Formulation of drugs and vaccines in the form of percutaneous injectable needles

摘要

The invention relates to percutaneous administration of drugs and vaccines in form of solid penetrating needles, “injectable needles”, comprising a polymeric matrix resulting from the polymerization of a polymerizable paste or mixture. The injectable needles are hard enough to penetrate the skin and can be administered percutaneously by simple pusher or injector delivery devices. The manufacturing procedure of the injectable needles allows for the incorporation of the drug as preformulated stable microparticles and incorporation of modifying agents to modulate stiffness, solubility and drug release. Drugs formulated in these injectable needles offer a safe, simple and effective alternative to conventional percutaneous drug delivery systems based on hypodermic needles and syringes that require refrigerated storage and reconstitution prior to administration.

主权项

1. An injectable needle, with a diameter ranging from 0.2 to 2 mm, comprising:
a) 30% to 90% in mass of a solid polymeric matrix continuous phase having a flexural strength over 10 MPa and comprising (i) an addition polymer formed by the polymerization of addition monomers, wherein the addition polymer is selected from the group consisting of polycyanoacrylates, polyacrylates, polymethacrylates, polyvinyls, and any combination thereof, and (ii) a polymeric modifying agent selected from the group consisting of polylactides, polyglycolides, polylactide-co-glycolides or polyvinylpyrrolidones, and any combination thereof, wherein the polymeric matrix is at least partially biodegradable or resorbable, and b) a solid discontinuous water-soluble phase containing a drug preformulated as particles or granules having a diameter between about 0.02 and about 500 microns, the solid discontinuous water-soluble phase in direct contact with the solid polymeric matrix, wherein the injectable needle is formed within a mold by polymerization of the addition monomers in the presence of the polymeric modifying agent to form an interpenetrating polymeric network (IPN) that incorporates the solid discontinuous water-soluble phase.