The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as conjugated lipomers or lipomers) containing one or more groups of the formula (iii): ##STR00001##
wherein R.sup.3 and R.sup.4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.

Formulations are described, containing silibinin or other active ingredients incorporated in lipid nanoparticle systems of the SLN and NLC type, and based on calixarenes, possibly mucoadhesive, or in micellar and nanoparticle systems based on amphiphilic inulin copolymers for use in the treatment of neurodegenerative ocular diseases. The versatility of the calixarene compound is also described, capable of charging and releasing active ingredients characterized by low water solubility, easy chemical and enzymatic degradation, low bioavailability, either of natural origin or not, to be used in the treatment of ocular diseases.

The present invention provides a vesicle, a conjugate, a composition comprising the vesicle or the conjugate, for use in delivering a drug to the brain, and a method for administering the same. The composition of the present invention is a composition for administration to a subject according to a dosing regimen, comprising a carrier for drug delivery, wherein the dosing regimen comprises administering the composition to a subject who has been fasted or caused to have hypoglycemia and inducing an increase in blood glucose level in the subject, and the carrier is modified at the outer surface thereof with a GLUT1 ligand.

There is provided a phospholipid composition which is a bilayer or micelle comprising at least one embedded protein-polymer surfactant conjugate comprising an anchor protein, wherein the anchor protein is a cationised protein or an anionised protein, the composition characterised in that the anchor protein is: a) an active enzyme; orb) is a protein which does not comprise a CH.sub.2C(O)NCH.sub.3(CH.sub.2).sub.3NCH.sub.3).sub.2H.sup.+ linker covalently bonded to an amino acid side chain.

The present invention provides a composition that controls pharmacokinetics. Specifically, the present invention provides: a composition for controlling pharmacokinetics, the composition containing a polyvalent cation as an active ingredient; and a method for controlling pharmacokinetics using the polyvalent cation.

Micelle-forming amphiphilic block copolymers for use in targeting cardiac cells (e.g. fibrotic cells) of a subject suffering from heart failure, micelles containing the micelle-forming amphiphilic block copolymers together with a cardioactive agent, and related compositions and methods for treating or preventing heart failure, e.g. heart failure with preserved ejection fraction (HFpEF) also known as diastolic heart failure.

Provided are a method of delivering target materials into extracellular vesicles including exposing the target materials and the extracellular vesicles to extracorporeal shockwaves, a method of preparing target material-introduced extracellular vesicles, extracellular vesicles prepared by the method, drug delivery vehicles including extracellular vesicles, and a method of delivering target materials into cells. The present disclosure exposes extracellular vesicles derived from natural organisms such as animal cells, plant cells, and microorganisms including bacteria and eukaryotic bacteria as well as artificially produced extracellular vesicles to extracorporeal shockwaves extracellularly. Thus, the high-level energy extracorporeal shockwaves can be used to deliver the target material into the extracellular vesicle efficiently. When treating with extracorporeal shockwaves, the ability of target material-introduced extracellular vesicles to incorporate into target cells also increases. According to the method of the present disclosure, the target materials can be delivered into cells with high efficiency, being utilized in various fields.

A method of preparing a nanoparticle pharmaceutical delivery system. A nanoparticle pharmaceutical delivery system. A method of preparing a targeted nanoparticle pharmaceutical delivery system. A targeted nanoparticle pharmaceutical delivery system.

The present invention provides a peptide of a length from 10 to 50 amino acid residues, which comprises the amino acid sequence Xaa.sub.1KXaa.sub.2WXaa.sub.3Xaa.sub.4Xaa.sub.5Xaa.sub.6Xaa.sub.7W (SEQ ID NO: 1), wherein Xaa.sub.1, Xaa.sub.2 Xaa.sub.3, Xaa.sub.4 Xaa.sub.5, Xaa.sub.6 and Xaa.sub.7 are each independently any amino acid, in particular, which comprises the amino acid sequence LKXaa.sub.1WXaa.sub.2Xaa.sub.3GAIW (SEQ ID NO: 19), wherein Xaa.sub.1, Xaa.sub.2, and Xaa.sub.3, are each independently any amino acid. The invention also provides a conjugate comprising the peptide, a pharmaceutical composition comprising the conjugate, a method for delivering a cargo into a cell, a nucleic acid molecule encoding the peptide, and a host cell comprising said nucleic acid molecule.

A method of preparing a nanoparticle pharmaceutical delivery system. A nanoparticle pharmaceutical delivery system. A method of preparing a targeted nanoparticle pharmaceutical delivery system. A targeted nanoparticle pharmaceutical delivery system.