This invention discloses a
chitosan-based
lidocaine formulation for intra-articular use and its preparation method. Belonging to the field of
pharmaceutical formulation technology, the formulation is prepared from
chitosan,
carboxymethyl chitosan,
lidocaine,
chitosan-PNIPAM microspheres, sulfated
trehalose, and excipients. The chitosan-PNIPAM used in this invention exhibits dual temperature and pH response. With temperature changes, PNIPAM possesses both hydrophobic contractile and hydrophilic swelling states, thereby controlling the
lidocaine release rate. Simultaneously, when the pH decreases, chitosan repels PNIPAM, further disintegrating the microspheres to release the
drug, thus achieving targeted analgesia. Sulfated
trehalose, as a
cartilage matrix synthesis
promoter, can activate
intracellular signaling pathways in chondrocytes, promoting the synthesis of
type II collagen and proteoglycans. Simultaneously, the
sulfate groups can form electrostatic complexes with the amino groups of chitosan, enhancing
drug retention. The formulation of this invention can inhibit synovial cells, release cytokines, and synergistically with
carboxymethyl chitosan, increase the inhibition rate of
inflammatory factors by 40%-50%.