Formulation of thymoquinone loaded chitosan nano vesicles: In-vitro evaluation and in-vivo anti-hyperlipidemic assessment

J., Fakhria A.; Gilani, Sadaf Jamal; Imam, Syed Sarim; Chandrakala,

doi:10.1016/j.jddst.2019.01.033

Cited by 38 publications

(20 citation statements)

References 43 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It is well‐known that the strong lipophilicity of TQ causes limited bioavailability and TQ is an unstable compound as a result of its thermal‐ and light‐sensitive nature . Therefore, encapsulation of TQ in nanoparticles is anticipated to enhance its bioavailability and stability.…”

Section: Resultsmentioning

confidence: 99%

Fabrication of Thymoquinone‐Loaded Albumin Nanoparticles by Microfluidic Particle Synthesis and Their Effect on Planarian Regeneration

Kazan

Yeşil-Çeliktaş

Zhang

2019

Macromolecular Bioscience

View full text Add to dashboard Cite

Thymoquinone is the main bioactive component of the plant Nigella sativa, which is commonly known as black seeds and has several therapeutic effects. However, clinical applications of thymoquinone are limited due to its hydrophobic nature. In this study, thymoquinone is encapsulated in albumin nanoparticles by using a microfluidic platform to overcome this limitation. The mean particle sizes of empty and thymoquinone‐loaded nanoparticles are determined as 271.3 and 315.6 nm, respectively, with polydispersity index values both lower than 0.25. In addition to particle size distribution measurements, characterizations of the prepared nanoparticles such as zeta potential measurements, in vitro release studies, as well as scanning electron microscopy, Fourier‐transform infrared, and differential scanning calorimetry analyses are also carried out. To determine the effect of thymoquinone on neural regeneration, planarians are used as the model organism. After application of free and encapsulated thymoquinone, planarians are amputated and the fragments are observed in terms of head and tail regeneration, swimming pattern, and behavior. The results indicate that thymoquinone affects their behavior and primarily enhances head regeneration of planarians. In addition, it is shown that encapsulation of thymoquinone not only enhances the thermal stability of the molecule but also decreases its toxicity.

show abstract

Section: Resultsmentioning

confidence: 99%

Fabrication of Thymoquinone‐Loaded Albumin Nanoparticles by Microfluidic Particle Synthesis and Their Effect on Planarian Regeneration

Kazan

Yeşil-Çeliktaş

Zhang

2019

Macromolecular Bioscience

View full text Add to dashboard Cite

show abstract

“…The prepared solid block was placed in a microtome cutter and a cross-section was cut and stained with haemotoxylin and eosin. 27 Finally, the slide was examined by using a digital motic microscope (Motic digital Microscope, B3 DMWB, Pal system, Japan) at 40x and the images were compared with the normal saline-treated cornea (0.9% NaCl, control).…”

Section: Histopathological Examinationmentioning

confidence: 99%

<p>Clarithromycin-Loaded Ocular Chitosan Nanoparticle: Formulation, Optimization, Characterization, Ocular Irritation, and Antimicrobial Activity</p>

Bin-Jumah

Gilani

Jahangir³

et al. 2020

IJN

Self Cite

View full text Add to dashboard Cite

The topically administered drugs through conventional delivery systems have low bioavailability. Henceforth, the present study was designed to prepare and optimize clarithromycin (CTM)-loaded chitosan nanoparticles (CHNPs) to demonstrate the efficacy against microorganisms. Methods: Clarithromycin-loaded chitosan nanoparticles (CTM-CHNPs) were prepared by ionotropic gelation method. The formulation was optimized by box-Behnken design using the formulation variables like CH (A), STPP concentration (B), and stirring speed (C). Their effects were evaluated on the independent variables like particle size (Y 1) and entrapment efficiency (Y 2). Further, CTM-CHNPs were evaluated for physicochemical parameters, invitro drug release, ex-vivo permeation, bioadhesive study, corneal hydration, histopathology, HET-CAM, and antibacterial study. Results: The optimized formulation (CTM-CHNPopt) showed the low particle size (152±5 nm), which is desirable for ocular delivery. It also showed high encapsulation (70.05%), zeta potential (+35.2 mV), and was found in a spherical shape. The drug release study revealed a sustained drug release profile (82.98±3.5% in 12 hours) with Korsmeyer peppas kinetic (R 2 =0.996) release model. It showed a 2.7-fold higher corneal permeation than CTMsolution. CHNPs did not exhibit any sign of damage to excised goat cornea, which is confirmed by hydration, histopathology, and HET-CAM test. It exhibited significant (P<0.05) higher antibacterial susceptibility than CTM-solution. Conclusion: The finding of the study concluded that CTM-CHNPs can be used for effective management of bacterial conjunctivitis by increasing the precorneal residence time.

show abstract

“…TQ is a lipophilic compound with molecular weight of 164.2 42 , log P of 2.54 43 and a low aqueous solubility of about 500 μg/ml 44 . TQ possesses antioxidant 45,46 , anti-inflammatory 47,48 , anti-hyperlipidemic 49 , anti-depressant 50 and antimicrobial activities 51 , and its use in combination with chemotherapeutic agents reduces their side effects 52,53 . TQ possesses antiproliferative activity on various types of cancer including colorectal carcinoma 54 , and was found to induce cell cycle arrest and apoptosis in HCT-116 human colon cancer cells 55 .…”

mentioning

confidence: 99%

Novel thymoquinone lipidic core nanocapsules with anisamide-polymethacrylate shell for colon cancer cells overexpressing sigma receptors

Ramzy

Metwally

Nasr

et al. 2020

Sci Rep

View full text Add to dashboard Cite

the biggest challenge in colorectal cancer therapy is to avoid intestinal drug absorption before reaching the colon, while focusing on tumor specific delivery with high local concentration and minimal toxicity. in our work, thymoquinone (tQ)-loaded polymeric nanocapsules were prepared using the nanoprecipitation technique using Eudragit S100 as polymeric shell. Conjugation of anisamide as a targeting ligand for sigma receptors overexpressed by colon cancer cells to Eudragit S100 was carried out via carbodiimide coupling reaction, and was confirmed by thin layer chromatography and 1 H-nMR. tQ nanocapsules were characterized for particle size, surface morphology, zeta potential, entrapment efficiency % (EE%), in vitro drug release and physical stability. A cytotoxicity study on three colon cancer cell lines (HT-29, HCT-116, Caco-2) was performed. Results revealed that the polymeric nanocapsules were successfully prepared, and the in vitro characterization showed a suitable size, zeta potential, EE% and physical stability. TQ exhibited a delayed release pattern from the nanocapsules in vitro. Anisamide-targeted tQ nanocapsules showed higher cytotoxicity against HT-29 cells overexpressing sigma receptors compared to their non-targeted counterparts and free TQ after incubation for 48 h, hence delineating anisamide as a promising ligand for active colon cancer targeting. Sigma receptors are expressed in normal cells of various organs including brain, kidney, liver, immune, endocrine and reproductive organ 1,2. Two distinguished subtypes were recognized and known as sigma-1 and sigma-2 3. Neurosteroids are the likely endogenous ligands for sigma-1 receptors 4 , and N,N-dimethyltryptamine; a natural alkaloid, was also found to be an endogenous ligand for sigma-1 receptors 5,6. A correlation between sigma receptors and diseases such as Parkinson's, Alzheimer's disease and cancer has been proposed 7 , and ligands for sigma-1 receptor were proven to improve various neurodegenerative disorders 8. Sigma-2 receptor is thought to be crucial for cell morphology, survival and differentiation 9. Sigma receptors are overexpressed in cancer cells of various organs 10 including cancers of the brain 11 , lung 12,13 , breast 14 , prostate gland 15 , kidney and colon 16. The tumor environment characterized by oxidative stress, hypoxia, low pH and insufficient supply of glucose and amino acids mediates disruption of endoplasmic reticulum protein folding. This in turn contributes to sigma-1 receptors activation to promote cell survival 7,17. In addition, sigma-2 receptors upregulation in cancerous tissues compared to healthy ones has been widely demonstrated 18,19. Benzamide derivatives demonstrate a high affinity towards sigma receptors 20-22. Anisamide (AA); a small molecular weight benzamide derivative was proven to exhibit high affinity for sigma receptors 23-25. In a review article previously published by our team the use of AA as a targeting ligand in several drug delivery systems was detailed 26. AA-functionalized doxorubicin-loade...

show abstract

Formulation of thymoquinone loaded chitosan nano vesicles: In-vitro evaluation and in-vivo anti-hyperlipidemic assessment

Cited by 38 publications

References 43 publications

Fabrication of Thymoquinone‐Loaded Albumin Nanoparticles by Microfluidic Particle Synthesis and Their Effect on Planarian Regeneration

Fabrication of Thymoquinone‐Loaded Albumin Nanoparticles by Microfluidic Particle Synthesis and Their Effect on Planarian Regeneration

<p>Clarithromycin-Loaded Ocular Chitosan Nanoparticle: Formulation, Optimization, Characterization, Ocular Irritation, and Antimicrobial Activity</p>

Novel thymoquinone lipidic core nanocapsules with anisamide-polymethacrylate shell for colon cancer cells overexpressing sigma receptors

Contact Info

Product

Resources

About