Transdermal delivery of medicinal cetylated fatty esters using phonophoresis or iontophoresis
View Patent ↗The use of phonophoresis or iontophoresis to enhance transdermal delivery of medicinal Cetylated fatty esters when applied in cream or gel compositions is disclosed. These compositions provide hydrophilic salt forms and penetration-enhancing vehicles that work in conjunction with phonophoresis or iontophoresis to increase the efficacy of the medicinal actives.
1. A method of enhancing the rate of permeation of cetylated fatty esters through the skin comprising steps:
a. Topically applying to a portion of skin a composition comprising:
i. four or more cetylated fatty acid esters, said cetylated esters are present in amounts ranging from 4-40%, and are selected from the group consisting of cetyl oleate, cetyl palmitate, cetyl myristoleate and those having saturated or unsaturated hydrocarbon chains having 10 or more carbon atoms; and
ii. one or more polar solvents present in amounts ranging from 5-30%, wherein the solvents are selected from the group consisting of 1,2,4-butane triol, dimethicone copolyol, ethylene glycol, glycerol, glyceryl monostearate, 1,2,6-hexane triol, propylene glycol ether of methyl glucose or sorbitol, PEG 40 hydrogenated caster oil, polyethylene glycol and propylene glycol; and
b. Applying phonophoresis or ionophoresis to the same portion of skin; wherein step b can optionally be performed before step a.
2. The method according to claim 1 , wherein the one or more polar solvents comprises a polyethylene glycol selected from the group consisting of PEG 50 , PEG 100 and PEG 500 .
3. The method according to claim 1 , wherein the composition is in the form of a gel, lotion, foam, spray or cream.
4. The method according to claim 1 , wherein the composition further comprises menthol in amounts ranging from 1-20%.
5. The method according to claim 1 , wherein the composition has a pH ranging from 4.0 to 8.0.
6. The method according to claim 1 , wherein the phonophoresis utilizes ultrasound, with continuous or discontinuous pulsing, in the range of 20 to 2,500 kHz to enhance the delivery of the cetylated fatty acid ester of claim 1 .
7. The method according to claim 1 , wherein the phonophoresis utilizes a beam intensity of less than 5.0 W cm −2 .
8. The method according to claims 1 , where the penetration of the cetylated fatty acid ester though the skin is enhanced by 200% or more, when the phonophoresis utilizes ultrasound, with continuous or discontinuous pulsing, in the range of 20 to 2,500 kHz , and has a beam intensity of less than 5.0 W cm −2 .
9. The method according to claim 1 , wherein the ionophoresis generates a low level electric current, with a current intensity ranging from 0.5 to 20 mA, which facilitates the transdermal flux of the cetylated fatty acid esters.
10. A method of treating inflammatory conditions, comprising the steps of
a. Topically applying to a portion of skin a composition comprising:
i. four or more cetylated fatty acid esters, said cetylated esters are present in amounts ranging from 4-40%, and are selected from the group consisting of cetyl oleate, cetyl palmitate, cetyl myristoleate and those having saturated or unsaturated hydrocarbon chains having 10 or more carbon atoms; and
ii. one or more polar solvents present in amounts ranging from 5-30%, wherein the solvents are selected from the group consisting of 1,2,4-butane triol, dimethicone copolyol, ethylene glycol, glycerol, glyceryl monostearate, 1,2,6-hexane triol, propylene glycol ether of methyl glucose or sorbitol, PEG 40 hydrogenated caster oil, polyethylene glycol and propylene glycol; and
b. Applying phonophoresis or ionophoresis to the same portion of skin; where step b can optionally be performed before step a;
wherein the inflammatory condition is selected from the group consisting of osteoarthritis, rheumatoid arthritis, inflammation of the spine, discogenic back pain, polymyalagia pheumatic, musculocutaneous injuries, tendinitis, Achilles tendinitis, tenosynovitis, bursitis, chronic patellar tendinitis, epicondylitis, periarticular soft tissue swelling, repetitive strain injuries, myofascial pain syndrome, fibrositis, fibromyalgia, peripheral neuropathies, herpetic neuropathy and Sjogren's syndrome.