32results about How to "Enhanced EPR effect" patented technology

The invention relates to a multi-function nano prodrug system based on a dendrimer, which belongs to the technical field of biomedicines and nano medical science. The nano system comprises four function parts: an outermost layer RGD (arginyl-glycocoll-aspartate) cyclic peptide as an active targeting head group (1), a polyethylene glycol (PEG) hydrophilic chain segment (2) connected with the targeting head group and the dendrimer, an anti-tumour drug (3) connected with the dendrimer by an acid sensitive chemical bond and a dendrimer kernel (4). The general formula of the nano system is RGD-PEG-Dendrimer-DOX (doxorubicine), wherein the macromolecule attribute of a dendrimer vector makes a vector system passively target to tumor tissues through an EPR (Enhanced Permeability and retention) effect; the RGD cyclic peptide makes the vector system actively target to the tumor tissues through the interaction of a ligand and a receptor and promotes the endocytosis of the tumor tissues; the acid sensitive chemical bond ensures that a drug-carrying system is stable in systemic circulation and releases active drugs after arriving tumor positions and entering an acid organelle to perform the function of cytotoxicity.

The invention relates to a preparation method and application of an EPR effect-enhanced combined drug system, which can effectively solve the problem of preparation of antitumor drugs. Substrate, Fe 3+ As a cross-linking agent and gating switch, hydroxychloroquine and compretidine are used as model drugs, and compretidine is used as a blood vessel target molecule to construct a nanogel as an anti-tumor delivery system; the preparation process of the invention is simple and stable Reliable, energy-saving and environmentally friendly, the prepared EPR effect-enhanced combined drug system can efficiently accumulate at the tumor target site to achieve long-term controlled release; under the stimulation of the tumor microenvironment, the particle size can be transformed from large to small, and deep tumor penetration can be achieved; activation Endogenous H 2 o 2 →•OH transformation, used for local and efficient treatment of tumors, the combination of anti-angiogenesis and autophagy inhibition can have a synergistic and significant therapeutic effect, providing a new strategy for improving the efficiency of tumor treatment.

The disclosure provides a chemical exchange saturation transfer contrast agent and its preparation method and application, belonging to the technical field of nuclear magnetic resonance imaging. The contrast agent is a new type of LipoCEST contrast agent. On the basis of retaining the advantages of high sensitivity of the original iodine-based CEST contrast agent, it also has high biocompatibility and safety, and solves the problem of traditional CEST contrast agents such as iohexol. The disadvantages such as fast excretion in the tumor area and low retention rate improve the EPR effect in the tumor area. The contrast agent is formed by wrapping an iodine contrast agent with a surfactant, and the surfactant is selected from one or more of phosphatidylcholine liposomes, phosphatidylethanolamine liposomes, phosphatidylserine, lecithin or cholesterol. mixture of species. This contrast agent is used in magnetic resonance imaging.

The present invention discloses multifunctional imaging cross-linked stable nanometer drug-loading micelles and a preparation method thereof. The preparation method comprises: adding 200 mg of an amphiphilic drug carrier mPEG-S-Trityl-Cys-Dopa and a hydrophobic anti-cancer drug to an organic solvent, dissolving, and carrying out dialysis by using a dialysis bag to remove free Fe<3+>; carrying out centrifugation, and filtering the supernatant by using a 0.45 [mu]m microporous filtration membrane; and carrying out freeze drying on the filtrate, wherein the freeze-dried product is the multifunctional imaging cross-linked stable nanometer drug-loading micelles mPEG-S-Trityl-Cys-Dopa-Fe<3+> / hydrophobic anti-cancer drug. According to the present invention, the obtained nanometer micelles have the stability and the pH-sensitivity, and can be visible by MRI, can break through the single-function mode of the traditional drug delivery system, can integrate the MRI imaging function and the drug carrier function, and can achieve the synchronous diagnosis and treatment of cancers.

The invention discloses a multifunctional lanthanide nanoparticle, a preparation method thereof, a method for generating singlet oxygen by using the nanoparticle and a photodynamic therapy system. The lanthanide is excited by a near-infrared laser in combination with a hyperbaric oxygen chamber. Nanoparticles can realize oxygen supply sensitization, thereby promoting the targeted delivery of nanoparticle drugs and the generation of singlet oxygen, thereby solving the technical problems of insufficient generation of singlet oxygen and poor effect of photodynamic therapy systems in the prior art.

The invention relates to medicine preparation which is characterized by having a special physical shape, and further relates to a pro-medicine of curcumin micelle with high medicine loading and a preparation method of the pro-medicine. The preparation method comprises the following steps of: bonding the curcumin modified by flutaric anhydride and MPEG-PLA (Methoxy poly(ethylene glycol)-poly(lactic acid)) with polyhydroxy distal end in an ester bond manner to form a curcumin micelle monomer with high grafting percent; and preparing medicine-loading micelle of the curcumin through a dialysis method. The pro-medicine of the curcumin micelle with the high medicine loading, obtained by the method disclosed by the invention breaks through a medicine administration mode of a traditional carrier-coating medicine so that a medicine is a part of a carrier; in addition, by controlling the usage of inert carrier materials, the medicine loading, the grain diameter and the stability of a micelle system are remarkably modified, and an EPR (Electron Paramagnetic Resonance) effect is reinforced.

The invention relates to a somatostatin receptor-mediated tumor-targeting drug composition, which uses functional polypeptides targeting somatostatin receptors and polyethylene glycol to simultaneously modify the pharmaceutical carrier, and anti-tumor drugs or / and anti-tumor drugs Vascular drug delivery to the tumor site, enhancing the efficacy of tumor therapy.

The invention belongs to the technical field of biological medicines, and relates to a PM (PTXPEG-PLA micelles)-coated nano-cluster and a preparation method thereof. The preparation method comprises the following steps of using an emulsifying ultrasonic method to prepare prepared PM into the PM-coated nano-cluster through a crosslinking agent; finally, adding hydrophilic micromolecules with negative charges to neutralize surface positive charges, and improving the hydrophilic property of a system. The PM-coated nano-cluster has the advantage that the PM is coated into a hydrophobic kernel of the micelles, so that on the basis of not influencing the higher drug carrying amount of the original micelles, the particle size of the system is effectively increased, the hydrophilic property of the system is improved, the circulating time in a human body is prolonged, the tumor EPR (enhanced permeability and retention) effect is enhanced, and the validity and safety of the medicine in the clinical application are improved.

The invention relates to an injection anticancer long circulating targeting liposome which is characterized in that anti-angiogenic drug is combined with anticancer drug, the liposome modified by polypeptide with tumor targeting function and hydrophilic polyethyleneglycol is adopted for loading and transporting the two drugs to tumor positions, and the tumor curative effect is enhanced through the different releasing rates and action mechanism of the two drugs.

The invention discloses a demethylcantharidate-loaded mesoporous silica nanoparticle. A preparation method of the demethylcantharidate-supported mesoporous silica nanoparticle comprises the steps of preparing ammonia-modified mesoporous silica through a co-precipitation method and preparing DM-NCTD@NH2-MSN by electrostatic adsorption loading of demethylcantharidate. The prepared DM-NCTD@NH2-MSN has obvious slow-release effects and long-acting tumor suppression effects, and has a better application prospect as a DM-NCTD tumor target delivery system.

The invention relates to curcumin prodrug micelle with oxidation and reduction sensitivity, a micellar monomer and a preparation method of the micellar monomer. The invention aims at providing a synthesis design method of the curcumin prodrug micelle with oxidation and reduction sensitivity. A molecular formula of the curcumin prodrug micelle monomer is as follows: MPEG-PLA-SS-Cur. According to the preparation method of the curcumin prodrug micelle monomer, raw materials for reaction comprise (methoxyl poly(ethylene glycol)-polylactic acid (MPEG-PLA), and curcumin Cur-SS-COOH modified by dithiodipropionic acid. The curcumin prodrug micelle with oxidation and reduction sensitivity, the micellar monomer and the preparation method provided by the invention have the following advantages that the micellar monomer product obtained by the preparation method has reduction responsiveness on the curcumin prodrug micelle, breaks through a conventional drug administration mode of encapsulating a drug by using a carrier, i.e., the drug is a part of the carrier; by controlling the use of inert carrier materials, the drug loading capacity, particle size and stability of a micellar system are improved significantly, and the EPR (Ethylene Propylene Rubber) effect is enhanced.