Liposomal compositions and methods of use thereof for improved stability, bioavailability and sustained release
The embodiments disclosed herein relate to a liposomal composition for sustained release of an active ingredient. In various implementations, the liposomal composition may have a first liposomal core of Phosphatidylcholine (PC), phosphatidylethanolamine (PE), or phosphatidylserine (PS) and the active ingredient dispersed within the first liposomal core. A second core may surround the first liposomal core, with the second core optionally containing one or more polypeptide and a polysaccharide.
1 . A liposomal composition for sustained release of an active comprising:
a) a first liposomal core comprising Phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidylserine (PS) and the active dispersed within the first liposomal core; and
b) a second core surrounding the first liposomal core, the second core comprising one or more polypeptide and at least one polysaccharide.
2 . The liposomal composition of claim 1 , wherein the amount of PC in the first liposomal core is at least about 50 wt %.
3 . The liposomal composition of claim 2 , wherein the amount of PE in the first liposomal core is from about 5-8 wt %.
4 . The liposomal composition of claim 3 , wherein the amount of PS in the first liposomal core is from about 8-10 wt %.
5 . The liposomal composition of claim 1 , wherein the first liposomal core has a phase transition temperature of at least about 37° C.
6 . The liposomal composition of claim 1 , wherein the second core polypeptide comprises pea protein hydrolysate and/or brown rice protein.
7 . The liposomal composition of claim 6 , wherein the second core polypeptide comprises at least about 10 wt % dipeptides and tripeptides.
8 . The liposomal composition of claim 1 , wherein the second core polysaccharide comprises sodium hyaluronate, gum Arabic, sodium alginate and/or trehalose.
9 . The liposomal composition of claim 8 , wherein the second core polysaccharide has a positive charge.
10 . The liposomal composition of claim 8 , wherein the second core polysaccharide has a negative charge.
11 . The liposomal composition of claim 1 , wherein the liposomal composition further comprises a coating of ethyl cellulose.
12 . The liposomal composition of claim 11 , wherein the liposomal composition exhibits an increased in sustained release of the active relative to an otherwise identical liposomal composition without a coating of ethyl cellulose.
13 . The liposomal composition of claim 1 , where in the second liposomal core has a diameter of about 200 nm or less.
14 . The liposomal composition of claim 13 , where in the second liposomal core has a diameter of from about 140-185 nm.
15 . The liposomal composition of claim 14 , where in the second liposomal core has a diameter of about 145 nm.
16 . The liposomal composition of claim 1 , wherein the first and second liposomal cores of the liposomal composition collectively have a zeta potential of from about −30.1 meV to about −61.8 meV.
17 . The liposomal composition of claim 1 , wherein the liposomal composition releases a greater percentage of the active in simulated intestinal fluid (SIF) than in simulated gastric fluid (SGF).
18 . The liposomal composition of claim 1 , wherein the composition has an entrapment efficacy of at least about 80 wt %.
19 . The liposomal composition of claim 1 , wherein the liposomal composition remains stable for at least about 240 days when stored at a temperature of from about 20° C. to about 25° C.