285 results about "Peg modification" patented technology

The invention provides a folic acid and polydopamine modified tumor targeted mesoporous silica nanoparticle and a preparation method and application thereof. The preparation method particularly comprises the following steps: (1) dissolving mesoporous silica and a chemical in a solvent, performing a full reaction, and performing separation; (2) adding mesoporous silica initial nano-particles obtained in the step (1) in a solution, adding dopamine hydrochloride, performing a full reaction, and performing separation; and (3) adding the dopamine hydrochloride coated mesoporous silica initial nano-particles loaded with the chemical in a weakly basic water solution, sequentially adding a reducing agent and polyethylene glycol modified sulfydryl grafted targeted ligand folic acid, performing a full reaction, then performing separation to obtain the folic acid and polydopamine modified tumor targeted mesoporous silica nanoparticle. The preparation method of the folic acid and polydopamine modified tumor targeted mesoporous silica nanoparticle is simple, and favorable tumor targeting ability, biocompatibility and biodegradability are achieved.

The invention discloses a mono-functionalized polyethylene glycol with a nitrogen atom branched center and its preparation method and biologically-relevant matter. The mono-functionalized polyethylene glycol with a nitrogen atom branched center is shown in the general formula (1). The polyethylene glycol-modified biologically-relevant matter is shown in the general formula (2). X1 and X2 represent alkyl containing 1-20 carbon atoms, n1 and n2 are integers of 2-2000, n3 is an integer of 1-2000, L1, L2 and L3 represent connection groups stably existing under the conditions of light, heat, enzyme, redox, acidic or alkaline condition, R represents a functional group or is in a protected form, D represents a biologically-relevant matter, Z1 represents a connection group, and L4 represents residue formed by a reaction of R and the biologically-relevant matter. The branched polyethylene glycol with the nitrogen atom center can interact with a substrate easily so that the substrate protection based on polyethylene glycol is promoted, the state of the substrate in the human body can be effectively improved and a prospect is wide.

Glutenase proteins, such as prolyl endopeptidases, are stabilized by covalent PEG modification.

A novel anti-polyethylene glycol monoclonal antibody and its preparation are disclosed. Such an antibody can be used for determining polyethylene glycol concentration in vitro or accelerating the clearance of a polyethylene glycol containing compound from the blood circulation in the human body thereby reducing the toxicity associated with the polyethylene glycol containing conjugate. The antibody is particularly useful in cancer therapy where the therapeutic agent is selectively delivered to the tumor by increasing the tumor / blood ratio of the polyethylene glycol containing compound.

The invention discloses a thiol-polyethylene glycol modified magneto-optical composite nano-material and its application. An up-conversion nano material is taken as a basal layer, the surface of the basal layer is provided with a polyacrylic acid layer, the surface of the polypropylene layer is provided with a layer of dopamine modified ferriferrous oxide magnetic particles, a golden shell layer is covered on the dopamine modified ferriferrous oxide magnetic particles layer, and the thioctic acid modified polyethylene glycol is provided on the golden shell layer; the thiol-polyethylene glycolmodified magneto-optical composite nano-material has guidance functions of up-conversion imaging and magnetic resonance imaging dual imaging, under the physical induction action of the magnetic field, the nano-material of the invention enables magnetic targeting to the specific position, so that the distribution in other internal organs can be reduced, and the damage in other internal organs during the treatment process is reduced. The nano-material can be taken as a good reagent for photo-thermal treatment by using the strong absorption property on the surface. The magnetic targeting photo-thermal treatment is combined under the imaging guidance, thereby the composite nano-material of the invention plays an important effect in clinical medical science and biological technology in future.

The invention discloses a preparation method of RGD-modified ultra-small magnetic iron oxide nanoparticles. The preparation method comprises the following steps: preparing ultra-small magnetic iron oxide nanoparticles by taking ferric acetylacetonate as a reaction raw material and a precursor, taking oleylamine as a surfactant and a reducing agent and taking dibenzyl ether as a solvent; replacing oleylamine molecules wrapped on the surfaces of the nanoparticles by utilizing dopamine-modified HOOC-PEG-COOH to realize PEG-modification of the surfaces of the nanoparticles; and finally, chemically coupling RGD cyclic peptide by virtue of free carboxyl at the tail end of the PEG to obtain the RGD-modified ultra-small magnetic iron oxide nanoparticles. The method of synthesizing the ultra-small magnetic iron oxide nanoparticles has the characteristics of a simple process, a high raw material conversion ratio, strong repeatability and the like. The synthesized magnetic iron oxide nanoparticles have the characteristics of a regular morphology, an ultra-small dimension, good stability, good monodispersity, high biocompatibility, and tumor specific targeting, and the like, and can be used as a T1-weighted imaging high-performance magnetic resonance imaging contrast agent with a tumor active targeting function.

The present invention relates to a compound comprising a peptide moiety, a spacer moiety and a water-soluble polymer moiety such as a poly(ethylene glycol) moiety. The spacer moiety is between the peptide moiety and the water-soluble polymer moiety. The spacer moiety has the structure: —NH—(CH2)α—[O—(CH2)β]γ—Oδ—(CH2)ε—Y—wherein α, β, γ, δ, and ε are each integers whose values are independently selected.

The invention provides a liposome-modified spermine derivative and a liposome prepared by the derivative. The spermine derivative is directly applied or is mixed with one or more selected from cholesterol, neutral lipids and polyethylene glycol (PEG)-modified lipids, which can be adopted as a carrier for entrapping or absorbing bioactive molecular drugs to be loaded into cells. In this way, the effect of regulation, intervention or treatment is realized. In a general formula (1), X1 represents -(CH2)- or carbonyl group, wherein n represents 1, 2 or 3; X2 represents -(CH2)-, ester group, amide group, oxygen, or sulfur; R1 and R2 independently represent C6-C18 alkyl group or lipophilic cholesterol molecules, respectively.

The invention relates to a preparation method of Fe3O4 / Au composite nanoparticles, which comprises the following steps: carrying out PEG modification on PEI; coating the PEI subjected to PEG modification so as to synthesize gold nanoparticles; synthesizing PEI-coated Fe3O4 / Au composite nanoparticles by using a hydrothermal method; and carrying out surface acetylation modification on the PEI-coated Fe3O4 / Au composite nanoparticles. According to the invention, the reaction conditions are mild, and the synthetic steps are simple; and prepared Fe3O4 / Au composite nanoparticles are good in colloidal stability, biocompatibility, T2 relaxation effect and X-ray attenuation properties, and have a potential application value in the field of MR / CT bi-modal imaging diagnosis.

The invention relates to a series of polyethylene glycol modified cationic antibacterial peptide with different molecular weight. The modified antibacterial peptide is self-assembled into a nanometer micelle in an aqueous medium. The formation of the micelle can play a role in protecting the antibacterial peptide and weakening the degradation effect of protease on the antibacterial peptide, and simultaneously improves the stability and antibacterial activity of polypeptide in serum. In addition, the modification of polyethylene glycol obviously reduces the hemolytic toxic side effects of the antibacterial peptide.

A high-molecular mPEG-PLGA-mPEG (PELGE) used as the axcessory of injection, oral-applied medicine, and the water-soluble medicine or the medicine difficult to dissolve in water is an amphipathic three-block copolymer, which is prepared from stannous octoate as catalyst, diisocyanate as coupling agent, polyethene glycol with single terminated end, glycollide, and lactide or polylactic acid-glycollic acid copolymer.

The invention relates to a preparation method of meso-porous silicon nanoparticle with reducing / enzyme dual response and targeting property. The preparation method of the meso-porous silicon nanoparticle with the reducing / enzyme dual response and targeting property comprises the following steps: synthesizing a meso-porous silicon nanoparticle; modifying a disulfide bond on the surface of the meso-porous silicon nanoparticle by adopting a chemical method, and grafting the disulfide bond with hyaluronic acid as a targeting molecule; by taking carboxyl on the targeting molecule as a reaction site, modifying polyethylene glycol to the surface of the compound nanoparticle, thus improving biocompatibity of the nanoparticle, and connecting the hyaluronic acid molecule with the targeting effect to the surface of the nano particle, thus obtaining the meso-porous silicon nanoparticle diagnosis agent with medicinal response releasing and imaging functions. The prepared particle has good dispersity, is uniform in particle size and is easy to prepare, the prepared multifunctional diagnosis agent has good biocompatibility, medicine can be released in a tumour part in a responding manner, and diagnosis integration of the tumour can be realized.

The invention discloses a mutated hFGF-21 protein mature peptide and coding gene and applications thereof, as well as polyethylene glycol-modified mutated hFGF-21 protein mature peptide and applications thereof. The mutated hFGF-21 protein mature peptide is protein shown in sequence 3 of a sequence table. The invention further discloses a conjugate of the protein and polyethylene glycol, namely the protein is modified by the polyethylene glycol. The drug for treating diabetics has a good hypoglycemic activity, especially the drug taking the conjugate as an active ingredient also has the advantages of being high in stability, long in half-life period, low in immunogenicity and the like.

Disclosed herein are exendin singly modified with polyethylene glycole or a derivative thereof, a method for the preparation of the same, and uses thereof. Exendin modified at lysine (27) with polyethylene glycol shows biological activity similar to that of natural exendin, but is improved in half life. In addition, the modification position and the number of PEG or its derivative are restricted so as to minimize the side effects caused by a variety of combinations of such factors. The exendin is useful in the prevention and treatment of diseases caused by the over-secretion of insulin, or diseases caused due to a decrease in plasma glucose level, the inhibition of gastric or intestinal motility, the promotion of satiety, or the inhibition of food intake, especially diabetes, obesity and irritable colon syndrome.

The invention discloses a nano probe material for imaging, which is capable of efficiently breaching blood-brain barriers. Firstly, a high temperature pyrolysis method is adopted for preparing inner core NaYF4:Yb / TM / Gd hydrophobic nano-particles, then an NaGdF4 shell is formed through epitaxial growth so as to form core / casing structured NaYF4: Yb / Tm / Gd and NaGdF4 nano-particles, then hydrochloric acid hydrophilic modification and sulfhydryl PEG modification are performed, and finally, the nano probe material is prepared through Angiopep-2 grafting, and is marked as ANG / PEG-UCNPs. The material can be used for efficient blood-brain barrier breaching, magnetic resonance imaging diagnosis and positioning before an cranial cavity glioma operation, near infrared fluorescence imaging in the operation and image mediating, the imaging effect is good, the sensitivity is high, the physiological system toxicity is low, and the material plays an important significance in successful clinic glioma removing operations and the development and the application of medical image diagnostic techniques.

The invention discloses a PEGylated scutellarin compound and a preparation method thereof. The PEGylated scutellarin compound is as the shown formula (IV) and the PEGylated scutellarin compound can be applied to preparing medicaments applied to treating cerebral thrombosis, cerebral infarction, cerebral apoplexy, sequelaes caused by cerebral apoplexy, coronary heart disease or angina. Compared with the original scutellarin compound, the water solubility of the scutellarin compound is increased obviously; simultaneously, pharmacodynamics experiment on the mice model of cerebral ischemia-reperfusion shows that: compared with the original medicament, the biological activity of the scutellarin promedicament is strengthened obviously.

The invention belongs to the field of new auxiliary materials and new dosage forms of medicine preparations and relates to a chemotherapeutic drug-photosensitizer co-assembled nanoparticles and construction thereof. A chemotherapeutic drug is an anthracycline chemotherapeutic drug selected from mitoxantrone, doxorubicin or epirubicin; a photosensitizer is a porphyrin photosensitizer selected fromchlorine e6, hematoporphyrin monomethyl ether or a chlorophyll derivative, wherein the molar ratio of the chemotherapeutic drug to the photosensitizer is 3:1-1:3. A certain quantity of the chemotherapeutic drug and the photosensitizer or a mixture of the chemotherapeutic drug, the photosensitizer and PEG is dissolved in a proper quantity of organic solvent, and the solution is slowly dropwise added to water while stirring to form uniform nanoparticles spontaneously. The preparation process is simple, enlarged production is easy, particle size is small and uniform, and the nanoparticles can beenriched at tumor parts through a reinforced permeation retention effect; the nanoparticles have ultrahigh drug loading capacity and can reduce related toxicity of auxiliary materials; and surface modification is easy, and the circulation time of the nanoparticles in blood can be prolonged by PEG modification.

The invention discloses an RP-HPLC detection method for the content of free polyethylene glycol in samples or products, which is characterized by making use of the non-polar difference of polyethylene glycol from other substances on the reversed-phase chromatography column and using UV detector combining evaporative light detector or diode array detector combining evaporative light detector signal contrast to screen signal peaks of free polyethylene glycol and to determine the content thereof by means of the external standard method. Based on the method, the invention also can be used for detecting the purity of polyethylene glycol modified products and the modification degree of modified products. The analysis method is highly sensitive, good in repetitiveness and selectivity, fast, efficient and simple, and is suitable for being used in the samples which have more complex components and are interfered in the polyethylene glycol-barium compound colorimetric determination provided by pharmacopoeia, especially suitable for being used in the polyethylene glycol modified samples or products.

The present invention is directed to methods of modulating viral replication in vivo comprising administering to an individual a therapeutically or prophylactically effective amount of a composition comprising arginine deiminase modified with polyethylene glycol, to methods of concurrently modulating viral replication and treating cancer, and to methods of modulating nitric oxide levels in a patient, among others.

The invention discloses an alpha conus polypeptide derivative, amino acid residues of which are shown in sequence 1 in a sequence table. To effectively resist the degradation digestion of partial protease in a human body, and improve the bioavailability and the drug metabolism performance, an N end of the alpha conus polypeptide derivative can be connected with a benzoyl group. The alpha conus polypeptide derivative can also be subjected to cyclization, fattening or PEG modification to strengthen the treatment effect of the alpha conus polypeptide derivative. A big mouse experiment shows that the alpha conus polypeptide derivative shows strong analgesic activity in a neuropathic pain model of a big mouse, and the analgesic activity is remarkably higher than that of control peptide Vc1.1 and shows dose-dependent relation.

The invention relate to polyethylene glycol modified hydroxycamptothecin stealth greasy nano balls for intravenous injection and its preparing process, which comprises treatment effective amount of hydroxycamptothecin, polyethylene glycol esters, oil for injection, phosphatides and pharmaceutically acceptable auxiliary material by the weight ratio of 0.01-0.2%, 1-10%, 5-25%, 0-10%, 0-10%, and balancing water. The invention also discloses the preparing prcesss including dissolving liposoluble materials into organic solvents, dissolving water-soluble auxiliary materials and addition agents into water, mixing with organic phase, homogenizing or carrying out supersonic treatment.

The invention discloses a preparation method of a tumor targeted photothermal therapy nanocarrier. The method comprises steps as follows: with GO as a carrier, loading MoS2 on GO with a hydrothermal method, and performing PEG modification to obtain the GO-MoS2 composite carrier. A composite of GO and MoS2 is taken as a phototherapeutic drug carrier for the first time, the preparation method is simple and convenient, and conditions are mild; the prepared GO-MoS2 drug-carrying composite has good photothermal conversion characteristic and higher drug carrying ratio which is higher than or equal to 80%. The drug release rate of the GO-MoS2 drug-carrying composite is 78% under laser power of 1.8 W / cm<2> in the presence of NIR laser. Compared with a conventional photothermal therapy nano-drug carrier, the GO-MoS2 drug-carrying composite has higher photo-thermal conversion rate due to synergistic effect of the two materials.

A process for preparing the polyethanediol modified asparaginase includes reaction between asparaaginas and linear polyethanodiol whose linear chain length is 1000-5000 in ratio of 1:5-30, and reaction between linear polyethanediol whose linear chain length is 5000-3000 and biologic macro-molecular compound in ratio of 1:10.

The invention relates to modification method of polyethyleneglycol of protein, which takes hydrophobic chromatography chromatographic column as solid phase reaction carrier. The method comprises the following steps: as for the protein with strong hydrophobicity, absorbing the protein on the hydrophobic chromatography chromatographic column under a high-salt state, taking a polyethyleneglycol modification agent as a mobile phase, and taking salt ion for gradient elution after the completion reaction to obtain polyethyleneglycol modified protein; as for the protein with hydrophobicity, absorbing the polyethyleneglycol modification agent in the hydrophobic chromatography chromatographic column under the high salt sate, taking protein solution as the mobile phase, and taking salt ion for gradient elution after the completion reaction to obtain polyethyleneglycol modified protein. The PEG modified protein prepared by the invention has high retention rate of activity and better simplicity, and the single modified rate reaches more than 40 percent, and the retention rate of activity reaches more than 80 percent. The method provides a new process for the realization of PEG modification of the protein.

The invention belongs to the technical field of medicine, and relates to pegylated celastrol and a preparation method and application thereof. The pegylated celastrol has a structure shown as a general formula in the specifications. The invention also provides application of the pegylated celastrol and methoxy amino polyethylene glycol 10kDa mono-modified celastrol (mPEG10k-NHCO-celastrol) to preparation of medicines for treating various malignant tumors such as prostatic cancer, lung cancer, liver cancer and cervical cancer. Celastrol is subjected to chemical structural modification by PEG, so that the problem that the celastrol has low solubility can be solved; and an injection can be prepared after the celastrol is modified by the PEG, so that the elimination half life of the celastrol can be prolonged through in-vivo injection, the toxic and side effects of the celastrol are reduced, and the administration frequency of a patient is reduced.

The invention relates to a method for preparing a multifunctional manganous manganic oxide nano-particle nuclear magnetic resonance contrast agent mediated by polyethyleneimine. The method comprises the following steps: preparing PEI modified Mn3O4 nano-particles by using a solvothermal method, and then separating and purifying the nano-particles; then, marking tracer molecule fluorescein isothiocyanate FI on the nano-particles; modifying polyethylene glycol PEG molecules on the amino of PEI; and finally, modifying targeted reagent folic acid FA molecules on the PEI through PEG modification and performing complete acetylation treatment to obtain the contrast agent. The contrast agent prepared in the invention can trace the phagocytosis condition of the cancer cells to nanoparticles in a cellular level, has a significant targeting function on a high-expression cancer cell strain of an FA receptor and can be used for achieving early diagnosis of cancer, meanwhile, since the preparation method of the contrast agent is simple and easy and the raw materials are cheap and easy to obtain, the contrast agent can be produced in large batches.

The invention provides a construction and modification method of recombinant porcine long-acting-alpha interferon and a preparation method of a lyophilized injection. Recombinant porcine-alpha interferon provided by the invention is prepared by adopting colon bacillus soluble expression, and the recombinant porcine long-acting-alpha interferon is obtained by using polyethylene glycol to perform modification according to the characteristics of polyethylene glycol, so that the half life of the recombinant porcine long-acting-alpha interferon in a pig body is prolonged to 44.5h and the porcine immunity is enhanced. The recombinant porcine long-acting-alpha interferon provided by the invention has excellent expression under high density and high volume of bacteria, production and purification processes are simple and novel, the cost is low, and the product yield and purity are improved. The lyophilized injection of the recombinant porcine long-acting-alpha interferon, provided by the invention, has the advantages of low cost, significant curative effect and stable product quality.

The invention discloses an MRI contrast agent taking a chitosan derivative as a carrier and a preparation method of the contrast agent. The contrast agent comprises chitosan which serves as a main body of the contrast agent and modified with polyethylene glycol and a secondary polyamide dendrimer which is mainly connected to a main chain of chitosan and provided with a gadolinium chelate. The preparation method of the contrast agent comprises the steps that chitosan modified with polyethylene glycol is provided, a chelating ligand of gadolinium is coupled to the secondary polyamide dendrimer modified with an alkynyl group, then the modified secondary polyamide dendrimer is connected to chitosan, and the contrast agent is obtained. The MRI contrast agent taking the chitosan derivative as the carrier is good in biocompatibility, easy to biologically degrade and high in relaxation rate, the preparation method is simple, the needed reaction temperature is moderate, and control is easy.