53 results about "Targeted liposomes" patented technology

The invention belongs to the technical field of biological medicines, and particularly relates to application of a targeted liposome as an active component in preparation of a medicine for treating ischemic brain injury. The targeted lipidosome for treating cerebral arterial thrombosis is prepared by fusing the lipidosome and the platelet-neutrophil aggregate membrane, realizes efficient and specific targeting of an ischemic brain region, effectively reduces brain tissue infarction and damage of a new region, relieves brain inflammation through multi-channel regulation and control, and improves the cerebral arterial thrombosis treatment effect. The compound can be used as an active ingredient for preparing a medicine for treating ischemic brain injury. And after the target liposome is further coated with a rutin drug, the synergistic treatment effect is realized. The liposome medicine can be used as an active component and has a good application prospect in treatment of ischemic brain injury diseases.

The invention relates to the technical field of biological medicine, in particular to a functionalized targeted liposome and application thereof, and the functionalized targeted liposome comprises lipid and a targeted ligand, wherein the targeting ligand can be specifically combined with a TREM2 receptor. According to the lipidosome, the targeting ligand can be specifically combined with the TREM2 receptor, accurate targeting of cells with the surface containing the TREM2 receptor is achieved, it is ensured that the cells directly act on target cells, the accuracy of a delivered substance is further improved, and the lipidosome has the advantages of being targeting, high in stability, small in side effect and high in bioavailability. The functionalized targeted liposome can be applied to the development of drug carriers, pharmaceutical compositions and the like, and has wide application prospects, for example, the liposome is dynamically connected with hydrogel molecules through a borate bond to prepare a hydrogel pharmaceutical composition containing the functionalized targeted liposome, and the application prospect is wide. The liposome disclosed by the invention can respond to an inflammatory environment according to pH and ROS changes of a surrounding environment to release the liposome disclosed by the invention, targets cells with TREM2 receptors on the surfaces, namely microglial cells (with the TREM2 receptors on the surfaces) by virtue of the target ligands exposed on the surfaces, regulates the polarization state of the cells, inhibits the polarization of the cells to a pro-inflammatory M1 type and promotes the polarization of the cells to an anti-inflammatory M2 type, so that the anti-inflammatory effect of the liposome is improved. Therefore, the local microenvironment of the spinal cord injury part is improved, and nerve regeneration is promoted.

The invention belongs to the technical field of medicine, and discloses a sea cucumber and ganoderma lucidum immune steady-state compound and a composite enzymatic hydrolysis targeted liposome co-delivery preparation process thereof.The sea cucumber and ganoderma lucidum immune steady-state compound is composed of sea cucumber, ganoderma lucidum, American ginseng, dried oyster meat, fructus lycii and perilla leaves; the ganoderma triterpenes release free polysaccharides and are combined with a liposome intestinal targeted delivery system, so that the absorption rate of the polysaccharides is greatly improved to 18-22% from 5% in the traditional process, the ganoderma triterpenes are emulsified and entrapped through a liposome double-layer membrane, and meanwhile, the permeation promotion effect of perillaldehyde in the perilla leaf volatile oil is supplemented, so that the transmembrane transport efficiency is remarkably enhanced, the absorption rate is improved to 12-15% from 2%, and the bioavailability is improved. The zinc element decomposes oyster zinc protein into free zinc ions through a composite enzymolysis technology, and the free zinc ions and vitamin C form a stable chelate, so that the antagonism of intestinal tracts is reduced, the zinc absorption rate is increased from 20% to 45-50%, and a solid foundation is laid for fully playing a compound immune regulation effect.

The invention discloses an emulsifier for preparing a Pickering emulsion, the Pickering emulsion as well as a preparation method and application of the Pickering emulsion. The emulsifier of the Pickering emulsion is obtained by dissolving distearoyl phosphatidylcholine, cholesterol and distearoyl phosphatidyl ethanolamine-polyethylene glycol 2000 in ethanol, carrying out rotary evaporation to remove ethanol, then adding an antigen aqueous solution containing an antigen, continuing rotary evaporation to obtain liposome nanoparticles, heating the liposome nanoparticles with mannose in a water bath, and carrying out freeze drying. The Pickering emulsion is obtained by dispersing an emulsifier in water as a water phase, taking squalene as an oil phase, mixing the water phase and the oil phase, and homogenizing. The Pickering emulsion disclosed by the invention is prepared by taking antigen presenting cell targeted liposome nanoparticles as a raw material; and the antigen has excellent ion concentration characteristic, pH stability, temperature stability and storage stability, and can protect the integrity of the antigen.

The application discloses a method for modifying phospholipids and application thereof in preparation of liver-targeted liposomes, relates to the field of drug delivery, and first utilizes cholate and mannose to modify phospholipid molecules DSPE-PEG 2000 respectively 2000 Two raw materials DSPE-PEG 2000 -CA and DSPE-PEG 2000 -MAN for synthesizing liposomes are synthesized, and then cholesterols, DSPC and DC-cholesterols are added in a certain proportion to obtain liposomes with liver targeting property, which have high cell safety and liver cell targeting property.

Methods and compositions for the treatment of viral infections, such as HIV infection, are disclosed herein. In certain embodiments, a molecular conjugate comprising a viral capture domain and an immunostimulant molecule is provided.

The application discloses a liver-targeting lipid carrier as well as a preparation method and application thereof, relates to the field of drug delivery, and utilizes cholate and mannose to respectively modify a phospholipid molecule DSPE-PEG 2000 After two raw materials DSPE-PEG-CA and DSPE-PEG-MAN composed of synthetic liposomes are obtained, the liver-targeting lipid carrier is obtained according to a certain proportion of cholesterol, DSPC, DC-cholesterol and the like, and the liposome has high cell safety and liver targeting.

The invention provides a synthesis method and a synthesis device of lipidosome, and the method comprises the following steps: respectively introducing two liquids of an organic phase and a water phase into two sample introduction channels of a Y-shaped flow channel; the Y-shaped flow channel comprises the two sample introduction channels and a synthesis channel communicated with the convergence position of the two sample introduction channels; and driving a regular pentagonal special ultrasonic device arranged at the bottom of the synthesis channel to work, and mixing the two liquids in the synthesis channel at least through micro vortexes which are generated in the liquids in the synthesis channel and are distributed at the positions of the edges of the regular pentagon when the special ultrasonic device works, so as to generate the target liposome. Through collaborative design of the micro-channel structure and the special ultrasonic device, the synthesis efficiency of the lipidosome can be remarkably improved, and the average particle size and uniformity of a product in the synthesis process of the lipidosome are optimized.

This invention relates to the fields of pharmaceuticals and nanomedicine, specifically disclosing the preparation of a dual-targeting liposome drug delivery system and its application in stroke. The dual-targeting liposome drug delivery system comprises neutrophils, artemisinin, edaravone, and liposomes. The liposomes co-load artemisinin and edaravone, and their surfaces are modified with sialic acid derivatives and phosphatidylserine to form liposome nanomedicines. The neutrophils act as carriers, transporting the drug across the brain border (BBB) ​​and targeting it to the ischemic brain region. This dual-targeting strategy achieves precise two-stage drug delivery to the ischemic brain region. This delivery system can inhibit NLRP3 inflammasome activation, reduce pyroptosis, and promote microglial polarization towards the M2 anti-inflammatory phenotype, thereby effectively treating cerebral ischemia-reperfusion injury or ischemic stroke.

The invention discloses a targeted liposome and application thereof, a targeted liposome preparation and a preparation method and application thereof, and relates to the technical field of biology.The targeted liposome is prepared from, by mole, 50%-55% of distearoyl phosphatidylcholine, 30%-35% of cholesterol, 4%-6% of phosphatidyl glycerol, 7%-8% of DSPE-PEG2000 and 0.3%-0.6% of DSPE-PEG2000-targeted peptide, and the targeting peptide in the DSPE-PEG2000-targeting peptide comprises at least one of an ANG2 peptide, a Tf peptide and an ApoE peptide. According to the application, the targeted liposome crosses the blood brain barrier, and efficient release of drug molecules aiming at brain glioma cells is realized.

The invention relates to the technical field of biological medicine, and particularly discloses a lipidosome targeting SELENOP + macrophages, a preparation method of the lipidosome and application of the lipidosome in lung squamous cell carcinoma treatment. According to the lipidosome, an SELENOP antibody is used as a targeted modification molecule, si-SELENOP and s-ABCA1 / G1 are loaded, and accurate delivery of siRNA in target cells is achieved through specific binding of the antibody and a SELENOP receptor on the surface of a SELENOP + macrophage. The targeting liposome prepared by the invention can specifically inhibit cholesterol efflux pathways of SELENOP + macrophages, reverse tumor phenotypic polarization, remodel a tumor immune microenvironment and recover anti-tumor activity of immune cells such as CD8 + T cells, NK cells and the like. When the liposome is independently used or combined with a PD-1 antibody, the growth and metastasis of the lung squamous cell carcinoma can be remarkably inhibited, the treatment effect is improved, a brand new metabolism-immunity synergistic targeted treatment strategy is provided for the lung squamous cell carcinoma, and the liposome has a good clinical application prospect.

The application belongs to the technical field of medicine, and relates to preparation and application of a liposome prodrug overcoming adriamycin resistance. 2000 On the basis, the prodrug is loaded in a constructed targeted liposome (DSPE-PEG The preparation method is simple, the stability is good, high-efficiency drug loading and delivery are realized, and the liposome prodrug is stable, slow-released, safe, and the like. The liposome prodrug can target the folate receptor on the surface of a tumor, under the action of high-level GSH in a tumor cell, the disulfide bond is broken and BQR and DOX are released. BQR can induce tumor cell ferroptosis and hinder DNA repair, and can synergistically kill tumor cells with adriamycin while overcoming cell resistance to adriamycin. The liposome prodrug prepared in the application realizes targeted delivery of drugs, has good in-vitro anti-tumor activity, overcomes adriamycin resistance, and has a broad development prospect.

A natural immune agonist complex, consisting of an immune agonist and a targeted liposome, where the immune agonist is M(cGAMP)Ln. The targeted liposome is formed by a nanobody targeting a tumor microenvironment, a cell membrane-targeted penetrating peptide, or a blood-brain barrier-targeted penetrating peptide with a liposome through chemical bonding. This application further provides a preparation and application of the natural immune agonist complex.

The present application relates to the technical field of biological medicine, in particular to a functionalized targeted liposome and application thereof, comprising: lipids and a targeting ligand; wherein the targeting ligand can specifically bind to a TREM2 receptor. The liposome of the present application can specifically bind to the TREM2 receptor by means of the targeting ligand, realize precise targeting of cells containing the TREM2 receptor on the surface, ensure direct action on target cells, and further improve the precision of delivered substances. The liposome has targeting property, high stability, small side effects, and can be applied to the development of drug carriers, pharmaceutical compositions, etc., and has a wide application prospect. For example, the liposome of the present application is dynamically connected with a hydrogel molecule by a borate ester bond to prepare a hydrogel pharmaceutical composition containing the functionalized targeted liposome of the present application. The hydrogel pharmaceutical composition can release the liposome of the present application according to the change of pH and ROS in the surrounding environment in response to an inflammatory environment, and target cells containing the TREM2 receptor on the surface, i.e. microglial cells (having the TREM2 receptor on the surface), by virtue of the targeting ligand exposed on the surface, and regulate the polarization state of the cells, inhibit the polarization of the cells to the pro-inflammatory M1 type, and promote the polarization of the cells to the anti-inflammatory M2 type, thereby improving the local microenvironment of the spinal cord injury site and promoting nerve regeneration.

The invention relates to the technical field of drug nano delivery, and discloses a disulfiram derivative CPD12C15 folic acid targeted liposome as well as a preparation method and application thereof. The lipidosome is of a closed vesicle-shaped structure, and a lipid shell layer of the lipidosome is enclosed by a lipid bilayer which is jointly formed by lecithin, cholesterol and a DSPE lipophilic end of DSPE-PEG2000-Fa; a PEG-folic acid hydrophilic end of the DSPE-PEG2000-Fa extends and is exposed on the outer surface of a lipid shell layer, so that a folic acid receptor is endowed with a targeting function; the inner water phase core is a water-based cavity enclosed by a lipid shell layer, and the active component CPD12C15 is encapsulated in the inner water phase core. Compared with the prior art, the liposome disclosed by the invention has the advantages of high encapsulation efficiency, high drug loading capacity, pH-sensitive controlled release and targeted enrichment in hepatocellular carcinoma tissues, can remarkably inhibit tumor proliferation, migration and angiogenesis and induce apoptosis, and improves the curative effect and reduces the toxicity by regulating a PI3K / AKT pathway.

The present application relates to an exosome fusion liver-targeting liposome drug delivery system and its preparation method and application, and belongs to the field of polymer materials and pharmaceutical preparations. The present application discloses an exosome fusion liver-targeting liposome drug delivery system, which uses high-concentration PEG 8000 and Nycodenz in combination to synergistically improve the exosome and liposome fusion efficiency, form biomimetic vesicles with uniform size and high drug loading. The exosome not only can play the characteristics of anti-inflammatory and antioxidant, but also plays a role in resisting harsh gastrointestinal environment and crossing biological barriers. In addition, the liposome is modified by cholic acid derivative by using EDC / NHS mediated amidation reaction, which realizes precise targeting of liver and sufficient accumulation in liver. The above-mentioned effects synergistically realize the treatment of type II diabetes and non-alcoholic fatty liver disease.

The invention discloses a multifunctional medical coupling agent and a preparation method and application thereof, and belongs to the field of medical materials.The coupling agent comprises (1) an electric insulation gel matrix formed by perfluoropolyether oil and fluorinated gel; (2) temperature-responsive nanoparticles which are uniformly dispersed in the gel matrix and have surfaces subjected to hydrophobic modification, wherein the temperature-responsive nanoparticles contain rare earth ions Y < 3 + >, Yb < 3 + > and Er < 3 + >; and (3) fluorinated targeted liposome which is uniformly dispersed in the gel matrix and is modified with sulfhydrylated RGD peptide on the surface, wherein a therapeutic drug is encapsulated in the fluorinated targeted liposome. Wherein the perfluoropolyether oil ensures the electrical insulation safety; the temperature response type nanoparticles emit fluorescence signals, and the fluorescence signals can be inverted into temperature values; the sulfhydrylated RGD peptide recognizes and is combined with tumor angiointegrin alpha v beta 3, so that active targeting can be realized. The multifunctional medical coupling agent disclosed by the invention has multiple functions of electrical insulation safety guarantee, temperature monitoring, targeted drug delivery and the like, and meets the requirements of complex medical scenes.

The invention particularly relates to a cabozantinib and osimertinib co-loaded targeting liposome and application thereof in overcoming EGFR-TKI drug resistance, and belongs to the technical field of biological medicine. The co-drug-loaded targeting liposome disclosed by the invention is coated with osimertinib and cabozantinib at the same time, and a GE11 peptide targeting ligand is connected to a membrane material of the co-drug-loaded targeting liposome; wherein the mass ratio of osimertinib to cabozantinib is 1: (0.5-2), preferably 1: 1; the membrane material comprises hydrogenated soybean phosphatidylcholine, cholesterol and DSPE-PEG2000, and the mass ratio of the hydrogenated soybean phosphatidylcholine to the cholesterol to the DSPE-PEG2000 is (2.5-3.5): 1: 1. According to the co-drug-loading targeting liposome disclosed by the invention, a drug can be synergistically delivered to a tumor site through active targeting mediated by GE11 peptide, an EGFR main pathway and key drug-resistant bypasses such as MET are efficiently inhibited, and the co-drug-loading targeting liposome shows a remarkable synergistic interaction effect in the aspect of reversing acquired drug resistance of osimertinib.

The invention belongs to the technical field of drug carriers, and particularly relates to tumor-targeted luteoloside liposome loaded paclitaxel and a preparation method thereof. According to the tumor targeted liposome, luteoloside and soya bean lecithin are used as membrane materials, a blank liposome (C-Blank) is prepared through a membrane hydration method and a high-pressure homogenization method, and a hydrophobic drug paclitaxel (PTX) is loaded to obtain a drug-loaded liposome (C-PTX). Wherein the luteoloside can significantly enhance the mechanical strength and thermodynamic stability of the lipid bilayer, and also can realize active tumor targeting through a glucose transporter GLUT1 mediated endocytosis pathway, and meanwhile, PTX is efficiently entrapped in a liposome hydrophobic core. The C-PTX liposome prepared by the invention is small in particle size, relatively good in endocytosis capability, good in blood long-circulation effect and drug delivery capability, good in stability and dispersity, high in drug encapsulation efficiency and beneficial to effective delivery and release of drugs. The oral bioavailability of PTX is improved, and C-PTX has an obvious inhibition effect on lung cancer cells. The drug loading system effectively overcomes the defects that a traditional paclitaxel preparation is poor in water solubility, large in system toxicity, insufficient in targeting performance and the like, the highly-uniform dispersion state and long-term storage stability of the drug loading system lay a foundation for industrial production, and the drug loading system shows important clinical application potential in the fields of precision medicine and transformation medicine.

The application discloses a liposome construction recommendation method and device based on drug molecular structure, and the recommendation method is characterized in that, after receiving the molecular information of a target drug input by a user, firstly, the molecular information is subjected to data preprocessing; then, a pre-trained liposome recommendation model is used to make a recommendation based on standard molecular characteristic data; finally, the construction parameters are optimized based on the target liposome construction type, so that the target liposome construction parameters are obtained. The pre-trained neural network model is used to make a recommendation on the construction type of the liposome based on the drug molecular information, and the construction parameters of the liposome are optimized to obtain the optimal liposome construction parameters. The drug molecular structure characteristics are directly associated with the liposome construction scheme, and the efficiency and accuracy of the liposome construction are improved.

The invention discloses an engineered exosome for targeted improvement of an ovarian function as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The engineered exosome is prepared by performing membrane fusion on an exosome from human umbilical cord mesenchymal stem cells overexpressing VEGFA (vascular endothelial growth factor A) genes and an FSH (follicle stimulating hormone) beta subunit derived peptide modified liposome. The exosome has the functions of promoting angiogenesis and resisting apoptosis of VEGFA (vascular endothelial growth factor A) and the ovarian targeting capability of the FSH beta peptide fragment, can accurately act on ovarian granular cells, and effectively improves the ovarian microenvironment and follicle development. The preparation method comprises the following steps: constructing VEGFA overexpression engineering cells, extracting exosomes, synthesizing targeted lipidosome, performing ultrasonic induction fusion and the like. The engineered exosome provided by the invention has the advantages of strong targeting, definite curative effect, high uniformity, good safety and the like, and provides a new strategy for cell-free treatment of ovarian function decline and related reproductive disorders.

The invention discloses a preparation method and application of glucose transporter 1 targeting brucea javanica fatty acid prodrug liposome, and belongs to the technical field of pharmaceutical preparations. Specifically, the invention relates to a targeting material based on glucose transporter 1 (GLUT1), a tumor sensitive bond bridged brucea javanica-fatty acid prodrug, construction of an active targeting liposome containing the prodrug, and application of the active targeting liposome in preparation of antitumor drugs. The anti-liver cancer effect of the liposome is investigated. Results show that the lipidosome designed by the invention can realize targeted drug delivery to tumor tissues, the anti-tumor efficacy of the brucea javanica terpene drug is remarkably improved, the biosafety is high, and the toxicity is reduced by two times compared with that of the original drug brucea javanica bitter alcohol. The tolerance dose of the chemotherapeutic drug is expected to be increased, the anti-tumor effect of the chemotherapeutic drug is improved, and a new direction and a new thought are provided for the delivery of the chemotherapeutic drug.

The invention provides a nasal drug delivery three-stage recursion type targeting hydrogel microsphere as well as a preparation method and application thereof, and belongs to the technical field of drug delivery. The invention develops a three-stage recursive targeting nasal drop, and the first-stage nasal mucosa targeting is realized by non-invasive drug delivery into the brain through the charge modified hydrogel microsphere nasal cavity; a targeting liposome carrying CTLA-4 is combined with the activated microglial cells, so that second-stage cell targeting is realized; mitochondrial regulation and control are carried out by releasing DHEA to complete three-stage targeting, and finally, multi-stage precise targeting and intracerebral regulation and control are realized. The three-stage recursion type targeted nasal drops can break through the complex physiological and pathological microenvironment of a brain body layer by layer to directly reach lesion core mitochondria of microglia cells, the Drp-1 pathway is regulated and controlled through DHEA, the abnormal mitochondrial division is remarkably inhibited, the mitochondrial morphological function is stabilized, microglia cell activation is inhibited, and cognitive impairment caused by anesthesia operation is relieved. In conclusion, the research provides a new method for treating various central nervous system diseases.

The application provides a liposome synthesis method and a synthesis device, and the method comprises the following steps: two liquids of an organic phase and an aqueous phase are respectively introduced into two sample introduction channels of a Y-shaped flow channel; the Y-shaped flow channel comprises the two sample introduction channels and a synthesis channel which is in communication with the converging position of the two sample introduction channels; a special ultrasonic device in the shape of a regular pentagon arranged at the bottom of the synthesis channel is driven to work, and at least through the micro-vortices generated in the liquid in the synthesis channel and distributed at the positions of the edges of the regular pentagon during the working of the special ultrasonic device, the two liquids in the synthesis channel are mixed to generate target liposomes. Through the cooperative design of the micro-flow channel structure and the special ultrasonic device, the synthesis efficiency of the liposomes can be significantly improved, and the average particle size and uniformity of the product in the synthesis process of the liposomes are optimized.

The invention discloses a cabozantinib liver-targeting lipid nanoparticle injection as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The cabozantinib injection is prepared from the following components in percentage by mass: 0.8 to 1.5 percent of cabozantinib, 2.5 to 4.0 percent of DSPE-PEG2000-galactose, 35.0 to 42.0 percent of dipalmitoyl phosphatidylcholine, 6.0 to 8.0 percent of sitosterol, 3.0 to 5.0 percent of composite freeze-drying protective additive and the balance of citric acid-sodium citrate buffer solution with the pH value of 4.0, and the composite freeze-drying protective additive is a mixture of hydroxypropyl-cyclodextrin and mannitol in a mass ratio of 2 to 1. The preparation provided by the invention reduces systemic toxicity, significantly improves the drug concentration of liver and tumor parts, has better tumor inhibition effect than clinical positive drug adriamycin, is suitable for treatment of liver cancer and hepatic metastatic tumor, and has a relatively high application prospect.

The invention relates to an application of TLR < 4 > siRNA (TLR < 4 > siRNA (at) LNP-CSA-BP) coated with TLR < 4 > siRNA (TLR < 4 > siRNA) connected with placental Chondroitin sulfate A binding peptide (Placental Chondroitin sulfate A binding peptide, CSA-BP) injected in a maternal pregnancy period, in improvement of pregnancy complications and prevention of progeny neurodevelopment disorder diseases, in particular to an application of TLR < 4 > siRNA coated with LNP-CSA-BP coated with TLR < 4 > siRNA coated with LNP-CSA-BP. According to the invention, TLR4siRNA (at) LNP-CSA-BP is used for carrying out caudal vein injection on a pregnant mouse, so that a placenta and fetal brain inflammation microenvironment (induced by toxoplasma gondii STAg) maternal immune activation can be inhibited. Behavior experiments further prove that under a maternal immune activation model, TLR4siRNA (at) LNP-CSA-BP caudal vein injection pregnant mice can significantly improve phenotypes of neurodevelopmental disorder diseases of filial generation mice, such as core symptoms (social ability and repeated engraving behaviors) of autism behaviors, and the promising transformation prospect is proved.

The invention discloses a polypeptide specifically bound with human lung cancer cells and application of the polypeptide. The amino acid sequence of the disclosed polypeptide is FGWQTNHNTSFM. The polypeptide is combined with human lung adenocarcinoma, and the tissue specificity and sensitivity are good. The polypeptide is used for preparing a lung cancer targeted doxorubicin (DOX) liposome, and in-vitro experiments prove that the targeted liposome drug has a better lung cancer cell killing effect than common DOX. The polypeptide sequence has an important use value prospect in early imaging diagnosis of lung cancer and research and development of targeted antitumor drugs.

This invention relates to an immunoliposome containing tebuconazole, its preparation method, and its application in anti-breast cancer treatment. The tebuconazole immunoliposome is composed of tebuconazole coated with phospholipids and cholesterol, and modified with trastuzumab. The preparation method of the tebuconazole immunoliposome of this invention is simple and exhibits excellent anti-tumor effects. The novel tebuconazole immunoliposome can overcome the drawback of tebuconazole's non-selectivity for tumor cells, thus enhancing its anti-tumor efficacy. Furthermore, the actively targeted immunoliposome with trastuzumab as a target exhibits significant targeting in vivo, and its anti-tumor effect is significantly different from that of non-targeted liposomes. This invention provides a new avenue for the anti-tumor application of tebuconazole and is of great significance for advancing the clinical application of tebuconazole.

The present application relates to ligands targeted to epidermal growth factor receptor (EGFR) and compositions for use in treating tumors. Specifically, a ligand targeted to EGFR is disclosed. The ligand comprises a heavy chain variable domain and a light chain variable domain. The ligand may be selected from the group consisting of a single chain variable fragment, a fusion protein, a monoclonal antibody, and an antigen-binding fragment thereof. The ligand may be conjugated to a liposome or a nanoparticle that encapsulates at least one chemotherapeutic agent to form a ligand-targeted liposomal or nanoparticle drug. Also disclosed are conjugates and formulations for use in treating tumors such as squamous cell carcinoma of head and neck. A method for making a ligand-targeted liposomal drug is also disclosed. The drug may be a chemotherapeutic agent selected from the group consisting of doxorubicine and vinorelbine.