117 results about "Lipotropic" patented technology

The invention provides a drug-oligomer conjugate having the following general formula:wherein D is a therapeutic drug moiety; H and H' are each a hydrophilic moiety, independently selected from the group consisting of straight or branched PEG polymers having from 2 to 130 PEG subunits, and sugars; L is a lipophilic moiety selected from the group consisting of alkyl groups having 2-26 carbon atoms, cholesterol, adamantane and fatty acids; o is a number from 1 to the maximum number of covalent bonding sites on H; m+n+p together have a value of at least one and not exceeding the total number of covalent bonding sites on D for the -H', -L and -H-L substituents; the H-L bond(s) are hydrolyzable and the D-L' bond(s), when present, are hydrolyzable; the conjugate being further characterized by one of the following: (i) m is 0 and p is at least 1; (ii) n is 0 and p is at least 1; (iii) m and n are each 0 and p is at least 1; (iv) p is 0 and m and n are each at least 1. The therapeutic drug moiety is preferably a therapeutic protein or peptide, preferably insulin or a functional equivalent thereof.

This invention relates to a galenical gel formulation for nasal administration of neurotransmitters / neuromodulators such as dopamine, serotonin or pregnenolone and progesterone. The special lipophilic or partly lipophilic system of the invention leads to high bioavailability of the active ingredient in plasma and brain caused by sustained serum levels and / or direct or partly direct transport from nose to the brain.

This invention relates to a gel formulation for nasal administration of a controlled release formulation of hormones to the systemic circulation and / or to the brain. The special lipophilic or partly lipophilic system of the invention leads to higher bioavailability of the active ingredient caused by sustained serum levels in plasma but also leads to a more favorable serum level profile. The special lipophilic or partly lipophilic system also allows for the modulation of brain functioning. The invention also relates to the nasal administration of steroid hormones for treatment of female sexual dysfunction (FSD) or female arousal disorder.

The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C8-C22 fatty acid, and preferably may be a saturated or unsaturated C10-C18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer. Many compounds can be administered according to the present invention including, but not limited to, tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine.

A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and / or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and / or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and / or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

The invention provides methods and compositions for the delivery of lipophilic drugs that are useful for the treatment of various ophthalmological diseases, disorders, and pathologies, including the treatment of age-related macular degeneration, diabetic retinopathy, diabetic macular edema, cancer, and glaucoma.

This invention discloses a method for preparing a complex comprised of a VEGF Nucleic Acid Ligand and a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound by identifying a VEGF Nucleic Acid Ligand by SELEX methodology and associating the VEGF Nucleic Acid Ligand with a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound. The invention further discloses Complexes comprising one or more VEGF Nucleic Acid Ligands in association with a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound. The invention further includes a Lipid construct comprising a VEGF Nucleic Acid Ligand or Complex and methods for making the same.

A complex coacervate delivery system is provided which encapsulates lipophilic nutrients such as, for example, fish oils high in omega-3 fatty acids. The complex coacervate delivery system protects the lipophilic nutrient from degradation, e.g., oxidation and hydrolysis, and also reduces or eliminates the unpleasant taste and odor of the lipophilic nutrient. The complex coacervate delivery system upon ingestion is operative to substantially release the lipophilic nutrient in the lower gastrointestinal tract in a pH-controlled manner. The complex coacervate delivery system may be included in a food or beverage product having a pH value within the range of about 1.5 to about 5.0.

The invention provides a liposome-modified spermine derivative and a liposome prepared by the derivative. The spermine derivative is directly applied or is mixed with one or more selected from cholesterol, neutral lipids and polyethylene glycol (PEG)-modified lipids, which can be adopted as a carrier for entrapping or absorbing bioactive molecular drugs to be loaded into cells. In this way, the effect of regulation, intervention or treatment is realized. In a general formula (1), X1 represents -(CH2)- or carbonyl group, wherein n represents 1, 2 or 3; X2 represents -(CH2)-, ester group, amide group, oxygen, or sulfur; R1 and R2 independently represent C6-C18 alkyl group or lipophilic cholesterol molecules, respectively.

The present method involves the photodynamic treatment of hyperactive gland disorders. The method involves the topical administration of a photosensitizer composition comprising hydrophobic and / or lipophilic green porphyrins such as lemuteporfin, polyethylene glycol and skin penetration enhancers such as oleyl alcohol and TRANSCUTOL™ to affected skin and subsequent exposure of that skin to energy of a wavelength capable of activating the photosensitizer.

Disclosed are ingestible additives and ingestible supplements that are capable of promoting liver function, promoting liver health, or reducing alcoholic hepatopathy in a subject. The ingestible additive or supplement can include at least one essential amino acid, at least non-essential amino acid, at least one antioxidant, at least one lipotropic compound, at least one water-soluble vitamin, or at least one plant or extract thereof.

The present invention relates to cell culture medium compositions comprising lipophilic compounds and solubilizing agent and methods of using such compositions for the culturing of cells. The invention also relates to methods of treating disorders of the nervous system such as peripheral neuropathy.

This invention relates to a galenical gel formulation for nasal administration of neurotransmitters / neuromodulators such as dopamine, serotonin or pregnenolone and progesterone. The special lipophilic or partly lipophilic system of the invention leads to high bioavailability of the active ingredient in plasma and brain caused by sustained serum levels and / or direct or partly direct transport from nose to the brain.

The disclosure provides a pharmaceutical composition for treating social anxiety, performance anxiety, and social phobia comprising a therapeutic amount for die treatment of a patient of a β-adrenergic receptor antagonist, an anti-diarrheal compound, and an optional anticholinergic compound. The β-adrenergic receptor antagonist may be the lipophilic β-blocker propranolol HCl, the anti-diarrheal compound may be the opioid diphenoxylate HCl, and the optional anticholinergic compound may be atropine sulfate. The composition for treating performance anxiety and social phobia can further include a pharmaceutically acceptable carrier. A method of preventing or treating social anxiety, performance anxiety, and social phobia in a patient is also provided, comprising administering a composition of the disclosure to a patient in need of such treatment. The composition administered in the present method comprises a therapeutic amount of a β-adrenergic receptor antagonist, an anti-diarrheal compound, and an optional anticholinergic compound.

The present invention provides diastereomeric peptides derived from the T Cell Receptor alpha Transmembrane Domain, and lipophilic conjugates thereof, which peptides and conjugates are effective in preventing or treating T cell mediated inflammatory diseases. The invention provides pharmaceutical compositions comprising these diastereomeric peptides and conjugates, and uses thereof for therapy of inflammatory diseases, autoimmunity and graft rejection.

Non-peptide somatostatin receptor ligands with conformationally restricted side chains exhibiting high binding affinity toward somatostatin receptors are provided. The compounds exhibit a high selectivity and act as agonists at human subtype 2 somatostatin receptors. The compounds are long acting for advantageous use as medicaments in peripheral diseases where somatostatinergic therapy is indicated. Furthermore, many of the compounds are lipophilic and are particularly useful for treating central nervous system and ophthalmic diseases where penetration of the blood brain and blood retinal barriers is required. It is a further object to describe the preferred stereoisomers of these somatostatin agonists and processes for their preparation. Further objects will become apparent from reading the following description.

A mitochondria targeted gold nanoparticle (T-3-BP-AuNP) decorated with 3-bromopyruvate (3-BP) and delocalized lipophilic triphenylphosphonium (TPP) cations to target the mitochondrial membrane potential (Δψm) was developed for delivery of 3-BP to cancer cell mitochondria by taking advantage of higher Δψm in cancer cell compared to normal cells. This construct showed remarkable anticancer activity in prostate cancer cells compared to non-targeted construct NT-3-BP-AuNP and free 3-BP. Anticancer activity of T-3-BP-AuNP was further enhanced upon laser irradiation by exciting the surface plasmon resonance band of AuNP and thereby utilizing a combination of 3-BP chemotherapeutic and AuNP photothermal effects. T-3-BP-AuNPs showed markedly enhanced ability to alter cancer cell metabolism by inhibiting glycolysis and demolishing mitochondrial oxidative phosphorylation in prostate cancer cells. Our findings demonstrated that mitochondria targeted and concerted chemo-photothermal treatment of glycolytic cancer cells with a single NP may have promise as a new anticancer therapy.

The present invention provides lipid emulsions and methods of intravenously administering lipid emulsions to treat systemic toxicity caused by foreign lipophilic and amphiphilic substances. In particular, methods are provided to treat cardiovascular impairment, such as cardiotoxicity, asystole and ischemia of the brain and heart, and neurological impairments, such as seizures and comas, caused by foreign lipophilic and amphiphilic substances, including cardiovascular impairment caused by local anesthetics, tricyclic antidepressants, sodium channel blockers, and calcium channel blockers.

The embodiments herein provide a nanoparticle system for targeted gene delivery or a drug delivery and a method of synthesising the same. The nanoparticle composition for targeted gene transfer and drug delivery comprises a protein, a chitosan and a lipid. A method of synthesizing the nanoparticles involves preparing a gelatine and chitosan gel. A milky colloid solution is prepared with the gelatine, chitosan solution and a phosphatidylcholine. The milky colloid is homogenized for the self assembly of the nanoparticles. The milky colloid is subjected to high speed and high pressure homogenizer. The CHO cells are transfected with nanoparticles and lipofectamine 2000 for comparing the transfection efficiency. The nanoparticles deliver DNA, RNA, ribozyme and nucleotide sequences. The nanoparticles deliver lipophylic and hydrophilic drugs. The transfection efficiency of gene and drug is higher when the target cells are transferred with nanoparticles, compared to the cells transferred with lipofectamine 2000.

This invention relates to a gel formulation for nasal administration of a controlled release formulation of hormones to the systemic circulation and / or to the brain. The special lipophilic or partly lipophilic system of the invention leads to higher bioavailability of the active ingredient caused by sustained serum levels in plasma but also leads to a more favorable serum level profile. The special lipophilic or partly lipophilic system also allows for the modulation of brain functioning. The invention also relates to the nasal administration of steroid hormones for treatment of female sexual dysfunction (FSD) or female arousal disorder.

The invention discloses a lipopeptid for restraining HIV with a broad spectrum, derivatives, a drug compound and an application thereof. The lipopeptid is a) or b) as follows: a) the lipopeptid comprises a polypeptide, a connecting arm, an amino acid X residual group and a lipotropy compound, wherein the polypeptide has an antiviral activity, the connecting arm is connected with the carboxyl terminal of the polypeptide, the amino acid X residual group is connected with the connecting arm and the lipotropy compound is connected with the amino acid X residual group; b) the lipopeptid comprises the polypeptide and the lipotropy compound, wherein the polypeptide has the antiviral activity and the lipotropy compound is connected with the carboxyl terminal of the polypeptide; the virus is any one of v1 to v7 as follows: v1, HIV-1, HIV-2 and SIV; v2, HIV-1 and HIV-2; v3, HIV-1 and SIV; v4, HIV-2 and SIV; v5 and HIV-1; v6 and HIV-2; v7 and SIV; the amino acid X is K, C, S, T or Y. The lipopeptid can be used for treating and / or preventing HIV infection.

This invention relates to cationic lipids. More particularly the invention relates to biodegradable cationic lipids having a plurality of cationic headgroups and one or more lipophilic tail groups. The lipids are of utility in various applications, and in particular in permitting transfection of molecules, and in particular DNA and RNA, into cells. As such the lipids have specific utility in the field of gene therapy as well as other applications such as delivery of small molecules into cells, detergents, and metal ion complexation for medical or industrial applications.

A complex coacervate delivery system is provided which encapsulates lipophilic nutrients such as, for example, fish oils high in omega-3 fatty acids. The complex coacervate delivery system protects the lipophilic nutrient from degradation, e.g., oxidation and hydrolysis, and also reduces or eliminates the unpleasant taste and odor of the lipophilic nutrient. The complex coacervate delivery system upon ingestion is operative to substantially release the lipophilic nutrient in the lower gastrointestinal tract in a pH-controlled manner. The complex coacervate delivery system may be included in a food or beverage product having a pH value within the range of about 1.5 to about 5.0.

The invention discloses an active peptide with an oil oxidation resisting function, a preparation method of the active peptide and an application of the active peptide, and belongs to the technical field of plant-derived biological active peptides. Oil processing by-products, namely, oil crops after oil extraction serve as raw materials, the oil oxidation resisting peptide with the functional characteristics of removing DPPH, chelating metal ions, inhibiting lipid peroxidation, prolonging plant oil oxidation induction time, enhancing emulsion stability and the like is prepared by the steps ofprotein extraction, infrared pretreatment, proteolysis, freeze-drying, lipotropic portion extraction, vacuum concentration, drying and the like, can serve as a natural antioxidant, is applied to storage and preservation of oil and other oil-containing food, solves the problems of product deterioration and harmful product generation caused by oil oxidation and prolongs food shelf life. The method has great practical significance and social significance for restraining oil oxidation, guaranteeing food safety and promoting technical progress.

The invention discloses a phospholipids compound of bicyclo-ethanol and a preparation method thereof, in particular relates to a phospholipids compound of bicyclo-ethanol, a preparation method of the phospholipids compound of bicyclo-ethanol and a preparation containing the phospholipids compound of bicyclo-ethanol. The phospholipids compound of bicyclo-ethanol comprises bicyclo-ethanol and phospholipids material with the weight proportion of 1 to 2-12. The phospholipids compound can be selectively added with antioxidative stabilizer and / or srobent. In the invention, bicyclo-ethanol is prepared into the phospholipids compound so that the water-dispersible property and the lipotropy of the bicyclo-ethanol are both improved. Compared with the raw material medicine of the bicyclo-ethanol, the phospholipids compound of bicyclo-ethanol can remarkably improve the blood concentration after being orally taken, and has higher biological validity when used for clinic treatment for chronic hepatitis.

The invention relates to the solubilization of lipophilic substances, preferably from the group of lipids, steroids, terpenes, and polar lipids, by means of a lecithin / polyol matrix or a lecithin / carbohydrate matrix so as to obtain water-soluble, emulsive, transparent concentrates which are used in cosmetic, dietary, and pharmaceutical products.

The invention discloses application of dendrobium stem alkaloids in preparation of medicament for treating diabetes mellitus and a product. The dendrobium stem alkaloids are components of lipotropismtotal alkaloids, which are extracted from dendrobium stems. Compared with the prior art, the invention further defines the pharmacologic action and the pharmacologic mechanism of the treatment of thediabetes mellitus through researching the influences of the dendrobium stem alkaloids to a mice blood sugar raising model and a high blood sugar and high blood fat chained streptozotocin induced diabetes mellitus rat model which are caused by epinephrine, and provides a pharmacology basis for the development of dendrobium stem medicinal materials.

The invention relates to a preparation method and of a liver cancer targeting glycoside ligand molecule and a preparation method of a liposome of the liver cancer targeting glycoside ligand molecule, and especially relates to a liver ASGPR target targeting glycoside ligand molecule and the liposome prepared by using the targeting glycoside ligand. The glycoside ligand molecule is formed by a liver targeting glycoside group, a lipophilic anchor and a substituted or non-substituted -(CH2)8 linear spacer arm for connecting the liver targeting glycoside group with the lipophilic anchor through an ester bond. The liver cancer targeting glycoside ligand molecule makes antitumor drugs in a drug delivery system maximally concentrated in liver tumor cells, improves the drug treatment index, reduces toxic and side effects on whole bodies, and improves patients' survival quality.

The present invention provides 3-substituted amino-1, 2, 4-substituted phentriazine-1, 4-dioxides in the general expression as shown. The compounds are prepared with substituted one-nitroaniline as main material and through acylation to produce urea, cyclization, chlorination, amino substitution, oxidation and other steps. The tests show that the compounds of the present invention have anticancer activity and hypoxia selectivity higher than those of TPZ and may be used in preparing hypoxia selective anticancer medicine.