16 results about "Tissue distribution" patented technology

The invention belongs to the technical field of biological medicines, and discloses a cationic polymer targeted nano material modified siRNA (small interfering ribonucleic acid) nano-drug and application thereof. The siRNA nano-drug disclosed by the invention has the capability of effectively penetrating through the blood brain barrier and improving the brain tissue distribution of the siRNA drug.

The invention discloses a lipophilic modified nucleic acid medicine composition and application thereof, the lipophilic modification is saturated or unsaturated C4-C30 alkyl, the composition comprises an absorption enhancer, and the method is that the lipophilic modified nucleic acid medicine is delivered to the brain through the nasal mucosa. Nucleic acid drugs are transmitted into the olfactory bulb region through a neural pathway, namely, cross-olfactory mucosa, bypass BBB and directly enter the brain, the drug concentration content of the olfactory bulb is far higher than that of other tissues of the brain, and the tissues except the olfactory bulb are uniformly distributed, so that the olfactory bulb can be used as a drug reservoir and gradually and slowly spread to the other tissues of the brain; the long-time drug effect can be maintained by one-time drug administration, so that the drug administration frequency can be reduced. Compared with intrathecal injection, by adopting the composition disclosed by the invention for nasal administration and using 1 / 2 of intrathecal administration dosage, the same intrathecal steady-state distribution as intrathecal distribution can be achieved, so that the method disclosed by the invention is safer, noninvasive and efficient.

The application discloses a kind of recombinant fusion protein and its application in preparation anti-gastric cancer angiogenesis drug, it is related to biological medicine technical field.The amino acid sequence of the recombinant fusion protein is as shown in SEQ ID NO.1.The amino acid sequence of gastric cancer vascular targeting peptide CNTGSPYEC is recombined with the strong vascular inhibitor Endostatin gene to construct recombinant fusion protein, using the selective distribution ability of targeting peptide, can carry anti-vascular drug Endostatin more specifically enriched in gastric cancer vascular endothelial cells, to improve anti-vascular effect and antitumor effect, simultaneously because Endostatin is reduced in normal vascular and tissue distribution, can reduce corresponding toxic side effect, it has important significance to improve gastric cancer anti-vascular treatment present situation.

The invention provides a method for quantitatively detecting plant polysaccharide in a biological sample, the biological sample is plasma of a rat or tissue of the rat, the content of characteristic monosaccharide in the biological sample is quantitatively detected, and then the content of the plant polysaccharide in the biological sample is calculated according to the proportion of the characteristic monosaccharide in the plant polysaccharide. The characteristic monosaccharide comprises rhamnose and arabinose. The method provided by the invention avoids interference and structural damage introduced by an exogenous marker, and has high specificity and high sensitivity (LLOQ signal-to-noise ratio gt; 10: 1), high accuracy (the accuracy is 85-115%) and high precision (RSDlt; compared with an FITC (fluorescein isothiocyanate) labeling method, the method is proved to be successfully applied to quantitative analysis of target characteristic monosaccharide content in blood plasma and tissues of rats for intravenous injection of plant polysaccharide, and is successfully applied to in-vivo pharmacokinetics and tissue distribution research of hedysarum polybotrys polysaccharide. A key methodological tool is provided for explaining the in-vivo process and the pharmacological mechanism.

The invention provides composite particles for regulating and controlling bioavailability and tissue distribution of resveratrol and piperine and a preparation method of the composite particles, and belongs to the technical field of nutritional active ingredient delivery systems. According to the resveratrol-zein-lecithin-piperine-konjac glucomannan composite particle and the preparation method thereof, firstly, a particle core is formed through an anti-solvent coprecipitation method, then a piperine solution and a konjac glucomannan solution are sequentially injected, and the resveratrol-zein-lecithin-piperine-konjac glucomannan composite particle of a core-shell structure is formed through layer-by-layer assembly. Compared with a free form, the composite particle has the advantages that the physical and chemical stability of the resveratrol and the piperine is remarkably improved, the residence time of the resveratrol and the piperine in intestinal tracts is prolonged, and the oral bioavailability and the liver tissue enrichment capacity of the resveratrol and the piperine are effectively enhanced. The composite particle provided by the invention is clear in structure, the preparation method is simple and convenient to operate, and the composite particle has a good application prospect in functional food and drug development.

The invention belongs to the technical field of biological medicine, and relates to an intelligent cantharidin drug delivery system. According to the present invention, the cantharidin is delivered through the polymer hybrid carrier having the accurate pH response function, such that the efficient delivery of the cantharidin is achieved, the tissue distribution and the drug release performance of the cantharidin are significantly improved, especially the system can have the good lysosome escape function, and the anti-breast cancer treatment effect and the safety of the cantharidin are significantly improved.

The invention provides an ALK5 PROTAC compound and application thereof, and belongs to the field of medicinal chemistry and biological medicine. A series of PROTAC small molecule compounds for targeted degradation of ALK5 protein are prepared, and the structures of the PROTAC small molecule compounds are as shown in a formula I in the specification. The compounds can be degraded through an ALK5 ubiquitination-proteasome pathway, and the bioavailability gt is injected in the intraperitoneal cavity; and the tissue distribution is good. The ALK5 PROTAC compound provided by the invention provides a new accurate intervention means for treating ALK5 mediated fibrosis diseases and tumors.

Disclosed in the present invention is a thyroid hormone receptor β (THR-β) agonist. The present invention provides a compound as represented by formula I, or a stereoisomer or pharmaceutically acceptable salt thereof. Compared with VK-2809, the compound provided in the present invention has significantly superior agonistic activity against THR-β than VK-2809, or in terms of in vivo organ / tissue distribution, has a liver / heart distribution ratio or plasma / heart distribution ratio superior to that of VK-2809.

The present application relates to the technical field of medicine, in particular to a polysaccharide composition, nano-polysaccharide and its preparation method and application.The polysaccharide composition comprises polysaccharide and lipid material;the weight ratio of polysaccharide to lipid material is 2-50:1.The composition disclosed in the present application can change the mode of polysaccharide and cell interaction, pharmacokinetics and tissue distribution behavior, improve the cell uptake of polysaccharide, improve the oral bioavailability, delay the clearance of polysaccharide from blood circulation, prolong the residence time in vivo, thereby significantly improving the in vitro and in vivo activity and efficacy of active polysaccharide.

The application provides an ALK5 PROTAC compound and application thereof, and belongs to the field of pharmaceutical chemistry and biological medicine. A series of PROTAC small-molecule compounds for targeted degradation of ALK5 protein are prepared, and the structure is shown as formula I. The compounds can be degraded through an ALK5 ubiquitination-proteasome pathway, the bioavailability of intraperitoneal injection is greater than 70%, and the tissue distribution is good. The ALK5 PROTAC compound provided by the application provides a new precise intervention means for treating ALK5-mediated fibrosis diseases and tumors.

This invention belongs to the field of biomedical technology and relates to a smart drug delivery system for cantharidin. This invention utilizes a polymer hybrid carrier with precise pH response to deliver cantharidin, achieving efficient delivery and significantly improving the tissue distribution and drug release properties of cantharidin. In particular, this system exhibits excellent lysosomal escape capabilities, significantly enhancing the efficacy and safety of cantharidin in treating breast cancer.

The invention discloses a coronavirus 2 '-O-methyltransferase inhibitor and an application of the coronavirus 2'-O-methyltransferase inhibitor. The inhibitor provided by the invention takes the coronavirus 2 '-O-methyltransferase as a target spot, can effectively inhibit the enzymatic activity of the coronavirus 2'-O-methyltransferase, shows a good antiviral effect on human and animal coronaviruses (including new coronaviruses and mutant strains thereof) on a cellular level, and shows good pharmacokinetic level, tissue distribution and safety in a mouse body. The inhibitor can effectively inhibit the enzymatic activity of coronavirus 2 '-O-methyltransferase, so that an efficient antiviral effect is achieved; the safety is high, and the clinical application potential is high; the method is wide in applicability and can be used for various types of coronaviruses; moreover, the oral administration utilization rate is high, the antiviral effect is good, and the application scene is greatly enriched. The application scheme also provides another thought for developing more safe, effective and broad-spectrum anti-coronavirus small molecule drugs, and has extremely high scientific research significance and practical value.

The invention belongs to the field of biological nano medicines, and particularly relates to a preparation method of water-soluble lipid nanoparticles based on combination of film dispersion and active drug loading. According to the invention, a polyethylene glycol derivative is used as a carrier skeleton, a specific targeting group is introduced to construct an intelligent delivery system, and a film dispersion method and a pH response type active drug loading technology are innovatively combined, so that the key problems of non-selective tissue distribution, narrow therapeutic window and the like of a traditional chemotherapeutic drug are effectively improved. The prepared nanoparticles have the following remarkable advantages that a tumor part is positioned through a targeting ligand-receptor recognition mechanism, the bioavailability of the medicine is effectively improved, the dosage is reduced, the toxic and side effects are reduced, and a scheme with high efficiency and safety is provided for tumor treatment through the diagnosis and treatment integrated design.