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

被引:116
|
作者
Malvajerd, Soroor Sadegh [1 ]
Azadi, Amir [2 ]
Izadi, Zhila [3 ]
Kurd, Masoumeh [4 ]
Dara, Tahereh [5 ]
Dibaei, Maryam [5 ]
Zadeh, Mohammad Sharif [6 ]
Javar, Hamid Akbari [5 ,7 ]
Hamidi, Mehrdad [4 ,8 ]
机构
[1] Univ Tehran Med Sci, Dept Pharmaceut Nanotechnol, Fac Pharm, Tehran 14174, Iran
[2] Shiraz Univ Med Sci, Dept Pharmaceut, Sch Pharm, Shiraz 4513956184, Iran
[3] Kermanshah Univ Med Sci, Pharmacut Sci Res Ctr, Kermanshah 451354, Iran
[4] Zanjan Univ Med Sci, ZPNRC, Dept Pharmaceut Nanotechnol, Sch Pharm, Zanjan 4513956184, Iran
[5] Univ Tehran Med Sci, Dept Pharmaceut, Fac Pharm, Tehran 13169, Iran
[6] Univ Tehran Med Sci, Dept Pharmacol & Toxicol, Fac Pharm, Tehran 1316943551, Iran
[7] Univ Tehran Med Sci, Tehran Endocrinol & Metab Res Inst, Tehran 1316943551, Iran
[8] Zanjan Univ Med Sci, Dept Pharmaceut, Sch Pharm, Zanjan 4513956184, Iran
来源
ACS CHEMICAL NEUROSCIENCE | 2019年 / 10卷 / 01期
关键词
Curcumin; Alzheimer's disease; nanostructured lipid carriers; optimization; solid lipid nanoparticles; pharmacokinetic; IN-VITRO; ALZHEIMERS-DISEASE; CELLULAR UPTAKE; P-GLYCOPROTEIN; DRUG-DELIVERY; MOUSE MODEL; VIVO; BARRIER; FORMULATION; PACLITAXEL;
D O I
10.1021/acschemneuro.8b00510
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 (AUC(0-t) = 505.76 ng/g h) compared to free curcumin (AUC(0-t) = 0.00 ng/g h) and curcumin-loaded SLNs (AUC(0-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.
引用
收藏
页码:728 / 739
页数:23
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