Brain Delivery of Curcumin Using Solid Lipid Nanoparticles and Nanostructured Lipid Carriers: Preparation, Optimization, and Pharmacokinetic Evaluation

Curcumin is a multitherapeutic agent with great therapeutic potential in central nervous system (CNS) diseases. In the current study, curcumin was encapsulated in solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for the purpose of increasing brain accumulation. The preparati...

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Published in:ACS chemical neuroscience 2019-01, Vol.10 (1), p.728-739
Main Authors: Sadegh Malvajerd, Soroor, Azadi, Amir, Izadi, Zhila, Kurd, Masoumeh, Dara, Tahereh, Dibaei, Maryam, Sharif Zadeh, Mohammad, Akbari Javar, Hamid, Hamidi, Mehrdad
Format: Article
Language:English
Subjects:
Animals
Biological Availability
Brain - drug effects
Chemistry, Pharmaceutical
Curcumin - chemistry
Curcumin - pharmacology
Drug Carriers - chemistry
Drug Carriers - pharmacology
Drug Delivery Systems - methods
Lipids - chemistry
Male
Nanoparticles - chemistry
Nanostructures - chemistry
Rats, Sprague-Dawley
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Summary:Curcumin is a multitherapeutic agent with great therapeutic potential in central nervous system (CNS) diseases. In the current study, curcumin was encapsulated in solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for the purpose of increasing brain accumulation. The preparation processes have been optimized using experimental design and multiobjective optimization methods. Entrapment efficiency of curcumin in SLNs and NLCs was found to be 82% ± 0.49 and 94% ± 0.74, respectively. The pharmacokinetic studies showed that the amount of curcumin available in the brain was significantly higher in curcumin-loaded NLCs (AUC0‑t = 505.76 ng/g h) compared to free curcumin (AUC0‑t = 0.00 ng/g h) and curcumin-loaded SLNs (AUC0‑t = 116.31 ng/g h) (P < 0.005), after intravenous (IV) administration of 4 mg/kg dose of curcumin in rat. The results of differential scanning calorimetry and X-ray diffraction showed that curcumin has been dispersed as amorphous in the nanocarriers. Scanning electron microscopy images confirmed the nanoscale size and spherical shape of the nanoparticles. The DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging study indicated that preparation processes do not have any significant effect on the antioxidant activity of curcumin. The results of this study are promising for the use of curcumin-loaded NLCs in more studies and using curcumin in the treatment of CNS diseases.
ISSN:1948-7193
1948-7193
DOI:10.1021/acschemneuro.8b00510