Patent classifications
A61K9/5192
Nanoparticle, preparation process and uses thereof
The present disclosure provides a nanoparticle, a preparation process thereof, a method for treating cancer, a method for enhancing effect of a liver cancer drug, a method for ameliorating tumor hypoxia, and a method for enhancing effect of a liver cancer vaccine by using the nanoparticle.
PROCESS FOR THE PREPARATION OF A NANOPARTICULATE ACTIVE INGREDIENT
A process for the preparation of a nanoparticulate active ingredient comprises the steps of: a) providing a solvent, a pharmaceutical active ingredient dissolved in the solvent, a liquid antisolvent and a stabilizer which is dissolved in the solvent or in the antisolvent and wherein the antisolvent is miscible in the solvent; b) mixing the solvent, the active ingredient, the antisolvent and the stabilizer in a micromixer, thereby obtaining a suspension comprising a precipitate of the active ingredient, the solvent and the antisolvent. The active ingredient precipitate is present in the form of nanoparticles having an average particle size of ≥10 nm to ≤999 nm and a particle size distribution, determined by dynamic light scattering (DLS) according to ISO 22412:2017, having a polydispersity index of ≤0.2.
Metal-nucleic acid nanoparticle, preparation method therefor and use thereof
The present application relates to a metal-nucleic acid nanoparticle which is a nanoparticle having a spherical structure formed by assembly of metal ions with nucleic acids via coordination. The preparation thereof is mixing a metal ion solution with a nucleic acid solution to obtain a mixture followed by vortex, heating, centrifugation, washing with water and resuspension to obtain the metal-nucleic acid nanoparticles.
BISPHOSPHONATE LOADED STARCH NANOPARTICLE
A phosphorous compound such as STMP is used as a cross-linking agent while making a starch nanoparticle with a bisphosphonate drug in an emulsion process. Negative charge of the nanoparticle is optionally reduced or reversed by adding cations and/or cationizing the starch optionally while forming the nanoparticles. Anionic active agents, such as a bisphosphonate, are optionally incorporated into the nanoparticle during the formation process. For example, a bisphosphonate salt can be added, which promotes the crosslinking reaction while also providing bisphosphonate in the nanoparticle. The retention of both calcium and bisphosphonate in the nanoparticle is improved when both salts are used. Alternatively, the nanoparticle may be used without added calcium. The nanoparticles may be useful for the treatment of osteoporosis or other skeletal disorders or cancer.
SEQUENTIAL MULTI-STEP FLASH NANOPRECIPITATION FOR THE FORMATION OF NANOPARTICLES WITH HIGH CORE LOADINGS
From diagnostic imaging to drug delivery, nanoparticles have found a tremendous variety of uses across fields. Often, when designing these nanoscale constructs, the two most important criteria are particle size and core loading. For example, small particles below 100 nm can have many advantages for drug delivery—including improved specificity to tumors through the enhanced permeability and retention (EPR) effect. Likewise, higher loading nanoparticles translate very well to more effective drug delivery and cancer imaging—allowing for lower dosage and reduced costs. Traditional formulations of nanoparticles using drug absorption or precipitation methods generally struggle to obtain >50% loading. Disclosed herein is a precipitation process allowing for production of stable particles at very high core loading by taking advantage of different time scales while maintaining biologically relevant sizes. New mixing designs allow for the separation of the precipitation and stabilization steps to generate these high loading nanoparticles.
NOVEL METHOD OF POLYMERIC NANOPARTICLE FABRICATION FOR CANCER TREATMENT AND OTHER DRUG DELIVERY APPLICATIONS
A novel and innovative method of fabricating nanoparticles with reproducible characteristics from batch-to-batch and during scale-up. The method is a dipolymerization-precipitation reaction facilitated by the inverse electron demand Diels-Alder (IEDDA) reaction.
Polymer complex for anticancer immune therapy based on ultrasound comprising oxalate derivatives and Method of preparation thereof
The present invention relates to a polymer composite for ultrasound-based cancer immunotherapy, which comprises an peroxalate derivatives, and a preparation method thereof. The polymer composite according to the present invention is a structure in which the peroxalate derivatives are encapsulated in an amphipathic polymer compound in which a biocompatible polymer and a sonosensitizer are combined. The peroxalate derivatives produce free electrons and carbon dioxide (CO.sub.2) by reaction with a high concentration of hydrogen peroxide (H.sub.2O.sub.2) in cancer tissue, the generated electrons raise the energy level of the sonosensitizer in the polymer composite to increase the amount of reactive oxygen species (ROS) production, thereby exhibiting an effect of increasing the death rate of cancer cells. In addition, by ultrasound treatment, immunogenic cell death (ICD) is induced due to the cavitation effect of the produced CO.sub.2, so molecules capable of activating immune cells in cancer cells are released without damage to induce an immune response to cancer. Therefore, the polymer composite according to the present invention is expected to be effectively used as an ultrasound-based cancer immunotherapeutic agent.
NICOTINAMIDE ADENINE DINUCLEOTIDE ACTIVATOR AND USE THEREOF
Disclosed are methods for treating muscular diseases that involve the use of a nicotinamide adenine dinucleotide (NAD) activator.
GM3 functionalized nanoparticles
Embodiments disclosed herein relates to ganglioside GM3-containing mixed lipids nanoparticles having an overall size between 60-100 nm, the making thereof and the uses. The nanoparticles selectively targeted to CD169+ expressing cells such as dendritic cells and macrophage. The nanoparticles are endocytosed by the CD169+ expressing cells.
Ocular compositions
The invention provides methods of making microparticle and nanoparticle ocular implants from a compositions comprising: 99 to 60% (w/w) of a photopolymerizable composition selected from the group of fragments or monomers consisting of polyalkylene glycol diacrylate and polyalkylene glycol dimethacrylate, wherein the photopolymerizable composition has a molecular weight in the range of 100 to 20,000 Dalton; a biodegradable polymer selected from the group consisting of aliphatic polyester-based polyurethanes, polylactides, polycaprolactones, polyorthoesters and mixtures, copolymers, and block copolymers thereof; a photoinitiator; and a therapeutic agent.