# US 10,245,234 B1 · Method of treating cancer with edible oil derived excipients

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- Number: US 10,245,234 B1
- Document ID: US10245234B1
- Status: Granted
- Kind: B1
- Application number: 15/859,561
- Filed: 2017-12-31
- Granted: 2019-04-02
- Earliest claimed: 2017-12-31
- Applicants: Bhalchandra Shripad Lele
- Inventors: Bhalchandra Shripad Lele
- Web page: https://patentgrep.com/patent/US10245234B1

## CPC

- A61K 9/5123: {Organic compounds, e.g. fats, sugars}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/5138: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/5146: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides}
- A61K 31/337: having four-membered rings, e.g. taxol
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14)
- A61P 35/00: Antineoplastic agents
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Present invention teaches an improved method of treating cancer comprising intravenously administering to a subject in need thereof substantially ethanol free nanoparticles comprising an anticancer drug and a substantially hydroxyl free unsaturated edible oil saturated at least at one site of unsaturation by a covalently attached hydrogen atom and a covalently attached water soluble polymer.

## Claims

### Claim 1

A method of treating breast cancer consisting intravenously administering to a subject in need thereof a therapeutically effective amount of substantially ethanol free nanoparticle composition wherein nanoparticle composition consists nanoparticles having hydrodynamic diameter of 10 to 200 nm consisting 1 to 10 percent by weight of a taxane and 90 to 99 percent by weight of a substantially hydroxyl free unsaturated oil saturated at least at one site of unsaturation by a covalently attached hydrogen atom and a covalently attached water soluble polymer of formula
—S—(CH2)n—S-X-POLY
wherein n is an integer selected from 2 to 12,
X is thiol reactive linker containing functionalities selected from a group consisting maleimido, acrylate, methacrylate, isocyanate, isothiocyanate, iodoacetamido, bromoacetamido, sulfovinyl, thioether,
POLY is substantially biocompatible water soluble polymer selected from a group consisting polyethylene glycol, polyethylene oxide, polyethylene glycol methyl ether, homo and heterobifuctional polyethylene glycols, polyethylene glycol-co-polypropylene glycol, polyethylene oxide-block-polypropylene oxide, polyethylene glycol-acrylate, polyethylene glycol-methacrylate, methoxypolyethylene glycol-acrylate, methoxypolyethylene glycol-methacrylate, poly(polyethyleneglycol-metahcrylate)s, poly(methoxypolyethyleneglycol-methacrylate)s, poly(N-2-hydroxypropylmethacrylamide), poly(N-vinylpyrrolidone), poly(N-isopropylacrylamide), poly(acrylic acid), poly(methacrylic acid), poly(2-aminoethyl methacrylate), poly(N,N-dimethylaminoethyl methacrylate), poly(2-methacryloyloxyethylphosphorylcholine) and combinations thereof,
substantially hydroxyl free unsaturated oil is oil selected from a group of edible oils consisting olive oil, corn oil, canola oil, soybean oil, rapeseed oil, linseed oil, trilinolein, triolein, peanut oil, sunflower oil, mustard oil, almond oil, palm oil, sesame oil, safflower oil, cottonseed oil, grape seed oil, rice bran oil, mono, di, triglycerides of unsaturated fatty acids of C7 to C22 chain length, unsaturated fatty acids of C7 to C22 chain length, and mixtures thereof,
and taxane is selected from a group consisting paclitaxel, docetaxel, cabazitaxel.