Calcium Carbonate-Based Mucoadhesive Microcontainers for Intranasal Delivery of Drugs Bypassing the Blood–Brain Barrier

There is an opinion in the medical associations that intranasal administration of medicine allows direct olfactory transfer of drugs into the central nervous system bypassing the blood–brain barrier. This approach could be a valuable solution to the problem of cerebral pathology treatment. We propose a new system of microcontainers for the delivery of an active component to the brain by intranasal administration. The microcontainers were fabricated on the base of porous calcium carbonate particles modified with mucoadhesive biocompatible polymer or polymer/surfactant coating. Loperamide was encapsulated in the proposed microcontainers as a model drug, which cannot pass the blood–brain barrier. The efficiency of microcontainers loaded with the anesthetic loperamide has been assessed by the formalin test in rats in vivo. The results of the in vivo experiments demonstrate decrease in the pain sensitivity after intranasal administration of proposed system, and benefit of mucoadhesive biocompatible coating aiming to improve the anesthetic effect. © 2016, Springer Science+Business Media New York.