Preparation and optimization of rivastigmine-loaded tocopherol succinate-based solid lipid nanoparticles

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Malekpour-Galogahi, Fariba
Hatamian-Zarmi, Ashrafalsadat
Ganji, Fariba
Ebrahimi-Hosseinzadeh, Bahman
Nojoki, Fahimeh
Sahraeian, Razi
Mokhtari-Hosseini, Zahra Beagom
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2018
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Abstract

Rivastigmine hydrogen tartrate (RHT) is a pseudo-irreversible inhibitor of cholinesterase and is used for the treatment of Alzheimer's. However, RHT delivery to the brain is limited by the blood-brain barrier (BBB). The purpose of this study was to improve the brain-targeting delivery of RHT by producing and optimizing rivastigmine hydrogen tartrate-loaded tocopherol succinate-based solid lipid nanoparticles (RHT-SLNs). RHT-SLNs were prepared using the microemulsion technique. The impact of significant variables, such as surfactant concentration and drug/lipid ratio, on the size of RHT-SLNs and their drug loading and encapsulation efficiency was analysed using a five-level central composite design (CCD). The minimum size of particles and the maximum efficiency of loading and encapsulation were defined according to models derived from a statistical analysis performed under optimal predicted conditions. The experimental results of optimized RHT-SLNs showed an appropriate particle size of 15.6 nm, 72.4% drug encapsulation efficiency and 6.8% loading efficiency, which revealed a good correlation between the experimental and predicted values. Furthermore, in vitro release studies showed a sustained release of RHT from RHT-SLNs.

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Journal of Liposome Research

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28

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3

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Pharmacology and pharmaceutical sciences

Science & Technology

Life Sciences & Biomedicine

Biochemistry & Molecular Biology

Pharmacology & Pharmacy

Rivastigmine

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Malekpour-Galogahi, F; Hatamian-Zarmi, A; Ganji, F; Ebrahimi-Hosseinzadeh, B; Nojoki, F; Sahraeian, R; Mokhtari-Hosseini, ZB, Preparation and optimization of rivastigmine-loaded tocopherol succinate-based solid lipid nanoparticles, Journal of Liposome Research, 2018, 28 (3), pp. 226-235

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