Phospholipid nanoformulation of thymoquinone with enhanced bioavailability: Development, characterization and anti-inflammatory activity

Rathore, Charul; Upadhyay, Navneet Kumar; Sharma, Aditi; Lal, Uma Ranjan; Raza, Kaisar; Negi, Poonam

doi:10.1016/j.jddst.2019.04.041

Cited by 26 publications

(15 citation statements)

References 33 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Moreover, NPs could also decrease the dose and off-target toxicities, thereby enhancing treatment potential for arthritic drug delivery [ 49 , 50 ]. To improve the stability and oral bioavailability of TQ, various nanoformulations, including an oral phospholipidic nanomatrix (particle size > 100 nm) [ 1 ], topical ethosomes (particle size 105.2 ± 8.0) [ 51 ], and liposomal chitosan gel [ 52 ], were developed which enhanced the therapeutic efficacy of TQ as investigated in a carrageenan-induced paw inflammation model. The phospholipidic nanomatrix made up of lipidic core and surfactant mixture enhances TQ aqueous solubility and intestinal absorption relative to TQ suspension [ 1 ].…”

Section: Rheumatoid Arthritismentioning

confidence: 99%

“…To improve the stability and oral bioavailability of TQ, various nanoformulations, including an oral phospholipidic nanomatrix (particle size > 100 nm) [ 1 ], topical ethosomes (particle size 105.2 ± 8.0) [ 51 ], and liposomal chitosan gel [ 52 ], were developed which enhanced the therapeutic efficacy of TQ as investigated in a carrageenan-induced paw inflammation model. The phospholipidic nanomatrix made up of lipidic core and surfactant mixture enhances TQ aqueous solubility and intestinal absorption relative to TQ suspension [ 1 ]. Besides this, lipidic NPs are directly taken up by intestinal lymph and deliver the drugs directly into the bloodstream, which leads to avoidance of the first-pass metabolism process.…”

Section: Rheumatoid Arthritismentioning

confidence: 99%

“…As per the WHO, approximately 80% of the global population utilizes indigenous systems of medicine for their primary health care [ 1 ]. Recently, various potential phytocandidates such as β-elemene, brazilin, bufalin, cardamonin, cryptotanshinone, isogarcinol, curcumin, celastrol, lapachol, nobiletin, oroxylin A, thymoquinone, resveratrol, torilin, and swertiamarin have been identified to have pharmacological properties [ 2 ].…”

Section: Introductionmentioning

confidence: 99%

“…The absolute bioavailability (BA) of TQ in rabbits after oral (20 mg/kg PO) and IV (5 mg/kg) administration revealed a *58% lag time of 23 min with slower absorption and rapid elimination rates [ 11 ]. It is an acidic molecule with a pKa value of 5.1 [ 12 ] that is extensively degraded in the aqueous medium, especially at higher pH concentrations [ 1 ]. Low aqueous solubility, bioavailability, thermal, and photodegradability are some major drawbacks in utilizing its maximum potential as therapeutic.…”

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis

et al. 2021

View full text Add to dashboard Cite

Cancer causes a considerable amount of mortality in the world, while arthritis is an immunological dysregulation with multifactorial pathogenesis including genetic and environmental defects. Both conditions have inflammation as a part of their pathogenesis. Resistance to anticancer and disease-modifying antirheumatic drugs (DMARDs) happens frequently through the generation of energy-dependent transporters, which lead to the expulsion of cellular drug contents. Thymoquinone (TQ) is a bioactive molecule with anticancer as well as anti-inflammatory activities via the downregulation of several chemokines and cytokines. Nevertheless, the pharmacological importance and therapeutic feasibility of thymoquinone are underutilized due to intrinsic pharmacokinetics, including short half-life, inadequate biological stability, poor aqueous solubility, and low bioavailability. Owing to these pharmacokinetic limitations of TQ, nanoformulations have gained remarkable attention in recent years. Therefore, this compilation intends to critically analyze recent advancements in rheumatoid arthritis and cancer delivery of TQ. This literature search revealed that nanocarriers exhibit potential results in achieving targetability, maximizing drug internalization, as well as enhancing the anti-inflammatory and anticancer efficacy of TQ. Additionally, TQ-NPs (thymoquinone nanoparticles) as a therapeutic payload modulated autophagy as well as enhanced the potential of other drugs when given in combination. Moreover, nanoformulations improved pharmacokinetics, drug deposition, using EPR (enhanced permeability and retention) and receptor-mediated delivery, and enhanced anti-inflammatory and anticancer properties. TQ’s potential to reduce metal toxicity, its clinical trials and patents have also been discussed.

show abstract

Section: Rheumatoid Arthritismentioning

confidence: 99%

Section: Rheumatoid Arthritismentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis

et al. 2021

View full text Add to dashboard Cite

show abstract

“…TQ protects against toxic medications such as bleomycin-induced lung fibrosis [ 24 , 25 ], gentamicin-induced kidney and liver injury [ 19 , 20 ], and titanium dioxide nanoparticle-induced toxicity [ 26 ]. However, it has limitations in effectiveness due to its narrow therapeutic window and poor oral bioavailability [ 27 , 28 ]. TQ is a hydrophobic molecule and has poor water solubility and poor formulation.…”

Section: Introductionmentioning

confidence: 99%

Ameliorative Effect of Thymoquinone‐Loaded PLGA Nanoparticles on Chronic Lung Injury Induced by Repetitive Intratracheal Instillation of Lipopolysaccharide in Rats

Saghir

Al-Gabri

Ali

et al. 2021

Oxidative Medicine and Cellular Longevity

View full text Add to dashboard Cite

Thymoquinone (TQ), the active constituent of Nigella sativa, possesses several benefits in traditional and modern medicines. This study examined the effect of a single dose of Nano-TQ on chronic lung injury induced by repetitive intratracheal installation of lipopolysaccharide (LPS). Rats received LPS twice weekly for 8 weeks via intratracheal installation and a single dose of TQ-PLGA NPs on the day after the last dose of LPS. Six rats from each group were sacrificed after 8 and 10 weeks, and samples were collected for analysis. Repetitive intratracheal installation of LPS caused histopathological alterations, including partial or complete obstruction of the alveoli, interstitial edema, mild fibroblastic proliferation, fibrous strands besides lymphocytes and plasma infiltrations, suffered fetalization, bronchiectasis, hypertrophied arterioles, and others. Investigation of the ultrastructure revealed prominent necrotic pneumocytes with destructed chromatin and remnant of necrotic debris in the narrowing alveolar lumen in LPS-induced rats. TQ-PLGA NPs effectively ameliorated LPS-induced histopathological and ultrastructural alterations in the lung of rats. In addition, TQ-PLGA NPs significantly alleviated serum levels of IL-10 and TGF-β1 in LPS-induced rats. In conclusion, TQ-PLGA NPs prevented inflammation and tissue injury in the lungs of rats challenged with repetitive intratracheal installation of LPS. Therefore, TQ-PLGA NPs represent a promising candidate for the prevention of lung injury induced by LPS, pending further studies to determine its safety and exact protective mechanism.

show abstract

Advancement of nanomedicines in chronic inflammatory disorders

et al. 2022

View full text Add to dashboard Cite

Chronic diseases, as stated by the WHO, are a threat to human health which kill 3 out of every 5 people worldwide. Therapeutics for such illnesses can be developed using traditional medicine. However, it is not an easy path from natural products to Western pharmacological and pharmaceutical methods. For several decades, chronic inflammatory disorders, especially in Westernized countries, have increased incidence and prevalence. Several NSAIDs are used to decrease inflammation and pain; however, there are numerous negative consequences of these anti-inflammatory medications, whereas plant-based natural products have anti-inflammatory therapeutic benefits that have little or no adverse effects. Nanoparticles are a new type of drug delivery device that may be designed to provide excellent target selectivity for certain cells and tissues while also having a high drug loading capacity, resulting in better pharmacokinetics, pharmacodynamics (PKPD), and therapeutic bioavailability. The size and polarity of phytochemical compounds make it hard to pass the blood–brain barrier (BBB), blood-vessel endothelial lining, gastrointestinal tract and mucosa. In addition, the gastrointestinal system is enzymatically destroyed. Therefore, nanoparticles or nanocrystals might also be used for encapsulation or conjugation of these chemicals as a method to improve their organic effectiveness through their gastrointestinal stability, absorption rate and dispersion. The therapy of numerous inflammatory illnesses, including arthritis, gastritis, Nephritis, Hepatitis (Type A, B &C), ulcerative colitis, Alzheimer's disease, atherosclerosis, allergic responses (asthma, eczema) or autoimmune disorders, is characterised by nanoparticles. This review paper provides information on the numerous nanosystem described with their probable mechanism to treat chronic inflammatory diseases.

show abstract

Phospholipid nanoformulation of thymoquinone with enhanced bioavailability: Development, characterization and anti-inflammatory activity

Cited by 26 publications

References 33 publications

Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis

Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis

Ameliorative Effect of Thymoquinone‐Loaded PLGA Nanoparticles on Chronic Lung Injury Induced by Repetitive Intratracheal Instillation of Lipopolysaccharide in Rats

Advancement of nanomedicines in chronic inflammatory disorders

Contact Info

Product

Resources

About