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

Ravi Raj Pal,Priya Singh,Vasundhara Rajpal,Shubhini A Saraf

doi:10.3390/pharmaceutics13060775

Ravi Raj Pal, Priya Singh + Show 2 more

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https://doi.org/10.3390/pharmaceutics13060775

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Journal: Pharmaceutics	Publication Date: May 22, 2021
Citations: 19	License type: CC BY 4.0

Affiliation: Babasaheb Bhimrao Ambedkar University

Abstract

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.

Highlights

As per the WHO, approximately 80% of the global population utilizes indigenous systems of medicine for their primary health care [1]
Thymoquinone (TQ) is a crucial active ingredient obtained from the black seed of the plant Nigella sativa (NS) and Caramcarvil, with potential antioxidant and anti-inflammatory activities [3]
The following keywords were selected based on MeSH terms: thymoquinone, nanoparticle, nanocarrier, targeted nanoparticle, rheumatoid arthritis, nano, inflammation, cancer, neoplasm, toxicity, and antioxidant

Summary

Introduction

As per the WHO, approximately 80% of the global population utilizes indigenous systems of medicine for their primary health care [1]. 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]. Thymoquinone (TQ) is a crucial active ingredient obtained from the black seed of the plant Nigella sativa (NS) and Caramcarvil, with potential antioxidant and anti-inflammatory activities [3]. It holds a wide range of other therapeutic properties, including hepatoprotective, cardioprotective, anticancer, antidiabetic, and antimicrobial properties [4]. Dithymoquinone, TQ, trans-anethol, (2-isopropyl-5-methylbenzo-1, 4-quinone), limonine, carvone, nigellidine, hedrin and p-cymene are some of the majorly identified terpenes.

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