48results about How to "Increase endocytosis" patented technology

Compositions and methods for transport or release of therapeutic and diagnostic agents or metabolites or other analytes from cells, compartments within cells, or through cell layers or barriers are described. The compositions include a membrane barrier transport enhancing agent and are usually administered in combination with an enhancer and / or exposure to stimuli to effect disruption or altered permeability, transport or release. In a preferred embodiment, the compositions include compounds which disrupt endosomal membranes in response to the low pH in the endosomes but which are relatively inactive toward cell membranes (at physiologic pH, but can become active toward cell membranes if the environment is acidified below ca. pH 6.8), coupled directly or indirectly to a therapeutic or diagnostic agent. Other disruptive agents can also be used, responsive to stimuli and / or enhancers other than pH, such as light, electrical stimuli, electromagnetic stimuli, ultrasound, temperature, or combinations thereof. The compounds can be coupled by ionic, covalent or H bonds to an agent to be delivered or to a ligand which forms a complex with the agent to be delivered. Agents to be delivered can be therapeutic and / or diagnostic agents. Treatments which enhance delivery such as ultrasound, iontopheresis, and / or electrophereis can also be used with the disrupting agents.

The invention discloses preparation and application of a docetaxel lipid nanoparticle. The docetaxel lipid nanoparticle mainly consists of docetaxel, a solid-state lipid material, a liquid-state lipid material, an emulsifying agent and normal saline for injection with treatment effective dose. The docetaxel lipid nanoparticle is proper in grain size, uniform in distribution and high in packaging ratio, can be stably stored, and has good biocompatibility and degradability; and moreover, the docetaxel is carried in the lipid nanoparticle, so that the targeting property and endocytosis of cancer cells can be improved, the antineoplastic curative effect is improved, and the toxic and side effects are reduced.

The invention relates to a method of preparing a release pharmaceutical carrier, in particular to a method of preparing a stepwise release pharmaceutical carrier based on an aqueous two-phase system and aims to solve the problem that a pharmaceutical carrier of the prior art has a release curve that is an index curve and arrives at a release platform right after burst release. The method comprises: 1, performing ITO (indium tin oxide) surface cleaning; 2, preparing an aqueous two-phase solution; 3, preparing a vesicle solution; 4, assembling a closed preparation apparatus, and allowing reacting to obtain the stepwise release pharmaceutical carrier based on the aqueous two-phase system. The stepwise release pharmaceutical carrier based on the aqueous two-phase system prepared by the invention is stored in two phases and released separately, the release platform is pushed back, and the carrier has the advantages such as convenience of use, maintenance of normal blood concentration, avoidance of pharmaceutical accumulation, low toxic and side effect for normal cell tissues, improved therapeutic effect, safety and high speed. The stepwise release pharmaceutical carrier based on the aqueous two-phase system can be prepared by the method.

The present invention discloses hyaluronic acid- g ‑Folic acid amphiphilic polymer and its application, the main chain is hydrophilic hyaluronic acid, and the side chain is hydrophobic folic acid, which can efficiently and stably load small molecule anticancer drugs and prolong the blood circulation time of drugs; The enrichment amount is high, reaching 12.0%ID / g. After reaching the tumor tissue, the dual-targeted nanomedicine tightly binds to the surface of tumor cells and effectively enters the tumor cells through receptor-mediated endocytosis, and then realizes The drug is released quickly, resulting in a highly effective therapeutic effect. The polymer of the present invention has good biocompatibility and degradability, and is convenient to be excreted from the body; it overcomes the shortcomings of low drug delivery efficiency, less accumulation in tumor sites, low cell endocytosis efficiency, and slow intracellular release; and the method is simple to prepare , the source of raw materials is abundant, and the obtained nanomedicine has excellent freeze-drying redispersibility, which is conducive to large-scale production and application.

The invention relates to a pH-responsive polymer micelle for mucus penetration and a preparation method thereof; PLGA and PEG are combined through a pH-responsive hydrazone bond to form an amphiphilic polymer conjugate, and post-assembled to form a pH-responsive polymer micelle. polymer micelles. Hydrazylated PLGA and aldehydelated PEG were dissolved in dimethyl sulfoxide and reacted under nitrogen; the reaction solution was dialyzed in N,N-dimethylformamide for 12 to 24 hours, then precipitated with ice ether, and centrifuged Drying of the precipitate yielded a pH-responsive hydrazone-linked amphiphilic conjugate. The prepared self-assembled drug carrier maintains a uniform and small particle size, has better biocompatibility, and has pH responsiveness. It can break the hydrazone bond and remove the protection of PEG in the mucus microenvironment with a low pH value. The exposed positively charged groups interact electrostatically with the negatively charged cell membranes, increasing the endocytosis of the micelles, allowing more carriers to enter the cells for slow and controlled release of drugs, and play the role of carriers.

The invention discloses a dopamine ligand-containing two-block polymer, a synthesis method and application thereof. The polymer uses polyethylene glycol as a hydrophilic end, and phenylboronic acid-modified polyethylene glycol is used as a targeting ligand. With glutamate and glutamate dopamine as repeating units as hydrophobic ends. The dopamine ligand-containing diblock polymer prepared by the invention can be used to encapsulate doxorubicin to form drug-loaded nano micelles, and then add iron ions to form coordination bonds between dopamine and iron ions for cross-linking to form nuclear cross-linking Doxorubicin-loaded nanomicelles. The nuclear cross-linked micelle prepared by the invention is simple and convenient in preparation method, and has high drug encapsulation rate, the micelle can be kept stable in the process of blood circulation, and can realize pH-sensitive drug release in tumor cell lysosomes.