Micelles are colloidal particles with a size around 5–100 nm which are currently under investigation as carriers for hydrophobic drugs in anticancer therapy. Currently, five micellar formulations for anticancer therapy are under clinical evaluation, of which Genexol-PM has been FDA approved for use in patients with breast cancer. Micelle-based drug delivery, however, can be improved in different ways. Targeting ligands can be attached to the micelles which specifically recognize and bind to receptors overexpressed in tumor cells, and chelation or incorporation of imaging moieties enables tracking micelles in vivo for biodistribution studies. Moreover, pH-, thermo-, ultrasound-, or light-sensitive block copolymers allow for controlled micelle dissociation and triggered drug release. The combination of these approaches will further improve specificity and efficacy of micelle-based drug delivery and brings the development of a ‘magic bullet’ a major step forward.

/pdf/polymeric-micelles-in-anticancer-therapy-targeting-imaging-95w28h8ukv.pdf

Polymeric Micelles in Anticancer Therapy: Targeting, Imaging and Triggered Release

3.2.1. Linear F-Alkyl/H-Alkyl Diblocks 1720 3.2.2. Unsaturated Diblocks 1721 3.2.3. Branched Diblocks 1722 3.2.4. Diblocks with Heteroatoms 1723 3.2.5. Diblocks with Heavy Halogens 1724 3.3. Triblocks and Multiblocks 1724 3.3.1. FnHmFn Triblocks 1724 3.3.2. HmFnHm Triblocks 1725 3.3.3. Star-Shaped Triblocks 1725 3.3.4. Multiblocks and Polyaffine Compounds 1726 4. Basic Properties of (F-Alkyl)alkyl Diblocks 1726 4.1. The “Polarity” Issues“Apolar”, yet Dipolar 1726 4.2. Surfactant Properties 1727 4.2.1. Surfactant Effects of FnHm Diblocks at Interfaces with Air, Fluorocarbons, and Hydrocarbons 1728

Chemistry, physical chemistry, and uses of molecular fluorocarbon--hydrocarbon diblocks, triblocks, and related compounds--unique "apolar" components for self-assembled colloid and interface engineering.

From being a niche area only a few decades ago, fluorous chemistry has gained momentum and is, nowadays, a fervent area of research. It has brought forth, in fact, numerous applicative innovations that stretch among different fields: from catalysis to separation science, from supramolecular to materials and analytical chemistry. Recently, the unique features of perfluorinated compounds have reached the attention of the biochemists' audience. This tutorial review introduces the basic concepts of fluorous chemistry and illustrates its main biomolecular applications. Special attention has been given to fluorous microarrays and their combination with Mass-Spectroscopy (MS) techniques, to protein properties modification by the introduction of local fluorous domains, and to the most recent applications of 19F-Magnetic Resonance Imaging (19F-MRI).

The fluorous effect in biomolecular applications

While knowledge of the composition and mode of action of bee and wasp venoms dates back 50 years, the therapeutic value of these toxins remains relatively unexploded. The properties of these venoms are now being studied with the aim to design and develop new therapeutic drugs. Far from evaluating the extensive number of monographs, journals and books related to bee and wasp venoms and the therapeutic effect of these toxins in numerous diseases, the following review focuses on the three most characterized peptides, namely melittin, apamin, and mastoparan. Here, we update information related to these compounds from the perspective of applied science and discuss their potential therapeutic and biotechnological applications in biomedicine.

/pdf/three-valuable-peptides-from-bee-and-wasp-venoms-for-1eksqwh8av.pdf

Three Valuable Peptides from Bee and Wasp Venoms for Therapeutic and Biotechnological Use: Melittin, Apamin and Mastoparan

Melittin, a major peptide component of bee venom, and its conjugates in cancer therapy.

The therapeutic potential of cytolytic peptides is plagued by nonspecificity and enzymatic degradation. We report the first stable incorporation of melittin (a 26 amino acid amphipathic peptide) into an outer lipid monolayer of perfluorocarbon nanoparticles. Melittin binds avidly to the nanoparticles (dissociation constant ∼3.27 nM) and retains its pore-forming activity after contact-mediated delivery to model bilayer membrane (liposomes) thereby demonstrating the effectiveness of perfluorocarbon nanoparticles as unique nanocarriers for cytolytic peptides.

/pdf/synthesis-and-characterization-of-stable-fluorocarbon-2a1ib488nm.pdf

Synthesis and Characterization of Stable Fluorocarbon Nanostructures as Drug Delivery Vehicles for Cytolytic Peptides

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Synthesis and Characterization of Stable Fluorocarbon Nanostructures as Drug Delivery Vehicles for Cytolytic Peptides