Abstract: A nanoparticulate composition is disclosed for the targeted therapeutic treatment of tumors. The stable self assembled nanocomposition according to the invention comprises (i) a carrier and targeting system comprising an optionally modified polyanion, and optionally a polycation, which may also be modified; at least one targeting agent which is linked to either the polycation/modified polycation or the polyanion/modified polyanion, or both or to the surface of the nanoparticle; (ii) an active compound selected from the group of docetaxel and its pharmaceutically acceptable salts and derivatives especially its hydrates, especially docetaxel trihydrate and docetaxel trihydrate monohydrochloride; and optionally (iii) at least one complexing agent, a metal ion and a stabilizer/formulating agent, or a PEGylating agent.

Abstract: A nanoparticulate composition for the targeted therapeutic treatment of tumors. The stable self assembled nanocomposition according to the invention comprises (i) a carrier and targeting system comprising an optionally modified polyanion, and optionally a polycation, which may also be modified; at least one targeting agent which is linked to either the polycation/modified polycation or the polyanion/modified polyanion, or both, or to the surface of the nanoparticle; (ii) an active compound selected from the group of doxorubicin and its pharmaceutically acceptable salts, especially hydrochloride; and optionally (iii) at least one complexing agent, a metal ion, a stabilizer/formulating agent, or a PEGylating agent. The present invention furthermore relates to a process for the preparation of the above-mentioned composition, the therapeutic uses thereof, and pharmaceutical compositions containing the nanocomposition according to the invention.

Abstract: Method and apparatus for characterizing drug-modified polymers, macromolecules, proteins, antigens, antibodies or nanoparticles and quantitative determination of their impurity profile by two-dimensional liquid chromatography analysis. The first dimension is preferably size exclusion chromatography (SEC)—which is also known as gel permeation chromatography in case of non-aqueous samples (GPC)—for complete molecular weight analysis of nanoscale particles. It is not just included the application of separating small molecules from big molecules, but it is also the separation of different sorts of oligomers (e.g. monomers, dimers, trimers, tetramers). The second dimension is adapted for separating and characterizing small molecules which can be impurities or non-reacted modifiers with high-performance liquid chromatography (HPLC). Between the dimensions it is feasible to use solid phase extraction column(s) to collect small molecules, wash off or change solvent, or minimize broadening of their peaks.

Abstract: The invention relates to cancer receptor-specific bioprobes for single photon emission computed tomography (SPECT) and computed tomography (CT) or magnetic resonance imaging (MRI) for dual modality molecular imaging. The base of the bioprobes is the self-assembled polyelectrolytes, which transport gold nanoparticles as CT contrast agents, or SPION or Gd(III) ions as MR active ligands, and are labeled using complexing agent with technetium-99m as SPECT radiopharmacon. Furthermore these dual modality SPECT/CT and SPECT/MR contrast agents are labeled with targeting moieties to realize the tumorspecificity.

Abstract: New types of nanoparticle-based dual-modality positron emission tomography/magnetic resonance imaging (PET/MRI) and positron emission tomography/computed tomography (PET/CT) tumorspecific contrast agents have been developed. The base of the new type contrast agents is biopolymer-based nanoparticle with PET, MRI and CT active ligands. The nanoparticle contains at least one polyanion and polycation, which form nanoparticles via ion-ion interaction. The self-assembled polyelectrolytes can transport gold nanoparticles as CT contrast agents, or SPION or Gd(III) ions as MRI active ligands, and are labeled using a complexing agent with gallium as PET radiopharmacon. Furthermore, these dual modality PET/MRI and PET/CT contrast agents are labeled with targeting moieties to realize the tumorspecificity.

Abstract: A nanoparticulate composition for the targeted therapeutic treatment of tumours. The stable self assembled nanocomposition according to the invention comprises (i) a carrier and targeting system comprising an optionally modified polyanion, and optionally a polycation, which may also be modified; at least one targeting agent which is linked to either the polycation/modified polycation or the polyanion/modified polyanion, or both, or to the surface of the nanoparticle; (ii) an active compound selected from the group of doxorubicin and its pharmaceutically acceptable salts, especially hydrochloride; and optionally (iii) at least one complexing agent, a metal ion, a stabilizer/formulating agent, or a PEGylating agent. The present invention furthermore relates to a process for the preparation of the above-mentioned composition, the therapeutic uses thereof, and pharmaceutical compositions containing the nanocomposition according to the invention.

Abstract: Targeting contrast agent for magnetic resonance imaging (MRI). In preferred embodiments, self-assembled polyelectrolytes coated superparamagnetic iron oxide contrast agent particles are provided, which are labeled with targeting moieties, afforded enhanced relaxivity, improved signal-to-noise and targeting ability. Accordingly, the invention relates to a stable targeting contrast nanosystem applicable for magnetic resonance imaging (MRI) having at least one nanoparticle polyelectrolyte polyanion; a targeting agent conjugated to the biopolymer; and a superparamagnetic ligand. In another embodiment the nanosystem according to the invention has at least two biocompatible and biodegradable nanoparticle polyelectrolyte biopolymer. Particularly, the superparamagnetic iron oxide particles are coated by a polyelectrolyte biopolymer and this system self-assembles with the other biopolymer to produce stable nanosystem for magnetic resonance imaging.