Topical composition and delivery system and its use
The described invention provides a topical delivery system comprising a pharmaceutical composition for application directly to a skin of a subject in need thereof comprising (a) an effective therapeutic amount of an active therapeutic agent; (b) chemical drivers comprising an amino benzoate local anesthetic, ethoxydiglycol and methylsulfonylmethane (MSM) that in combination are effective to synergistically deliver the therapeutic agent; and (c) a depot component for keeping the pharmaceutical composition in the skin. Methods for delivering an active therapeutic agent into skin, for keeping it in the skin, for reducing systemic side effects attributable to entry of the active agent into the blood stream, and a method for treating a condition, disease or disorder of skin topically also are described in accordance with the embodiments of the described invention.
1. A method of delivering a pharmaceutical composition topically that is effective to reduce systemic side effects of an amino benzoate local anesthetic agent comprising
applying topically directly to skin of a subject over an area of pain a therapeutic amount of the pharmaceutical composition comprising:
(i) the amino benzoate local anesthetic agent in an amount of 1-20% w/w,
(ii) a penetration enhancer comprising a penetration enhancing amount of an ethoxydiglycol component in an amount of 0.10-5% w/w and a methylsulfonylmethane (MSM) component in an amount of 1-10% w/w; and
(iii) a liposome depot component wherein the pharmaceutical composition is effective:
(a) to deeply penetrate the skin of the subject;
(b) to remain in the skin and block nerve signals affecting sensation of pain, and
(c) to provide pain relief.
2. The method according to claim 1 , wherein the amount of the amino benzoate local anesthetic agent in the bloodstream is less than a therapeutic amount.
3. The method according to claim 1 , wherein the liposome depot component is effective to facilitate controlled or delayed type release of the amino benzoate local anesthetic agent.
4. The method according to claim 1 , wherein the liposome depot component is a polymer.
5. The method according to claim 1 , wherein the liposome comprises a phosphatidyl choline, cholesterol and at least one anionic or cationic phospholipid.
6. The method according to claim 5 , wherein the liposome comprises a pharmaceutically acceptable salt of the amino benzoate local anesthetic agent.
7. The method according to claim 1 , wherein the liposome depot component comprises a polymer.
8. The method according to claim 1 , wherein the liposome depot component is a polymersome.
9. The method of claim 1 , comprising the amino benzoate local anesthetic agent in an amount of 4% w/w, a penetration enhancer comprising a penetration enhancing amount of an ethoxydiglycol component in an amount of 1% w/w, and a methylsulfonylmethane (MSM) component in an amount of 3% w/w.