Zhou Shuwen, Zheng Xinmeng, Chen Jun, Xu Yiyang, Du Xuancheng, Wang Cheng, Cui Pengfei, Qiu Lin, Jiang Pengju, Ni Xinye, Wang Jianhao
The Affiliated Changzhou No.2 People's Hospital of Nanjing Medical University, Changzhou, 213003, P. R. China.
School of Pharmacy, Changzhou University, Changzhou, 213164, P. R. China.
J Biomed Nanotechnol. 2022 Feb 1;18(2):571-580. doi: 10.1166/jbn.2022.3253.
Intranasal administration, which can bypass the blood-brain barrier (BBB), is widely recognized as a promising strategy for high-efficiency drug delivery to the brain. Herein, for the purpose of effectively delivering drugs to the brain via intranasal administration, glutathione (GSH)-modified gellan gum (GSH-GG) with ion/temperature dual responsive properties was synthesized and encapsulated on galanthamine hydrobromide (GH)-loaded liposomes (GH-Lipo) for effective GH delivery to the brain (GH-Lipo@GSH-GG). Our results demonstrated that GSH-GG greatly decreased the gelation temperature of GG from 44.0 °C to 22.1 °C without compromising its ion responsiveness. Moreover, GSH-GG had a good protection ability for GH-loaded liposomes without affecting its drug release. Most importantly, the finally obtained GH-Lipo@GSHGG showed acceptable targeted delivery of GH to the brain upon in vivo administration. Therefore, this formulation can be employed as a potential delivery system in nasal-to-brain delivery.
鼻内给药可绕过血脑屏障（BBB），被广泛认为是一种向大脑高效给药的有前景的策略。在此，为了通过鼻内给药有效地将药物递送至大脑，合成了具有离子/温度双重响应特性的谷胱甘肽（GSH）修饰的结冷胶（GSH-GG），并将其包裹在载有氢溴酸加兰他敏（GH）的脂质体（GH-Lipo）上，以实现将GH有效递送至大脑（GH-Lipo@GSH-GG）。我们的结果表明，GSH-GG在不影响其离子响应性的情况下，将GG的胶凝温度从44.0℃大幅降低至22.1℃。此外，GSH-GG对载有GH的脂质体具有良好的保护能力，且不影响其药物释放。最重要的是，最终获得的GH-Lipo@GSHGG在体内给药后显示出可接受的GH向大脑的靶向递送。因此，该制剂可作为鼻脑递送的潜在递送系统。
