A process can be used for preparing nanoparticles containing at least one bio-resorbable polyester. The nanoparticles are in the form of a powder with a Z-Average particle size D, in the range of 3 to 450 nm, and with a polydispersity index PDI in the range of 0.01 to 0.5. The process involves emulsion-solvent extraction or emulsion-solvent evaporation, and application of ultrasonic sound.

Formulations containing pH-sensitive nanoparticles for the enteric delivery of therapeutic agents are provided. The nanoparticles include a pH-sensitive polymer that protects the therapeutic agent against degradation in the stomach and allows it to be released in the small intestine or colon. The nanoparticle formulation is particularly effective at protecting sensitive biotherapeutic agents from degradation when administered orally, and makes it possible to avoid administration of such agents by injection. Also provided are methods for producing the formulations, as well as methods of treating diseases employing the formulations.

The present invention relates to the use of a methacrylate or acrylate modified polysaccharide; or a single-chain polysaccharide methacrylate or acrylate-based nanoparticle, having a surface tension measured by Du Noüy Ring method equal to or lower than 63 mN/m, as oil-in-water emulsion stabilizer; and an oil-in-water emulsion stabilizer composition, and an oil-in-water emulsion containing them. It also relates to processes for their preparation, and their uses.

Formulations containing pH-sensitive nanoparticles for the enteric delivery of therapeutic agents are provided. The nanoparticles include a pH-sensitive polymer that protects the therapeutic agent against degradation in the stomach and allows it to be released in the small intestine or colon. The nanoparticle formulation is particularly effective at protecting sensitive biotherapeutic agents from degradation when administered orally, and makes it possible to avoid administration of such agents by injection. Also provided are methods for producing the formulations, as well as methods of treating diseases employing the formulations.

A process for producing a pharmaceutical formulation comprising the steps of: A) providing particles of a polymer, wherein particles of a pharmaceutical active substance are additionally at least partially embedded in the particles of the polymer; B) heating the particles of the polymer to a predetermined temperature for a predetermined time and C) cooling the particles of the polymer after the predetermined time to a temperature of 18° C. to 24° C., wherein the polymer is at least partially soluble in water and the active substance is at least partially soluble in the polymer.

The particulate pharmaceutical active substance is present in the form of particles having a d.sub.90 value in the particle size distribution of ≤1 μm. The predetermined temperature is within a range from 10 K below the glass transition temperature (determined by DSC in accordance with DIN EN ISO 11357-2 at a heating rate of 10 K/min) of the polymer to the melting temperature of the active substance. The total proportion of the active substance in the polymer is greater than the amount of active substance soluble in the polymer at the predetermined temperature.

The invention further relates to a pharmaceutical formulation comprising a particulate pharmaceutical active substance coated with an at least partially water-soluble polymer, to a process for producing a suspension of a pharmaceutical formulation and to a suspension of a pharmaceutical active substance.

Amphiphilic copolymers and compositions including amphiphilic copolymers. The amphiphilic copolymers include modified maleimide subunits, for example, as illustrated by the structures of Formula I.sup.A and Formula I.sup.B. The compositions form water-soluble complexes upon association with biological material wherein such biological material can include lipids or membrane proteins. Methods for producing, purifying, analyzing, and using the compositions and complexes are provided.

A nanoparticulate composition comprises a gene editing ribonucleoprotein system complexed within a cationic polymer. The cationic polymer may be a Poly-beta amino ester hyperbranched polymer, especially a 4-branching hyperbranched polymer. The gene editing ribonucleoprotein system may be a CRISPR-Cas9 gene editing system configured to excise a mutation or exon in a gene, replace a mutation in a gene, or produce a knock-down or knock-out of a gene, and in particular configured to excise exon 80 of the COL7A1 gene which codes for the collagen VII protein. Data shows that using

A precipitation route to form nanoparticles with a hydrophilic core containing water soluble materials and a hydrophobic shell is described. The process requires a stabilizing polymer composed of more polar and more non-polar regions. These regions can be arranged as a linear block copolymer, or as a comb polymer with a linear or branched polar backbone and non-polar side chains or substituents. Nucleic acids, including DNA and RNA, as well as proteins, peptides, and polysaccharides or combinations can be encapsulated in the nanoparticle core. The encapsulation of nucleic acids can require partially or fully neutralizing the acid with a base to enhance the solubility of the nucleic acid in the process solvent stream. The core or the shell of the resulting nanoparticles can be crosslinked. The nanoparticles may be coated with additional polymer to bring them into water, or processed into microparticles or larger monoliths.

This invention relates to methods of preparing nanotherapeutic compounds and compositions comprising nanotherapeutic compounds. The nanotherapeutic compounds prepared according to the methods provided herein are useful for the treatment of disease, for example, cancer, in a subject in need thereof.

An “inverse” precipitation route to precipitate aqueous soluble species with copolymers as nanoparticles having a hydrophilic, polar core and a less polar shell is described.