The present disclosure generally relates to nanoparticles comprising an endo-lysosomal escape agent, a nucleic acid, and a polymer. Other aspects include methods of making and using such nanoparticles.

A DDS preparation of a platinum complex, which exhibits a superior antitumor effect required as a medicine and reduced side effects, that is, a clinically usable DDS preparation of a platinum complex, which is conjugated to a polymer carrier that is different from conventional carriers, is desired. Provided is a polymer conjugate of a platinum(II) complex, the polymer conjugate including: a block copolymer having a polyethylene glycol structural moiety and a polyaspartic acid moiety or a polyglutamic acid moiety; a sulfoxide derivative introduced into a side-chain carboxyl group of the block copolymer; and a platinum(II) complex coordinate-bonded to a sulfoxide group of the sulfoxide derivative.

A nanocomplex containing a delivery agent and a pharmaceutical agent. The nanocomplex has a particle size of 50 to 1000 nm, the delivery agent binds to the pharmaceutical agent via non-covalent interaction or covalent bonding, and the pharmaceutical agent is a modified peptide or protein formed of a peptide or protein and an added chemical moiety that contains an anionic group, a disulfide group, a hydrophobic group, a pH responsive group, a light responsive group, a reactive oxygen species responsive group, or a combination thereof.

Phosphonium-based ionic conjugates (PBICs) are described. The PBICs each include a cationic binding partner comprising a phosphonium ion and an anionic binding partner comprising a pharmaceutically active compound, or prodrug, or derivative thereof. The conjugate can have at least one enhanced physiochemical, pharmacokinetic and/or therapeutic quality as compared to the pharmaceutically active compound when not provided in a PBIC. The phosphonium-containing cationic binding partner can also serve to enhance delivery of the anionic binding partner to the cytosol and/or the inner mitochondrial space. Methods of preparing the PBICs and using the PBICs to treat disease are also described.

The present invention relates to a methods of preparing active compounds complexed with lipids using aqueous systems that are free of organic solvents, and methods of using the complexes, e.g., in treating a disease in a subject. In some embodiments, the present invention comprises a composition comprising a complex comprising at least one active compound, e.g., a polyene antibiotic, an immunosuppressant agent such as tacrolimus or a taxane or taxane derivative, and one or more lipids. In some embodiments, the present invention provides a method comprising preparing a composition comprising a lipid complex comprising at least one active compound and at least one lipid and administering the composition to a subject. In certain embodiments the subject is a mammal. In certain preferred embodiments, the subject is human.

The present invention provides a salt of an acidic drug and a hydrophobic cation, pharmaceutical compositions comprising such salts and methods of using such salts to treat or prevent a disease or disorder.

This invention relates to pharmaceutical formulations comprising 1-(2-thien-2-yl-2-oxo-ethyl)-3-(methanesulfonyl hydrazine carbonyl) pyridinium, its pharmaceutically acceptable salts, salt-cocrystals and co-crystals, particularly 1-(2-thien-2-yl-2-oxo-ethyl)-3-5(methanesulfonyl hydrazine carbonyl) pyridinium chloride. The formulations are suitable for oral administration and also comprise a permeability enhancer or a suitable base or a mixture thereof. The formulations of this invention are for treating diseases associated with advanced glycation end products.

Methods for encapsulating water-soluble biologic and small molecule active pharmaceutical ingredients (APIs) into nanoparticles by applying nanoprecipitation techniques and ion-pairing the nanoparticles with hydrophobic counterions to produce new API salts that exhibit altered solubilities are presented.

Provided are ligand-conjugates and methods for targeted receptor-mediated cellular uptake of an entity of interest of desired activity and function.

The present disclosure provides method of making a nanoparticle complex wherein the nanoparticle complex comprises a ligand and a metal cation. The disclosure also provides nanoparticle complexes, methods of treating a disease in a patient utilizing the nanoparticle complexes, methods of identifying a disease in a patient utilizing the nanoparticle complexes, and kits involving the nanoparticle complexes.