PAMAM dendrimer based CEST imaging agents, pharmaceutical compositions comprising the same and methods of uses thereof are disclosed.

The present invention relates to a hyperbranched polyether of formula (I) R.sub.mQ.sub.n-0-R.sup.1 (I), wherein Q is a branching unit of formula, n is 2.sup.k1, m is 2.sup.k, k is 2, 3, 4, 5 or 6, each R is independently a hydrocarbon radical having at least 10 carbon atoms, R.sup.1 is a polymer having a number average molecular weight M.sub.n of at least 250 g/mol, wherein each branching unit Q is connected via ether linkage to adjacent branching units Q and each terminal oxygen of Q, not connected to adjacent branching units Q, is connected to R via ether linkage, as well as mixtures thereof. The present invention further relates to formulations comprising said hyperbranched polyether or mixture of ethers as well as their use.

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Provided are a method for preparing a polyamide by using a molecular weight controller having a double active group in anionic ring-opening copolymerization of a polyamide, thereby enabling molecular weight to be controlled through the addition reaction of the molecular weight controller, and a polyamide prepared thereby.

The present invention relates to new molecular design that allows micelles to report their activation and disassembly by an enzymatic trigger. The molecular design is based on introduction of a labeling moiety selected from a fluorescent dye, a dark quencher, combinations of dyes or dyes/quenchers, and a fluorinated moiety (a .sup.19F-magenetic resonance (MR) probe for turn ON/OFF of a .sup.19F-MR signal) through covalent binding to the focal point of amphiphilic polymer-dendron hybrids with the labeling moiety. At the assembled micellar state, the dyes are closely packed and hence the probability for intermolecular interactions increases significantly, leading to alteration of the fluorescent properties (signal quench or shift) or the .sup.19F-MR signal (OFF state) of the micelles. Upon enzymatic cleavage of the hydrophobic end-groups from enzyme-responsive dendron, the polymers become hydrophilic and disassemble. This structural change is then translated into a spectral change as dye-dye interactions are halted and the dyes regain their intrinsic fluorescent properties, or alternatively by turn ON the .sup.19F-MR signal. The high modularity of the design allows the introduction of various types of dyes and thus enables rational adjustment of the spectral response. Two major types of responses are described: Turn-On/Off and spectral shift, depending on the type of labeling dye. The present invention further provides methods of use of the hybrid delivery system and to a kit comprising the same.

Dendrimer-based compositions and methods are provided, that are useful for administering pharmaceutical compositions to target cells and tissues for treatment of ocular diseases including macular degeneration, diabetic retinopathy, and retinitis pigmentosa.

Provided herein are dendrimers comprising: a core unit, five generations of building units which are lysine residues or analogues thereof, first terminal groups comprising a cabazitazel residue covalently attached to a diglycolyl linker group, and second terminal groups comprising a PEG group. Also provided herein are pharmaceutical compositions comprising the dendrimers, and methods and uses of the dendrimers in therapy of disorders such as cancers. Processes for making the dendrimers and intermediates are also provided.

A polymer composition comprising star macromolecules is provided. Each star macromolecule has a core and five or more arms, wherein the number of arms within a star macromolecule varies across the composition of star molecules. The arms on a star are covalently attached to the core of the star; each arm comprises one or more (co)polymer segments; and at least one arm and/or at least one segment exhibits a different solubility from at least one other arm or one other segment, respectively, in a reference liquid of interest.

Particles comprising a branched polymer and either a block copolymer or a linear dendritic hybrid represent a category of useful materials. They may be used in for example drug delivery applications. They may be prepared by a method comprising the steps of: dissolving the branched polymer and block copolymer or linear dendritic hybrid, and optionally other component(s), in a solvent to form a solution; adding said solution to a different liquid; and removing said solvent to form a dispersion of co-precipitated particles.

Methods for processing polynucleotide-containing biological samples, and materials for capturing polynucleotide molecules such as RNA and/or DNA from such samples. The RNA and/or DNA is captured by polyamindoamine (PAMAM (Generation 0)) bound to a surface, such as the surface of magnetic particles. The methods and materials have high efficiency of binding RNA and of DNA, and of release, and thereby permit quantitative determinations.

The present invention is related to a targeted type shell for drug delivery system. The object of the present invention is to provide the targeted type shell for DDS, which comprises a carbosilane dendrimer containing a silole produced by which is formed by utilizing the reaction between thiol group and alkyl halide, and a targeted protein containing a labeled proteins such as green fluorescent protein with a target recognition site. The shell may incorporate compounds having a variety of molecular weight and biopolymers, and selectively deliver them into targeted cells.