SELF MICRO-EMULSIFYING DRUG DELIVERY SYSTEM WITH INCREASED BIOAVAILABILITY
The invention provides a formulation comprising (a) a drug that is poorly water-soluble, (b) at least one surfactant, and (c) at least one polar lipid, wherein the formulation is substantially free of a polar solvent, as well as methods of preparing the formulation and methods of increasing the bioavailability of a drug using the formulation.
1 . A formulation comprising:
(a) a drug that is poorly water-soluble,
(b) at least one surfactant, and
(c) at least one polar lipid,
wherein the formulation is substantially free of a polar solvent.
2 . The formulation of claim 1 , wherein the at least one surfactant is selected from the group consisting of nonionic, cationic, and anionic surfactants.
3 . The formulation of claim 1 , wherein the at least one polar lipid is selected from the group consisting of mono- and di-glycerides, esters of fatty acids, and polysilane esthers.
4 . The formulation of claim 1 , wherein formulation contains 10-90% surfactants.
5 . The formulation of claim 1 , wherein the formulation contains 10-90% polar lipids.
6 . The formulation of claim 5 , wherein the formulation contains two polar lipids.
7 . The formulation of claim 6 , wherein the at least one surfactant is a polysorbate and the two polar lipids are propylene glycol monocaprylate and propylene glycol dicaprate.
8 . The formulation of claim 7 comprising 10-30% (w/w) propylene glycol monocaprylate, 20-60% (w/w) propylene glycol dicaprate, and 10-30% (w/w) polysorbate.
9 . The formulation of claim 7 comprising 15-20% (w/w) propylene glycol monocaprylate, 35-50% (w/w) propylene glycol dicaprate, and 15-20% (w/w) polysorbate.
10 . The formulation of claim 7 comprising 15-17% (w/w) propylene glycol monocaprylate, 38-42% (w/w) propylene glycol dicaprate, and 15-17% (w/w) polysorbate.
11 . The formulation of claim 7 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, polysorbate 80, and mixtures thereof.
12 . The formulation of claim 8 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, polysorbate 80, and mixtures thereof.
13 . The formulation of claim 9 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, polysorbate 80, and mixtures thereof.
14 . The formulation of claim 10 , wherein the polysorbate is selected from the group consisting of polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 65, polysorbate 80, and mixtures thereof.
15 . The formulation of claim 7 , wherein the polysorbate is polysorbate 80.
16 . The formulation of claim 8 , wherein the polysorbate is polysorbate 80.
17 . The formulation of claim 9 , wherein the polysorbate is polysorbate 80.
18 . The formulation of claim 10 , wherein the polysorbate is polysorbate 80.
19 . A method of increasing the bioavailability of a drug that is poorly water-soluble comprising preparing the formulation of claim 1 , and administering the formulation to a host.
20 . The method of claim 19 , wherein the at least one surfactant is a polysorbate, and wherein the formulation contains two polar lipids that are propylene glycol monocaprylate and propylene glycol dicaprate.