143 results about "Mixed micelle" patented technology

Pharmaceutical compositions comprising a macromolecular pharmaceutical agent in micellar form are disclosed. The micelles are formed from an alkali metal alkyl sulfate, and at least one additional micelle-forming compound as described in the specification. An alkali metal salicylate and a pharmaceutically acceptable edetate are also included in the composition. Micelle size ranges between about 1 and 10 nanometers. Methods for making and using the compositions are also disclosed.

Personal care and hygiene formulations for topical application to mucosal surfaces. These formulations include an amphiphilic lipid carrier in the form of a colloidal composition which can include a micellar aggregate or mixed micelles dispersed in a continuous aqueous phase, or an emulsion of lipid droplets suspended in a continuous aqueous phase, and an active agent which is an anti-microbial agent. The lipid carrier has high adhesiveness to mucous membranes such as the soft tissues of the oral cavity. The lipid carrier also has a high load capacity for the active agent to be carried to these tissues. These formulations have the desirable properties of carrying a large amount of active agent for controlled and prolonged release thereof at the desired site, such as mucous membrane surfaces and surrounding tissue. Accordingly, the present invention provides a formulation for oral or topical application including an anti-microbial agent and a lipid. The agent is held by the carrier through a hydrophobic interaction and is released from the carrier in a controlled manner over a prolonged period of time. The lipid is also characterized by having a high adhesive capability towards mucous membrane surfaces. The lipid and the agent are preferably present in a ratio in a range of from about 1:10 to 10:1, more preferably from about 1:5 to about 5:1, and most preferably from about 1:3 to about 3:1 in the formulation.

The present invention discloses a novel mixed micelle structure with a functional inner core and hydrophilic outer shells self-assembled from a graft macromolecule and one or more block copolymer, and preferably from a graft copolymer and two or more diblock copolymers. The micelle synthesized in the present invention has a size of about 50-200 nm, which can be used as a cancer diagnosis agent and a cancer drug delivery carrier.

Pharmaceutical compositions comprising a macromolecular pharmaceutical agent in mixed micellar form are disclosed. The mixed micelles are formed from an alkali metal alkyl sulfate, and at least three different micelle-forming compounds as described in the specification. Micelle size ranges between about 1 and 10 nanometers. Methods for making and using the compositions are also disclosed. A preferred method for administering the present composition is through the buccal region of the mouth.

Pharmaceutical compositions comprising a narcotic analgesic in mixed micellar form are disclosed. The mixed micelles are formed from an alkali metal alkyl sulfate, and other micelle-forming compounds as described in the specification. Micelle size ranges between about 1 and 10 nanometers. Methods for making and using the compositions are also disclosed. A preferred method for administering the present composition is through the buccal mucosa of the mouth.

The invention provides block polymers, micelles, and micelle formulations for combination drug therapy. Polyamide block polymers, such as those of formulas I and II are useful, for example, for preparation of mixed drug micelles, including simply mixed micelles, physically mixed micelles, and chemically mixed micelles. The invention further provides methods of treating cancer, and inhibiting and killing cancer cells. Also provided are methods for the preparation of polymer drug conjugates and intermediates for their synthesis.

The invention discloses a preparation method of a polyene-containing taxol nanoparticle mixed micelle preparation and a freeze-drying agent, which prepares docetaxel PLA-PEG nanoparticles or micelle or nanoparticle mixed micelle through a modified solvent evaporation method, takes PLA-PEG copolymer as a carrier, and wraps docetaxel in a PLA hydrophobic core. When in use, the docetaxel PLA-PEG containing long cycle freeze-dried preparation only needs to be added with water and is dissolved, and uniform nanoparticle suspension, micellar solution or mixed micellar nanoparticle suspension can be prepared. The preparation method does not need tween-80 and ethanol solubilization, only takes the biodegradable PLA-PEG as the carrier, and does not contain any surfactant; and compared with the docetaxel injection on sale, the preparation can reduce the toxicity and the adverse reactions of the medicine, and improve the clinical application safety of the medicine.

The invention concerns mixed micelles or micro-aggregates for inducing an immune response containing at least a first lipopeptide comprising a CTL epitope and at least a first lipid motif; and a second lipopeptide comprising at least an auxiliary T epitope and at least a lipid motif, whereof the type can be different from the first lipopeptide motif. Said micelles can be used as medicines and vaccines.

The invention discloses a paclitaxel mixed micelle preparation, comprising 100 to 300 milligram of tocopherol polyethylene glycol succinate 1000 (TPGS), 0 to 50 milligram of phosphatide, 0.5 milliliter of anhydrous ethanol and 6 milligram of paclitaxel. The preparation method is as follows: the TPGS is dissolved in the anhydrous ethanol, or the TPGS and the phosphatide are dissolved in the anhydrous ethanol; the paclitaxel is added and dissolved under stirring; the mixture is filtered with a millipore filtration of 0.22 micrometer so as to obtain the paclitaxel mixed micelle preparation. In the invention, the TPGS and the phosphatide are used to form mixed micelles which have good stability and little toxic and side effects; the preparation method is simple and practicable, having a good application prospect. Compared to the prior art, polyoxyethylene castor oil in conventional prescription is substituted in the invention, thereby reducing toxic side effects of paclitaxel injections and greatly enhancing the safety of the injections on condition that solubility is guaranteed.

The invention relates to a new mixed micelle core-shell SiO2/Fe3O4 nanometer solid phase extracting agent in the chemical analysis test instrument device field, which has the big specific surface area of the nanometer material, the strong magnetic separating property of the magnetic material, the good satiability of SiO2 shell layer and the good extraction property of the semi micelle and the absorption micelle, and is fit for the large scale batch preconditioning of bulk water sample, and has the small usage extracting agent, high efficient extraction, the simple operation, the high extracting speed, the friendly environment, the wide using range, the low cost and the reactivation property. Selecting bisphenol A(BPA), nonyl phenol(4-OP), octyl phenol (4-NP) as the represent of the hydrophobic pollution material and selecting perfluorine enanthic acid (PFHeA), perfluorooctanoic acid (PFOA), perfluorine octane sulfonic acid (PFOS), perfluorine n-nonanoic acid (PFDeA) or the like perfluorine compound as the represent of amphipathic nature pollution material, there are 0. 1g extracting agent and 50mg surface activator in 800ml environmental water simple, and the extracting ratio of the organic pollution materials is more than 90%.

The invention discloses preparation and application of an insoluble drug-entrapped poloxamer/amphiphilic polysaccharide mixed micelle. The insoluble drug-entrapped poloxamer/amphiphilic polysaccharide mixed micelle is prepared through a dialysis method or a solvent evaporation method. The mixed micelle is low in critical micelle concentration, is high in drug-loading rate, is capable of obviously prolonging the stabilization time and has the long-circulation function of a nanomicelle and has dual functions of restraining the metabolism of P-glycoprotein and cytochrome P450 enzyme and is capable of increasing the bioavailability of oral administration. The mixed micelle is simple in preparation method, is mature in process and is high in yield and can be prepared into preparations for the oral administration, such as tablets, capsules, pills and syrups.

A pharmaceutical formulation for absorption through oral mucosae comprising an effective amount of (a) a pharmaceutical agent in mixed micellar form, (b) at least one micelle-forming compound selected from the group comprising an alkali metal alkyl sulfate and a polyoxyethylene sorbitan monooleate, (c) a block copolymer of polyoxyethylene and polyoxypropylene, (d) at least one additional micelle-forming compound, and (e) a suitable solvent. The invention also provides a metered dose dispenser (aerosol or non-aerosol) containing the present formulation and a method of administering insulin using the metered dose dispenser comprising administering split doses of a formulation containing insulin before and after each meal.

The invention discloses blank mixed micelle, and a preparation method and applications thereof. The blank mixed micelle comprises an amphiphilic copolymer and ginsenoside represented by formula I, ishigh in efficiency, is safe, is stable, is high in targeting performance, is excellent in homogeneity, is stable in quality, is convention in preparation technology, can be used for coating one or a plurality of active substances in drugs or cosmetics and health care substances, and is capable of forming mixed micelle containing loaded active substances. Compared with conventional nanometer micelle, the blank mixed micelle possesses following advantages: the mixed micelle loaded with active substances is excellent in drug forming performance, multiple drug resistance, stability, homogeneity, and safety performance, and is small in particle size; and the curative effect of loaded active drugs on drug resistant cells is better.

The invention discloses a docetaxel-loading mixed micelle preparation and a preparation method thereof. The mixed micelle preparation is prepared by the following steps of: preparing docetaxel mixed micelle by using a thin-film dehydration method; and coating the docetaxel with hydrophobic nuclei by taking amphiphilic TPGS, MPEG-PLA and CSO-SA as carrier materials of the mixed micelle. The docetaxel-loading mixed micelle preparation is prepared by using the amphiohilic materials of TPGS, MPEG-PLA and CSO-SA, so that drug-loading rate is increased, solubility and oral bioavailability are improved, and the problems of poor water solubility, low medicine release speed, improper particle size and the like when hydrophilic medicines are prepared are solved.

The present invention provides compositions containing endoxifen, formulations and liposomes of endoxifen, methods of preparation of such agents and formulations, and use of such agents and formulations for the treatment of breast cancer and other breast diseases and diseases susceptible to endoxifen. In particular, the compositions of the present invention include liposomes, complexes, vesicles, emulsions, micelles and mixed micelles of endoxifen in which the compositions further contain any of a variety of neutral or charged lipids and desirably, cholesterol and cholesterol derivatives, sterols, Z- and E-guggulsterones, phospholipids, fatty acids, vitamin D, and vitamin E. The present invention also provides methods of preparing endoxifen. The present invention provides methods for treating and preventing breast cancer and other breast related diseases by administrating novel formulations or compositions comprising a therapeutically effective amount of endoxifen.

Mixed micelles containing poly(L-histidine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer are a pH-sensitive drug carrier that release the drug in an acidic microenvironment, but not in the blood. Since the microenvironment of solid tumors is acidic, these mixed micelles are useful for treating cancer, including those cancers exhibiting multidrug resistance. Targeting ligands, such as folate, can also be attached to the mixed micelles for enhancing drug delivery into cells. Methods of treating a warm-blooded animal with such a drug are disclosed.

Mixed micelles containing poly(L-histidine-co-phenylalanine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer are a pH-sensitive drug carrier that release the drug in an acidic microenvironment, but not in the blood. Since the microenvironment of solid tumors is acidic, these mixed micelles are useful for treating cancer, including those cancers exhibiting multidrug resistance. Targeting ligands, such as folate, can also be attached to the mixed micelles for enhancing drug delivery into cells. Methods of treating a warm-blooded animal with such a drug are disclosed.

The invention relates to a pH responsive polymer mixed micelle and application thereof and belongs to the technical field of medicinal functional carrier materials. the mixed micelle is prepared by mixing two polymers (MPEG-b-PDEAEMA and MPEG-b-PCL) with a hydrophobic anti-tumor drug according to a certain ratio, wherein the MPEG-b-PDEAEMA is prepared by the following steps: bromizing a hydrophilic block mono methyl polyethylene glycol MPEG; and then introducing methacrylic acid (N, N)-diethylamino ethyl ester (serving as a pH responsive block) into a polymer; and the MPEG has pH responsiveness; the other polymer MPEG-b-PCL is prepared by carrying out ring opening polymerization on a hydrophilic block (epsilon)-caprolactone under the direct initiating effect of the hydrophilic block mono methyl polyethylene glycol MPEG, and MPEG-b-PCL is amphiphilic. The mixed polymer micelle is amphiphilic and has pH responsiveness, the drug loading amount of hydrophilic anti-tumor drug can reach up to 26.79%, and the micelle has a good pH control release effect, so that the drug stably exists for a long time in a neutral pH condition and the drug is released at a space velocity in an acidic pH condition. In addition, the synthetic routes and preparation methods of the two polymers are quite short.

The invention discloses a vitamin K1 micelle injection and a preparation method thereof, and belongs to the field of micelle injection and preparation thereof. The invention discloses a vitamin K1 micelle for the first time. The vitamin K1 micelle is prepared from vitamin K1, cholate, phospholipid, a pH regulator and water for injection. The preparation method of the vitamin K1 micelle injection comprises the steps that an organic solvent freezing and drying method is adopted, a mixed micelle composed of phospholipid and cholate is adopted as a carrier, and the vitamin K1 is entrapped in hydrophobic nuclei of the mixed micelle. Due to the fact that the vitamin K1 is not dissolved into water, the solubility of the vitamin K1 in water is remarkably improved through the cholate/phospholipid mixed micelle preparation technology, polysorbate-80 and propylene glycol are not added into the vitamin K1 micelle injection, only phospholipid and cholate named as physiological excipient are adopted as auxiliary materials, and compared with vitamin K1 injections on sale currently, the preparation can reduce adverse drug effect and improve the clinic application safety.

This disclosure is directed to mixed micelle compositions for administration of e.g., therapeutic agents or imaging agents to a subject.

Nanoparticles containing retinoic acid have reduced irritancy of retinoic acid and are suitable for subcutaneous or intravenous administration, as well as for use in sustained-release preparation. The high skin permeability of the nanoparticles makes them suitable for use in pharmaceutical or non-pharmaceutical external preparations or cosmetics intended for skin application. The present invention provides a method for adjusting the particle size of such nanoparticles and nanoparticles produced by such a method. Specifically, the method involves dispersing retinoic acid dissolved in a lower alcohol in an aqueous alkali solution; adding a nonionic surfactant to the dispersion to form a mixed micelle; adding to the micelle a halide or acetate of divalent metal along with a carbonate or phosphate of alkali metal so that the molar ratio of the former to the latter is 1:0 to 1:1.0, thereby depositing a coating of inorganic salt of polyvalent metal on the surface of the micelle; and adjusting the average particle size of the resulting nanoparticles to 5 to 300 nm. The inorganic salt of polyvalent metal may be calcium carbonate, zinc carbonate, or calcium phosphate.