# US 10,245,272 B2 · Transmembrane penetration enhancer

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- Number: US 10,245,272 B2
- Document ID: US10245272B2
- Status: Granted
- Kind: B2
- Application number: 12/911,593
- Filed: 2010-10-25
- Published: 2012-04-26
- Granted: 2019-04-02
- Earliest claimed: 2010-10-25
- Applicants: Iryna Kravchenko; Sergiy Lozovsky
- Inventors: Iryna Kravchenko; Sergiy Lozovsky
- Web page: https://patentgrep.com/patent/US10245272B2

## CPC

- A61K 31/5513: 1,4-Benzodiazepines, e.g. diazepam {or clozapine}
- A61K 47/28: Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
- A61P 25/08: Antiepileptics; Anticonvulsants
- 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

A transmembrane penetration enhancer includes a thermotropic liquid crystal suitably prepared for use in a therapeutic system to improve delivery of at least one active ingredient across a biomembrane and/or skin. The thermotropic liquid crystal comprises at least one cholesteryl ester and is effective in a mesomorphic state at a temperature of the biomembrane and/or skin. A therapeutic system includes the prepared thermotropic liquid crystal for enhanced transmembrane penetration and at least one active ingredient for delivery by the thermotropic liquid crystal. A method for making and using the transmembrane penetration enhancer is presented.

## Claims

### Claim 1

A method for delivering an active agent through the skin of a patient in need thereof, said method comprising contacting the skin of said patient with a transmembrane penetration enhancer consisting of said active agent, wherein said transmembrane penetration enhancer is a thermotropic liquid crystal transmembrane penetration enhancer consisting of:
1) one or a fused mixture of two or more cholesteryl esters in an amount of 90% or more; and
2) an active agent selected from the group consisting of diazepam, oxazepam, lorazepam, clonazepam, bromazepam, alprazolam, clotiazepam, clobazam, buspirone, amphetamine, methamphetamine, methylphenidate, cathine, fenfluramine, piracetam, and meclofenoxate, in an amount of 10% or less;
wherein said thermotropic liquid crystal transmembrane penetration enhancer delivers said active agent through the skin of the patient when said cholesteryl esters are in a mesomorphic state.

### Claim 2 (depends on 1)

The method as recited in claim 1, in which said one or more cholesteryl esters is selected from a group consisting of cholesteryl pelargonate, cholesteryl valerate, cholesteryl succinate, cholesteryl adipinate, cholesteryl nanilsuccinate and cholesteryl propionate.

### Claim 3 (depends on 1)

The method as recited in claim 1, in which said combination is operable to improve transmembrane penetration.

### Claim 4 (depends on 1)

The method as recited in claim 1, in which said combination is operable to improve transmucosal penetration.