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CHAPTER 13
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Thymoquinone-Loaded Nanocarriers for
Healthcare Applications
RUQAIYAH KHAN,1 HIMANI NAUTIYAL,2 and SHAKIR SALEEM
1
; shakir.saleem@chitkara.edu.in
(S. Saleem)
2
Siddhartha Institute of Pharmacy, Dobachi, Dehradun,
ABSTRACT
Nano drug delivery system deals with the enhancement of bioavailability
of orally administered therapeutic agents, target-specific drug delivery, and
prolonged half-life of parenteral. Thymoquinone (TQ) is the chief active
ingredient of Nigella sativa and has been incorporated in innumerable nanoformulations to assess its diverse pharmacological activity against many
human illnesses including cancer, hypertension (HTN), diabetes, allergies,
eczema, and immunogenic disorders. The major problem in developing TQ
based nanoformulation is its highly hydrophobic nature which limits its solubility and its bioavailability. However, the emergence of surface engineering
of the nanoparticle carrier systems has fixed this problem for TQ and hence,
several nanoformulations have been developed and evaluated. This chapter
briefly discusses the health applications of TQ based nanoformulations
prepared through different techniques.
1
Over the last couple of decades, remarkable progress has been envisaged in
the field of nanotechnology-related to therapeutics and radio-imaging agents
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thereby minimizing the interventions (Martins et al., 2013). Nanotherapeutics aims to provide maximum pharmacological efficacy and minimum side
effects by lowering the frequency of administration. Several nano-formulations like dendrimers, nanocrystals, nanoemulsions, liposomes, solid lipid
nanoparticles (SLN), nano micelles, and polymeric nanoparticles have been
developed to achieve better therapeutic compliance (Onoue et al., 2014). In
the year 1996, the first nano-drug, Doxil, was approved by the FDA, hence
laying the foundation of nano-drug delivery system. It was then followed by
cascade of approvals including but not limited to oxaliplatin nanoparticles,
nanoparticle comprising rapamycin and albumin as an anticancer agent,
calcipotriol monohydrate nanocrystals, liposomes comprising docetaxel,
nanoemulsion of 5-aminolevulinic acid and treatment of systemic fungal
infections with phospholipid particles encapsulating polyene antibiotics
(Krukemeyer et al., 2015).
Recently, various approaches involving polymer-based nanoparticles
for oral administration of the drug has been undertaken for the treatment of
cancer and several other diseases (Cho et al., 2008; Ravindran et al., 2010).
Polymer-based nanoparticles have also been employed to deliver natural
products like coenzyme Q10 (Ankola et al., 2007), estradiol (Hariharan et
al., 2006), ellagic acid (Bala et al., 2006), curcumin (Bisht et al., 2007),
and chemotherapeutic agents as paclitaxel (Mu et al., 2003) and doxorubicin
(DOX) (Vasey et al., 1999).
Bioactive compounds are one of the best alternative sources which can
be employed in the prevention and treatment of various kinds of diseases
including cancer (Shanmugam et al., 2018). Nigella sativa, also known as
Black cumin, is an ancient herbal drug which is traditionally used to cure
several conditions like asthma, bronchitis, inflammation, eczema, fever,
influenza, hypertension (HTN), cough, headache, dizziness (Schneider et
al., 2014; Ballout et al., 2018). Additionally, recent researches have revealed
that black cumin can also be used to alleviate ailments like diabetes, renal,
and liver malfunction, nervous system problems, rheumatic diseases, cancer,
inflammatory diseases, gastrointestinal problems, and also for overall general
wellness (Banerjee et al., 2010; Asaduzzaman et al., 2017).
Nigella sativa L. (Family-Ranunculaceae) contains Thymoquinone (TQ),
which is the main bioactive component in the essential oil (EO) extracted
from its seeds (Figure 13.1).
303 Thymoquinone-Loaded Nanocarriers for Healthcare Applications
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The seeds of Nigella sativa, its chemical structure, and its constituents.
Nigella sativa has been anciently used and is extensively reported as a
folk medicine for numerous therapeutic applications like allergic rhinitis,
eczema, HTN, diuretic, immunomodulation, analgesic, antioxidant, hepatoprotective, and renal protective agent (Salem et al., 2005; Ahmad et al.,
2013) (see Table 13.1).
TABLE 13.1 The Therapeutic Areas Covered by Thymoquinone
Sl. Therapeutic Use References
No.
1. Anti-allergic Aziz et al., 2011
2. Anti-bacterial Chaieb et al., 2011
3. Anti-inflammatory Inci et al., 2013
4. Antioxidant activity Inci et al., 2013
5. Anti-depressant Aquib et al., 2015
6. Anti-anxiety Gilhotra et al., 2011
7. Anti-tumor Zhang et al., 2016
8. Anti-diabetic El-Mahmoudy et al., 2005; Sangi et al., 2015
9. Neuroprotective Ramachandran et al., 2016
10. Hepatoprotective Oguz et al., 2012
11. Anti-cancer drug-induced toxicity Alenzi et al., 2010
12. Hemorrhagic cystitis Gore et al., 2016
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