The present invention provides a preparation method for agomelatine-resorcinol and agomelatine-hydroquinone co-crystals using the solvent-antisolvent method that enables a commercial mass production. The co-crystals prepared by the preparation method of the present invention displays high dissolution rate and high stability in acidic-to-neutral media.

The present disclosure generally relates to nanoparticles comprising a substantially hydrophobic acid, a basic therapeutic agent having a protonatable nitrogen, and a polymer. Other aspects include methods of making and using such nanoparticles.

The present invention provides methods utilizing redox-active surfactants to provide electrochemical control over polymer interactions. In one embodiment, the invention is directed to a transfection method using a redox-active transfection agent that preferentially promotes transfection dependent on the oxidation state of the transfection agent. Accordingly, certain methods according to the invention provide spatial and/or temporal control of cell transfection.

Pharmaceutical formulations containing lipoic acid derivatives are made.

Disclosed are preparations and formulations of high thermodynamic activity lipophilic associations (LA), in which there is pairing between an ionizable pharmaceutical agent and a lipophilic species having ionic characteristics opposite to that of the pharmaceutical agent. Such lipophilic associations manifest high thermodynamic activity, as evidenced by their being predominantly in a liquid phase at room temperature or solvated in a lower-than-water dielectric solvent. Further the pharmaceutical agent being solubilized means that dissolution is not rate limiting to transmucosal absorption. This LA or LA-solvate is formulated into a low dielectric dosage form, from whence, upon the dosage form's hydration, the pharmaceutical agent is driven through the mucosal tissue and into systemic circulation. The invention therefore provides an enhanced transmucosal drug delivery system for ionizable pharmaceutical agents at or near physiological pH.

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.

The present disclosure provides compositions and methods for treating endometrial growth disorders in a patient, such as a human patient, and particularly pre-menopausal female human patients. Exemplary disorders that may be treated using the compounds and therapeutic regimens described herein include adenomyosis and rectovaginal endometriosis. The compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others.

The present invention relates to an ionic complex comprising a cationic polypeptide and an anionic excipient selected from: a PEG-carboxylic acid; a fatty acid having 10 or more carbon atoms; an anionic phospholipid; and a combination thereof. The invention also relates to a pharmaceutical composition comprising the ionic complex of the invention and a pharmaceutically acceptable carrier. The cationic polypeptide of the ionic complex has pharmacological activity and the complex can provide a more desirable pharmacokinetic profile for the cationic polypeptide of the complex as compared to the cationic polypeptide alone following administration. As such, the invention also relates to the use of the ionic complex and pharmaceutical composition comprising same to treat a subject suffering from a disease or disorder that is responsive to the cationic polypeptide of the ionic complex.

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.

An immunostimulatory nanoparticle comprising a biocompatible lipid shell that defines an outer surface of the nanoparticle and a core, which is loaded with a Toll-like Receptor 9 (TLR9) agonist and a nucleic acid inhibitor of V domain Immunoglobulin Suppressor of T cell activation (VISTA), and optionally a plurality of targeting moieties linked to the outer surface, wherein the optional targeting moieties are configured to direct the nanoparticle to tumor-resident myeloid cells in a tumor microenvironment upon administration of the nanoparticle to a subject with cancer.