Hydrophobic Drug-Delivery Material, Method for Manufacturing Thereof and Methods for Delivery of a Drug-Delivery Composition

1 . A method for manufacturing a drug-delivery composition, comprising:

providing at least a pharmaceutically active composition;

providing a hydrophobic matrix; and

mixing the hydrophobic matrix and the pharmaceutically active composition to form a paste-like or semi-solid drug-delivery composition.

2 . The method according to claim 1 , wherein providing the hydrophobic matrix comprises mixing of at least a hydrophobic solid component and a hydrophobic liquid component.

3 . The method according to claim 1 , further comprising:

providing the pharmaceutically active composition as dry pharmaceutically active composition powder; and

homogeneous mixing the hydrophobic matrix with the dry pharmaceutically active composition powder to form the paste-like or semi-solid drug delivery composition.

4 . The method according to claim 1 , further comprising:

providing the pharmaceutically active composition in a dissolved state; and

homogeneous mixing the hydrophobic matrix with the dissolved pharmaceutically active composition to form the paste-like or semi-solid drug-delivery composition.

5 . The method according to claim 1 , wherein the pharmaceutically active composition comprises at least a pharmaceutically active compound and at least one excipient selected from the group consisting of monosaccharides, disaccharides, oligosaccharides, polysaccharides like hyaluronic acid, pectin, gum arabic and other gums, albumin, chitosan, collagen, collagen-n-hydroxysuccinimide, fibrin, fibrinogen, gelatin, globulin, polyaminoacids, polyurethane comprising amino acids, prolamin, protein-based polymers, copolymers and derivatives thereof, and mixtures thereof.

6 . The method according to claim 1 , wherein the pharmaceutically active composition comprises at least a pharmaceutically active compound without any excipients.

7 . The method according to claim 1 , wherein the forming of the paste-like or semi-solid drug-delivery composition includes repeated cycles of pressing and folding, in an algorithmic manner, of the mixture of the hydrophobic matrix and the pharmaceutically active composition.

8 . The method according to claim 4 , wherein the dissolved pharmaceutically active composition is added step-wise during mixing comprising repeated pressing and folding of the mixture of the hydrophobic matrix and the pharmaceutically active composition.

9 . The method according to claim 7 , wherein the pressing applies a pressure of not more than 10 6 N·m −2 .

10 . The method according to claim 1 , wherein the pharmaceutically active composition is dissolved in an aqueous solution before being mixed with the hydrophobic matrix.

11 . The method according to claim 1 , further comprising one of:

simultaneous mixing of at least a hydrophobic solid component, a hydrophobic liquid component, and the pharmaceutically active composition dissolved in an aqueous solution to form the paste-like or semi-solid drug-delivery composition; and

mixing of at least a hydrophobic solid component and a hydrophobic liquid component to form the hydrophobic matrix, and adding the pharmaceutically active composition dissolved in an aqueous solution to the hydrophobic matrix to form the paste-like or semi-solid drug-delivery composition.

12 . The method according to claim 3 , wherein the pharmaceutical active composition powder comprises particles in a size range from about 100 nm to about 50 μm.

13 . The method according to claim 1 , wherein the hydrophobic matrix comprises a solid component and a liquid hydrophobic component,

wherein the solid component is selected from waxes, fruit wax, carnauba wax, bees wax, waxy alcohols, plant waxes, soybean waxes, synthetic waxes, triglycerides, lipids, long-chain fatty acids and their salts like magnesium stearate, magnesium palmitate, esters of long-chain fatty acids, long-chain alcohols like cetyl palmitate, waxy alcohols, long-chain alcohols like cetylalcohol, oxethylated plant oils, oxethylated fatty alcohols, and

wherein the liquid hydrophobic component is selected from plant oils, castor oil, jojoba oil, soybean oil, silicon oils, paraffin oils, and mineral oils, cremophor, oxethylated plant oils, oxethylated fatty alcohols.

14 . The method according to claim 1 , wherein the pharmaceutically active composition comprises a pharmaceutically active compound selected from the group consisting of immunoglobulins, fragments or fractions of immunoglobulins, synthetic substance mimicking immunoglobulins or fragments or fractions thereof, proteins peptides having a molecular mass equal to or higher than 3 kDa, ribonucleic acids (RNA), desoxyribonucleic acids (DNA) including aptamers and spiegelmers, plasmids, peptide nucleic acids (PNA), steroids, and corticosteroids.

15 . The method according to claim 1 , wherein the pharmaceutically active composition comprises a pharmaceutically active compound selected from the group consisting of immunoglobulins, fragments or fractions of immunoglobulins, synthetic substance mimicking immunoglobulins or synthetic, semisynthetic or biosynthetic fragments or fractions thereof, chimeric, humanized or human monoclonal antibodies, Fab fragments, fusion proteins or receptor antagonists (e.g., anti TNF alpha, Interleukin-1, Interleukin-6 etc.), antiangiogenic compounds (e.g., anti-VEGF, anti-PDGF etc.), intracellular signaling inhibitors (e.g JAK1,3 and SYK inhibitors), peptides having a molecular mass equal to or higher than 3 kDa, ribonucleic acids (RNA), desoxyribonucleic acids (DNA), plasmids, peptide nucleic acids (PNA), steroids, corticosteroids, an adrenocorticostatic, an antibiotic, an antidepressant, an antimycotic, a [beta]-adrenolytic, an androgen or antiandrogen, an antianemic, an anabolic, an anaesthetic, an analeptic, an antiallergic, an antiarrhythmic, an antiarterosclerotic, an antibiotic, an antifibrinolytic, an anticonvulsive, an antiinflammatory drug, an anticholinergic, an antihistaminic, an antihypertensive, an antihypotensive, an anticoagulant, an antiseptic, an antihemorrhagic, an antimyasthenic, an antiphlogistic, an antipyretic, a beta-receptor antagonist, a calcium channel antagonist, a cell, a cell differentiation factor, a chemokine, a chemotherapeutic, a coenzyme, a cytotoxic agent, a prodrug of a cytotoxic agent, a cytostatic, an enzyme and its synthetic or biosynthetic analogue, a glucocorticoid, a growth factor, a haemostatic, a hormone and its synthetic or biosynthetic analogue, an immunosuppressant, an immunostimulant, a mitogen, a physiological or pharmacological inhibitor of mitogens, a mineralcorticoid, a muscle relaxant, a narcotic, a neurotransmitter, a precursor of a neurotransmitter, an oligonucleotide, a peptide, a (para)-sympathicomimetic, a (para)-sympatholytic, a protein, a sedating agent, a spasmolytic, a vasoconstrictor, a vasodilatator, a vector, a virus, a virus-like particle, a virustatic, a wound-healing substance, and combinations thereof.

16 . The method according to claim 1 , further comprising:

forming the drug-delivery composition into an applicable form.

17 . A drug-delivery composition, comprising:

a paste-like or semi-solid mixture comprising at least a hydrophobic matrix and a pharmaceutically active compound.

18 . The drug-delivery composition according to claim 17 , wherein the pharmaceutically active compound is dispersed in the hydrophobic matrix in particulate form.

19 . The drug-delivery composition according to claim 17 , wherein the pharmaceutically active compound is dispersed in the hydrophobic matrix in a dissolved state.

20 . The drug-delivery composition according to claim 19 , wherein the pharmaceutically active compound is dissolved in a solution comprising water and electrolytes.

21 . The drug-delivery composition according to claim 19 , wherein the pharmaceutically active compound is dissolved in a solution comprising water, electrolytes and at least one of monosaccharides, disaccharides, oligosaccharides, polysaccharides like hyaluronic acid, pectin, gum arabic and other gums, albumin, chitosan, collagen, collagen-n-hydroxysuccinimide, fibrin, fibrinogen, gelatin, globulin, polyaminoacids, polyurethane comprising amino acids, prolamin, protein-based polymers, copolymers and derivatives thereof, and mixtures thereof.

22 . The drug-delivery composition according to claim 17 , wherein the paste-like or semi-solid mixture has a modulus of elasticity at least of 10 −4 N·mm −2 .

23 . The drug-delivery composition according to claim 17 , wherein the paste-like or semi-solid mixture has a viscosity of at least 100 mPa·s.

24 . The drug-delivery composition according to claim 17 , wherein the pharmaceutically active compound is selected from the group consisting of immunoglobulins, fragments or fractions of immunoglobulins, synthetic substance mimicking immunoglobulins or fragments or fractions thereof, proteins, peptides having a molecular mass equal to or higher than 3 kDa, ribonucleic acids (RNA), desoxyribonucleic acids (DNA), plasmids, peptide nucleic acids (PNA), aptamers, spiegelmers, steroids, and corticosteroids.

25 . The drug-delivery composition according to claim 17 , wherein the pharmaceutically active compound is selected from the group consisting of: immunoglobulins, fragments or fractions of immunoglobulins, synthetic substance mimicking immunoglobulins or synthetic, semisynthetic or biosynthetic fragments or fractions thereof, chimeric, humanized or human monoclonal antibodies, Fab fragments, fusion proteins or receptor antagonists (e.g., anti TNF alpha, Interleukin-1, Interleukin-6 etc.), antiangiogenic compounds (e.g., anti-VEGF, anti-PDGF etc.), intracellular signaling inhibitors (e.g JAK1,3 and SYK inhibitors), peptides having a molecular mass equal to or higher than 3 kDa, ribonucleic acids (RNA), desoxyribonucleic acids (DNA), plasmids, peptide nucleic acids (PNA), steroids, corticosteroids, an adrenocorticostatic, an antibiotic, an antidepressant, an antimycotic, a [beta]-adrenolytic, an androgen or antiandrogen, an antianemic, an anabolic, an anaesthetic, an analeptic, an antiallergic, an antiarrhythmic, an antiarterosclerotic, an antibiotic, an antifibrinolytic, an anticonvulsive, an antiinflammatory drug, an anticholinergic, an antihistaminic, an antihypertensive, an antihypotensive, an anticoagulant, an antiseptic, an antihemorrhagic, an antimyasthenic, an antiphlogistic, an antipyretic, a beta-receptor antagonist, a calcium channel antagonist, a cell, a cell differentiation factor, a chemokine, a chemotherapeutic, a coenzyme, a cytotoxic agent, a prodrug of a cytotoxic agent, a cytostatic, an enzyme and its synthetic or biosynthetic analogue, a glucocorticoid, a growth factor, a haemostatic, a hormone and its synthetic or biosynthetic analogue, an immunosuppressant, an immunostimulant, a mitogen, a physiological or pharmacological inhibitor of mitogens, a mineralcorticoid, a muscle relaxant, a narcotic, a neurotransmitter, a precursor of a neurotransmitter, an oligonucleotide, a peptide, a (para)-sympathicomimetic, a (para)-sympatholytic, a protein, a sedating agent, a spasmolytic, a vasoconstrictor, a vasodilatator, a vector, a virus, a virus-like particle, a virustatic, a wound-healing substance, and combinations thereof.

26 . The drug-delivery composition according to claim 17 , wherein the hydrophobic matrix comprises at least a hydrophobic solid component and a hydrophobic liquid component, wherein the mass ratio of the hydrophobic solid component to the hydrophobic liquid component is below 2.8:1.

27 . The drug-delivery composition according to claim 17 , wherein the mass of the pharmaceutically active compound is up to 25% (w/w) of the total mass of the paste-like or semi-solid mixture.

28 . The drug-delivery composition according to claim 17 , wherein the mass of the pharmaceutically active compound is at least 0.01% (w/w) of the total mass of the paste-like or semi-solid mixture.

29 . A method for delivery a drug-delivery composition, comprising:

providing a drug-delivery composition comprising a paste-like or semi-solid mixture comprising at least a hydrophobic matrix and a pharmaceutically active compound; and

applying the drug-delivery composition into a human or animal body.

30 . The method of claim 29 , wherein applying the mixture into the human or animal body comprises at least one of:

implanting or injecting the mixture into a human or animal body;

intraocular injecting the mixture into a human, or animal body;

subcutaneous injecting the mixture into a human, or animal body;

intramuscular injecting the mixture into a human, or animal body;

intraperitoneal injecting the mixture into a human, or animal body;

intravenous injecting the mixture into a human, or animal body;

inhalative administering the mixture into a human, or animal body; and

intranasal administering the mixture into a human, or animal body.