Claims for Patent: 11,540,981

Summary for Patent: 11,540,981

Title:	Nanoemulsion formulation with improved stability and cell penetration
Abstract:	The present invention relates to a nanoemulsion comprising at least one aqueous component and a carrier, wherein the carrier comprises at least one lipophilic component, at least one surfactant and at least one alcohol. The present invention further relates to a composition comprising said nanoemulsion and an active agent. In particular, the composition is present as a gel and the active agent is 5-aminolevulinic acid, a derivative, precursor and/or metabolite thereof. The invention further relates to the preparation of said nanoemulsion and/or composition and to their use for the treatment of dermatological diseases, virus-associated diseases as well as diseases associated with cell proliferation, in particular, tumor diseases and/or psoriasis. The present invention is further directed to the use of said nanoemulsion in cosmetics.
Inventor(s):	Montserrat Foguet Roca
Assignee:	Biofrontera Bioscience GmbH
Application Number:	US12/520,759
Patent Claims:	1. A topical gel composition, the composition comprising: 3-15% by weight 5-aminolevulinic acid hydrochloride based on the total weight of the composition; 1-3% by weight xanthan gum based on the total weight of the composition; 1% to 3% by weight of at least two preservatives, one of the preservatives being propylene glycol based on the total weight of the composition; and a nanoemulsion; wherein the nanoemulsion is an oil-in-water nanoemulsion comprising: 50-98% by weight water based on the total weight of the nanoemulsion; 1-30% by weight surfactant and co-surfactant together wherein the surfactant is soy lecithin and the co-surfactant is polysorbate 80 based on the total weight of the nanoemulsion; 0.1-15% by weight triglycerides based on the total weight of the nanoemulsion; 1-2% by weight isopropyl alcohol based on the total weight of the nanoemulsion; and 5-30 mM phosphate buffer; and wherein the nanoemulsion comprises particles with a mean diameter from 5 nm to 35 nm, with a particle size standard deviation from the mean of about 5 nm, prior to incorporation into the topical gel composition. 2. The topical gel composition of claim 1, wherein the amount of 5-aminolevulinic acid hydrochloride is about 10% w/w based on the total weight of the composition. 3. The topical gel composition of claim 1, wherein the amount of nanoemulsion is from about 10% to about 30% w/w based on the total weight of the composition. 4. The topical gel composition of claim 1, wherein the amount of triglycerides in the nanoemulsion is from about 1% to about 8% w/w based on the total weight of the nanoemulsion. 5. The topical gel composition of claim 1, wherein the soy lecithin has a phosphatidylcholine content of at least 90% by weight based on the total weight of the soy lecithin. 6. A topical gel composition, the composition comprising: about 10% by weight 5-aminolevulinic acid hydrochloride based on the total weight of the composition; 1-3% by weight xanthan gum based on the total weight of the composition; 1% to 3% by weight of at least two preservatives, one of the preservatives being propylene glycol based on the total weight of the composition; and a nanoemulsion; wherein the nanoemulsion is an oil-in-water nanoemulsion comprising: water; 1-30% by weight surfactant and co-surfactant together wherein the surfactant is soy lecithin and the co-surfactant is polysorbate 80 based on the total weight of the nanoemulsion; 0.1-15% by weight triglycerides based on the total weight of the nanoemulsion; 1-2% by weight isopropyl alcohol based on the total weight of the nanoemulsion; and 5-30 mM phosphate buffer; wherein the soy lecithin has a phosphatidylcholine content of at least 90% by weight based on the total weight of the soy lecithin, and wherein the nanoemulsion comprises particles with a mean diameter from 5 nm to 35 nm, with a particle size standard deviation from the mean of about 5 nm, prior to incorporation into the topical gel composition. 7. The topical gel composition of claim 6, wherein the amount of 5-aminolevulinic acid hydrochloride is 10% w/w based on the total weight of the composition. 8. The topical gel composition of claim 6, wherein the amount of nanoemulsion is from about 10% to about 30% w/w based on the total weight of the composition. 9. The topical gel composition of claim 6, wherein the amount of triglycerides in the nanoemulsion is from about 1% to about 8% w/w based on the total weight of the nanoemulsion. 10. A topical gel composition, the composition comprising: about 10% by weight 5-aminolevulinic acid hydrochloride based on the total weight of the composition; 2-3% by weight xanthan gum based on the total weight of the composition; 1% to 3% by weight of at least one preservative wherein the preservative comprises propylene glycol based on the total weight of the composition; and a nanoemulsion; wherein the nanoemulsion is an oil-in-water nanoemulsion comprising: 70-95% by weight water based on the total weight of the nanoemulsion; about 1% by weight surfactant and co-surfactant together wherein the surfactant is soy lecithin and the co-surfactant is polysorbate 80 based on the total weight of the nanoemulsion; 0.1-1% by weight triglycerides based on the total weight of the nanoemulsion; 1-2% by weight isopropyl alcohol based on the total weight of the nanoemulsion; and 5-30 mM phosphate buffer; and wherein the nanoemulsion comprises particles with a mean diameter from 5 nm to 35 nm, with a particle size standard deviation from the mean of about 5 nm, prior to incorporation into the topical gel composition.