TRANSDERMAL DELIVERY OF CANNABINOIDS
The present invention overcomes the problems associated with existing drug delivery systems by delivering cannabinoids transdermally. Preferably, the cannabinoids are delivered via an occlusive body (i.e., a patch) to alleviate harmful side effects and avoid gastrointestinal (first-pass) metabolism of the drug by the patient. A first aspect of the invention provides a method for relieving symptoms associated with illness or associated with the treatment of illness in a mammalian subject, comprising the steps of selecting at least one cannabinoid from the group consisting of cannabinol, cannabidiol, nabilone, levonantradol, (−)-HU-210, (+)-HU-210, 11-hydroxy-Δ 9 -THC, Δ 8 -THC-11-oic acid, CP 55,940, and R(+)-WIN 55,212-2, selecting at least one permeation enhancer from the group consisting of propylene glycol monolaurate, diethylene glycol monoethyl ether, an oleoyl macrogolglyceride, a caprylocaproyl macrogolglyceride, and an oleyl alcohol, and delivering the selected cannabinoid and permeation enhancer transdermally to treat an illness.
1 . A method for relieving symptoms associated with illness or associated with the treatment of illness in a mammalian subject, comprising the steps of:
selecting at least one cannabinoid from the group consisting of: cannabinol, cannabidiol, nabilone, levonantradol, (−)-HU-210, (+)-HU-210, 11-hydroxy-Δ 9 -THC, Δ 8 -THC-11-oic acid, CP 55,940, and R(+)-WIN 55,212-2;
selecting at least one permeation enhancer from the group consisting of: propylene glycol monolaurate, diethylene glycol monoethyl ether, an oleoyl macrogolglyceride, a caprylocaproyl macrogolglyceride, and an oleyl alcohol; and
delivering the selected cannabinoid and permeation enhancer transdermally to treat an illness.
2 . The method of claim 1 , wherein the delivering step comprises: providing an occlusive body having the selected cannabinoid and permeation enhancer; and positioning the occlusive body on a patient.
3 . The method of claim 2 , wherein the occlusive body comprises:
an impermeable backing;
a rate-controlling microporous membrane, said backing and membrane defining a cavity therebetween;
the selected cannabinoid disposed within the cavity;
the selected permeation enhancer disposed within the cavity;
a viscous flowable gel confined between the backing and the membrane within the cavity for immobilizing the cannabinoid and the permeation enhancer; and
means for attaching the body to skin, wherein the selected cannabinoid and permeation enhancer are released through the membrane to the skin.
4 . The method of claim 1 , wherein the illness is selected from AIDS, cancer, Huntington's disease, arthritis, nervous-tissue inflammation, vascular inflammation, inflammatory bowel disease, and other inflammation-related conditions.
5 . The method of claim 1 , wherein the subject is selected from the group consisting of patients experiencing a loss of appetite, patients experiencing chronic pain, patients experiencing spasticity, patients experiencing dystonia, and patients experiencing nausea and vomiting.
6 . The method of claim 1 , wherein the cannabinoid is a combination of cannabinoids selected from the group consisting of: cannabinol, cannabidiol, nabilone, levonantradol, (−)-HU-210, (+)-HU-210, 1]-hydroxy-Δ 9 -THC, Δ 8 -THC-11-oic acid, CP 55,940, and R(+)-WIN 55,212-2.
7 . The method of claim 1 , wherein the permeation enhancer is a combination of permeation enhancers selected from the group consisting of: propylene glycol monolaurate, diethylene glycol monoethyl ether, an oleoyl macrogolglyceride, a caprylocaproyl macrogolglyceride, and an oleyl alcohol.
8 . The method of claim 1 , wherein the cannabinoid is cannabidiol and the permeation enhancer is diethylene glycol monoethyl ether.
9 . The method of claim 1 , wherein the selected cannabinoid is delivered via a topical formulation.
10 . The method of claim 1 , wherein the selected cannabinoid and permeation enhancer are delivered via a patch.
11 . The method of claim 1 , further comprising the steps of:
selecting an opiate; and
delivering the selected opiate transdermally with the selected cannabinoid and permeation enhancer.
12 . An occlusive body for the delivery of cannabinoids, comprising:
an impermeable backing;
a rate-controlling microporous membrane, said backing and membrane defining a cavity therebetween;
a cannabinoid disposed within the cavity;
a permeation enhancer disposed within the cavity; and
a viscous flowable gel confined between the backing and the membrane within the cavity for immobilizing the cannabinoid and the permeation enhancer.
13 . The occlusive body of claim 12 , wherein the cannabinoid is selected from the group consisting of: Δ 9 -THC, Δ 8 -THC, cannabinol, cannabidiol, nabilone, levonantradol, (−)-HU-210, (+)-HU-210, 11-hydroxy-Δ 9 -THC, Δ 8 -THC-11-oic acid, CP 55,940, R(+)-WIN 55,212-2, or any combination thereof.
14 . The occlusive body of claim 12 , wherein the permeation enhancer is selected from the group consisting of: propylene glycol monolaurate, diethylene glycol monoethyl ether, an oleoyl macrogolglyceride, a caprylocaproyl macrogolglyceride, and an oleyl alcohol.
15 . The occlusive body of claim 12 , further comprising an adhesive for attaching the occlusive body to a patient's skin and wherein the cannabinoid and permeation enhancer are released through the membrane to the patient's skin.
16 . The occlusive body of claim 12 , wherein the occlusive body is a patch.
17 . The occlusive body of claim 12 , wherein the membrane has an exterior surface coated with an adhesive.
18 . The occlusive body of claim 17 , wherein the adhesive is a silicone-based adhesive.
19 . The occlusive body of claim 12 , wherein the membrane is hydrophobic and the cavity includes a hydrophilic wetting agent.
20 . The occlusive body of claim 12 , wherein the cavity includes water and a surfactant selected from a viscosity modifier and a gelling agent.
21 . The occlusive body of claim 20 , wherein the surfactant comprises methyl cellulose.
22 . The occlusive body of claim 12 , further comprising an opiate confined in the cavity with the cannabinoid and permeation enhancer.
23 . A method for increasing the concentration of cannabinoids or cannabinoid metabolites in a subject, comprising:
contacting the subject's skin with a compound selected from the group consisting of: cannabinol, cannabidiol, nabilone, levonantradol, (−)-HU-210, (+)-HU-210, 11-hydroxy-Δ 9 -THC, Δ 8 -THC-11-oic acid, CP 55,940, and R(+)-WIN 55,212-2; and
contacting the subject's skin with a permeation enhancer selected from the group consisting of: propylene glycol monolaurate, diethylene glycol monoethyl ether, an oleoyl macrogolglyceride, a caprylocaproyl macrogolglyceride, and an oleyl alcohol.
24 . The method of claim 23 , further comprising contacting the subject's skin with a drug metabolism inhibitor.
25 . The method of claim 23 , wherein the compound is a combination of compounds selected from the group consisting of: cannabinol, cannabidiol, nabilone, levonantradol, (−)-HU-210, (+)-HU-210, 1]-hydroxy-Δ 9 -THC, Δ 8 -THC-11-oic acid, CP 55,940, and R(+)-WIN 55,212-2.