Transdermal formulations for delivery of capsaicinoids
The present application is directed to transdermal formulations comprising one or more capsaicinoinds, one or more 1,4-dialdehyde sesquiterpenes, a penetration enhancer comprising tetrahydropiperine and a transdermal formulation base. The formulations advantageously show improved color characteristics and cause less irritation compared to other known transdermal or topica formulations comprising capsaicinoinds.
1. A transdermal formulation comprising at least one capsaicinoid, at least one 1,4-dialdehyde sesquiterpene, a penetration enhancer comprising tetrahydropiperine, and a transdermal formulation base, wherein the transdermal formulation base comprises:
(a) an aqueous phase comprising water and at least one emulsion stabilizer;
(b) an oil phase comprising at least one emulsifier, at least one emulsion stabilizer, at least one emollient comprising at least one flavonoid, and at least one other emollient;
wherein the oil and aqueous phase form an emulsion;
(c) an external phase comprising at least one flavonoid containing-extract, the at least one penetration enhancer comprising tetrahyropiperine, the at least one capsaicinoid, the at least one 1,4-dialdehyde sesquiterpene, and at least one phospholipid-complexed flavonoid; and optionally
(d) at least one preservative phase.
2. The transdermal formulation of claim 1 , wherein the at least one 1,4-dialdehyde sesquiterpene is selected from polygodial, drimanial, isovelleral, warburganal and mixtures thereof.
3. The transdermal formulation of claim 2 , wherein the at least one 1,4-dialdehyde sesquiterpene comprises polygodial.
4. The transdermal formulation of claim 1 , wherein the transdermal formulation comprises Tasmannia lanceolata or Tazmanian Mountain Pepper (TMP), or an extract of Tasmannia lanceolata or TMP, as a source of the at least one 1,4-dialdehyde sesquiterpene.
5. The transdermal formulation of claim 4 , wherein the source of the at least one 1,4-dialdehyde sesquiterpene is present in the formulation in an amount of about 1% wt % to about 5 wt %, or about 2 wt % to about 4 wt %, of the total formulation.
6. The transdermal formulation of claim 1 , wherein the transdermal formulation comprises chili pepper or cayenne pepper, or an extract of chili pepper or cayenne pepper, as a source of the at least one capsaicinoid.
7. The transdermal formulation of claim 6 , wherein the source of the at least one capsaicinoid is present in the formulation in an amount of about 0.005% wt % to about 0.5 wt %, or about 0.01 wt % to about 0.1 wt %, of the total formulation.
8. The transdermal formulation of claim 1 , wherein the tetrahydropiperine is present in the formulation in an amount of about 0.01% wt % to about 1.0 wt %, or about 0.05 wt % to about 0.5 wt %, of the total formulation.
9. The transdermal formulation of claim 1 , wherein the at least one capsaicinoid comprises capsaicin, and wherein the at least one 1,4-dialdehyde sesquiterpene comprises polygodial.
10. The transdermal formulation of claim 9 , wherein the transdermal formulation comprises:
chili pepper or cayenne pepper, or an extract of chili pepper or cayenne pepper, as a source of capsaicin; and
Tasmannia lanceolata or Tazmanian Mountain Pepper (TMP), or an extract of Tasmannia lanceolata or TMP, as a source of polygodial.
11. The transdermal formulation of claim 10 , wherein the source of polygodial is TMP or an extract thereof, and the source of capsaicin is cayenne pepper or an extract thereof.
12. The transdermal formulation of claim 1 in the form of a cream, gel, liquid suspension, ointment, solution or patch.
13. The transdermal formulation of claim 1 , in the form of a cream.
14. The transdermal formulation of claim 13 , wherein the cream has a viscosity of about 50000 cps to about 500000 cps, or about 85000 cps to about 200000 cps as measured using a Brookfield RVT T4 2 RPM instrument at room temperature.
15. The transdermal formulation of claim 1 , having improved color characteristics.
16. A method for treating inflammation comprising administering an effective amount of one or more of the formulations according to claim 1 to a subject in need thereof.
17. A method for treating a capsaicinoid-responsive condition comprising administering an effective amount of one or more of the formulations of claim 1 to a subject in need thereof.
18. The method of claim 17 , wherein the capsaicinoid-responsive condition is selected from one or more of pain (including painful neuropathies and musculosketal pain), inflammation, itch, psoriasis, pruritis and microbial infections.
19. The method of claim 17 , wherein the formulations provide treatment with a lower amount of irritation or burning sensation compared to other transdermal or topical capsaicinoid formulations.