To determine the fate of polymeric micelles after oral administration, we investigated the possible transport of polymeric micelles across Caco-2 monolayers and their biodistribution in rats after per os administration of [14C]-labelled mmePEG750P(CL-co-TMC) micelles containing risperidone (BCS Class II drug). mmePEG750P(CL-co-TMC) was able to cross Caco-2 monolayer via a saturable transport me...

We developed camptothecin (CPT)-conjugated, core-cross-linked (CCL) micelles that are subject to redox-responsive cleavage of the built-in disulfide bonds, resulting in disruption of the micellar structure and rapid release of CPT. CCL micelles were prepared via coprecipitation of disulfide-containing CPT-poly(tyrosine(alkynyl)-OCA) conjugate and monomethoxy poly(ethylene glycol)-b-poly(tyrosin...

Redox-sensitive micelles are designed by using block copolymers of different architectures composed of a hydrophilic block of poly(ethylene oxide), and hydrophobic blocks of poly(ϵ-caprolactone) and poly(α-azide-ϵ-caprolactone). Stability of these micelles is insured in diluted media by cross-linking their core via the addition of a bifunctional cross-linker, while redox sensitivity is provided...

E5880, a novel platelet activating factor receptor antagonist, was dispersed in water for the preparation of injectable formulation and the physicochemical properties of the micelles were characterized. The critical concentration for formation of micelles was 0.12 mM. Using the area per molecule results, the critical packing parameter was calculated and showed that the structure was composed of...

Reverse micelles in the AOT/water/isooctane system, at various water contents (W(0)), were studied using rheometry and small angle X-ray scattering (SAXS) experiments under static conditions and under shear. The SAXS analysis confirmed the spherical shape of the micelles at low water content and revealed a transition into elongated micelles at higher water content. A population of spherical mic...

Polymeric micelles with a controlled size in the range between 41 and 80 nm were prepared by injecting the organic phase through a microengineered nickel membrane or a tapered-end glass capillary into an aqueous phase. The organic phase was composed of 1 mg·mL(-1) of PEG-b-PCL diblock copolymers with variable molecular weights, dissolved in tetrahydrofuran (THF) or acetone. The pore size of the...

Amphiphilic poly(ε-caprolactone)-block-poly[2-(α-D-mannopyranosyloxy) ethyl acrylamide] (PCL-b-PManEA) block copolymers were synthesized via a combination of ring-opening polymerization (ROP), reversible addition-fragmentation chain transfer (RAFT) polymerization and reactive ester-amine reaction. The PCL-b-PManEA block copolymers can self-assemble into micelles and encapsulate anticancer drug ...

We have developed a dual-functional nanocarrier composed of a hydrophilic polyethylene glycol (PEG) and a hydrophobic farnesylthiosalicylate (FTS, a nontoxic Ras antagonist), which is effective in delivery of hydrophobic anticancer drug, paclitaxel (PTX). To facilitate the retention of the therapeutic activity of the carrier, FTS was coupled to PEG via a reduction-sensitive disulfide linkage (P...

Hydrotropic polymer micelle system has been developed for delivery of poorly water-soluble drugs such as paclitaxel. Hydrotropic polymers based on N,N-diethylnicotinamide were synthesized and used as a hydrophobic block for constructing amphiphilic block copolymers. The hydrotropic block copolymers self-assembled to form micelles in aqueous media. The size of the prepared polymer micelles was i...

For cancer therapy, folate (FA) and β-cyclodextrin (β-CD) decorated micelles based on the biodegradable pluronic F127-b-poly(ε-caprolactone) copolymer were fabricated. These micelles were measured by dynamic light scattering measurements and atomic force microscopy. The in vitro release of doxorubicin hydrochloride (DOX·HCl) from the biodegradable polymer micelles was performed in a phosphate-b...