Geodate delivery vehicles

Abstract

The present invention provides geodate delivery vehicles and methods of manufacture and administration. A vehicle including a lipid monolayer disposed about a hydrophobic domain is disclosed, that can be part of an emulsion or other mixture, or further disposed in a lipid strata. A vehicle including a lipid strata disposed about a hydrophobic domain is also disclosed. The vehicle can be incorporated into a variety of medicinal, food preparations, and personal care products to deliver or stabilize a cargo moiety. Packaged delivery vehicles for to later addition of cargo moieties are also contemplated.

Description

RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Application Nos. 60 / 422,989, filed Nov. 1, 2002, 60 / 440,284, filed Jan. 14, 2003 and 60 / 507,361, filed Sep. 29, 2003, which applications are incorporated herein by this reference.BACKGROUND[0002]Liposomes are widely described in the literature, and their structure is well known. Typically, they have an onion-like multilamellar structure comprising a plurality of lipid bilayers spaced one from another by aqueous material. Another type of liposome is a unilamellar liposome, sometime referred to as a vesicle, which is a single lipid bilayer disposed about an aqueous material.[0003]The use of liposomes as carriers or vehicles for drugs is known, and can be achieved by a variety of methods. One method involves casting a film of lipid by evaporation from a solution in an organic solvent, for example chloroform, and then dispersing the film in a suitable aqueous medium. In the case of lipid-soluble biological...

AI Technical Summary

Benefits of technology

[0039]One advantage of the present invention is that cargo moieties can be incorporated into the geodate delivery vehicle at high concentrations. Another advantage of the present invention is the ability to incorporate multiple cargo moieties into one geodate delivery vehicle. Incorporation into a geodate delivery vehicle is also advantageous because it provides the cargo moiety with protection from both the environment, e.g., water and oxygen, and also the stomach. Additionally, the geodate delivery vehicle protects stomach from the cargo moiety. The present invention is advantageous because the formulation of geodate delivery vehicles involves no solvent. The present invention is also advantageous because the resultant geodate delivery vehicles are highly stable, e.g., they can withstand extreme temperature and pressure. Another advantage of the present invention is the ability of the geodate delivery vehicle to mask the taste and / or odor of cargo moieties.

[0040]In order to more clearly and concisely describe the subject matter of the claims, the following definitions are intended to provide guidance as to the meaning of specific terms used in the following written description, examples and appended claims.

[0041]The term “geodate delivery vehicle” refers to a delivery vehicle for a cargo moiety. Geodate delivery vehicles generally include a lipid monolayer disposed about a hydrophobic domain. A “hydrophobic domain” is a composition that is sufficiently hydrophobic in nature to allow formation of a lipid monolayer about its periphery. A hydrophobic domain can itself be one or more cargo moieties, or it can include a hydrophobic composition, such as oil or fat, associated with the cargo moiety, which can be, e.g., a hydrophobic or amphiphilic agent.

[0042]The term “lipid monolayer” generally refers to a lipid-containing layer one molecule thick (as contrasted with lipid bilayers that are two molecules thick). A lipid monolayer can contain further elements, such as cholesterol, steroids, or proteins. In contrast, “liposomes” refer to vesicles defined by lipid bilayers (two molecules thick) in a unilamellar or multilamellar structure.

[0043]In one aspect of the invention, the lipid monolayer includes and / or is composed primarily of negatively charged lipids. When a lipid strata is formed, the multivalent cation forms a cationic bridge between the negatively-charged lipid in the monolayer and the negatively charged lipid in the liposomes. In another embodiment, the lipid monolayer is composed primarily of positively charged lipids. In this case, the head groups interact with negatively charged lipid in the strata. In yet another embodiment, the lipid monolayer is composed primarily of neutral lipids. The coated hydrophobic domain, in this embodiment is trapped within the lipid strata, but does not ionically interact with the strata.

[0044]The term “lipid strata” refers to a structure of alternating cationic and lipid sheet-like layers. A lipid strata can be formed by introducing a cation to an emulsion containing liposomes. The lipid strata not only locks the hydrophobic domain within the geodate lipid monolayer, but can itself be associated with a cargo moiety (e.g., a hydrophilic agent disposed within the lipid strata). In one embodiment, the lipid strata entraps a hydrophobic domain. In another, the lipid strata entraps a hydrophobic domain disposed within a lipid monolayer.

Problems solved by technology

A disadvantage of this method is that the amount of active compound that can be incorporated into the lipid bilayer is limited.

Additionally, the casting method can not be scaled up to accommodate large batches.

Disadvantages of this method include the difficulty of incorporating sufficient quantities of the active compound in the vesicles, and instability and shelf life of the dispersion.

Another disadvantage of this method is the presence of trace amounts of solvent used in the creation of the vesicles.

The loss of the biologically active compound from liposomes into external aqueous medium is another factor which restricts the potential of these preparations as practical dosage forms.

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