Abstract: Methods are disclosed for preparing novel biodegradable nanoparticles based on complexation of poly-gamma-glutamic acid (?-PGA) or its cross-linked derivatives with bivalent lead ions. The final products are stable in aqueous media at low pH, neutral and mild alkaline conditions. The size of the complexes depends on the pH, concentrations and the ratios of ?-PGA and lead ions The ?-PGA nanoparticles made from biodegradable biopolymers with high flocculating and heavy metal binding activity of the present invention may be used for various water treatment applications in aqueous media.

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 is disclosed 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; (ii) an active compound selected from the group of epirubicin and its pharmaceutically acceptable salts, especially hydrochloride; and optionally (iii) at least one complexing agent, metal ion and stabilizer/formulating agent. The 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: A nanoparticulate composition is disclosed 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) paclitaxel as active compound; and optionally (iii) at least one complexing agent, a metal ion and a stabilizer/formulating agent or a PEGylating agent. The 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: 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: A nanoparticulate composition is disclosed 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 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: 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.

Abstract: Disclosed are novel, targeting, paramagnetic nanoparticles as contrast agent for magnetic resonance imaging. The compositions of the nanoparticles are composed of self-assembled polyelectrolyte biopolymers having targeting moieties, which can suitable for targeted delivery of paramagnetic ions complexed to the nanoparticles. The nanoparticulate contrast agent can internalize into the targeted tumor cells to realize the receptor mediated uptake, and therefore afford enhanced relaxivity and improved signal-to-noise effect on the examined tissue areas. Methods for making these targeting MRI contrast agents are also provided.

Abstract: Disclosed are novel, targeted, self-assembled nanoparticles radiolabeled with technetium-99m (Tc-99m) as radiodiagnostic compositions, methods of using these compositions and methods for preparing such radiolabeled compositions. Specifically, the compositions of the nanoparticles are composed of self-assembled polyelectrolyte biopolymers having targeting moieties, which can be suitable for targeted delivery of radionuclide metal ions complexed to the nanoparticles. These radiolabeled nanoparticles can specifically bind and internalize into the targeted tumor cells to realize the receptor mediated uptake. Radiolabeled, targeted nanoparticulate composition, methods for making, radiolabeling and using such compositions in the field of diagnosis and therapy are also provided.

Abstract: Macromolecular contrast agents for magnetic resonance imaging are described. Biomolecules and their modified derivatives form stable complexes with paramagnetic ions thus increasing the molecular relaxivity of carriers. The synthesis of biomolecular based nanodevices for targeted delivery of MRI contrast agents are described. Nanoparticles (NP) have been constructed by self-assembling of chitosan (CHIT) as polycation and poly-gamma glutamic acids (PGA) as polyanion. NP's are capable of Gd-ion uptake forming a particle with suitable molecular relaxivity. Folic acid (FA) is linked to the NP's to produce NP-FA bioconjugates that can be used for targeted in vitro delivery to a human cancer cell line.

Abstract: Methods are disclosed for preparing novel biodegradable cross-linked nanoparticles based on covalently cross-linking modifications of hyaluronic acid. The final products of the present invention are stable in aqueous media, and may be used as detergents and as additives for pharmaceutical compositions for drug delivery, DNA carrier system and other applications. The nanoparticles made from the biopolymers of the present invention may also be used in controlled release applications, super-absorbent materials as well as biomaterials like enzyme immobilization.

Abstract: The present invention relates to core/shell vinyl polymers wherein an at least partially crosslinked core is formed from a monovinyl monomer and/or a di/tri/ or higher multivinyl monomer wherein the degree of crosslinking in the core ranges from slight to high depending on the ratio of monovinyl and/or di/tri/ or higher multivinyl monomers, and wherein the outer shell is formed from a monovinyl and/or a di/tri/ or higher multi-vinyl monomer that optionally may be crosslinked, and wherein the outer shell has on its surface linear or branched C.sub.3-C.sub.30 alkyl chains formed from substituted vinyl monomers.

Abstract: Methods are disclosed for preparing crosslinked core and core-shell nanoparticle polymers from chitosan. The final products of the present invention may be used as detergents and as additives for pharmaceutical composition and for drug delivery, and DNA carrier system. The nanoparticles made from biopolymers of the present invention may also be used in controlled release, superabsorbent materials and biomaterials like enzyme immobilization.

Abstract: A method is disclosed in which modified and generic dental resins are combined as mixtures with reactive polymeric nanoparticles (RPNPs). Nanoparticles as additives clearly demonstrate that the RPNPs significantly influence the mechanical and shrinkage properties of the matrix and composites.

Abstract: Macromolecular contrast agents for magnetic resonance imaging are described. Biomolecules and their modified derivatives form stable complexes with paramagnetic ions thus increasing the molecular relaxivity of carriers. The synthesis of biomolecular based nanodevices for targeted delivery of MRI contrast agents are described. Nanoparticles (NP) have been constructed by self-assembling of chitosan (CHIT) as polycation and poly-gamma glutamic acids (PGA) as polyanion. NP's are capable of Gd-ion uptake forming a particle with suitable molecular relaxivity. Folic acid (FA) is linked to the NP's to produce NP-FA bioconjugates that can be used for targeted in vitro delivery to a human cancer cell line.

Abstract: The present invention relates to the preparation of hydrophilic nanoparticles and in particular hydrophilic nanoparticles that are biocompatible. Free radical monovinyl-divinyl monomer copolymerization/cross-linking reactions of water-soluble, monovinyl N-vinyl-2-pyrrolidone (NVP) with a bi-unsaturated divinyl, comonomer (poly{ethylene glycol}dimethacrylate) (PEGDMA), has been found to yield hydrophilic nanoparticles (NPs). These nanoparticles are built from three-dimensional nanopolymer networks. In the polymers' synthesis the composition of the monomers, and the total monomer concentration were varied. The characteristics of copolymers were determined by nuclear magnetic resonance spectroscopy (NMR), Fourier transform infrared (FTIR) and elemental analysis. Particle size and morphology of nanoparticles were confirmed by dynamic light scattering (DLS), transmission electron microscope (TEM) and scanning electron microscope (SEM) methods.