scholarly journals Development and Characterization of Solid Lipid Nanoparticles Containing Herbal Extract: In Vivo Antidepressant Activity

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
P. Vijayanand ◽  
V. Jyothi ◽  
N. Aditya ◽  
A. Mounika

In alternate systems of medicine like Ayurveda and traditional Chinese medicine, Hibiscus rosa sinensis and its extracts have been traditionally prescribed for their antidepressant activity. Crude extracts and rudimentary formulations approaches are good for proof-of-concept studies; however, these formulations are fraught with problems like poor oral bioavailability and high variability between subjects. Systematic drug delivery approaches could prove effective in addressing some of these problems. In this study, we report the development of Hibiscus rosa sinensis extract loaded solid lipid nanoparticles (HSLNs) using glycerol monostearate or beeswax as lipids. The HSLNs were evaluated for their size, surface charge, and morphology. The optimized HSLNs were tested for antidepressant activity in male Swiss albino mice. It was found that, with the optimized procedure, HSLNs of ~175 nm, carrying negative charge and nearly spherical shape, could be obtained. The in vivo test results suggested that there were marked differences in the immobility times of the test animals. Moreover, with HSLNs, it was found that at doses several times lower than the native crude extract dose, similar pharmacological effect could be obtained. These initial findings suggest that encapsulating phytopharmaceuticals into advanced delivery systems like solid lipid nanoparticles can be an effective strategy in improving their in vivo performance.

Author(s):  
VIJAYANAND P. ◽  
JYOTHI V. ◽  
MOUNIKA A.

Objective: The objective of the present research was to investigate the wound-healing potency of solid lipid nano particles of Hibiscus rosa sinensis extract. Crude herbal extracts and rudimentary formulations containing herbal extracts are good for demonstrating the feasibility of the concept; however, such formulations suffer with poor oral bioavailability and variability within groups of subjects. Converting herbal extracts into novel drug delivery systems may prove effective in addressing some of these problems. Methods: In the present study an attempt was made to develop Hibiscus rosa sinensis extract loaded solid lipid nanoparticles (HSLNs) using lipids glycerol monostearate (GMS) or beeswax. The prepared HSLNs were characterised for their size, surface charge and morphology. The optimized HSLNs were incorporated into Carbopol gel and tested for wound healing activity in male Wistar albino rats using excision wound model. Results: HSLNs of ~175 nm in size carrying negative charge were obtained with the optimised procedure using beeswax. The shape of the HSLNs was nearly spherical. The HSLNs (10 mg/ml) treated wounds healed much faster compared to raw crude extract and healing was comparable to marketed preparation. Conclusion: It is concluded that converting crude herbal extracts into SLNs can be an effective way to enhance the effectiveness of herbal extracts and their in vivo activity.


Author(s):  
Sara Faghihi ◽  
Mohammad Reza Awadi ◽  
Seyyedeh Elaheh Mousavi ◽  
Seyyed Mahdi Rezayat Sorkhabadi ◽  
Mandana Karboni ◽  
...  

Purpose: To overcome side effects of repetitive administration of Diazepam (Dzp) besides gaining benefits from sustaining release (SR) of the drug, which contributes to patient compliance, we concentrated on designing and preparing Dzp Solid Lipid Nanoparticles (SLNs). Methods: Using cholesterol (CHOL), stearic acid (SA) and glycerol monostearate (GMS), SLNs were prepared by high shear homogenization technique coupled with sonication. Polysorbate 80 (Tween 80) was used as a nonionic surfactant. After modification of prepared SLNs, particle size, zeta potential, drug-loading efficiency, morphology and scanning calorimetry as well as release studies were conducted. To increase the stability of desired particles, freeze-drying by cryoprotectant was carried out. In the final stage, In-vivo study was performed by oral (PO) and intraperitoneal (IP) administration to Wistar male rats. Results: Results indicated that optimized prepared particles were in average 150 nm diameter in spherical shape with 79.06 % loading efficiency and release of more than 85% of loaded drug in 24 hours. In-vivo investigations also illustrated differences in blood distribution of Dzp after loading this drug into SLNs. Conclusion: Based on the findings, it seems that drug delivery using SLNs could be an opportunity for solving complications of Dzp therapy in future.


2020 ◽  
Vol 20 (13) ◽  
pp. 1044-1052
Author(s):  
Nasrin Abbasi Gharibkandi ◽  
Sajjad Molavipordanjani ◽  
Jafar Akbari ◽  
Seyed Jalal Hosseinimehr

Background: Solid Lipid Nanoparticles (SLNs) possess unique in vivo features such as high resistivity, bioavailability, and habitation at the target site. Coating nanoparticles with polymers such as chitosan greatly affects their pharmacokinetic behavior, stability, tissue uptake, and controlled drug delivery. The aim of this study was to prepare and evaluate the biodistribution of 99mTc-labeled SLNs and chitosan modified SLNs in mice. Methods: 99mTc-oxine was prepared and utilized to radiolabel pre-papered SLNs or chitosan coated SLNs. After purification of radiolabeled SLNs (99mTc-SLNs) and radiolabeled chitosan-coated SLNs (99mTc-Chi-SLNs) using Amicon filter, they were injected into BALB/c mice to evaluate their biodistribution patterns. In addition, nanoparticles were characterized using Transmission Electron Microscopy (TEM), Fourier-transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Powder Diffraction (XRD) and Dynamic Light Scattering (DLS). Results: 99mTc-oxine with high radiochemical purity (RCP~100%) and stability (RCP > 97% at 24 h) was used to provide 99mTc-SLNs and 99mTc-Chi-SLNs with high initial RCP (100%). TEM image and DLS data suggest 99mTc- SLNs susceptibility to aggregation. To that end, the main portion of 99mTc-SLNs radioactivity accumulates in the liver and intestines, while 99mTc-Chi-SLNs sequesters in the liver, intestines and kidneys. The blood radioactivity of 99mTc-Chi-SLNs was higher than that of 99mTc-SLNs by 7.5, 3.17 and 3.5 folds at 1, 4 and 8 h post-injection. 99mTc- Chi-SLNs uptake in the kidneys in comparison with 99mTc-SLNs was higher by 37.48, 5.84 and 11 folds at 1, 4 and 8h. Conclusion: The chitosan layer on the surface of 99mTc-Chi-SLNs reduces lipophilicity in comparison with 99mTc- SLNs. Therefore, 99mTc-Chi-SLNs are less susceptible to aggregation, which leads to their lower liver uptake and higher kidney uptake and blood concentration.


2013 ◽  
Vol 10 (6) ◽  
pp. 656-666 ◽  
Author(s):  
Sandipan Dasgupta ◽  
Surajit Ghosh ◽  
Subhabrata Ray ◽  
Bhaskar Mazumder

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