7 results about "Brain targeting" patented technology

The application discloses a preparation method of a novel hierarchical drug release lemon exosome nano preparation and application thereof in brain glioma treatment and belongs to the field of nano medicines. The method comprises the following steps: extracting and purifying lemon exosomes, introducing an anti-glioma drug and a first part of LRP1 up-regulating agent into the inner cavity of the exosomes through electroporation, instantaneously constructing a tumor microenvironment responsive nanogel core to fix the drug, embedding a second part of LRP1 up-regulating agent into the lipid layer of the exosome, modifying Angiopep-2 to realize brain targeting, and obtaining the nano preparation through purification. The preparation has the hierarchical drug release characteristics of outer layer early release and inner cavity delayed release, can improve the efficiency of drug crossing the blood-brain barrier and accumulation at the tumor site, enhance the anti-glioma effect, solves the technical problem that the existing drug loading system is difficult to realize multi-drug phased release, and provides a new strategy for brain glioma treatment.

This invention relates to an insoluble drug formulation based on dialkylimidazolium biomimetic lipids, its preparation method, and its application, belonging to the field of pharmaceutical formulations. First, an insoluble drug is directly coupled to the primary amine group of the dialkylimidazolium biomimetic lipid or coupled via a linker to form a lipid-drug conjugate. Then, the lipid-drug conjugate, along with other lipid excipients, is dissolved in the dialkylimidazolium biomimetic lipid, and self-assembled in an aqueous phase to form a drug-loaded lipid nanoparticle delivery system with significant drug solubilizing effect. This drug delivery system exhibits good biocompatibility and plasma stability. It can cross the blood-brain barrier and selectively deliver drugs to glioma cells, achieving sustained release of the conjugated insoluble drug in the tumor microenvironment. This provides a new strategy for improving the pharmacokinetic properties of insoluble small-molecule antitumor drugs, including brain targeting, half-life, and bioavailability.

This invention relates to an enzyme-responsive brain-targeting sustained-release formulation based on dialkylimidazolium biomimetic lipids, its preparation method, and its application, belonging to the field of drug delivery. First, dialkylimidazolium biomimetic lipids are covalently coupled with natural phospholipids to form a dialkylimidazolium conjugate. Then, this dialkylimidazolium conjugate is self-assembled with dialkylimidazolium biomimetic lipids, natural phospholipids, cholesterol, and a therapeutic drug to form a drug-loaded lipid nanoparticle delivery system. This drug delivery system can effectively cross the blood-brain barrier to achieve brain-targeted delivery of the loaded drug. In the glioma microenvironment, this drug delivery system can gradually hydrolyze the dialkylimidazolium conjugate through an enzyme-responsive mechanism to achieve sustained release of the loaded drug, providing a new strategy for improving the brain targeting and efficacy of different types of anti-glioma drugs, such as small nucleic acid drugs, peptide drugs, and small molecule drugs.

The application discloses a cannabinoid 1 type receptor-mediated brain-targeting lipid nanocapsule drug loading system and a preparation and application thereof, and belongs to the technical field of targeted drugs. The brain-targeting lipid nanocapsule drug loading system comprises a drug-loaded lipid nanocapsule, the surface of the lipid nanocapsule is modified with a ligand compound of a CB1 receptor, and the ligand compound is one of quebrachamine, methoxylated myristicin, chelerythrine, ostruthol or cannabigerol. The application utilizes the lipid nanocapsule carrier to load a compound X with neuroprotective activity, prolongs the circulation time of the compound X in the body, adsorbs a ligand compound Y on the surface of the lipid nanocapsule, can specifically recognize the CB1 receptor highly expressed on the brain nerve epidermal cells, can transport across the blood-brain barrier, and improves the drug concentration in the brain tissue and cells. The preparation method provided by the application is simple in operation, easy to popularize, can be used for preparing drugs crossing the blood-brain barrier, and has a wide application prospect.

The present application provides a kind of drug composition and its application for targeting neuroinflammation, the composition is composed of active ingredient and natural nanometer delivery carrier for encapsulating active ingredient, the active ingredient includes fisetin, pyrrole quinoline quinone, resveratrol, bauhinia A, apigenin, saffron, quercetin and hair monkey element;The natural nanometer delivery carrier is the plant source extracellular vesicle of surface modification brain targeting molecule.The composition of the present application realizes the intervention to vascular cognitive impairment by multi-component scientific compatibility, combined with two-stage brain targeting delivery design, solves the pain points of low blood-brain barrier penetration rate and poor bioavailability of natural active ingredient, has the effect of strong anti-inflammatory and significantly improving cognitive function, excellent safety, can be used for preparing the medicine for preventing or adjuvant therapy neuroinflammation related vascular cognitive impairment, has very high clinical conversion value.

Disclosed in the present invention are a non-natural amino acid, and a preparation method therefor and the use thereof. The present invention provides, for the first time, a new class of non-natural amino acids designed by introducing a long and flexible side-chain amino acid into a side chain of a canonical ASF. The design not only enhances the stability of the resulting non-natural amino acids, but also expands the reaction radius thereof, thus enabling same to access more distant amino acid residues and thereby improving the reactivity thereof. Moreover, compared with other covalent amino acids, the non-natural amino acid exhibits a higher reaction rate and binding efficiency. Polypeptides obtained on the basis of the non-natural amino acid and related drugs thereof exhibit high safety, can cross the blood-brain barrier to achieve brain targeting, and have a better anti-tumor activity, thereby demonstrating an extremely high medical value.

The application discloses a kind of functionalization exosome-traditional Chinese medicine small molecule composite preparation T-pEXOs@GB and its preparation method and application.The composite preparation encapsulates ginkgolide B (GB) in the exosome of healthy plasma, and is functionally modified neuron target peptide RVG (DSPE-PEG-RVG) on its surface, so that it has brain targeting and oxygen supply functions.The preparation method provided by the application can efficiently and controllably prepare the composite preparation with uniform particle size and good stability.The T-pEXOs@GB composite preparation of the application can be targeted to deliver to brain ischemia and hypoxia injury area, significantly reduce oxidative stress and inflammatory response, reduce cerebral infarction volume, improve neurological deficit score, and improve the survival rate of animal model, and can be used to prepare drugs for preventing and treating acute high altitude cerebral hypoxia, ischemic stroke, neonatal hypoxic-ischemic encephalopathy and other cerebral ischemia and hypoxia injury, and has good market prospect.