The present invention provides novel, long-acting nanoformulated drugs and targeted drug delivery methods, and uses thereof. In one embodiment, the nanoformulated drug is a retroviral drug. In one embodiment, the nanoformulated composition comprises a nanocarrier with one or more incorporated drugs. In an exemplary embodiment, the drug is efavirenz (EFV). In a further embodiment, the nanocarrier is associated with an agent for targeting microfold cells (M-cells). In a specific embodiment, the targeting agent binds to an M-cell marker known as glycoprotein 2 (GP2). Via this mechanism, the nanodrug is targeted toward GALT.

The present invention relates, in part, to a biocompatible hydrophobic-core carrier comprising a carrier, and a plurality of hydrophobic groups covalently linked to the polymeric carrier. The hydrophobic groups are capable of dissociably linking load molecules such as therapeutic agents. The hydrophobic-core carrier may also comprise protective side chains, orienting molecules, and targeting molecules.

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.

A peptide-polymer conjugate is provided for use in treating malaria infections, and in particular terminal or drug resistant malaria infections. The conjugate is formed from a polymer to which a peptide having activity against a malaria parasite is co-valently attached. The peptide is a cyclic decapeptide from the closely-related group of tyrocidines, tryptocidines, phenycidines and gramicidin S, and the polymer is a hydrophilic and biocompatible polymer with a terminal thiol, such as poly(N-vinylpyrrolidone) (PVP). The polymer chains can be decorated with a hydrophilic targeting ligand that specifically targets an epitope on red blood cells, and in particular red blood cells infected with a plasmodial parasite. A method for synthesising the peptide-polymer conjugate is also provided.

The present invention aims to provide a pharmaceutical composition for transcolonic absorption capable of delivering a physiologically active substance (in particular, a water-soluble physiologically active substance of high molecular weight) having an intracellular site of action into specific tissue cells with high specificity, noninvasively by a means of administration other than injection. The pharmaceutical composition for transcolonic absorption of the present invention is characterized by comprising at least the following (a) and (b); (a) a physiologically active substance having an intracellular site of action and bound with an introduction substance into lipoprotein, and (b) a compound having an action of enhancing large intestinal mucosal epithelial permeability of the physiologically active substance.

The invention provides methods and compositions for delivering a nucleic acid to a cell or the cytosol of the target cell. The method includes contacting the cell with, 1) a membrane-destabilizing polymer; and 2) a nucleic acid conjugate. The nucleic acid conjugate includes a targeting ligand bound to an optional linker and a nucleic acid.

The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.

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 relates to micelle drug carriers and methods of using the micelles to deliver drugs to target cells. The micelles are useful, for example, for carrying and targeting drugs for the treatment of cancer to cancer cells. As one example, the disclosure provides pegylated octadecyl lithocholate micelles that are labeled with a peptide ligand for colorectal neo-plasia and that carry the small molecule mTOR inhibitor rapamycin to colorectal cancer cells.

A nanocomplex, 50 to 1000 nm in size, containing a lipid-like nanoparticle formed of a cationic lipid-based compound and a modified protein formed of a protein and an anionic polymer that includes a plurality of polar groups, the lipid-like nanoparticle and the modified protein being non-covalently bonded to each other. Also disclosed are a method of preparing the above-described nanocomplex and use thereof for treating a medical condition. Further disclosed is a pharmaceutical composition containing a nanocomplex.