Formulations for aripiprazole delivery transdermally
Formulations for topical application of aripiprazole are provided. The formulations, when applied topically to the skin of a subject, provide a therapeutic amount of aripiprazole in the blood for a sustained period of time for treatment of conditions responsive to aripiprazole including but not limited to depression, schizophrenia, and bipolar disorder.
1. A transdermal formulation consisting essentially of:
between about 1-12 wt %; aripiprazole;
between about 15-25 wt % dimethyl sulfoxide;
between about 5-40 wt % of a glycol selected from hexylene glycol, propylene glycol, or a mixture thereof;
between about 5-20 wt % glycerol;
between about 0.5-10 wt % lauryl lactate;
between about 0.5-10 wt % lactic acid;
optionally between about 2-15 wt % water or a surfactant; and
a polymeric vehicle,
wherein the formulation does not comprise any selected from N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, isopropyl myristate, diethyl sebacate, medium-chain triglyceride, and propylene carbonate.
2. The formulation of claim 1 , wherein the surfactant is a sorbitan monolaurate.
3. The formulation of claim 1 , wherein the polymeric vehicle is present in an amount between 5-40 wt %.
4. The formulation of claim 3 , wherein the polymeric vehicle comprises a combination of a polyvinylpyrrolidone and a hydroxyalkylcellulose.
5. The formulation of claim 3 , wherein the polymeric vehicle comprises a copolymer of methacrylic acid and methyl methylacrylate monomers.
6. The formulation of claim 4 , wherein the hydroxyalkylcellulose is selected from hydroxymethylcellulose, hydroxyethylcellulose, and hydroxypropylcellulose.
7. A transdermal formulation consisting essentially of:
between about 1-12 wt %; aripiprazole;
between about 5-40 wt % of a glycol selected from hexylene glycol, propylene glycol, or a mixture thereof;
between about 10-25 wt % glycerol;
between about 0.5-10 wt % lauryl lactate;
between about 0.5-10 wt % lactic acid;
optionally, between about 2-15 wt % water or a surfactant; and
between 5-35 wt % of a polymeric vehicle comprising a polyvinylpyrrolidone or a hydroxyalkylcellulose or both,
wherein the formulation does not comprise any selected from N,N-dimethylformamide, N,N-dimethylacetamide, N-methyl-2-pyrrolidone, isopropyl myristate, diethyl sebacate, medium-chain triglyceride, and propylene carbonate.
8. The formulation of claim 7 , wherein the surfactant is a sorbitan monolaurate.
9. The formulation of claim 7 , wherein the hydroxyalkylcellulose is selected from hydroxymethylcellulose, hydroxyethylcellulose, and hydroxypropylcellulose.
10. The formulation of claim 7 , wherein the polyvinylpyrrolidone is selected from polyvinylpyrrolidone homopolymers and polyvinylpyrrolidone copolymers.
11. A method for administering aripiprazole transdermally, comprising: providing a formulation according to claim 1 or 7 with instructions to apply the formulation to skin of a subject in need.
12. A method for treating depression, schizophrenia, or bipolar disorder comprising: providing a formulation according to claim 1 or 7 with instructions to apply the formulation to skin of a subject in need.
13. A transdermal delivery device, comprising: a formulation according to claim 1 or 7 .