姜黄素包裹的壳聚糖包裹的聚（乳酸-共-乙醇酸）纳米颗粒和姜黄素/羟丙基-β-环糊精包合物作为阿尔茨海默病治疗策略鼻内给药的体外和体内比较,Molecular Pharmaceutics

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姜黄素包裹的壳聚糖包裹的聚（乳酸-共-乙醇酸）纳米颗粒和姜黄素/羟丙基-β-环糊精包合物作为阿尔茨海默病治疗策略鼻内给药的体外和体内比较
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-10-21 , DOI: 10.1021/acs.molpharmaceut.0c00675
Li Zhang _{1,

2} , Shili Yang ₂ , Ling Rong Wong ₂ , Hui Xie ₃ , Paul Chi-Lui Ho _{1,

2}

Affiliation

姜黄素 (CUR) 具有抗氧化和抗炎作用，对阿尔茨海默病 (AD) 有益。然而，CUR 的溶解性差和高度不稳定性极大地影响了其应用。在本研究中，CUR 包裹的壳聚糖包裹的聚（乳酸-共-乙醇酸）纳米粒子（CUR-CS-PLGA-NPs）和羟丙基-β-环糊精包裹的 CUR 复合物（CUR/HP-β-CD 包合物）通过鼻内给药进行开发和比较。体外研究表明，CUR/HP-β-CD 包合物中的 CUR 在生理条件下在 72 小时内保持稳定，剩余 95.41±0.01%，高于 CUR-CS-PLGA-NPs 中的 49.66±3.91%。同时，在 SH-SY5Y 细胞中，CUR/HP-β-CD 包合物显示出比 CUR-CS-PLGA-NPs 更高的 CUR 细胞摄取水平。两种配方都可以降低 CUR 的细胞毒性，并显示出相当的抗氧化作用。两种制剂在 BV-2 细胞中以 20 μM CUR 显示出抗炎作用，与阳性对照相比，TNF-α 和 IL-6 水平分别降低至约 70% 和 40%。体内药代动力学研究表明，鼻内给药后，CUR/HP-β-CD包合物组CUR在血浆和脑中的AUC值分别比CUR-CS-PLGA-NP组高2.57倍和1.12倍组分别以 2 mg/kg 的相同剂量给药。总之，CUR/HP-β-CD 包合物作为 CUR 鼻内递送用于 AD 的载体显示出比 CUR-CS-PLGA-NP 更好的特性。

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In Vitro and In Vivo Comparison of Curcumin-Encapsulated Chitosan-Coated Poly(lactic-co-glycolic acid) Nanoparticles and Curcumin/Hydroxypropyl-β-Cyclodextrin Inclusion Complexes Administered Intranasally as Therapeutic Strategies for Alzheimer’s Disease

Curcumin (CUR) has antioxidant and anti-inflammatory effects that are beneficial to Alzheimer’s disease (AD). However, the poor solubility and high instability of CUR compromise its application greatly. In this study, CUR-encapsulated chitosan-coated poly (lactic-co-glycolic acid) nanoparticles (CUR-CS-PLGA-NPs) and hydroxypropyl-β-cyclodextrin-encapsulated CUR complexes (CUR/HP-β-CD inclusion complexes) were developed and compared through intranasal administration. In vitro studies indicated that CUR in CUR/HP-β-CD inclusion complexes was stable under physiological conditions over 72 h with 95.41 ± 0.01% remaining, which was higher than 49.66 ± 3.91% remaining in CUR-CS-PLGA-NPs. Meanwhile, CUR/HP-β-CD inclusion complexes showed a higher cellular uptake level of CUR than CUR-CS-PLGA-NPs in SH-SY5Y cells. Both formulations could reduce CUR’s cellular cytotoxicity and showed a comparable antioxidant effect. Both formulations displayed the anti-inflammatory effect at 20 μM CUR in BV-2 cells, which decreased TNF-α and IL-6 levels to approximately 70 and 40%, respectively, when compared to the positive control, respectively. In vivo pharmacokinetic studies indicated that after intranasal administration, the AUC values of CUR in the plasma and brain of the CUR/HP-β-CD inclusion complex group were 2.57-fold and 1.12-fold higher than those in the CUR-CS-PLGA-NP group at the same dose of 2 mg/kg, respectively. In conclusion, CUR/HP-β-CD inclusion complexes displayed better properties than CUR-CS-PLGA-NPs as a carrier for intranasal delivery of CUR for application in AD.

更新日期：2020-11-02

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