extravasation and accumulation in a variety of pathological sites, where the permeability of the vascular endothelium is increased, such as infarct zones and tumors. [3][4][5][6] This fact provides a unique opportunity for physiology-based targeting of drugs and/ or drug-loaded pharmaceutical carriers, such as micelles, to these pathological areas via the enhanced permeability and retention (EPR; or "passive" targeting) effect. 7,8 An additional advantage of micelles as drug carriers, from the practical application view, is that they are easy to prepare on a large scale.…”

Novel Nanomaterials for Clinical Neuroscience

“…Polymeric micelles are another type of nanomaterial that have attracted considerable attention as carriers for drug delivery (Kataoka et al 2001;Kabanov and Alakhov 2002;Kwon 2003;Allen and Cullis 2004;Torchilin 2004;Aliabadi and Lavasanifar 2006) and diagnostic imaging agents (Torchilin 2002). These micelles form spontaneously in aqueous solutions of amphiphilic block copolymers and have core-shell architecture.…”