Nanoemulsion formulation with improved stability and cell penetration
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.
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.