ROS-responsive copolymer micelles for inflammation triggered delivery of ibuprofen.

Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly used for the treatment of pain, inflammation and fever. However, most NSAIDs are poorly water soluble, making it difficult to be administered thus high doses are required to reach the intended therapeutic effect, resulting in associated side effects. In this study, ROS-responsive micellar systems based on a block copolymer consisting of methylpropyl thioether (MTPA) and N'N-dimethylacrylamide was developed and loaded with ibuprofen (IBU). Using lipopolysaccharide activated RAW 264.7 macrophage like cells, we demonstrated that IBU was released from the copolymer, specifically in the presence of ROS. Interestingly, IBU encapsulated in ROS-responsive nanoparticles exhibited greater anti-inflammatory potency compared to its free form. The work highlights the potential of the ROS-responsive micellar system developed in this work to be used as carrier of NSAIDs for the treatment of relevant inflammatory conditions.

Physical Texturing for Superhydrophobic Polymeric Surfaces: A Design Perspective.

Surface wetting on the textured surface is classically explained by the theories of Cassie-Baxter or Wenzel. However, in recent years, an increasing number of complex surface topographies with superhydrophobic properties have been achieved without prediction or simulation using these theories. One example is biomimetic surfaces. In many instances, theories were used to explain surface properties found in nature but have not led to or predicted the complex topographies. Although new wetting theories continue to emerge, there is not yet a set of design rules to guide the selection of surface topographies to achieve superhydrophobicity. By grouping known surface topographies into common geometrical descriptions and length scale, this paper suggests a set of surface topography classifications to provide selection guidelines for engineering superhydrophobic surfaces. Two key outcomes emerged from the design analysis: first, categorization of frequently reported surface patterns shows that there exists a set of commonly used descriptions among diverse designs; second, the degree of hydrophobicity improvement within a class of topography design can be used to predict the limit of improvement in superhydrophobicity for a given material. The presentation of topography descriptors by categories of design and performance may serve as a prologue to an eventually complete set of design guidelines for superhydrophobic performance.

Mechano-responsive polymer solutions based on CO2 supersaturation: shaking-induced phase transitions and self-assembly or dissociation of polymeric nanoparticles.

Mechanical stimulation of supersaturated aqueous CO2 solutions is accompanied by a pH increase within seconds. In solutions of tailored homo- and AB diblock copolymers this is exploited to induce micelle formation, or, taking advantage of an aqueous upper critical solution temperature transition, nanoparticle disassembly.

Amidine functionality as a stimulus-responsive building block.

This mini-review describes basic features and applications of small molecules and macromolecules containing amidine, and to a lesser extent, guanidine functional groups. The emphasis in this article is on the exploitation of such functionality as species that are capable of reversibly binding carbon dioxide in the presence of water, a process that also commonly involves a hydrophobic-to-hydrophilic transition. The review is not intended to be exhaustive but rather serves to highlight this one particular feature and demonstrate its application in areas ranging from reversible emulsion stabilization, purification and reversible self-assembly of polymeric nanoparticles.

Block copolymer micelles with pendant bifunctional chelator for platinum drugs: effect of spacer length on the viability of tumor cells.

Three monomers with 1,3-dicarboxylate functional groups but varying spacer lengths were synthesized via carbon Michael addition using malonate esters and ethylene- (MAETC), butylene- (MABTC), and hexylene (MAHTC) glycol dimethacrylate, respectively. Poly[oligo-(ethylene glycol) methylether methacrylate] (POEGMEMA) was prepared in the presence of a RAFT (reversible addition-fragmentation chain transfer) agent, followed by chain extension with the prepared monomers to generate three different block copolymers (BP-E80, BP-B82, and BP-H79) with similar numbers of repeating units, but various spacer lengths as distinguishing features. Conjugation with platinum drugs created macromolecular platinum drugs resembling carboplatin. The amphiphilic natures of these Pt-containing block copolymers led to the formation micelles in solution. The rate of drug release of all micelles was similar, but a noticeable difference was the increasing stability of the micelle against dissociation with increasing spacer length. The platinum conjugated polymer showed high activity against A549, OVCAR3, and SKOV3 cancer cell lines exceeding the activity of carboplatin, but only the micelle based on the longest spacer had IC(50) values as low as cisplatin. Cellular uptake studies identified a better micelle uptake with increasing micelle stability as a possible reason for lower IC(50) values. The clonogenic assay revealed that micelles loaded with platinum drugs, in contrast to low molecular weight carboplatin, have not only better activity within the frame of a 72 h cell viability study, but also display a longer lasting effect by preventing the colony formation A549 for more than 10 days.