238 results about "Folate receptor" patented technology

A cell population expressing folate receptors is selectively targeted with a folate mimetic. The folate mimetic is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.

Conjugates of antifolates, releasable linkers, and drugs, and pharmaceutical compositions containing them are described. The conjugates are useful for treating diseases arising from pathogenic cell populations. Methods for treating such diseases are also described.

The present invention provides folate receptor binding ligand‐drug delivery conjugates having the formula (F) nL1L2D. The conjugates have high affinity to folate receptor‐positive tumor cells and low toxicity for normal cells. The present invention also relates to preparation methods for such conjugates, pharmaceutical compositions comprising such conjugates, and use of such conjugates for preparing anti‐tumor medicaments.

The invention provides compositions and methods for treating ovarian cancer. Specifically, the invention relates to administering a genetically modified T cell having alpha-folate receptor (FR-alpha) binding domain and CD27 costimulatory domain to treat ovarian cancer. In an embodiment, the FR-alpha binding domain is fully human, thereby preventing a host immune response.

The invention discloses a labeled 99mTc hydrazino-nicotinamide-dioxodecoyl-folic acid coordination compound with a general formula of 99mTc(HYNIC-NOON-FA)(Tricine)(L). In the structural formula, L is triphenyl sodium phosphate or triphenyl sodium photrisulfonic acid, wherein 1,8-diamido-3,6-octane dioxide is used as a connecting chain for generating a hydrazino-nicotinamide-3,6-dioxodecoyl-folic acid coupler respectively with folic acid and hydrazino-niacin through amido bonds and coordinating with oxygen atoms and phosphorus atoms in a co-ligand Tricine and an L molecule and 99mTc, and the 99mTc(HYNIC-NOON-FA)(Tricine)(L) coordination compound is obtained through two steps of: (a) synthesizing the hydrazino-nicotinamide-3,6-dioxodecoyl-folic acid coupler used as a ligand; and (b) labeling the 99mTc-hydrazino-nicotinamide-dioxodecoyl-folic acid coordination compound. The coordination compound has the advantages of high radiochemical purity, good stability, high tumor intake, good retention, low non-target organ background and clear tumor SPECT (Single Photon Emission Computed Tomography) development and can be prepared into a novel 99mTc labeled folic acid receptor tumor developer widely applied to the technical field of radioactive pharmaceutical chemistry and nuclear medicine.

The invention relates to a method for preparing medical nanoparticles and belongs to the technical field of nano material preparation. The method comprises the following steps: modifying poly(amidoamine) by polyethylene glycol; modifying folic acid on the polyethylene glycol; coating quantum dots by the poly(amidoamine) modified by the polyethylene glycol and the folic acid; clamping anti-cancer medicaments into poly(amidoamine) or connecting the medicaments to the surface of the poly(amidoamine); using oil-soluble quantum dots coated by the poly(amidoamine) as nano ligands of nuclear shell structures; modifying the folic acid and polyethylene glycol on the surface of the poly(amidoamine); and positioning the poly(amidoamine) onto the surfaces of tumor cells by using the special affinity between folic acid receptors on the surface of the tumor cells and the folic acid. Meanwhile, due to the special structural characteristics of PAMAM, the internal cavities of the poly(amidoamine) can hold the anti-cancer medicaments or the surface of the poly(amidoamine) can be connected with the anti-cancer medicaments, so the toxic and side effects of the medicaments on normal tissues are reduced greatly and the stability and water solubility of the quantum dots are improved.

The present invention relates to a novel selection system for use in a eukaryotic cell culture process and for expression of a recombinant product of interest. The selection system is based on the introduction of an exogenous functional membrane-bound folate receptor gene together with the polynucleotide or gene encoding the product of interest into a eukaryotic cell and can be widely utilized with eukaryotic cells for which cellular viability is dependent upon folic acid uptake.

The invention discloses a method for preparing folic acid coupled acetyl pullulan polysaccharide and the nanoparticles thereof, a preparation of drug-loaded nanoparticles which take the compound as the carrier and the role of the drug-loaded nanoparticles on the tumor cells. Firstly, the water soluble pullulan polysaccharide is converted to hydrophobic polymers by acetylation, so as to be conductive to the preparation of the nanoparticles and the loading of a hydrophobic drug, and the tumor cells with the high expression of the folate receptor can be targeted after the coupling of the folic acid by esterification. The drug-loaded nanoparticles are prepared by taking epirubicin as a model drug and adopting the solvent dispersion method, and the role of the drug-loaded nanoparticles on the tumor cells are evaluated by the in vitro cell uptake test. The results show that the method for preparing the folic acid-acetyl pullulan polysaccharide nanoparticles by the solvent dispersion method is simple, the reproducibility is good, the expanded production is easy, the drug-loading ratio is high, and the drug-loaded nanoparticles can be taken into the tumor cells by the route of the folate receptor.

The present invention discloses one kind of folic acid acceptor targeting liposome as medicine carrier and its preparation process and application. The liposome has components including synthetic phospholipid, cholesterol, folic acid acceptor targeting anchor point and polyglycol hydrating anchor point. The present invention has relatively simple preparation process, and can prepare liposome of size smaller than 200 nm in large scale and prepare freeze dried powder of weak alkali medicine, including leurocristine, etc. carried on the liposome with greatly raised use convenience and stability. The medicine is re-constructed with bacteria-free water or brine before use, and the medicine leakage rate is lower than 10 %.

The invention discloses a folic acid-modified O-carboxymethyl chitosan-deoxycholic acid complex which is an active-targeting nano-micelle carrier material prepared by using folic acid, O-carboxymethyl chitosan and deoxycholic acid as raw materials; O-carboxymethyl chitosan is used as a carrier material; deoxycholic acid is used for hydrophobicity reconstruction; folic acid is used for surface modification; and folic acid-mediated tumor tissue-targeting polymer micelle is prepared. Drug-loaded nano-micelle is prepared by a self-assembly method with paclitaxel as a model drug; experiment demonstrates that the drug-loaded nano-micelle has high drug load and encapsulation efficiency, has sustained release effect, is intaken into tumor cells through a folic acid acceptor approach, can increase the distribution of the drug in tumor tissue, thus improves curative effect, reduces toxic and side effect, and reaches the purpose of targeting treatment. The invention provides an ideal and novel drug carrier and preparation form for hard-soluble antitumor drugs.

The invention relates to a preparing method for a probe molecule which identifies tumor cells specifically, belonging to the nanometer material and biology technical field; the method comprises the following steps: (1) biocompatible folate is used for modifying PEG with the two sides being amino groups; (2) the PEG connected with the folate is modified to the surface of dendrimer PAMAM; (3) oil-soluble ligand on the surface of a quantum dot is replaced by a ligand exchange method, thus preparing a water-soluble quantum dot; the invention can lead the quantum dot to identify cancer cells expressed with high-level folate receptors, thus being capable of being used as a fluorescent probe used for the study of cytology; at the same time, the PAMAM and the PEG are modified to the surface of the quantum dot, thus improving the stability of the quantum dot greatly; furthermore, the PAMAM and the PEG have good biocompatibility and little toxicity, thus providing feasibility for the application thereof in the biology.

The invention discloses a folic acid-porous platinum-graphene oxide composite nano material as well as an application thereof in detecting tumor cells. The folic acid-porous platinum-graphene oxide composite nano material is prepared by the following steps: by taking graphene oxide as a substrate, carrying out amidation to crosslinked folic acid molecules; and carrying out in-situ synthesizing on platinum nano particles with porous structures. The folic acid-porous platinum-graphene oxide composite nano material can specifically identify a folate receptor on the surface of the cell, and meanwhile has a characteristic of simulating peroxidase and can catalyze hydrogen peroxide oxidized 3, 3', 5, 5'-tetramethyl benzidine hydrochloride to develop color. The number of the tumor cells can be quickly and agilely detected by means of chromogenic reaction, and 30 MCF-7 (Michigan Cancer Foundation-7) cells can be detected to the minimum extent. The material further can catalyze diaminobenzidine to generate a reddish brown precipitate on the surface of the cell so as to realize targeted positioning detection.

Disclosed are low-molecular weight, water-soluble chitosan nanoparticles with folic acid conjugated thereto as a target ligand and a preparation method thereof. The nanoparticles can be simply prepared since the strong reactivity of the chitosan allows folic acid to be readily introduced thereinto. Also, the folic acid-conjugated, low-molecular weight, water-soluble chitosan nanoparticles can be useful as gene carriers because they are of low or zero-toxicity, have sizes suitable for use as gene carriers, can readily form complexes with DNA, allow high gene expression rates, and are excellent in targeting tumor cells which are rich in folic acid receptors.

The invention discloses a targeting ginkgolide B solid lipid nanoparticle and a preparation method thereof. The ginkgolide B solid lipid nanoparticle targeting a blood brain barrier is prepared with an oil-in-water emulsion process by taking a ginkgolide B as a treating medicament, taking a solid lipid material as a carrier, taking a folic acid-modified surfactant as a targeting material and taking a mixture obtained by mixing a surfactant with the folic acid-modified surfactant in a certain ratio as an emulsifier. The particle diameter is 80-200 nanometers, and the polydispersion coefficient is 0.30+/-0.10. According to the solid lipid nanoparticle, a brain targeting effect is achieved by using the folic acid-mediated phagocytosis on the surfaces of brain cells and the phagocytosis way of adsorption of a brain cell membrane by using the nanoparticle.

The present invention discloses one kind of folic acid receptor mediated targeting chitosan carrier and its preparation process and application. The present invention has folic acid and its derivative as targeting agent, chitosan and its derivative as carrier and chemotherapeutic medicine adriamycin and other synergistic antisense nucleic acid as acting medicine to raise the stability and targeting property of the administration system. Therefore, the nanometer carrier has wide application foreground in treating tumor.

The present invention provides the synthetic method and superparamagnetic iron oxide nanoparticles capable of targeting to the folic acid receptors existing on the cell membranes and with high relaxivity. The iron oxide nanoparticles of the present invention can further be used as the contrast agents for magnetic resonance imaging (MRI).

The disclosure provides a liposomal antifolate composition comprising a liposome including an interior space, a bioactive antifolate agent disposed within said interior space, a steric stabilizer attached to an exterior of the liposome, and a targeting moiety comprising a protein with specific affinity for at least one folate receptor, said targeting moiety attached to at least one of the steric stabilizer and the exterior of the liposome.