Formulations comprising anionic agents such as nucleic acids within a lipid-containing particle methods of formulating a lipid-containing particle comprising an anionic agent such as a nucleic acid, methods for preparing a lipid-containing particle comprising an anionic agent such as a nucleic acid, methods for therapeutic delivery of an anionic agent to a patient in need thereof, where the anionic agent is formulated in a lipid-containing particle as described herein.

The present invention relates to high-efficiency encapsulation of hydrophilic substances in the hydrophilic space of unilamellar liposomes. High-efficiency encapsulation is achieved by the use of a polyhydric alcohol selected from propylene glycol or glycerine for dissolving the hydrophobic compounds forming the lipid bilayer of the liposomes. The invention provides unilamellar liposomes (UL) as well as a method for preparing same by way of low temperature extrusion. The invention also relates to use of these UL in the manufacturing of a medicament, a cosmetic product, a food additive or a disinfectant.

Disclosed are dendritic anionic lipids which are compounds of Formula (I): wherein R and R.sup.1 are non-polar groups, L is a linking moiety, and Dm is a dendritic moiety of m generations, each as defined herein. These dendritic anionic lipids are useful for delivery and expression of m RNA and encoded protein, e.g., as a component of liposomal delivery vehicle, and accordingly can be useful for treating various diseases, disorders and conditions, such as those associated with deficiency of one or more proteins. ##STR00001##

The present invention provides liposomes loaded with chelating agents, pharmaceutical formulations including these liposomes and methods of making chelating agent liposomes. Because the chelating agents are loaded in the liposome with high efficiencies, the liposomes are of use in treatment of metal ion overload in subjects. The liposomes can also contain essential trace metals to compensate for the off target effect of removal of endogenous non-target trace metals by administration of the chelator. The liposomes can include two or more different chelating agents of different structures and affinities for metal ions.

A method of producing positively charged liposome vesicles for use as carriers of lipophilic molecules. A mixture of hydrogenated phospholipids, a cationic excipient and a lipophilic molecule are dissolved in a solvent to form a composition. The composition is dried to remove the solvent. The dried composition is hydrated to form liposome vesicles and optionally the liposome vesicles are homogenized to form smaller vesicles. The vesicles are useful for delivery lipophilic molecules, such as, but limited to, lutein and zeaxanthin, to ocular tissues using iontophoresis.

Disclosed herein is a lipid having a net charge at physiological pH, and being covalently attached to a lipid moiety. The lipid moiety comprises a hydrocarbon structure having two or more linked hydrocarbon chains, optionally having cis or trans C═C, at least one of said chains being covalently attached to the head group optionally via the linker region. The hydrocarbon chains are bonded to one another at a branch point at an internal carbon of the chain attached to the linker region, which branch point comprises a functional group having an electronegative atom. The hydrocarbon chains each have between 1 and 40 carbon atoms, wherein the hydrocarbon structure in total comprises between 10 and 150 carbon atoms. Advantageously, the hydrocarbon structure may assume a generally flared shape for enhanced delivery of cargo molecules. Further provided are delivery vehicles comprising the lipids.

Disclosed herein are compositions including a plurality of plant messenger packs, (e.g., including a plant extracellular vesicle (EV), or segment, portion, or extract thereof), that are modified to have enhanced cell uptake (e.g., animal plant cell uptake, bacterial cell uptake, or fungal cell uptake), e.g., for use in a variety of agricultural or therapeutic methods.

This disclosure provides a range of tyrosine amino acid lipid compounds and compositions useful for drug delivery, therapeutics, and the diagnosis and treatment of diseases and conditions. The amino acid lipid compounds and compositions can be used for delivery of various agents such as nucleic acid therapeutics to cells, tissues, organs, and subjects.

The present invention provides a cationic lipid represented by the formula (I)

##STR00001##

wherein R.sup.1 and R.sup.2 each represents alkyl having 8 to 24 carbon atoms or the like; R.sup.3 represents a hydrogen atom, alkyl having 1 to 3 carbon atoms, the formula (A)

##STR00002##

wherein R.sup.4 and R.sup.5 each represents a hydrogen atom or the like, and n.sup.3 represents an integer from 2 to 6, or the formula (B)

##STR00003##

wherein R.sup.6 and R.sup.7 each represents a hydrogen atom or the like, and n.sup.4 represents an integer from 1 to 6; n.sup.1 represents an integer from 0 to 4; and n.sup.2 represents an integer from 1 to 4, provided that the case where n.sup.1 is 0 and n.sup.2 is 1 is excluded, and a composition which contains the cationic lipid and a nucleic acid, or the like.

A group of inventions relates to pharmaceutics and refers to a method for preparing a liposomal composition and a pharmacologically active liposomal composition for ophthalmotherapy prepared by this method. The method is implemented by creating a mixture of solutions of latanoprost, egg phosphatidylcholine and cholesterol in organic solvents, vacuum drying thereof, emulsifying in an aqueous medium, and dispersing an emulsion under pressure. According to the invention, a solution of dipalmytoyl phosphatidylglycerol is introduced into the mixture of solutions, wherein latanoprost, egg phosphatidylcholine, and cholesterol are dissolved in ethyl alcohol, while dipalmytoyl phosphatidylglycerol is dissolved in a mixture of ethyl alcohol and chloroform. The emulsifying of the dried mixture is conducted by a lactose solution in a pH 7.1 buffer, while the dispersing of the emulsion is conducted at a stepwise pressure increase from 300 to 800 at followed by a sterilizing filtration and a freeze drying.

The composition prepared by this method is a frozen-dried powder and a formulation thereof comprises:

TABLE-US-00001 Latanoprost 1, Egg phosphatidylcholine 20.0-30.0, Dipalmytoyl  0.6-0.75, phosphatidylglycerol Cholesterol 0.5-0.9, Lactose 40.0-60.0, Water residue the remainder.

The pharmacologically active liposomal composition has a prolonged antihypertensive and neuroprotective action in case of ocular hypertension and glaucoma, and it is suitable for preparation a solution for an instillation use and/or injectable subconjunctival administration.

2 ind.cls., 2 d.cls.