Lipid encasing amphipathic peptides
Described herein are linear peptides for creation of colloidal particles and micelles for delivery of active agents. The colloidal particles facilitate encapsulation and delivery of hydrophobic and/or poorly water soluble active agents within the particle hydrophobic core. The compositions are suitable for delivery of active agents to plants and animals.
1 . A composition comprising a plurality of colloidal particles suspended in an aqueous carrier, said colloidal particles each comprising a peptide matrix with a hydrophobic core and hydrophilic exterior surface,
wherein the peptide matrix comprises a plurality of linear peptides forming a peptide monolayer, each peptide having a first terminal end and a second terminal end and comprising a hydrophobic segment at the first terminal end directly connected to a hydrophilic segment at the second terminal end, said hydrophilic segment comprising 1 to 7 lysine residues,
wherein said peptide monolayer comprises said plurality of linear peptides arranged such that said hydrophilic segments orient outward in each particle to form said hydrophilic exterior surface, and said hydrophobic segments point towards the hydrophobic core, said hydrophobic core sequestering a non-polar lipid, oil, or non-polar solvent, optionally along with one or more hydrophobic and/or poorly soluble active agents dispersed or distributed therein.
2 . The composition of claim 1 , wherein said hydrophobic segments interact with said non-polar lipid, oil, or non-polar solvent in said hydrophobic core.
3 . The composition of claim 1 , wherein said hydrophobic segment comprises XLIVI (SEQ ID NO: 2), where X is F or V.
4 . The composition of claim 3 , wherein the hydrophobic segment is capped with an acetyl group at the N-terminus.
5 . The composition of claim 1 , wherein said hydrophilic segment comprises KKKKK (SEQ ID NO:3).
6 . The composition of claim 5 , further comprising a cysteine residue adducted to the C-terminal lysine residue.
7 . The composition of claim 1 , wherein said peptide is FLIVIKKKKK (SEQ ID NO: 1, where X is F) or VLIVIKKKKK (SEQ ID NO: 1, where X is V).
8 . The composition of claim 1 , said exterior surface comprising one or more functional moieties extending therefrom.
9 . The composition of claim 1 , wherein the peptide matrix is homogenous.
10 . The composition of claim 1 , wherein said colloidal particles have a maximum surface-to-surface dimension of about 100 nm to about 1000 nm.
11 . The composition of claim 1 , said composition having a polydispersity index of about 2% to about 30%.
12 . The composition of claim 1 , said composition having a shelf life of at least 12 months.
13 . The composition of claim 1 , wherein said active agent is present and selected from the group consisting of fungicides, anticancer agents, insecticides, herbicides, and metabolic inhibitors.
14 . A method of delivering hydrophobic and/or poorly soluble active agents to plants, said method comprising applying a composition according to claim 1 to at least a portion of a plant and/or to the soil where a plant is or will be planted.
15 . The method of claim 14 , wherein said active agent is an insecticide, wherein said composition is applied to at least a portion of a plant and/or to the soil where a plant is or will be planted where it will come into contact with or be ingested by an insect pest.
16 . A method of delivering hydrophobic and/or poorly soluble active agents to insects, said method comprising contacting an insect with a composition according to claim 1 , said composition comprising an insecticide active agent.
17 . The method of claim 16 , wherein contacting the insect comprises applying said composition to at least a portion of a plant and/or to the soil where the plant is or will be planted, such that the composition comes into contact with said insect.