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® EPO (EPO) and anionic Eudragit® 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.
In this work, two types of interpolyelectrolyte complexes, based on Eudragit® EPO/L100–55 and Eudragit® EPO/PEGylated L100–55 were prepared as nanoparticles for nasal drug delivery systems. The first type of nanoparticles had superior mucoadhesive properties, whereas the second type demonstrated mucus-penetrating properties. The efficiency of these interpolyelectrolyte complexes with haloperidol was evaluated in vivo in rats.
Natalia N. Porfiryeva, Irina I. Semina, Ilgiz A. Salakhov, Rouslan I. Moustafine, Vitaliy V. Khutoryanskiy,
Mucoadhesive and mucus-penetrating Interpolyelectrolyte complexes for nose-to-brain drug delivery,
Nanomedicine: Nanotechnology, Biology and Medicine, 2021, 102432,
https://doi.org/10.1016/j.nano.2021.102432.