Enteric-coated capsule containing cationic nanoparticles for oral insulin delivery

Inventors

Qian, Yu • ZHANG, Li Juan • WU, Zhi Min • ZHOU, Li Ying • Jiang, Wei • Ling, Li • Luo, Qian • GUO, Xin Dong

Assignees

Nano and Advanced Materials Institute Ltd

Abstract

The invention relates to an enteric-coated capsule containing cationic nanoparticles for oral insulin delivery, in particular to a type of cationic nanoparticle including a polycationic and mucoadhesive polymer and a biodegradable polymer, wherein each of the nanoparticles has positive surface charge and enhanced permeability for paracellular insulin delivery; the enteric-coated capsule further includes a pH-sensitive polymer as the coating. The enteric-coated capsule containing cationic nanoparticles, when being orally administered to a subject, are configured to prevent the acidic degradation of the active substance such as insulin before being released from said cationic nanoparticles to a specific absorption site along the gastrointestinal tract.

Core Innovation

The invention relates to an enteric-coated capsule enclosing a plurality of nanoparticles and a solubilizer, for oral delivery of a bioactive substance. Each nanoparticle comprises a polycationic polymer, a hydrolysis-degradable biodegradable polymer that is a copolymer degradable by hydrolysis following exposure to a physiological environment of the human intestine, and a stabilizer. The nanoparticles further comprise the bioactive substance, and the capsule coating is pH-sensitive to protect the bioactive substance in acidic gastric conditions while dissolving in the small intestine to release the nanoparticles.

The nanoparticles include a polycationic, mucoadhesive component and have positive surface charge, with pH-dependent behavior supporting paracellular insulin absorption. The enteric-coated capsule coating protects against degradation in the stomach and enables pH-triggered release in the intestinal environment. The pH sensitivity and the nanoparticle surface properties are described as supporting mucoadhesion and intestinal absorption behavior.

A solubilizer is included as trehalose, and the composition further incorporates formulation aspects such as stabilizer effects during freeze-drying, including maintaining nanoparticle size and zeta potential. The described system includes material combinations for the polycationic polymer and hydrolysis-degradable copolymer nanoparticles, and it evaluates pH-dependent zeta potential and mucoadhesion behavior, together with pH-dependent in vitro release comparing enteric-coated versus uncoated conditions. In vivo results are described for oral administration in diabetic rats with glucose-lowering outcomes including pharmacological availability parameters such as T_max and C_min.

Claims Coverage

The document provides one independent claim (clm-00001) describing the overall composition, including the enteric-coated capsule, trehalose solubilizer, and nanoparticle components. The remaining provided claim references are dependent refinements that specify additional material selections, structural variants, and quantitative performance parameters.

Across the independent claim and the dependent refinements referenced in the partial content, the inventive concept centers on an enteric-coated capsule that encloses nanoparticles containing a polycationic polymer and a hydrolysis-degradable biodegradable copolymer, together with a bioactive substance, where trehalose at 1.5% w/w or w/v is included as a solubilizer, and dependent claims further narrow specific material selections and performance-related parameters.

Stated Advantages

Documented Applications

No documented applications found