A61K9/5138

UNIVERSAL ORAL DELIVERY DEVICE OF INTACT THERAPEUTIC POLYPEPTIDES WITH HIGH BIOAVAILABILITY
20230044668 · 2023-02-09 · ·

The invention is related to the fully effective gastro-protected universal oral delivery device of gastro-protected nanoparticles for the transport of intact biologically active polypeptides into the circulatory system. This universal oral delivery device is made of gastro-protected nanoparticles that transport intact therapeutic polypeptides through the gastrointestinal system and it successfully performs the paracellular transepithelial passage of all therapeutic polypeptides from the intestinal lumen into the circulatory system, fully preserving the integrity and biological activity of those therapeutic polypeptides.

Therapeutic compounds, formulations, and uses thereof

Provided herein are compositions, formulations, and (e.g., oral) dosage forms comprising a compound of Formula (I). In specific instances, such compositions comprise an emulsifier, a solubilizer, a polyethylene glycol, a surfactant, and an antioxidant. In some instances, such compositions are useful for the treatment of fibrosis, cancer, and/or chronic inflammation.

Protein-polymer hybrid biomaterials

For applications in drug delivery, “smart” materials have been designed to respond to conditions within microenvironments of tissues or cells. The present invention features stimuli-responsive cross-linked hydrogels that respond to specific metabolites of disease. For example, protein-polymer materials of the present invention are configured to release their drug cargo upon encountering the higher lactate concentrations within tumor microenvironments.

COMPLEXES OF CELECOXIB AND ITS SALTS AND DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Disclosed herein are stable complexes with controlled particle size, increased apparent solubility and increased dissolution rate comprising as active compound Celecoxib, its salts, or derivatives thereof, which is useful in the treatment of osteoarthritis, rheumatoid arthritis, juvenile rheumatoid arthritis, ankylosing spondylitis, acute pain especially in cancer related acute pain, primary dysmenorrhea. More specifically, the complexes possess instantaneous redispersibility, increased apparent solubility and permeability that provide faster onset of action for acute pain relief and lower GI related side effects. Further disclosed are methods of formulating and manufacturing the complexes described herein, pharmaceutical compositions, and uses and methods of treatment.

BRUSH AMPHIPHILIC BLOCK COPOLYMERS, AND SELF-ASSEMBLED NANOPARTICLES THEREFROM
20180009924 · 2018-01-11 ·

The present application relates to brush amphiphilic block copolymers comprising at least one block which is hydrophilic and at least another block which is hydrophobic. The block copolymers can be used to prepare nanoparticles for biomedical applications including delivery of pharmaceuticals and other bioactive agents

Pharmaceutical compositions

The present invention relates to the field of methods for providing pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to compositions comprising stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions and in therapy.

Bi2O3 NANOPARTICLES PREPARED BY THE TOP-DOWN ULTRASONICATION ROUTE AS A BROAD-SPECTRUM ANTIMICROBIAL TO OVERCOME DRUG RESISTANCE IN ANTIBIOTICS

α-Bi.sub.2O.sub.3 NPs exhibit not only potent broad-spectrum antibacterial activity of killing both Gram-negative (MIC=0.75 μg/mL vs. P. aeruginosa) and Gram-positive (MIC=2.5 μg/mL vs. S. aureus) bacteria, but they are also effective against Ag-resistant and carbapenem-resistant bacteria (MICs=1.0 μg/mL and 1.25 μg/mL, respectively), and they are able to sensitize bacteria towards meropenem (mero), acting synergistically and thus allowing for its continued use with smaller therapeutic doses (fractional inhibitory concentration=0.45). Importantly, unlike other technologies that have been considered as effective metal antimicrobials, α-Bi.sub.2O.sub.3 NPs do not contribute to the generation of antimicrobial resistant phenotypes with no resistance observed after 30 passages. The Bi-based materials represent a critical tool against multidrug resistant bacteria.

MODIFIED GUANIDINE-CONTAINING POLYMERS FOR BIOLOGIC DELIVERY

The subject invention provides materials and methods for intracellular deliver of molecules and/or therapeutic agents. The subject invention also provides methods for synthesizing polymeric systems and nanomaterials that enhance or assist the passage of molecules and/or therapeutic agents across biological membranes. The compound, polymer or nanoparticle of the subject invention comprises a modified guanidine moiety in a plurality of repeating units of a polymer or on the surface of a nanoparticle where the guanidine moiety comprises, for example, a carbamoyl or thiourea modification. The polymer or nanoparticle can be used in a cancer treatment formulation.

NANOPARTICLES CONTAINING COMPLEXES OF NUCLEIC ACIDS AND CATIONIC COPOLYMERS, PROCESS FOR PREPARING THEM AND THEIR USE FOR GENE TRANSFER IN CELLS
20230218536 · 2023-07-13 ·

##STR00001##

The invention relates to nanoparticles containing complexes constituted by nucleic acids and cationic copolymers containing the recurring structural units of formulae (Ia) and (Ib) wherein R.sup.1 and R.sup.6 independently represent hydrogen, alkyl or —COOR.sup.9, R.sup.2 and R.sup.7 independently represent hydrogen or alkyl, R.sup.3 is selected from the group consisting of —O—R.sup.10—, —COO—R.sup.10, —CONH—R.sup.10- or —R.sup.10—, R.sup.4 represents hydrogen, alkyl, cycloalkyl, aryl, aralkyl or alkylaryl, R.sup.5 represents hydrogen, alkyl, cycloalkyl, aryl, aralkyl, alkylaryl or —(alkylene-NH—).sub.malkyl, or R.sup.4 and R.sup.5 together with the nitrogen atom they have in common form a heterocyclic ring, R.sup.8 is selected from the group consisting of —O—R.sup.11, —COO—R.sup.11, —CONH—R.sup.11 or —R.sup.11, R.sup.9 and R.sup.11 independently represent hydrogen or a monovalent organic residue, R.sup.10 represents a bivalent organic residue, and m is an integer from 1 to 5, with the proviso that the nanoparticles have a diameter (z-average) of less than or equal to 900 nm as determined by dynamic light scattering and that the molar ratio of nitrogen atoms in the copolymer to the phosphate groups in the nucleic acid ranges between 1 and 200. The nanoparticles according to the invention allow the transfer of nucleic acids into cells with great efficiency.

Process for encapsulating soluble biologics, therapeutics, and imaging agents

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.