Abstract: The present invention belongs to the field of pharmaceutical manufacturing technology. The present invention provides a pharmaceutical composition of a conjugate and a preparation method thereof. The pharmaceutical composition is preferably administered by injection. The docetaxel conjugate has a structural formula as shown in the following formula: (I).

Abstract: The use of oral colchicine solutions in combination with other therapeutics, while minimizing toxic drug to drug interactions are described herein. Related compositions are also provided.

Abstract: In a reference electrode for the potentiometric measurement of ion concentrations, comprising a swellable polymer body filled with at least one electrolyte salt and a potential sensing element of the second type located in the polymer body, preferably of the Ag/AgCl type, the polymer body is composed of preferably organic, hydrophobic prepolymer segments, which are three-dimensionally crosslinked by preferably organic, hydrophilic polymer chains.

Abstract: Formulations and uses of the formulations for treating a malignant mass in a mammal by administering an injectable formulation comprising a therapeutically effective amount of a chemotherapeutic agent dissolved or suspended in a biocompatible carrier directly into the malignant mass are disclosed. In certain preferred embodiments, the injectable formulation is a taxane (e.g. paclitaxel), a podophyllotoxin derivative (e.g., etoposide), or a camptothecin derivative (e.g., hydroxycamptothecin).

Abstract: The invention relates primarily to a method of modulation, preferably of in vitro and/or in vivo modulation, of the cold menthol receptor TRPM8, wherein the receptor is contacted with at least one modulator selected from the group consisting of the compounds of the structure type 1 described herein. The present invention further relates to corresponding uses and compositions comprising such compounds.

Abstract: This document relates to a composition comprising Cabazitaxel, or a pharmaceutically acceptable salt thereof, human serum albumin, and arginine, or a pharmaceutically acceptable salt thereof, wherein the human serum albumin and the Cabazitaxel, or a pharmaceutically acceptable salt thereof, in the composition have a ratio by weight of no less than 120:1. This document also relates to methods to prepare a composition comprising Cabazitaxel, or a pharmaceutically acceptable salt thereof, human serum albumin, and arginine, or a pharmaceutically acceptable salt thereof, as described herein.

Abstract: A nanoparticle comprising a keratin polypeptide and at least one lipophilic active ingredient, wherein the at least one lipophilic active ingredient is non-covalently bound to the keratin polypeptide and can be e.g. a therapeutic or diagnostic agent, a nutraceutical, a cosmetic ingredients, a dye or a cosmeceutical, the keratin polypeptide being water-soluble; optionally, the nanoparticle further comprises at least one hydrophilic active ingredient non-covalently bound to the keratin polypeptide, which can be e.g. a therapeutic or diagnostic agent, a nutraceutical, a cosmetic ingredients, a dye or a cosmeceutical.

Abstract: A system and method for applying a low strength, low frequency magnetic field therapy to biological tissues. A coil is excited with a low frequency oscillating current, e.g., 10-1000 Hz. The coil is, e.g., 5-200 turns, having a diameter of 2-20 mm, and produces a magnetic field strength of about 0.01-5 mTelsa at a distance of 1 cm from the coil, or a cover over the coil, into the tissue. The current is preferably controlled by a smartphone or other programmable device controlled by a downloadable app in accordance with a PEMF program which may be separately downloaded or updated, and may be provided through an audio jack. Alternately, a digital interface and/or wireless interface may control the current. An app on the smartphone may be used to control the frequency, amplitude/envelope modulation, waveform, duration, etc. of the oscillation. The coil may be in mineral housing with a simple filter, and TRRS-type audio jack.

Abstract: Compounds having the following structure (I) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined herein, and wherein at least one of R1, R2 and R3 is not H, are provided. Pharmaceutical compositions comprising the compounds and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.

Abstract: The present embodiments provide compositions, methods, and kits for the treatment or prevention of ocular conditions or maladies via non-invasive liquid depots. In at least one embodiment, the liquid depot is capable of sustained-release delivery of at least one pharmaceutical agent to the eye for days or weeks.

Abstract: A method of performing an intravenous drip injection includes a first step, a second step, a third step and a fourth step. A first step includes starting dosing an infusion solution containing a predetermined component by the intravenous drip injection to a dosing recipient. A second step includes extracting a body fluid from the dosing recipient being dosed with the infusion solution. A third step includes measuring a concentration of the predetermined component in the extracted body fluid. A fourth step includes varying the concentration of the predetermined component in the infusion solution, corresponding to the concentration of the predetermined component in the body fluid.

Abstract: A freshening composition is provided. The composition includes at least one particle, and an aqueous carrier. The composition includes a polysaccharide system having a first polysaccharide and a second polysaccharide. The first polysaccharide is xanthan gum and the second polysaccharide is selected from the group consisting of konjac gum, locust bean gum, tara gum, and combinations thereof. The composition may include an unencapsulated perfume.

Abstract: The present invention provides a pharmaceutical composition for oral administration, comprising (a) 4 to 40% by weight of a taxane, (b) 10 to 30% by weight of a medium chain triglyceride, (c) 30 to 70% by weight of monooleoyl glycerol, (d) 5 to 30% by weight of a surfactant, and (e) 10 to 30% by weight of polyoxyl glyceryl fatty acid ester and a process for preparing the same.

Abstract: The present invention relates to the composition of a nanoparticle based on a magnesium salt, and methods of drug delivery using the nanoparticle. A preferred embodiment uses magnesium phosphate, with or without a shell to deliver aiRNA and/or siRNA. The nanoparticles of the present invention are also effective when administered orally.

Abstract: The present technology relates generally to oligolactic acid conjugates of paclitaxel, rapamycin, selumetinib, and other anticancer agents, micelle compositions containing such conjugates and methods of preparing and using such compositions to treat various cancers. Specifically, there are provided oligolactic acid conjugates wherein the oligolactic acid comprises 2 to 24 lactic acid subunits and is attached through an ester linkage to the oxygen of the 7-hydroxyl of the paclitaxel or paclitaxel derivative, the 40-hydroxyl of the rapamycin or rapamycin derivative, and the 2?-hydroxyl of the selumetinib or selumetinib derivative. Compositions comprising water and a micelle comprising a polylactic acid-containing polymer and the oligolactic acid conjugate may be readily prepared. Methods of inhibiting or killing cancer cells and treating paclitaxel, rapamycin, and/or selumetinib cancers are also provided.

Abstract: Provided is a nasal implant assembly comprising a hollow implant having a distal end and a proximal end, the distal end configured to have a segment deposited with magnetic particles; and a medical syringe configured to be attachable to the proximal end of the hollow implant and also configured to be capable of retaining and transporting a magnetically active fluid composition through the implant to a nasal cavity of a subject. Also provided is a method of treating chronic rhinosinusitis in a subject, the method comprising the steps of positioning a nasal implant having magnetic particles into a nasal cavity; loading a medical syringe with a magnetically active fluid composition; and transporting the loaded magnetically active fluid composition to the nasal cavity to treat chronic rhinosinusitis.

Abstract: A freshening composition is provided. The composition includes at least one particle, and an aqueous carrier. The composition includes a polysaccharide system having a first polysaccharide and a second polysaccharide. The first polysaccharide is xanthan gum and the second polysaccharide is selected from the group consisting of konjac gum, locust bean gum, and combinations thereof. The composition may include an unencapsulated perfume.

Abstract: There is disclosed a platinum ion chelating dipyridoxyl compound according to Formula (I), or a pharmaceutically acceptable salt thereof, wherein the dipyridoxyl compound is uncoordinated or coordinated with a metal ion which is not a transition metal, for prevention or treatment of chemotherapy drug induced peripheral sensory neuropathy in a patient, wherein the chemotherapy drug comprises platinum ions. An example of such a chemotherapy drug is oxaliplatin. The drawbacks of previous metal complexed compounds containing manganese ions are eliminated. A more frequent use of the drug is possible since the problem in the prior art with accumulated manganese neurotoxicity is eliminated. The compounds can be administered both temporally and spatially separately from chemotherapy.

Abstract: Non-aqueous taxane pro-emulsion formulations are provided. Pro-emulsion formulations of embodiments of the invention include a taxane, an oil component, a surfactant component and, optionally, a non-aqueous solvent component. Also provided are methods of making and using the pro-emulsion formulations, as well as kits that include the pro-emulsion formulations.

Abstract: A pharmaceutical composition comprises a taxane (e.g., paclitaxel, docetaxel, cabazitaxel, larotaxel, ortataxel, and/or tesetaxel) in a mixture of first and second surfactants. The absorption of the taxane is increased from the pharmaceutical composition is greater than the sum of the absorption of docetaxel from either the first or the second surfactant. The increase in absorption is especially enhanced when the ratio of the first surfactant to the second surfactant in the pharmaceutical composition is between 60:40 and 85:15 by weight, and the total surfactant weight does not exceed 98% of the total weight. Polysorbate 80, polysorbate 20, and caprylocaproyl polyoxylglycerides serve as suitable first surfactants, and polysorbate 80 or polyethyoxylated castor oil serve as suitable second surfactants. The stability of the pharmaceutical composition may be enhanced by further including a stabilizer (e.g., citric acid and/or ascorbic acid).

Abstract: Provided herein are methods for analysis of target cells on a population or individual basis, including before and after contact with a stimulus in order to determine the effect of such stimulus on the target cells. Also provided are devices for performing such methods. The analysis methods involve identifying and measuring or tracking morphological changes that occur in target cells over a period of time. Tracking is accomplished using imaging systems capable of imaging target cells individually over a period of time either continuously or at discrete intervals of time.

Abstract: In order to reduce the side effects of paclitaxel derivatives having excellent anti-cancer effects, an attempt was made to produce a liposome encapsulating paclitaxel derivatives such as paclitaxel monoglycosides and docetaxel monoglycosides. However, the introduction efficiency of paclitaxel derivatives, etc., into a liposome was poor, and this technique was not developed to a practical level. The present invention provides a method for producing a liposome encapsulating a paclitaxel monoglycoside and/or a docetaxel monoglycoside, and having an antibody specifically recognizing a cancer cell, the method comprising a step of bringing a liposome encapsulating a polyoxyethylene ester derivative, a lower alcohol, and a buffer or water into contact with a solution in which a paclitaxel monoglycoside and/or a docetaxel monoglycoside is dissolved in an alkylene glycol-containing buffer or water.

Abstract: Provided herein are improved fluorogenic compounds and probes that can be used as reagents for measuring, detecting and/or screening hypochlorous acid or hydroxyl radical. The fluorogenic compounds of the invention can produce fluorescence colors, such as green, yellow, red, or far-red. Also provided herein are fluorogenic compounds for selectively staining hypochlorous acid or hydroxyl radical in the mitochondria of living cells. Provided also herein are methods that can be used to measure, directly or indirectly, the presence and/or amount of hypochlorous acid or hydroxyl radical in chemical samples and biological samples such as cells and tissues in living organisms. Also provided are high-throughput screening methods for detecting or screening hypochlorous acid or hydroxyl radical or compounds that can increase or decrease the level of hypochlorous acid or hydroxyl radical in chemical and biological samples.

Abstract: The present disclosure provides a composition comprising Compound 1, or a pharmaceutically acceptable salt thereof, cyclodextrin, and, optionally, pH adjusting agents.

Abstract: Therapeutic methods including administration of cyclosporin to an eye of a mammal in combination with administration of a therapeutically active agent effective for treatment of a cancer to said mammal to treat an ocular condition associated with the use of said therapeutically active agent are disclosed herein.

Abstract: According to the invention there is provided inter alia a medical device for delivering a paclitaxel to a tissue, the device the device having a coating layer applied to a surface of the device, the coating layer comprising components i), ii) and iii), wherein component i) is a therapeutic agent which is paclitaxel; and component ii) is urea or a pharmaceutically acceptable salt thereof, or a urea derivative or a pharmaceutically acceptable salt thereof; and component iii) is succinic acid, glutaric acid or caffeine, or a pharmaceutically acceptable salt of any one thereof.

Abstract: The present invention provides methods of treating cancer by administering an IL8-CXCR1 pathway inhibitor (e.g., an anti-CXCR1 antibody or Repertaxin) alone or in combination with an additional chemotherapeutic agent such that non-tumorigenic and tumorigenic cancer cells in a subject are killed. The present invention also provides compositions and methods for detecting the presence of and isolating solid tumor stem cells in a patient (e.g., based on the presence of CXCR1 or FBXO21).

Abstract: The invention includes taxoid compounds represented by the formula: wherein: R1 represents a methyl group or a fluorine; R2 represents an alkyl or alkenyl group having one to six carbon atoms; or a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; R3 represents an alkyl, alkenyl, dialkylamino, alkylamino, or alkoxy group having one to six carbon atoms; a cycloalkyl or cycloalkenyl group having three to seven ring carbon atoms; an aryl group having six to eighteen ring carbon atoms; or a heteroaryl group having three to seventeen ring carbon atoms; R4 represents hydrogen or a methyl group; and X represents hydrogen or fluorine.

Abstract: The present invention relates to pharmaceutical compositions for treating cancer comprising BRAF inhibitors, (e.g. vemurafenib) and/or MEK inhibitor, (e.g. trametinib, RO5068760), in combination with anti-tubulin compounds of the invention or other known tubulin inhibitors, and using such compositions for treating cancer such as melanoma, drug-resistant cancer, and cancer metastasis.

Abstract: Disclosed in the present invention is micellar polypeptide vaccine having pegylated phospholipid as carrier. The vaccine can prevent or treat tumors or can be used as combination formulation with anti-cancer activity formulation. The micellar polypeptide vaccine is formed of self-assembling pegylated phospholipid (PEG-PE) and antigenic polypeptides, the pegylated phospholipid being compound formed of polyethylene glycol (hydrophilic blocks) covalently bonded to nitrogenous bases on phospholipid molecule (hydrophobic blocks). The particle diameter of the micellar vaccine is 10-100 nm, and the antigenic polypeptides carried therein are polypeptides of 5-100 amino acids. The micellar polypeptide vaccine may also contain immunoadjuvant.

Abstract: The invention provides derivatives of decitabine with superior chemical stability and shelf life, with similar physiological activity. The derivatives are provided in a non-aqueous formulation, which further stabilizes the derivatives. Methods of treating one or more myelodysplastic syndromes, leukemia, or solid tumours using the formulations are described.

Abstract: The present technology relates generally to oligolactic acid conjugates of paclitaxel, rapamycin, selumetinib, and other anticancer agents, micelle compositions containing such conjugates and methods of preparing and using such compositions to treat various cancers. Specifically, there are provided oligolactic acid conjugates wherein the oligolactic acid comprises 2 to 24 lactic acid subunits and is attached through an ester linkage to the oxygen of the 7-hydroxyl of the paclitaxel or paclitaxel derivative, the 40-hydroxyl of the rapamycin or rapamycin derivative, and the 2?-hydroxyl of the selumetinib or selumetinib derivative. Compositions comprising water and a micelle comprising a polylactic acid-containing polymer and the oligolactic acid conjugate may be readily prepared. Methods of inhibiting or killing cancer cells and treating paclitaxel, rapamycin, and/or selumetinib cancers are also provided.

Abstract: The present invention belongs to the field of bio-pharmaceutical material preparation technology, and relates to a preparation method of albumin nanoparticle carrier entrapping taxane-typed drug. This preparation method rapidly forms nanoparticle solution of albumin entrapping taxane-typed drug under room temperature by adding solvent as the medium. Next, by the second time of freeze-drying, stable powder of albumin nanoparticles entrapping taxane-typed drug is obtained. The final freeze-dried powder only includes two components: albumin and taxane-typed drug. The particles are in regular spherical shape, and the diameter of particle is less than 100 nm. The present invention has high drug loading ratio and entrapment efficiency. The experiment of releasing in vitro shows that the present invention has a good slow-release effect. Taxane-typed drug nanoparticles provided by the present invention improves the safety and compliance of this type of reagent.

Abstract: The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule cytotoxins that are chemically modified to include one or more moieties that include hydrophobic portions. In some embodiments, the disclosure provides small-molecule cytotoxins that are chemically modified with fatty acid-containing moieties. In some aspects, the disclosure provides compositions, such as pharmaceutical compositions, that include such modified small-molecule cytotoxins and a protein. In some embodiments, the protein is albumin or an albumin mimetic. Further, the disclosure provides various uses of these compounds and compositions.

Abstract: The present invention relates to a stable liquid formulation of cabazitaxel. The formulation comprises cabazitaxel and at least one solubilizer. Typically, formulations are in the form of ready-to-use solutions or concentrates.

Abstract: Disclosed herein are embodiments of a method of accelerating bone healing in a subject in need thereof, comprising administering to the subject a compound disclosed here. The method may further comprise selecting or identifying a subject that has bone damage, or is a risk of developing bone damage. The compound may be administered after bone damage has occurred, or it may be administered prophylactically. The compound may be administered to a subject that has not and/or will not be exposed to radiation. In other embodiments, the subject has been and/or will be exposed to radiation.

Abstract: An anti-vascular diseases and antitumor pharmaceutical composition is provided in the present invention, and it includes effective ingredients including bleomycin antitumor antibiotic, adrenal glucocorticoid, epinephrine or pharmaceutically acceptable salts thereof in a weight ratio of (1-8):(2-5):(0.00005-0.001). The pharmaceutical composition provided can be used for treatment of vascular diseases and tumors.

Abstract: The present application provides a pharmaceutical formulation comprising a folate receptor (FR)-targeting antineoplastic substance or composition, wherein the pharmaceutical formulation is configured for administration by inhalation, wherein the FR-targeting antineoplastic substance or composition is comprised in a nanoparticle and wherein the nanoparticles are comprised in microparticles, and its use in the treatment of a proliferative disease affecting at least part of the respiratory tract. The present application further provides a pharmaceutical formulation comprising an antineoplastic agent and a FR-targeting excipient, for use in the treatment of a proliferative disease affecting at least part of the respiratory tract.

Abstract: The invention provides compounds of formula I: or a salt thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using the compounds of formula I.

Abstract: In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators with the ClpP endopeptidase; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of search in the particular art and is not intended to be limiting of the present invention.

Abstract: The present invention provides compositions of therapeutic agents and methods of use for reducing and/or treating gastrointestinal inflammation. In particular aspects, the tungstate salts described herein and pharmaceutical compositions thereof inhibit the activity of one or a plurality of anaerobic respiratory enzymes in facultative anaerobic bacteria such as, for example, Enterobacteriaceae, that can exacerbate inflammation. In particular embodiments, the present invention provides compositions of therapeutic agents for treating gastrointestinal inflammation, as well as methods for treating or preventing gut microbial imbalance due to an increase in the abundance of intestinal Enterobacteriaceae.

Abstract: Described here are devices, systems, and kits for delivering substances to tissues. The devices generally include one or more chambers (102) and a reservoir (108) within each chamber. The reservoir may locally deliver a microdose amount of a substance to a target tissue. In some variations, a microdose amount is used in early human studies, e.g., before a phase I clinical trial, to evaluate the effect of the substance on a target tissue, or to obtain pharmacokinetic or metabolic data. In other variations, a microdose amount is used to locally treat a medical condition. In yet other variations, a microdose amount is used to locally deliver a contrast agent for a structural or functional imaging procedure. Methods for delivering and retrieving the devices from the target tissue are also described.

Abstract: The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule cytotoxins that are chemically modified to include one or more moieties that include hydrophobic portions. In some embodiments, the disclosure provides small-molecule cytotoxins that are chemically modified with fatty acid-containing moieties. In some aspects, the disclosure provides compositions, such as pharmaceutical compositions, that include such modified small-molecule cytotoxins and a protein. In some embodiments, the protein is albumin or an albumin mimetic. Further, the disclosure provides various uses of these compounds and compositions.

Abstract: Systems and methods for determining whether a cancer patient may respond to inhibition of RNA polymerase II as a treatment for the patient are provided. Inhibition of RNA polymerase II may be by way of chemotherapy with an agent such as triptolide, an analog of triptolide, or a prodrug form of triptolide. The cancer patient may be a pancreatic cancer patient, an ovarian cancer patient, a gastric cancer patient, or an esophageal cancer patient. The patient may have any cancer in which c-Myc is over-expressed or over-amplified.

Abstract: The present invention includes compositions and methods for the treatment of cancer comprising an antineoplastic drug and an inhibitor of chromosome maintenance region 1 (CRM1) protein expression or activity, wherein the inhibitor of CRM1 enhances the anti-neoplastic effect of the antineoplastic drug.

Abstract: A method of crystallizing docetaxel is disclosed. The method comprises (a) combining docetaxel and at least one solubilizing solvent to obtain a solution, wherein the solubilizing solvent is selected from the group consisting of acetone, methyl-tert-butyl ether, tetrahydrofuran (THF), and acetonitrile and (b) adding an anti-solvent to the solution to obtain a crystalline docetaxel, wherein the anti-solvent is water.

Abstract: Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging in situ sialidase activities under physiological conditions.

Abstract: The present disclosure generally relates to a process for preparing therapeutic nanoparticles, where the process includes combining a therapeutic agent with an organic acid. The therapeutic nanoparticles may have, for example, improved drug loading and/or drug release properties.

Abstract: An in situ method to deploy and/or plasticize a shape-memory material in order to change the material's physical dimensions and/or mechanical properties, includes a method for deploying a shape memory polymer having a deformed or compressed shape in an environment at a first temperature, the shape memory polymer having a first glass transition temperature which is greater than the first temperature. The method also includes contacting the shape memory polymer with an activation fluid in an amount effective to decrease the glass transition temperature of the shape memory polymer from the first glass transition temperature to a second glass transition temperature which is less than or equal to the first temperature, where the activation fluid comprises a sugar present in an amount effective to raise a flash point of the activation fluid.

Abstract: Medical devices are provided for delivering a therapeutic agent to a tissue. The medical device has a layer overlying the exterior surface of the medical device. The layer contains a therapeutic agent and an additive. The additive has a hydrophilic part and a hydrophobic part and the therapeutic agent is not enclosed in micelles or encapsulated in particles or controlled release carriers.