Mucoadhesive and mucus-penetrating interpolyelectrolyte complexes for nose-to-brain drug delivery

Nasal administration offers a possibility of delivering drugs to the brain. In the present work, nasal drug delivery systems were designed based on cationic Eudragit (R) EPO (EPO) and anionic Eudragit (R) L100-55 (L100-55) methacrylate copolymers. Two types of nanocarriers were prepared using interpolyelectrolyte complexation between these polymers. The first type of nanoparticles was prepared by forming interpolyelectrolyte complexes between unmodified EPO and L100-55. The second type of nanoparticles was formed through the complexation between PEGylated L100-55 and EPO. For this purpose, PEGylated L100-55 was synthesized by chemical conjugation of L100-55 with O-(2-aminoethyl)polyethylene glycol. The mucoadhesive properties of these nanoparticles were evaluated ex vivo using sheep nasal mucosa. Nanoparticles based on EPO and L100-55 exhibited mucoadhesive properties towards nasal mucosa, whereas PEGylated nanoparticles were non-mucoadhesive hence displayed mucus-penetrating properties. Both types of nanoparticles were used to formulate haloperidol and their ability to deliver the drug to the brain was evaluated in rats in vivo. (C) 2021 Elsevier Inc. All rights reserved.

Automated summary

Nasal drug delivery systems based on cationic and anionic Eudragit copolymers were designed, resulting in nanoparticles with mucoadhesive or mucus-penetrating properties for delivering haloperidol to the brain. Analysis on sheep nasal mucosa and rats in vivo confirmed the effectiveness of these nanoparticles in drug delivery.