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Mucoadhesive and mucus-penetrating interpolyelectrolyte complexes for nose-to-brain drug delivery
Nanomedicine: Nanotechnology, Biology and Medicine ( IF 4.2 ) Pub Date : 2021-06-27 , DOI: 10.1016/j.nano.2021.102432
Natalia N Porfiryeva 1 , Irina I Semina 2 , Ilgiz A Salakhov 1 , Rouslan I Moustafine 3 , Vitaliy V Khutoryanskiy 4
Affiliation  

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.



中文翻译:

用于鼻-脑给药的黏膜粘附和黏液穿透性聚电解质间复合物

鼻腔给药提供了将药物输送到大脑的可能性。在目前的工作中,鼻给药系统的设计基于阳离子 Eudragit® EPO (EPO) 和阴离子 Eudragit® L100-55 (L100-55) 甲基丙烯酸酯共聚物。使用这些聚合物之间的聚电解质间络合制备两种类型的纳米载体。第一种纳米粒子是通过在未改性的 EPO 和 L100-55 之间形成聚电解质间复合物来制备的。第二种类型的纳米颗粒是通过聚乙二醇化 L100-55 和 EPO 之间的络合形成的。为此目的,聚乙二醇化的 L100-55 通过 L100-55 与 O-(2-氨基乙基) 聚乙二醇的化学共轭合成。这些纳米颗粒的粘膜粘附特性​​在体外进行了评估使用绵羊鼻粘膜。基于 EPO 和 L100-55 的纳米颗粒对鼻粘膜表现出粘膜粘附特性​​,而聚乙二醇化纳米颗粒是非粘膜粘附性的,因此表现出粘液穿透特性。两种类型的纳米颗粒都用于配制氟哌啶醇,并在大鼠体内评估了它们将药物输送到大脑的能力。

更新日期:2021-07-22
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