Polysorbate-coated mesoporous silica nanoparticles as an efficient carrier for improved rivastigmine brain delivery

被引:25
作者
Basharzad, Samaneh Fateh [1 ]
Hamidi, Mehrdad [1 ,2 ]
Maleki, Aziz [1 ,2 ,3 ]
Karami, Zahra [1 ,2 ]
Mohamadpour, Hamed [1 ]
Zanjani, Mohammad Reza Saghatchi [4 ]
机构
[1] Zanjan Univ Med Sci, Zanjan Pharmaceut Nanotechnol Res Ctr ZPNRC, Sch Pharm, Dept Pharmaceut Nanotechnol, Zanjan 4513956184, Iran
[2] Zanjan Univ Med Sci, Fac Pharm, Dept Pharmacol & Toxicol, Zanjan 4513956184, Iran
[3] Shahid Beheshti Univ Med Sci, Canc Res Ctr, Tehran 1989934148, Iran
[4] Islamic Azad Univ, Dept Clin Sci, Tabriz Branch, Tabriz, Iran
关键词
Alzheimer's disease; Central nervous system; Drug delivery; Blood-brain barrier; Mesoporous silica; Pharmacokinetics; DRUG-DELIVERY; IN-VIVO; PHYSICOCHEMICAL PROPERTIES; TARGETED DELIVERY; PARTICLE-SIZE; BARRIER; TRANSPORT; PHARMACODYNAMICS; PEPTIDE; ACETYLCHOLINESTERASE;
D O I
10.1016/j.brainres.2022.147786
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
Targeted delivery of neurological therapeutic to the brain has been attracting more and more attention to the treatment of central nervous system (CNS) diseases. Nonetheless, the main obstacle in this road map is the existence of a blood-brain barrier (BBB) which limits the penetration efficiency of most CNS drugs into the brain parenchyma. This present investigation describes a facile synthetic strategy to prepare a highly biocompatible calcium-doped mesoporous silica nanoparticles (MSNs) functionalized by polysorbate-80 (PS) as targeting ligand to deliver rivastigmine (RV) into the brain via crossing the BBB. The developed nanosystem was characterized by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), transmission electron microscopy (TEM), Zeta potential, and N-2-adsorption-desorption analysis. In vitro hemolysis studies were carried out to confirm the biocompatibility of the nanocarriers. Our in vivo studies in an animal model of rats showed that the RV-loaded nanosystem was able to enhance the brain-to-plasma concentration ratio, brain uptake clearance, and plasma elimination half-life of the drug compared to the free one drug following intravenous (IV) administration. The results revealed that functionalization of MSNs by PS is crucial to deliver RV into the brain, suggesting PS-functionalized MSNs could be an effective carrier to deliver RV to the brain while overcoming BBB.
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页数:12
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