33results about How to "Improved tissue penetration" patented technology

The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as inhibitors of Jak2 / STAT3 pathways and downstream targets and inhibit the growth and survival of cancerous cell lines.

The instant invention relates to modulated lysine variant species compositions comprising a protein, e.g., an antibody, or antigen-binding portion thereof, and methods, e.g., cell culture and / or protein purification methods, for producing such modulated lysine variant species compositions. Methods for using such compositions to treat a disorder, e.g., a disorder in which TNFα is detrimental, are also provided.

Nanocrystals that include a core / shell structure in which the a core of semiconductor material is coated with an inorganic capping agent. The nanocrystals are made by initially providing nanocrystal precursors that include a solubility agent which renders the precursors soluble in an organic solvent. The nanocrystal precursors are then coated with the inorganic capping agent in the presence of an organic solvent.

The invention provides a targeting nano carrier bearing nucleoside anti-tumor drugs and preparation method and application thereof. The targeting nano carrier comprises DNA tetrahedron, Affibody molecule and nucleoside anti-tumor drugs. The preparation method comprises the following steps: a, the nucleoside anti-tumor drugs are modified with phosphoramidite; B, synthesizing four DNA single strandsby DNA solid phase synthesis technology, integrating the nucleoside anti-tumor drugs into the 5 'ends of the four DNA single strands, and modifying NH2 at the 3' ends of one of the DNA single strands; C, linking the affibody molecule to the 3 'end of the NH2-modified DNA single strand through a linker; (d) mix and assembling that four DNA single strand in a molar ratio of 1: 1: 1: 1 to obtain DNAtetrahedron; and (d) assembling the four DNA single strands in a molar ratio of 1: 1: 1 to obtain DNA tetrahedron; Affibody targeting nanoparticles. The targeting nano carrier of the invention can precisely control the combined quantity of drugs, has faster tumor targeting ability and higher cell, tissue penetration ability, good pharmaceutical effect, and is suitable for popularization and application.

The invention discloses a 1-3 generation arylene ether-substituted dendritic phthalocyanine zinc complex, a preparation method and an application thereof. The method comprises the following steps of adopting a Frechet synthesis method to synthesize the first to third generation alcohol molecules which take the 1-3 generation cyan as an end group; leading the first to third generation alcohols to react with 4-nitrophthalonitrile respectively, thus synthesizing corresponding phthalocyanine precursor of dendrimer taking the 1-3 generation cyan as the end group; subsequently, leading the phthalocyanine precursor ring of dendrimer taking the 1-3 generation cyan as the end group to synthesize corresponding arylene ether dendritic phthalocyanine taking the first to third generation cyan as the end group and the arylene ether dendritic phthalocyanine taking the first to third generation carboxyl as the end group generated by hydrolysis. The 1-3 generation arylene ether dendritic phthalocyanine complex and the amphiphilic block copolymer are automatically dissolved to form the polymer nano-particle loading the 1-3 generation arylene ether dendritic phthalocyanine complex. The 1-3 generation diaryl ether dendritic phthalocyanine zinc complex and the loaded polymer nano-particle thereof are used as photosencitizers for photodynamic therapy.

The invention discloses a multifunctional nano template based on aggregation-induced emission and a preparation method and application thereof, and the preparation method comprises the following steps: carrying out reflux stirring on a mixed solution of dimethoxytriphenylamine thiophene and 1,3-indanedione to obtain MeOTTI; carrying out self-assembly on MeOTTI, DSPE-PEG2000-SH and NaYF4:Yb<3+> and Er<3+> (upconversion nanoparticles and UCNPs), and carrying out surface oxidation by using KMnO4, so as to obtain MeOTTI,UCNPs-coated DSPE-PEG-coated MnO2 nanoparticles. According to the nano template prepared by the method, on the basis of an I-type photodynamic photosensitizer with AIE property, endogenous glutathione is consumed by utilizing a MnO2 shell to retain active oxygen, and up-conversion nanoparticles are introduced to increase the tissue penetrability of light, so that a great-depth light diagnosis and treatment effect is realized.

The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as inhibitors of Jak2 / STAT3 pathways and downstream targets and inhibit the growth and survival of cancerous cell lines.

Provided is a tetraphenylbacteriochlorin derivative represented by the formula (I): [wherein R1, R2, R3 and R4, independently from each other, are a residue of a monosaccharide represented by the formulae: (wherein, R is a hydrogen or a protecting group)], or its salt. The tetraphenylbacteriochlorin derivative or its salt has a large molar extinction coefficient at long wavelengths which are expected to have a high tissue-penetrating property, and exhibits high selectivity to tumor cells and hydrophilicity.

The invention discloses a virus-like hollow oxide loaded near-infrared two-b region excited rare earth nanocrystal and a preparation method and application thereof. According to the nanocrystal and the preparation method, an Er and Ho doped NaErF4:2%Ho@NaYF4 rare earth nanomaterial is synthesized through a hydrothermal method, then the nanomaterial is modified on a surface of a virus-like hollow manganese oxide poured into IR1064 through an amidation reaction, and a fluorescent composite probe which is good in biocompatibility and responds to a tumor microenvironment is obtained. According to the fluorescent composite probe, after the manganese oxide is degraded at a tumor, manganese ions are used for chemodynamic therapy and nuclear magnetic resonance imaging contrast agents of metastasis, released rare earth nanocrystals have excitation of 1530 nm and emitted lights of 650 nm and 1180 nm, the light of 1180 nm can be used for tumor imaging navigation surgical resection with no background interference and high resolution and tissue penetrating power in a near-infrared second region, and the light of 650 nm can used for near-infrared first region fluorescence imaging.

An implantable system which includes a gene / protein delivery device and a pulse generator, as well as method of preparing the gene / protein delivery device and using the system, are provided. In one embodiment, the implantable system detects a predetermined condition or event and, in response, delivers gene(s) and / or protein(s) in conjunction with delivering pacing and / or defibrillation pulses.

The invention discloses a magnetic composite nano material and a preparation method and application thereof. The magnetic composite nano material comprises modified magnetic nano particles and a modified macromolecular layer located on the outer surfaces of the modified magnetic nano particles, wherein the modified macromolecular layer comprises macromolecules and polymers connected with the macromolecules through pH response groups, and the response pH value of the pH response groups is smaller than 6.8. The magnetic composite nano material exists in a cluster form before reaching a tumor part, and due to the large particle size, the magnetic composite nano material is not likely to be rapidly removed by kidney metabolism; after the magnetic composite nano material reaches the tumor part,an assembly (the magnetic composite nano material) is gradually dispersed under the tumor subacid condition, the magnetic composite nano material exists in the tumor part in a small-particle-size magnetic nano particle form, and therefore the penetration depth of tumor tissue is increased; and due to falling of the surface modification polymers, surface positive charges are increased, and the nano particles are more easily taken by cells. Therefore, the pH response type magnetic composite nano material cluster enhances the MRI imaging contrast effect and improves the tissue penetration.

The invention discloses a medicine delivery system for realizing specificity nanometer antibody medicine delivery through the vagina for the first time, and a preparation method and application thereof. The vector recipe is optimized, so that the nanometer antibody stability and the tissue penetration are maintained and enhanced; the application of the nanometer antibody vagina medicine delivery system to disease treatment and woman sanitation care is realized. Through the nanometer antibody vagina medicine delivery, the specificity nanometer antibody can realize the medicine effect in the vagina internal environment and positions near the organ local part; in addition, the nanometer antibody can penetrate through vagina tissues to enter human body blood for circulation; the goal of achieving the medicine effect in the preset focus position is realized. The nanometer antibody vagina medicine delivery system has the advantages that medicine is slowly released in the woman vagina and through vagina cortical tissues; no basic irritation and allergic reaction exists; the safe and efficient medicine delivery mode and the new dosage form of nanometer antibody biological medicine are opened up; the application prospects are very wide.

The present invention relates to a pharmaceutical composition for preventing and treating eye diseases, comprising, as an active ingredient, a fusion protein in which a tissue-penetrating peptide and an anti-vascular endothelial growth factor (anti-VEGF) preparation are fused. More particularly, the present invention relates to: a pharmaceutical composition for preventing and treating eye diseases, comprising, as an active ingredient, a fusion protein in which a tissue-penetrating peptide and an anti-VEGF preparation are fused; a method for prepraring an anti-VEGF preparation, which overcomes resistance and has an improved efficacy, the method comprising the steps of transforming a host cell with a recombinant vector comprising a nucleic acid sequence encoding a fusion protein in which a tissue-penetrating peptide and an anti-VEGF preparation are fused, culturing the cell, and recovering a fusion protein from the cell; a method for treating eye diseases, comprising administering an effective dose of the fusion protein according to the present invention to a subject in need thereof; and use of the fusion protein according to the present invention for preparing an agent for treating eye diseases. Compared to conventional anti-VEGF preparations, the composition according to the present invention is considered to have an improved efficacy and be able to be used for treating patients having drug resistance, by inhibiting various growth factors related to new blood vessels, besides VEGF, and by decreasing pericyte coverage. In addition, since drug delivery ability into the choroid tissue is improved when performing an intraocular injection, the composition can be developed as eye drops by reducing an administered dosage or extending an administration cycle, and by improving ocular penetrability.

The invention discloses a drug administration preparation system for a nano-antibody through inner and outer cuticulae of a head and a neck as well as a preparation method and application of the drug administration preparation system. A carrier formula is optimized and the stability and tissue penetration of the nano-antibody are maintained and enhanced so that drug administration of nano-antibody biological medicines is realized through the outer cuticular layers of the head and the neck and inner cuticular layers of a nasal cavity. The drug administration preparation system can be used for treating a plurality of types of diseases of brain and central nervous systems by the specific nano-antibody, and can also be used for maintaining and keeping health of a brain nervous system of old people. The drug administration preparation system disclosed by the invention explores novel preparations of the nano-antibody biological medicines and a safe and effective central nervous system drug administration way.

A method of photodynamic therapy is described that includes administering a therapeutically effective amount of a photosensitizer to an area of tissue such as the skin of a subject, delivering a first photoirradiation with light having a wavelength suitable to activate the photosensitizer to the area of skin, allowing a sufficient interval of time to pass for an effective amount of the photosensitizer to penetrate the tissue, and then delivering a second photoirradiation with light having a wavelength suitable to activate the photosensitizer to provide a therapeutic effect. Use of multiple photoirradiations increases the speed with which the photosensitizer can penetrate the tissue to reach the area where the source of the disease is present.

Nanocrystals that include a core / shell structure in which the a core of semiconductor material is coated with an inorganic capping agent. The nanocrystals are made by initially providing nanocrystal precursors that include a solubility agent which renders the precursors soluble in an organic solvent. The nanocrystal precursors are then coated with the inorganic capping agent in the presence of an organic solvent.

The invention discloses a water-soluble near-infrared two-region fluorescent tracing developer for joint bacterial infection. The method comprises the following steps: in a reaction system of RNase Aand NaOH, taking Pb(OAc)2.3H2O and Na2S as raw materials, preparing RNase A-PbS quantum dots by utilizing a microwave reaction high-temperature synthesis method, and crosslinking amino-beta-cyclodextrin or CGGG-UBI29-41 by utilizing an EDC-NHS or EDC-SMCC system, thereby obtaining the product. The fluorescent tracing developer has the characteristics of high fluorescence intensity, high quantum yield, light stability, wide excitation spectrum, narrow emission spectrum and the like, and can be bound with bacteria in a targeting manner; due to the functions of near-infrared two-region imaging and bacterial infection focus positioning, the fluorescent tracing developer can perform rapid detection, real-time tracing and living body imaging on clinically hidden joint infection, and auxiliary diagnosis of the joint infection is achieved.

The invention discloses a NIR-II imaging probe and a preparation method and application thereof, and belongs to the technical field of in vivo bioluminescence imaging of cells. The invention comprisesthe following steps: S1, incubating bone marrow mesenchymal stem cells (BMSCs) of fluorescent probe CP@mSiO2(subscript)-PEG nanoparticles; S2, injecting fluorescent material-labeled BMSCs into HepG2tumor-bearing nude mice through tail vein injection and local subcutaneous injection; and S3, carrying out near-infrared-II (NIR-II) window imaging on the tumor, and then performing imaging-guided tumor resection. In the study, NIR-II is a new strategy for tumor imaging in vivo and image-guided tumor resection surgery, the NIR-II in vivo bioluminescence imaging technology is used to induce the fluorescent material-labeled BMSCs to enrich in the tumor site, so that the outline of the tumor can be seen clearly, thus improving the accuracy of surgical resection and reducing the tumor recurrence rate and the mortality rate.

The invention relates to application of micelles formed by polyethylene glycol derivatives in paclitaxel or derivatives thereof, and belongs to the technical field of lipoid molecules. The polyethylene glycol derivative can be dispersed in a solvent to form micelles, and the micelles can be used for efficiently wrapping, delivering and releasing paclitaxel or paclitaxel derivatives. Micelles formed by the polyethylene glycol derivative have high tissue penetrability, long-acting stability and controllable release performance. Particularly, the polyethylene glycol derivative contains a phospholipid structure, so that the polyethylene glycol derivative has outstanding biocompatibility.

A method for HIFU treatment of localized prostate cancer in a patient includes identifying the cancer locations in a patient's prostate; visually segmenting the patient's prostate into areas for analysis and treatment, where the section including the area of most aggressive cancer is determined to be the primary area. The primary area is subjected to a first full HIFU treatment for a period intended to ablate the cancerous tumor. HIFU treatment is then stopped on the primary area and the primary area is allowed to rest while simultaneously subjecting the next contiguous area of the patient's prostate to a first HIFU treatment to ablate any additional areas of suspected cancer in the next contiguous area. HIFU treatment is then stopped in the contiguous area. The primary area is then subjected to a second full HIFU treatment for a period sufficient to ensure the complete ablation of the cancerous tumor. The method further includes repeating alternating full HIFU treatment processes on subsequent contiguous areas of the patient's prostate to ensure the complete ablation of any cancerous tumors in the patient's prostate. The entire process is completed under one treatment of anesthesia.

Provided is a tetraphenylbacteriochlorin derivative represented by the formula (I): [wherein R1, R2, R3 and R4, independently from each other, are a residue of a monosaccharide represented by the formulae: (wherein, R is a hydrogen or a protecting group)], or its salt. The tetraphenylbacteriochlorin derivative or its salt has a large molar extinction coefficient at long wavelengths which are expected to have a high tissue-penetrating property, and exhibits high selectivity to tumor cells and hydrophilicity.

The invention provides a novel acid response ionic liquid microcapsule as well as a preparation method and application thereof. The ionic liquid microcapsule comprises an inner core and a shell layer, wherein the inner core is ionic liquid, and the shell layer is a metal-polyphenol network coating. The preparation method of the microcapsule comprises the following steps: adding polyphenol into the ionic liquid, and performing stirring to dissolve the polyphenol to obtain polyphenol-ionic liquid; adding the polyphenol-ionic liquid into water, and performing ultrasonic and uniform dispersing; and then adding a metal ion solution, performing whirling to uniformly mix the system, then adjusting the pH value of the system, and performing centrifuging to obtain the microcapsule. According to the ionic liquid microcapsule prepared by the method, the stability of ionic liquid droplets can be remarkably improved, and various drug molecules, especially indissolvable drugs, can be effectively loaded; and MPN of the prepared microcapsule is dissociated in an acidic microenvironment, so that the ionic liquid carries the medicines to permeate into a target tissue, and the utilization rate of the medicines is greatly improved and the efficacy of the medicines is enhanced due to the relatively strong medicine permeation effect of the ionic liquid.

HIFU treatment of localized prostate cancer includes identifying the cancer locations in a patient's prostate and visually segmenting the patient's prostate into areas for analysis and treatment. The section including the most aggressive cancer is determined to be the primary area and subjected to a first full HIFU treatment for a period intended to ablate the cancer. HIFU treatment is then stopped on the primary area, allowing it to rest, while simultaneously subjecting the next contiguous area of the prostate to HIFU treatment to ablate any additional areas of suspected cancer. HIFU treatment is then stopped in the contiguous area. The primary area is then subjected to a second full HIFU treatment for a period sufficient to ensure the complete ablation of the cancerous tumor. Repeating alternating full HIFU treatment on subsequent contiguous areas of the prostate ensures the complete ablation of any cancerous tumors in the prostate.

The invention belongs to the technical field of small molecular photo-thermal materials, particularly relates to a thiazole orange derivative, preparation and application thereof, and provides a thiazole orange derivative, which has a structure represented by a formula I, wherein n is equal to 1, 2 or 3, X is I, Br or Cl, R1 is fatty acylamino, fatty carboxyl or fatty alkyl, and R2 is triphenyl phosphine or triphenyl amine. The invention also provides a preparation method of the thiazole orange derivative. The preparation method comprises the following steps: reacting a compound with a structure epresented by a formula IX with a compound with a structure represented by a formula VII to obtain a compound with a structure represented by a formula I, wherein n is equal to 1, 2 or 3, R2 is triphenyl phosphine or triphenyl amine, Y is I, Br or Cl, X is I, Br or Cl, and R1 is fatty acylamino, fatty carboxyl or fatty alkyl. The invention discloses an application of a thiazole orange derivative in preparation of a targeted photothermal therapy tumor drug or a targeted photoacoustic imaging signal drug.

The invention discloses an aminobenzopyranocyanine-based fluorescent dye and a probe as well as its synthesis method and application. The fluorescent dye is any one of structural formulas I to II: the aminobenzopyranocyanine of the present invention The near-infrared fluorescent dyes I and II of the structure have high fluorescence quantum yield and good photostability. Tissue sample tissue penetrating ability, reducing light damage, and biomolecular autofluorescence is weak, which can avoid the interference of autofluorescence in biological systems and obtain a higher signal-to-noise ratio, thereby improving sensitivity.

The invention provides photodynamic therapeutic compounds and photodynamic methods of treatment. The photodynamic therapeutic compounds may be activated by long wavelength light. The photo-activation by long wavelength light may allow improved tissue penetration. The compounds are selected from the group consisting of compounds of formula (i), or a pharmaceutically acceptable salt thereof: formula (i) wherein PDC is a photodynamic core and wherein R1; R2; R3; and R4 are H, phenyl, pyridine-4-yl, methylpyridinium, N-methylpyridinium-3-yl; 2-phenyl-N-methylpyridinium-4-yl, 3-phenyl-N-methylpyridinium-4-yl, 4-phenyl-N-methylpyridinium-4-yl, 2-phenyl-N-methylpyridinium-3-yl, 3-phenyl-N-methylpyridinium-3-yl or 4-phenyl-N-methylpyridinium-3-yl; and wherein any one or more of R1, R2, R3 and R4 may be optionally substituted.

The invention discloses a 1-3 generation arylene ether-substituted dendritic phthalocyanine zinc complex, a preparation method and an application thereof. The method comprises the following steps of adopting a Frechet synthesis method to synthesize the first to third generation alcohol molecules which take the 1-3 generation cyan as an end group; leading the first to third generation alcohols to react with 4-nitrophthalonitrile respectively, thus synthesizing corresponding phthalocyanine precursor of dendrimer taking the 1-3 generation cyan as the end group; subsequently, leading the phthalocyanine precursor ring of dendrimer taking the 1-3 generation cyan as the end group to synthesize corresponding arylene ether dendritic phthalocyanine taking the first to third generation cyan as the end group and the arylene ether dendritic phthalocyanine taking the first to third generation carboxyl as the end group generated by hydrolysis. The 1-3 generation arylene ether dendritic phthalocyaninecomplex and the amphiphilic block copolymer are automatically dissolved to form the polymer nano-particle loading the 1-3 generation arylene ether dendritic phthalocyanine complex. The 1-3 generation diaryl ether dendritic phthalocyanine zinc complex and the loaded polymer nano-particle thereof are used as photosencitizers for photodynamic therapy.