43results about How to "Enhance amphipathic" patented technology

The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier ("BBB") and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugate comprises a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.

Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, subcutaneous, and intravenous forms of the compounds and conjugates may be prepared as treatments and / or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.

Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and / or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.

The present invention relates generally to hydrolyzable drug-oligomer conjugates, pharmaceutical compositions comprising such conjugates, and to methods for making and using such conjugates and pharmaceutical compositions. For example, a conjugate of insulin, PEG, and oleic acid can be orally administered.

The invention features echinocandin class compounds. The compounds can be useful for the treatment of fungal infections.

The invention relates to a polymer viscosity reducer for thickened oil. The polymer viscosity reducer is a hydrophobically modified polyacrylamide and has a structural formula shown as formula (I), wherein n represents the total number of polyacrylamide monomers, ranges from 60,000 to 100,000, preferably from 7,000 to 85,000; x represents the number of acrylic monomers, ranges from 10,000 to 40,000, preferably 20,000 to 350,000; m represents the number of hydrophobic monomers, and ranges from 4000 to 10000, preferably from 6000 to 8000. The invention also relates to a preparation method and application of the polymer viscosity reducer for thickened oil.

The invention features echinocandin class compounds. The compounds can be useful for the treatment of fungal infections.

The invention discloses a double-targeted phthalocyanine anti-cancer photosensitizer and a preparation method thereof. Micromolecular target drugs N-(3-chloro-4-fluorophenyl)-7-methoxyl-6-(3-morpholine-4-propoxy) quinazoline-4-amine connected via alcoxyl long chains are introduced on a phthalocyanine parent ring in the axial direction to improve the amphipathy, biocompatibility and the targeting property of the photosensitizer; and a triphenylphosphine group is introduced at the other end of the phthalocyanine parent ring in the axial direction, thus, the photosensitizer can be selectively, accurately and intelligently positioned on mitochondria of tumor cells with overexpressed epidermal growth factor receptors (EGFR), and the photodynamic action efficiency is improved. The compound is single in structure and determined in composition, and does not have isomers, products are easy to separate and purify, meanwhile, the complexes are not easy to gather, and the cell uptake rate is increased favorably.

The invention discloses a piperazine-modified phthalocyanine complex as well as a preparation method and an application thereof. Piperazine molecules are introduced into the macrocyclic periphery of a metal phthalocyanine so as to enhance the amphipathy, the biocompatibility and the targeting of the phthalocyanine. A piperazine group contains two N atoms, so that after the synthesized phthalocyanine complex enters a tissue, if the tissue is normal, the single excitation state of the phthalocyanine can be quenched by lone pair electrons on the N atoms of the piperazine group under a light irradiation condition. Thus, the generation of singlet oxygen is avoided. If the tumor tissue is in a weak acid state, the N atoms are protonated, so that the single excitation state of the phthalocyanine cannot be quenched. Therefore, the singlet oxygen is generated so as to kill tumor cells. Based on the theory, the selectivity of the photodynamic therapy of the phthalocyanine is improved due to the introduction of the piperazine group, so that the damage of the phthalocyanine to the normal tissue is reduced. The piperazine-modified phthalocyanine complex has a single structure and does not contain isomers, and is easy to purify and low in cost, thereby being favorable for industrial production.

The invention discloses a heparin nano-drug loading system for loading an amido anti-tumor drug. The drug loading system is a conjugate for loading the amido anti-tumor drug on PEGylated heparin molecules. Natural polysaccharide heparin which is biodegradable, good in compatibility and high in availability is used as a drug carrier, and PEG modification and the amino anti-tumor drug are combined,so that nanoparticles show an anti-tumor treatment index and biological safety which are remarkably enhanced compared with those of a free drug in in-vivo treatment.

The invention discloses a PEGylated heparin nano-micelle for loading a carboxylic acid anti-tumor drug. A drug loading system is a conjugate for loading the carboxylic acid anti-tumor drug on PEGylated heparin molecules. Natural polysaccharide heparin which is biodegradable, good in compatibility and high in availability serves as a drug carrier, and PEG modification and the carboxylic acid anti-tumor drug are combined, so that nanoparticles show an anti-tumor treatment index and biological safety which are remarkably enhanced compared with those of a free drug in in-vivo treatment.

The invention relates to an adamantane-containing quaternary ammonium salt ionic liquid and a preparation method thereof. The structural formula of the adamantane-containing quaternary ammonium salt ionic liquid designed and prepared by the invention is shown in the specification, and in the formula, n is equal to 6, 9 or 11. According to the adamantane-containing quaternary ammonium salt ionic liquid disclosed by the invention, 1-adamantanecarboxylic acid is used as a raw material, and the ionic liquid is prepared by the following three steps: firstly, carrying out acylating chlorination reaction on 1-adamantanecarboxylic acid and thionyl chloride to synthesize 1-adamantanecarbonyl chloride, carrying out esterification reaction on the 1-adamantanecarbonyl chloride and OH(CH2)nBr, and thencarrying out quaternization with N,N-dimethylbenzylamine to form the adamantane-containing quaternary ammonium salt ionic liquid. The adamantane-containing quaternary ammonium salt ionic liquid obtained in the invention has the characteristics of mild reaction conditions, easily available raw materials and high product purity, and has potential application prospects in the fields of supramolecular chemistry, catalysis, batteries, nano materials and the like.

The invention belongs to the technical field of medicines, particularly relates to a paclitaxel lipid nanoparticle preparation method and provides a method for preparing paclitaxel lipid nanoparticles easy for intestinal mucosae to absorb. The method includes the steps: (1) preparing paclitaxel solid lipid nanoparticle according to a film dispersion method; (2) preparing SA-R8-PTX-SLN according to an incubation method, to be more specific, precisely weighing 10mg of SA-R8, adding into 5ml of PTX-SLN dispersion liquid, magnetically stirring, staying overnight at a temperature of 4 DEG C to obtain the SA-R8-PTX-SLN; (3) precisely weighing 10mg of paclitaxel, putting into a 100ml volumetric flask, dissolving in methyl alcohol to a certain volume, and well shaking to obtain a PTX methanol stock solution with the density being 100 microgram / ml; (4) putting 1ml of SLN containing paclitaxel in a dialysis bag (14000 in molecular weight), tightening two ends of the dialysis bag, respectively adding 100ml of dissolution media, observing paclitaxel release conditions under the conditions of 37 DEG C and 100r / min, taking 1ml of dialysis media, lyophilizing, adding 0.25ml of methanol, whirling, centrifuging at a high speed, and taking supernatant for sampling by 20 microlitres.

The invention discloses a poloxamer-adriamycin conjugate with an anti-tumor effect and a preparation method thereof. The poloxamer-adriamycin conjugate has micelle property, is a high-molecular polymer which contains terminal carboxyl group and is prepared by reaction between poloxamer and succinic anhydride, and the terminal carboxyl group in the polymer and primary amino radical in adriamycin are directly bound in an amido link way. Compared with an adriamycin raw material drug, the poloxamer-adriamycin conjugate has the following advantages: the anti-tumor activity of the covalent bonding adriamycin in the poloxamer-adriamycin conjugate is maintained, the drug resistance of tumor is reduced; the poloxamer-adriamycin conjugate has the property of self-assembly formed micelle, and the critical micelle concentration of the conjugate is lower than that of polyxamer; and the micelle of the poloxamer-adriamycin conjugate can be entrapped with other medicaments with the anti-tumor effect in a physical entrapping mode, so that the aim of combined treatment of anti-tumor medicaments can be achieved.

The invention relates to an amphiphilic fluorescent conjugated polymer, a preparation method and an application. The present invention adopts Sonogashira coupling and ester group hydrolysis reaction to obtain an amphiphilic conjugated macromolecule that contains both hydrophilic carboxylate groups and hydrophobic alkoxy side groups in a repeating unit, and dissolves it in In a mixed solvent with a volume ratio of tetrahydrofuran and water of 1:1, it is used for rapid sensing and detection of neomycin in water. The use of this amphiphilic fluorescent conjugated polymer can realize the specific detection of neomycin, and has a fluorescent color change that can be recognized by the naked eye, and the result can be obtained without the use of a large-scale instrument, and the operation is convenient. Realize more convenient, fast and efficient detection in practical application.

The invention discloses a PEGylated heparin nano-micelle loaded with carboxylic acid antineoplastic drugs. The drug loading system is a conjugate of carboxylic acid antineoplastic drugs loaded on PEGylated heparin molecules. Using the natural polysaccharide heparin, which is biodegradable, good compatibility and high availability, as a drug carrier, by combining PEG-modified and carboxylic acid anti-tumor drugs, the nanoparticles exhibit significantly enhanced anti-tumor therapy than free drugs in in vivo treatment Index and biosecurity.