NANOEMULSION WITHOUT PROPYLENE GLYCOL
The present invention relates to oil in water nanoemulsions which are essentially free of propylene glycol. The nanovesicle formulations are particularly stable in regard to shelf life at different storage temperatures.
1 . A formulation comprising:
(a) a nanoemulsion comprising:
(i) at least one aqueous component;
(ii) a carrier component comprising:
(1) at least one lipophilic component,
(2) at least one surfactant, and
(3) at least one alcohol; and
(b) an active agent comprising a carboxylic acid group, or a derivative, or salt of a carboxylic acid group,
wherein the formulation comprises less than 0.9% w/w of propylene glycol or no propylene glycol.
2 . (canceled)
3 . The formulation of claim 1 , wherein the formulation comprises essentially no propylene glycol.
4 . The formulation of claim 1 , wherein the formulation comprises no propylene glycol.
5 . The formulation of claim 1 , wherein the formulation comprises no, essentially no, less than 1%, or less than or equal to 0.99%, 0.95%, 0.9%, 0.8%, 0.7%, 0.6%, 0.5%, 0.4%, 0.3%, 0.2%, or 0.1% w/w of a non-cyclic polyol having 2 to 5 carbon atoms.
6 . The formulation of claim 1 , wherein the formulation comprises no, essentially no, less than 1%, or less than or equal to 0.99%, 0.95%, 0.9%, 0.8%, 0.7%, 0.6%, 0.5%, 0.4%, 0.3%, 0.2%, or 0.1% w/w of a polyol having 2 to 12 carbon atoms.
7 . The formulation of claim 1 , wherein the at least one alcohol comprises 3, 4 or 5 carbon atoms or 1-propanol, 2-propanol or mixtures thereof.
8 . The formulation of claim 1 , wherein the at least one lipophilic component is selected from triglycerides and mixtures thereof, preferably wherein the at least one lipophilic component is a caprylic and/or a capric triglyceride or a mixture thereof.
9 . The formulation of claim 1 , wherein the at least one surfactant is selected from the group consisting of a phospholipid, a lysophospholipid, a ceramide and/or a mixture thereof, and/or the at least one surfactant is a polyoxyethylene-type surfactant.
10 . The formulation of claim 1 , comprising a total aqueous component in an amount of 50% to 99% (w/w), preferably from 70% to 95% (w/w), more preferably from 75% to 95% (w/w), even more preferably from 80% to 90% (w/w).
11 . The formulation of claim 1 , comprising
(a) the at least one lipophilic component in an amount from 0.1% to 30% (w/w), preferably from 0.25% to 15% (w/w), preferably from 0.25% to 10% (w/w), and more preferably from 2% to 10% (w/w) or 3% to 8% (w/w); and/or
(b) the at least one alcohol in an amount from 0.1% to 10% (w/w), preferably from 0.5% to 5% (w/w), more preferably from 1% to 5% (w/w) and even more preferably from 1% to 3%,
based on the total weight of the nanoemulsion (a).
12 . The formulation of claim 1 , wherein the active agent is a hydrophilic active agent.
13 . The formulation of claim 1 , wherein the active agent is a photosensitizer or a metabolic precursor thereof.
14 . The formulation of claim 1 , wherein the active agent is 5-aminolevulinic acid, a derivative, a precursor, a metabolite, and/or a pharmaceutically acceptable salt thereof.
15 . The formulation of claim 1 , wherein the active agent is present in an amount of from 0.1% to 25% (w/w), based on the total weight of the formulation.
16 . The formulation of claim 1 , wherein the nanoemulsion comprises nanovesicles, wherein the nanovesicles have a size of less than or equal to 500 nm, preferably less than or equal to 200 nm, more preferably in the range of 5 nm to 200 nm when
a) stored for one month, two months, three months, six months, twelve months or at least one month, at least two months, at least three months, at least six months or at least twelve months at 2-25° C.; and/or
b) stored for one month, two months, three months, six months, twelve months, eighteen months, twenty-four months, thirty months, thirty-six months or at least one month, at least two months, at least three months, at least six months or at least twelve months, at least eighteen months, at least twenty-four months, at least thirty months or at least thirty-six months at 2-8° C.
17 . The formulation of claim 1 , characterized by a polydispersity index of less than or equal to 0.4 when
a) stored for one month, two months, three months, six months, twelve months or at least one month, at least two months, at least three months, at least six months or at least twelve months at 2-25° C.; and/or
b) stored for one month, two months, three months, six months, twelve months, eighteen months, twenty-four months, thirty months, thirty-six months or at least one month, at least two months, at least three months, at least six months or at least twelve months, at least eighteen months, at least twenty-four months, at least thirty months or at least thirty-six months at 2-8° C.
18 . The formulation of claim 1 , comprising at least one gelling agent, preferably wherein the gelling agent is selected from the group consisting of poloxamer, xanthan, bentonite, sodium carboxymethylcellulose, hydroxymethyl cellulose, carbomer, hydroxypropyl cellulose, gellan gum, guar gum, pectin, poly(ethylene)oxide, polycarbophil, alginate, tragacanth, povidone, gelatin, and mixtures thereof, more preferably wherein the gelling agent is selected from poloxamer, xanthan and mixtures thereof.
19 . The formulation of claim 1 , which is essentially free of parabens.
20 . The formulation of claim 1 , for use in medicine, in particular for use in a method of treatment and/or prevention of a dermatological disease or condition.
21 . The formulation of claim 7 , wherein the at least one alcohol comprises at least three carbon atoms.
22 . A method of treatment and/or prevention of treating a dermatological disease or condition, wherein the method comprises administration of an effective amount of the formulation of claim 13 to a subject in need thereof.