scholarly journals Endogenous Oleoylethanolamide Crystals Loaded Lipid Nanoparticles with Enhanced Hydrophobic Drug Loading Capacity for Efficient Stroke Therapy

2021 ◽  
Vol Volume 16 ◽  
pp. 8103-8115
Author(s):  
Shichao Wu ◽  
Di Liao ◽  
Xi Li ◽  
Zeyu Liu ◽  
Lin Zhang ◽  
...  
ACS Nano ◽  
2011 ◽  
Vol 5 (2) ◽  
pp. 1428-1435 ◽  
Author(s):  
Bin Luo ◽  
Shuai Xu ◽  
An Luo ◽  
Wen-Rui Wang ◽  
Shi-Long Wang ◽  
...  

2018 ◽  
Vol 171 ◽  
pp. 514-521 ◽  
Author(s):  
Soon-Seok Hong ◽  
Raj Kumar Thapa ◽  
Jin-Hee Kim ◽  
Soo-Yeon Kim ◽  
Jong Oh Kim ◽  
...  

2021 ◽  
Author(s):  
Shichao Wu ◽  
Di Liao ◽  
Xi Li ◽  
Zeyu Liu ◽  
Lin Zhang ◽  
...  

Abstract Background. Although the preparation of lipid nanoparticles (LNPs) achieves great success, their retention of highly hydrophobic drugs is still problematic. Results. Herein we report a novel strategy for efficiently loading hydrophobic drugs to LNPs for stroke therapy. Oleoylethanolamide (OEA), an endogenous highly hydrophobic molecule with outstanding neuroprotective effect, was successfully loaded to OEA-SPC&DSPE-PEG lipid nanoparticles (OSDP LNPs) with a drug loading of 15.9 ± 1.2 wt%, four times higher than those prepared via traditional methods. Efficient retention in OSDP LNPs greatly improved the pharmaceutical property and enhanced the neuroprotective effect of OEA. Through the data of positron emission tomography (PET) and TTC-stained brain slices, it could be clearly visualized that the acute ischemic brain tissues were preserved as penumbral tissues and bounced back with reperfusion. The in vivo experiments stated that OSDP LNPs could significantly improve the survival rate, the behavioral score, the spatial learning and memory ability of the MCAO (middle cerebral artery occlusion) rats. Meanwhile, the cerebral infarct volume, the edema degree, the apoptosis of the neurons, and the inflammation within the brain were also greatly decreased. Conclusions. These results suggest that the OSDP LNPs have a great chance to develop hydrophobic OEA into a potential anti-stroke formulation.


2021 ◽  
Vol 12 (4) ◽  
pp. 176-182
Author(s):  
A N Jyothsna Sree

Over the past few years, nanostructured lipid carriers became an emerging drug delivery system as lipid drug delivery systems are more focused. Within them, solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) have more advantages over other lipid carriers. This article is a cumulation of structure, types, composition, formulation methodologies, drug release from NLCs, various applications of NLCs. The key aspects for promising drug delivery systems are biocompatibility, drug loading capacity, ease of preparation, non-toxicity, and stability


2021 ◽  
Author(s):  
Shichao Wu ◽  
Di Liao ◽  
Xi Li ◽  
Zeyu Liu ◽  
Lin Zhang ◽  
...  

Abstract Background. Although the preparation of liposomes achieves great success and many have received regulatory approval, their retention of highly hydrophobic drugs is still problematic. Results. Herein we report a novel strategy for efficiently loading hydrophobic drug to liposomes for stroke therapy. N-oleoylethanolamine (OEA), an endogenous highly hydrophobic molecule with outstanding neuroprotective effect, was successfully loaded to OEA-SPC&DSPE-PEG liposomes (OSDP LNPs) with a drug loading of 15.9 ± 1.2 wt%, four times higher than those prepared via traditional methods. Efficient retention in OSDP LNPs greatly improved the pharmaceutical property and therefore enhanced the neuroprotective effect of OEA. Through the data of positron emission tomography (PET) and TTC-stained brain slices, it could be clearly visualized that the acute ischemic brain tissues were preserved as penumbral tissues and bounced back with reperfusion. The in vivo experiments stated that OSDP LNPs could significantly improve the survival rate, the behavioral score, the spatial learning and memory ability of the MCAO (middle cerebral artery occlusion) rats. Meanwhile, the cerebral infarct volume, the edema degree, the apoptosis of the neurons and the inflammation within the brain were also greatly decreased. Conclusions. These results suggest that the OSDP LNPs have a great chance to develop hydrophobic OEA into a potential anti-stroke formulation.


2012 ◽  
Vol 506 ◽  
pp. 389-392 ◽  
Author(s):  
N. Ratcharin ◽  
P. Wongtrakul ◽  
Ratana Indranupakorn

Solid lipid nanoparticles (SLNs) loaded ginger extract were prepared by microemulsion technique. The nanoparticles were composed of stearic acid as solid lipids, Cremophor RH 40 as surfactant and ethanol as co-surfactant. It was found that variation in the amount of surfactant and co-surfactant had profound effects on the mean particle size, the drug entrapment efficiency and loading capacity. Transmission electron microscope (TEM) revealed the spherical nature of the particles. The mean particle size of SLNs ranging between 453.1 and 551.7 nm were measured by dynamic light scattering (DLS). The entrapment efficiency (EE) and drug loading capacity (LC) determined by high performance liquid chromatography (HPLC) found to be in the range of 85.2390.07% and 1.411.49%, respectively.


Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis


2019 ◽  
Vol 233 ◽  
pp. 230-235 ◽  
Author(s):  
Li-li Lu ◽  
Wen-ya Xiong ◽  
Jun-bin Ma ◽  
Tian-fang Gao ◽  
Si-yuan Peng ◽  
...  

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