2158results about How to "High encapsulation efficiency" patented technology

A liposomal aqueous dispersion and method of making the liposomal aqueous dispersion is useful for encapsulation of drugs. The liposomal aqueous dispersion comprises: an aqueous suspension medium; multilamellar liposomes comprising an anionic phospholipid and cholesterol as essential components; neutral phospholipid in a mole ratio of 0 to 40% based on the total amount of said multilamellar liposomes; and a cation moiety-containing water-soluble drug, wherein the electrolyte concentration of said aqueous suspension medium is not more than 40 mM.

The present invention relates to a liquid-solid mixed lipid nano-slow release system for cosmetics and a preparation method thereof. The release system is composed of nanoparticles constituted by liquid lipid and solid lipid and at least one active ingredient coated in the nanoparticles. The preparation method includes: (1) dispersing a mixing carrier of the solid lipid and the liquid lipid to an organic solvent, adding the active ingredient, and heating in a water bath to dissolve the solid lipid to get an organic phase solution; (2) formulating polyvinyl alcohol into an aqueous phase solution, and adjusting the pH to be acidic to get an aqueous phase solution; and (3) adding the organic phase solution to the aqueous phase solution under the conditions of mechanical agitation with stirring to get a mixed lipid dispersion liquid which is then centrifuged and separated to obtain the nano-slow release system. The nano-slow release system is simple in preparation method and high in stability. The dimensions of the particles are in nanoscale, and the particle size is controllable. The entrapment efficiency of the liquid-solid mixed lipid nanoparticles has been greatly improved than simple solid nanoparticles.

The invention discloses a preparation method of essence microcapsules. The preparation method comprises the following steps: (1) dissolving chitosan in acetum; (2) adding emulsifier and essence into the chitosan acetum for high-speed emulsification and dispersion to obtain the chitosan essence emulsion; (3) adding the mixed solution of sodium alginate and sodium tripolyphosphate dropwise into the chitosan essence emulsion; (4) adjusting the pH value of the system to 5-7 with NaOH solution to obtain the condensed essence microcapsules; and (5) adding cross-linking agent into the condensed essence microcapsule system to perform chemical cross-linking process on the condensed essence microcapsules to obtain the essence microcapsules. For the essence microcapsules prepared according to the method disclosed by the invention, as chemical cross-linking process is implemented on the walls of the capsules, the density of the capsule walls and the resistance to the solution alkalinity / acidity are improved, and the application stability of the essence microcapsules is increased; moreover, with small size, the capsules can easily permeate into textile fiber, and the water-washing resistance of the textile fiber is greatly improved.

The triple composite microsphere preparation consists of mainly model medicine, calcium alginate, chitosan, and diglycolide-lactide copolymer. The preparation process includes W / O emulsification, washing with isopropanol to prepare small calcium alginate microcapsule, coating with chitosan to form compact double-layered alginic acid-chitonsan microcapsule, the subsequent emulsifying and solvent volatilization step to coat the double-layered alginic acid-chitonsan microcapsule into diglycolide-lactide copolymer to form the three-layered composite microsphere. The present invention can protect protein and polypeptide medicine in hydrophilic sodium alginate-chitonsan microcapsule environment to reduce abrupt release and incomplete release, prolong the medicine release time, and regulate the medicine releasing mode via altering PLGA composition.

The invention belongs to the field of pharmaceutical agents, relates to a polymer micelle lyophilized agent encapsulating an insoluble antitumor drug as well as a preparation method and an application thereof. The polymer micelle lyophilized agent is prepared by carrying out molecular self-assembly on a methoxy poly(ethylene glycol) 2000-polyester block copolymer to form micelles, and then encapsulating the insoluble antitumor drug in a hydrophobic core formed by the polyester. The lyophilized agent has high encapsulation rate, high drug loading and small particle size, can significantly improve the water solubility of the insoluble drug and result in passive targeting of more antitumor drugs to concentrate in the tumor tissues, thus improving an anti-tumor treatment effect and reducing the toxic and side effects of drugs, and can be used to prepare the drugs used for the treatment of lung cancer, intestinal cancer, mammary cancer, ovarian cancer, etc. The lyophilized agent can also be quickly dissolved and dispersed to form a transparent micellar solution after water for injection, normal saline solution and the like are added, and is used for the preparation of the drugs for treating primary intestinal cell carcinoma.

The invention discloses nanometer medicament microspheres. The microspheres comprise a medicament, nanoparticles, a polymer and medicinal auxiliary materials. The invention further provides a preparation method of the nanometer medicament microspheres. The method comprises the following steps of: preparing a medicament and medicinal auxiliary materials into a nanometer medicament; adding the nanometer medicament into a polymer-containing organic solvent mixed solution for emulsifying; adding a nanometer medicament-in-oil mixed suspension into a water mixed suspension containing nanoparticles or containing nanoparticles and a surfactant for emulsifying to obtain an oil-in-nanoparticle mixed suspension-nanometer medicament-in-oil compound emulsion; and curing the obtained compound emulsion, and centrifugally collecting microspheres, wherein the obtained microspheres comprise the medicament, nanoparticles, the polymer and the medicinal auxiliary materials. An appropriate polymer material and an appropriate microsphere preparation method are selected, the prepared microspheres have high envelop rate, and a layer of self-assembled nanoparticles on the surfaces of the microspheres has the effects of improving cell adhesion and reducing inflammation and microencapsulation caused by local excessive acid and hydrophobic materials. The method disclosed by the invention can be applied to preparation of other medicament slow release or controlled release microspheres.

The invention provides microparticles for sustained release formulation for physostigmine, pyridostigmine and other therapeutically active carbamates. The microparticles comprise the active compound and a biodegradable polymer such as polyester, poly(phosphate), poly(anhydride), poly(ortho ester), or mixture thereof. In one embodiment, the polymer is poly(d,l-lactide-co-glycolide). The desired release pattern of the active compound may be readily attained by varying the type and amount of the polymer used, including by using a mixture of two polymers, one of which is more hydrophobic. The invention also provides a method of preparing the microparticles and in one embodiment, the microparticles may be prepared by spray drying.

The invention discloses a method for preparing graphene oxide modified composite phase-change microcapsules. The method specifically comprises the following steps: preparing a graphene oxide solid from graphite powder, concentrated sulfuric acid, sodium nitrate, potassium permanganate and deionized water; mixing the obtained graphene oxide solid with absolute ethyl alcohol and a silane coupling agent, and performing a reaction so as to obtain a double-bond modified functional graphene oxide solid; uniformly mixing the obtained functional graphene oxide solid with a phase-change material, a reaction monomer, a cross-linking agent, a reactive emulsifier and deionized water, and performing ultrasonic dispersion so as to form an oil-in-water type pre-emulsion; and putting the obtained oil-in-water type pre-emulsion into a hot water bath, continuously stirring, further adding an initiator solution, and performing a heat-preservation reaction, thereby obtaining the graphene oxide modified composite phase-change microcapsules. By adopting the method disclosed by the invention, composite phase-change microcapsules which are high in encapsulation efficiency, stable in property, good in heat conductivity, appropriate in phase-change temperature and relatively high in phase-change latent heat enthalpy can be prepared.

The invention discloses slow-release microspheres coated with rivastigmine tartrate / rivastigmine for PLGA / PLA injection and a preparation method thereof. The slow-release microspheres mainly comprise rivastigmine tartrate / rivastigmine and PLGA and PLA serving as biodegradable polymer medicinal materials, and can be prepared by adopting a W1 / O / W2 composite emulsified solvent volatilization method, an O / W emulsified solvent volatilization method, an O1 / O2 emulsion drying method and a spray drying method. The grain diameter of the microspheres is less than 100 microns. The slow-release microspheres have high medicament loading amount, have no obvious burst release effect, can be continuously released for one week, one mouth or three mouths, are used for treating senile diseases such as Alzheimer's disease, Parkinson disease and the like, and can prolong the acting time of the medicament, reduce the application times and greatly improve the administration compliance of patients.

The invention relates to the field of medicine preparation, in particular to a melittin lipidosome preparation. The lipidosome preparation is composed of one part of melittin, 5-40 parts of phospholipid, 1.3-10 parts of cholesterin and 10-140 parts of poloxamer. The invention also discloses the preparing method of the melittin lipidosome preparation. The melittin lipidosome preparation not only can delay the medicine release in the lipidosome, prong the circulating time in the blood and improve the bioavailability of the medicine, but also can obviously reduce the side effect of the medicine and improve the adaptability of a patient.

The invention relates to a folate-targeted reduction sensitive drug-carrying polymer nano-micelle as well as a preparation method and application thereof. The delivery carrier is prepared by taking anamphiphilic triblock copolymer PCL-ss-PEG-ss-PCL as a material, and a chemotherapeutic drug adriamycin amycin and a photosensitizer indocyanine green are entrapped in a hydrophobic core of the micelle. Besides, phospholipid DSPE-PEG-NH2 with an active group is introduced into the preparation process, the DSPE end of the phospholipid has strong hydrophobic property and is inserted into the hydrophobic PCL core of the polymer micelle, the flexible hydrophilic PEG long chain exists on the outer surface of the micelle, FA with a targeting effect is connected to a PEG active distal end of the surface of the polymer micelle, and functions of active tumor targeting and reduction response drug release are integrated. The folate-targeted reduction sensitive drug-carrying polymer nano-micelle disclosed by the invention has the advantages of being small in particle size, high in dispersion property, high in drug loading capacity and encapsulation efficiency and excellent in photothermal conversion effect, can realize reduced trigger drug release, fluorescence imaging of tumor sites, tumor targeting drug delivery and chemotherapy-photothermal combination therapy and improve the tumor inhibition effect, and has wide application prospects in the targeted combination therapy aspect of tumors.

The invention relates to a pH / reduction dual-sensitive multifunctional nano-micelle for tumor chemotherapy and photothermal combined therapy and application of the pH / reduction dual-sensitive multifunctional nano-micelle. The pH / reduction dual-sensitive multifunctional nano-micelle is characterized in that a PCL-acetal-PEG polymer with pH sensitive characteristic, a PCL-ss-PEG-ss-PCL polymer withreduction sensitive characteristic and a phospholipid DSPE-PEG-NH2 with an active group are used as raw materials and are blended to prepare a pH / reduction intelligent responsive polymer nano-micelleas a carrier; a chemotherapeutic drug and a photosensitizer coat a hydrophobic core of the micelle; a casing is made of hydrophilic PEG and has the characteristic of long circulation and space stability; a folic acid targeting group is modified on the surface of the micelle by a covalent bond; the drug loading capacity is 4 to 10 percent, and the mass ratio of the chemotherapeutic drug to the photosensitizer is 0.5 to 2; the particle size is smaller than 200 nm. The pH / reduction dual-sensitive multifunctional nano-micelle disclosed by the invention has the advantages of good dispersity, smallparticle size, better photothermal conversion effect and high drug loading capacity and encapsulation efficiency; the effect of improving tumor suppression by tumor targeted administration, fluorescence imaging of a tumor site, pH / reduction triggered drug release and chemotherapy and photothermal combined therapy can be realized; the pH / reduction dual-sensitive multifunctional nano-micelle has a broad clinical application prospect in combined targeting therapy of tumors.

The invention relates to a multi-vesicular liposome, a blank multi-vesicular liposome and a preparation method and application thereof. The multi-vesicular liposome contains the following components in part by weight: 1 part of liposome, 0.01 to 20 parts of auxiliary emulsifier, 1 to 50 parts of osmotic pressure regulator and medicinal active ingredients; the medicament-to-lipid ratio of the multi-vesicular liposome is 1:(0.1-1):200; the lipid contains of a specific amount of neutral phospholipid, cholesterol and triglyceride; and the auxiliary emulsifier is selected from dextran, polyvinyl pyrrolidone, hydroxyethyl starch, gelatin, albumin, arginine and hydroxymethyl starch. The blank multi-vesicular liposome contains the following components in part by weight: 1 part of lipid, 0.01 to 20 parts of auxiliary emulsifier, 1 to 50 parts of osmotic pressure regulator and 0.1 to 50 parts of ion gradient regulator; the osmotic pressure of the in vivo water phase of the multi-vesicular liposome is equal to the osmotic pressure of human plasma; and the auxiliary emulsifier is as previously mentioned. The multi-vesicular liposome has high entrapment rate, and can achieve good sustained-release effect on in vivo and in vitro experiments.

A chitosen-quaternary ammonium salt nanoparticle as the carrier of protein-type medicine is prepared through dissolving chitosan-quaternary ammonium salt in distilled water, stirring while adding solution of sodium tripolyphosphate, cross-linking, centrifugal separation, and freeze drying. It has long relesing period (6 days).

Polymeric nanoparticles encapsulating inhibitory ribonucleic acids (RNAs) and methods of their manufacture and use are provided. Advantageous properties of the nanoparticles include: 1) high encapsulation efficiency of inhibitory RNAs into the nanoparticles, 2) small size of the nanoparticles that increases cell internalization, and 3) sustained release of encapsulated inhibitory RNAs by the nanoparticles that allows for administration of an effective amount of inhibitory RNAs to cells or tissues over extended periods of time. Encapsulation efficiency of inhibitory RNAs into the nanoparticles is greatly increased by complexing the inhibitory RNAs to polycations prior to encapsulation. Methods of using the polymeric nanoparticles for treating or inhibiting diseases or disorders are provided.

The invention belongs to the field of medicine preparation and particularly relates to a docetaxel solid lipid nanoparticle and a preparation method thereof. The docetaxel solid lipid nanoparticle consists of an effective curative dose of docetaxel, solid lipid materials, liquid lipid materials, an emulsifying agent, additives, long-circulating auxiliary materials and water for injection. The docetaxel solid lipid nanoparticle provided by the invention has the characteristics of stable docetaxel structure, phagocytosis prevention of an in-vivo reticuloendothelial system and active tumor targeting, and can be stably stored.

The invention discloses a quercetin nano-micelle preparation which is made from the following components in parts by weight: 20-40 parts of quercetin as a bulk drug and 220-330 parts of a pluronic surfactant as a drug carrier. A preparation method comprises the following steps: mixing the quercetin with the pluronic surfactant and dissolving in an organic solvent until being fully dissolved, and carrying out rotary evaporation at 15-60 DEG C for removing the organic solvent to obtain a drug-containing film; and drying the film in vacuum, adding a water phase for hydrating at 15-60 DEG C to obtain micelle solution, and filtering with a millipore filter to obtain the quercetin nano-micelle preparation. The obtained nano-micelle preparation has small nano-grade particle size of 20-60nm, a hydrophobic core and a hydrophilic shell, thus ensuring that the preparation has small possibility of being swallowed by a reticuloendothelial system in body, achieving effects such as targeting, long circulating and the like, and being beneficial to clinical application.

The invention discloses a method for preparing a lignin urea-formaldehyde pesticide microcapsule. According to the invention, the method comprises the following steps: taking modified lignin, formaldehyde and urea as a monomer, forming a water-soluble performed polymer under base catalysis, diluting and forming continuous phase, forming dispersed phase by pesticide, an organic solvent and a surfactant, mixing and stirring the continuous phase and the dispersed phase to form an oil-in-water emulsion, performing in situ condensation polymerization under the acidic condition, heating and solidifying, pumping filtration and washing, drying to obtain the solid microcapsule particles. The modified lignin is obtained by formaldehyde hydroxymethyl modification of the industrial grade wheat straw soda lignin. According to the invention, the waste wheat straw soda lignin in paper industry is taken as the main wall material, so that the production cost of the microcapsule can be effectively reduced and the resource utilization of waste biomass can be realized. The preparation method of the invention has the advantages of simple process, rapidity and controllable microcapsule particle size, and is capable of realizing the industrial production, increasing the pesticide utilization rate, prolonging the persistent period, minimizing the environmental pollution in the process of agriculturalproduction, reducing the agriculture production cost and the like, and has good market prospect.

A new formulation of dehydrated lipid vesicles employs a vesicle preserver and permits the control of release and delivery of active pharmaceutical ingredients into the respiratory system for treatment in particular of asthma. The typical formulation provides controlled release of the active pharmaceutical ingredient from 0% to 100% from 0 to 72 hours after inhalation, changes the systemic administration to topical administration, allows prolonged therapeutic period for one administration, increased stability, with reduced dose, reduced systemic side effects, reduced toxicity.

The invention discloses vesicles consisting of amphiphilic polymer and application of the vesicles. A main chain of the amphiphilic polymer consists of a hydrophilic chain segment and a biodegradable hydrophobic chain segment, wherein the molecular weight of the hydrophilic chain segment is 4 to 6kDa; the molecular weight of the hydrophobic chain segment is 3 to 5 times that of the hydrophilic chain segment; the hydrophobic chain segment is formed by performing random copolymerization on a monomer A and a monomer B in a molar ratio of (5-20):1; the monomer A is trimethylene carbonate or cyclic carbonate; the monomer B is acrylate-based carbonate or vinyl sulfone-based carbonate; the hydrophobic chain segment is grafted with a short branched chain; the grafting position is a double bond of the monomer B; a monomer forming the short branched chain is 3-mercaptopropionic acid, cysteamine hydrochloride or cysteine; and the grafting rate is 0.3 to 1. The vesicles are directly prepared from the amphiphilic polymer in an aqueous solution and used as a carrier and a release system of a protein medicine, the encapsulating efficiency and bioavailability of the protein medicine can be improved, and the stability of the encapsulated protein is enhanced.

The invention relates to a formula of a liraglutide sustained-release microsphere preparation. The preparation mainly comprises 5 to 60 parts of liraglutide and 50 to 200 parts of biodegradable substrate material, wherein the biodegradable substrate material is polylactic acid (PLA), polylactic acid-glycollic acid (PLGA) block copolymer, glycolide-lactide (PLCG) copolymer, polyglycolic acid (PGA), polycaprolactone (PCL), polylactic acid-glycollic acid-polycaprolactone (PLGA-PCL) copolymer or PLCG-polycaprolactone (PLCG-PCL) or a mixture of any two or more than two of the compounds, preferably the PLGA-PCL copolymer. The sustained-release microspheres have a high encapsulating rate and a good sustained-release effect.

The invention relates to flexible nanoliposomes with charges for cosmetics and a preparation method thereof. The flexible nanoliposomes with the charges for the cosmetics comprise the following components in part by weight: 1-1000 parts of neutral phospholipid, 0.5-500 parts of phospholipid with the charges, 1-1000 parts of cholesterol, 0.5-500 parts of surface active agent, 0.1-20 parts of hyaluronic acid, 0.5-250 parts of cosmetic active ingredients and 100-8000 parts of freeze drying protective agent. The flexible nanoliposomes with the charges for the cosmetics can obviously improve the stabilities of the cosmetic active ingredients, promote the percutaneous absorption and the interaction efficiency of the active ingredients, and also improve the retention and action time of the active ingredients on the skin surface and the skin deep layer; and the flexible nanoliposomes with the charges for the powdery cosmetic active ingredients are also benefit to the use, transportation and storage. The preparation method of the flexible nanoliposomes with the charges can adopt a mechanized method, so the stability of the product technology and quality is good, and the repeatability is high.

The invention relates to a preparation and application of a new macromolecule lipidosome. The structure is a vesicle which has a lipide dual-layer structure containing duoparental chitosan longchain alkyl quaternary ammonium salt as well as phospholipid with micromolecule. The chitosan longchain alkyl quaternary ammonium salt is characterized in that: the weight average molar mass is bigger than 2000; the chitosan longchain alkyl quaternary ammonium salt can be dissolved in chloroform and other organic solvent, which contains carboxyl, amino or quaternary ammonium salt radical and concretely is one of the duoparental chitosan longchain alkyl quaternary ammonium salt disclosed by 200710056993.4 of China Invention Patent. The surface of the macromolecule lipidosome can be connected with various Liver-Targeted preparations. The macromolecule lipidosome can carry water-soluble, oil-dissolving or duoparental materials including medicine, protein, gene, nutrition, vitamin, magnetic granule and quantum dot, etc. The macromolecule lipidosome has the advantages of high wrapping rate, simple and convenient operation, strong applicability and low cost; the macromolecule lipidosome after being covered has even distributed granule diameter which can be lower than 20nm for the smallest, has stable system and strong functions for carrying medical tiny balls and slowly controlling as well as releasing.

Disclosed is a process of preparing sustained release microspheres, containing a biodegradable polymer as a carrier and a drug, using spray drying. The process comprises preparing a solution, suspension or emulsion containing a biodegradable polymer, a drug and a solvent; spray drying the solution, suspension or emulsion; and suspending spray-dried microspheres in an aqueous solution containing polyvinyl alcohol to remove the residual solvent and increase the hydrophilicity of the microsphere surface. The process enables the preparation of microspheres having high drug encapsulation efficiency, almost not having a toxicity problem due to the residual solvent, and having good syringeability. The microspheres prepared according to the present invention release an effective concentration of a drug in a sustained manner for a predetermined period when administered to the body, and are thus useful in the treatment of diseases.

The invention provides a temperature-sensitive amphiphilic cyclodextrin polymer PCEC (polycaprolactone-polyethylene glycol-polycaprolactone, PCL-PEG-PCL). The polymer provided by the invention is the amphiphilic cyclodextrin polymer which is obtained by linking a PCL-PEG-PCL molecule with beta-CD (cyclodextrin) through utilizing the temperature-sensitive characteristic of a PCL-PEG-PCL triblock copolymer and the inclusion effect of beta-CD on a hydrophobic medicament, can effectively load and slowly release a hydrophobic or water-soluble medicament on the basis of the traditional hydrogel encapsulated water-soluble medicament, has proper critical gel temperature and can form in situ temperature-sensitive hydrogel after injection. According to the invention, the hydrophobic zone of the polymer is obviously enlarged, thereby effectively improving the loading capacity of the hydrogel on the hydrophobic medicament and obtaining high medicament encapsulation rate and medicament loading amount; and simultaneously, the controlled-release effect of the medicament after local injection delivery is realized by utilizing the temperature-sensitive gel performance of the polymer. The polymer provided by the invention has the following chemical structure shown in the specification.

The present invention relates to nanoparticles for encapsulating compounds, the preparation and uses thereof, said nanoparticles being based on half (C1-C4) alkyl esters of poly (methyl vinyl ether-co-maleic anhydride) (PVM / MA) copolymers. Said nanoparticles can encapsulate or incorporate a product of interest for use in the agricultural, cosmetic, food or pharmaceutical fields.

The present disclosure relates to processes for preparing microparticles using an emulsion process where both a solvent and a salt are used in the continuous phase of the emulsion. The present disclosure also relates to micropartices having an angle of repose of ≦35, as measured using a Hele-Shaw cell.

The invention discloses an oxaliplatin liposome glucose preparation and the preparation method and application, relating to an oxaliplatin liposome glucose solution preparation used for tumor resistance and the preparation method and application. An oxaliplatin liposome glucose preparation is formed by liposome which prepared by oxaliplatin, hydrogenated phosphorus, cholesterol and DSPE-PEG2000, and is dissolved in glucose solution; wherein the weight ratio of the hydrogenated phosophorus and the oxaliplatin is 1:1-50; the weight ratio of the hydrogenated phosophorus, cholesterol and the DSPE-PEG2000. The preparation method is that the hydrogenated phosophorus, cholesterol and the DSPE-PEG2000 are weighed according to proportioning by weight in a description and then fixed together; tertiary butyl alcohol is added into the fixture for the fixture to be stirred and dissolved, then the fixture is precooled; the oxaliplatin saturated water solution with 4-10 percent of glucose after cooling and drying is stirred, dissolved and emulsified by an emulsion balancing machine and then prepared into liposome solution by a homogenizer and a nanometer extruder, separated and refined through a filter column to prepare the oxaliplatin liposome glucose solution.

A method for implementing Identity and Locator Split is provided. The method is applied in a MPLS network. ITR and ETR are also LERs in the MPLS network. The method includes: establishing a point to point LSP tunnel between ITR and ETR by running a MPLS signaling protocol; the ITR storing an EID of endpoint and RLOC mapping as well as a RLOC and outer MPLS label mapping, and forwarding the endpoint's data packets in the MPLS network based on the outer MPLS label corresponding to the RLOC. A data encapsulation method for Identity and Locator Split and a LER device in the Identity and Locator Split network are also provided in the present invention. The present invention greatly improves the encapsulation and transmission efficiency of LISP data packets in the MPLS network.