The invention relates to conjugates in which a sterol is functionalized by an ether bond with a water-soluble polymer to which a guiding ligand is bound. These conjugates improve the physico-chemical and delivery properties of their carrying vesicles, making these more stable, homogeneous and effective. A method for their preparation, a pharmaceutical composition containing said liposomes, and their therapeutic use are described as well.

Disclosed herein are compositions and methods for inhibiting viral entry.

In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.

The invention provides certain nucleic acids (e.g., double stranded siRNA molecules), as well as conjugates that comprise a targeting moiety, a double stranded siRNA, and optional linking groups. Certain embodiments also provide synthetic methods useful for preparing the conjugates. The conjugates are useful to target therapeutic double stranded siRNA to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D).

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 present disclosure relates to chemical moieties which, when bonded to pharmacophores, cause the pharmacophores to undergo first pass metabolism. By undergoing first pass metabolism, a pharmacophore may be made less bioavailable. Such compounds and related pharmaceutical compositions may be used for targeted treatment of diabetic and non-diabetic gastrointestinal disorders, with minimal systemic circulation beyond the gastrointestinal tract.

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.

A conjugate of oligonucleotides and bile acid derivatives having the structure (I), (II) or (III), pharmaceutical compositions thereof, and uses thereof are described.

##STR00001##

Provided are an oral delivery composition including oxaliplatin, a water-soluble anticancer agent, and a preparation method thereof, including forming an ionic complex with a bile acid derivative, which is an oral absorption promoter, and oxaliplatin, and incorporating it into the inner aqueous phase of a water-in-oil-in-water (w/o/w) multiple nanoemulsions, thereby obtaining the oral delivery composition with improved oral bioavailability of oxaliplatin, a water-soluble anticancer agent, avoiding the inconvenience and problems of injection, improving patient compliance, and reducing medical costs.

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.