Novosom Ag

Marina Biotech, Inc.

Other

Biontech Delivery Technologies Gmbh

Pronai Therapeutics, Inc.

Novosom Verwaltungs Gmbh

Steffen Panzner

Capsulution Pharma Ag

Lipocalyx Gmbh

Gerold Endert

Frank Essler

Silke Lutz

Evgenios Siepi

Cornelia Panzner

Yvonne Kerwitz

Christian Reinsch

Stefan Fankhänel

Una Rauchhaus

Volkmar Wendisch

Christina Dreher

Claudia Müller

Stefan Fankhaenel

Anja Behrens

Neal Goodwin

Natalie Herzog

Wendi Rodrigueza

Nasr El-Mokdad

The invention concerns lipid assemblies, liposomes having an outer surface comprising a mixture of anionic and cationic moieties; wherein at least a portion of the cationic moieties are imino moieties that are essentially charged under physiological conditions, and their use for serum resistant transfection of cells.

Amphoteric liposomes comprising imino lipids

The invention proves an oligonucleotide comprising one or more carboxylated 2'-amino-LNA nucleotide units. The invention also provides a method of transfecting cells with the oligonucleotide, a method of treating a human or animal by therapy using the oligonucleotide, and a pharmaceutical composition comprising the oligonucleotide.

Carboxylated 2'-amino-LNA nucleotides and oligonucleotides comprising the same

Imino compounds for amphoteric liposomes and uses thereof

A serum-stable mixture of lipids capable of encapsulating an active agent to form a liposome, said mixture comprising phosphatidylcholine and phosphatidylethanolamine in a ratio in the range of about 0.5 to about 8. The mixture may also include pH sensitive anionic and cationic amphiphiles, such that the mixture is amphoteric, being negatively charged or neutral at pH 7.4 and positively charged at pH 4. Amphoteric liposomes comprising such a mixture may be used for encapsulating nucleic acid therapeutics, such as oligonucleotides and DNA plasmids. The drug/lipid ratio may be adjusted to target the liposomes to particular organs or other sites in the body.

Amphoteric liposomes

The invention provides polyamine derivatives, a use of the polyamine derivatives for the transfection of polyanions into cells, and a method of transfecting cells with a polyanion, comprising mixing said polyanion with a polyamine derivative e.g. in a buffer and treating said cells with the mixture obtained in the previous step.

Carboxylated polyamine derivatives as transfection reagents

The invention provides hydroxylated polyamine derivatives, their use for the transfection of polyanions into cells, and a method of transfecting cells with a polyanion, comprising mixing said polyanion with said hydroxylated polyamine derivative in a buffer and treating said cells with the mixture obtained in the previous step.

Hydroxylated polyamine derivatives as transfection reagents

The invention suggests amphoteric lipids wherein one or more amphoteric groups having an isoelectric point between 4 and 9 are substituted on a membranous or membrane-forming amphiphilic substance, as well as liposomes containing such compounds.

Components for producing amphoteric liposomes

An amphoteric liposome composed of a mixture of lipids, said mixture comprising a cationic amphiphile, an anionic amphiphile and optionally one or more neutral amphiphiles, at least one of said cationic and anionic amphiphiles being chargeable and the respective amounts of said cationic and anionic amphiphiles being selected such there is a stoichiometric excess of positively charged cationic amphiphile at a first lower pH, a stoichiometric excess of negatively charged anionic amphiphile at a second higher pH and said mixture has an isoelectric point intermediate said first and second pHs; characterised in that said positively charged cationic and negatively charged anionic amphiphiles are adapted to form a lipid salt with one another at said isoelectric point. Also disclosed are methods of predicting the fusogenicity of an amphoteric liposome at a given pH, formulating an amphoteric liposome and loading an amphoteric liposome with a cargo moiety.

Amphoteric liposomes, a method of formulating an amphoteric liposome and a method of loading an amphoteric liposome

This invention provides pH-responsive zwitterionic nucleotides and nucleic acids comprising said nucleotides, wherein said zwitterions are constituted from one or more anionic internucleoside linkages and one or more cationic moieties and said zwitterionic nucleotides further comprise either one or more hydrophobic moieties or one or more TEE's with the general structure (I) Hydrophobic element-pH-responsive hydrophilic elements (I).

Nucleic acid comprising zwitterionic nucleotides

The invention relates to compositions and methods to inhibit gene expression. In particular, the invention provides DNAi oligonucleotides sequestered by amphoteric liposomes for the treatment of cancer.

Amphoteric liposome formulation

Lipid assemblies, such as liposomes, comprising transfection enhancer elements (TEE's), which are complexed with the lipid assemblies by means of ionic interactions, or lipids incorporating such TEE's are disclosed for enhancing the fusogenicity of the lipid assemblies. The TEE's have the formula:hydrophobic moiety-pH sensitive hydrophilic moiety&#x2003;&#x2003;(II)The pH sensitive hydrophilic moiety of each TEE is a weak acid having a pka of between 2 and 6 or a zwitterionic structure comprising a combination of acidic groups with weak bases having a pKa of between 3 and 8. Lipids incorporating one or more such TEEs have the formula (I):Lipid moiety-[Hydrophobic moiety-pH sensitive hydrophilic moiety]&#x2003;&#x2003;(I).

Lipids and lipid assemblies comprising transfection enhancer elements

The invention suggests a pH-sensitive cationic lipid with a pKvalue between 3.5 and 8, according to the general formulacation-spacer-Y-spacer-X-lipid,wherein Y and X represent linking groups. Furthermore, liposomes are described, which liposomes include said optionally cationic lipids.

pH-sensitive cationic lipids, and liposomes and nanocapsules containing the same

Amphoteric liposomes are proposed, which comprise positive and negative membrane-based or membrane-forming charge carriers as well as the use of these liposomes.

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Halle, Germany

Steffen Panzner