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About OMICS Group
OMICS Group International is an amalgamation of Open Access
publications and worldwide international science conferences and
events. Established in the year 2007 with the sole aim of making the
information on Sciences and technology ‘Open Access’, OMICS
Group publishes 400 online open access scholarly journals in all
aspects of Science, Engineering, Management and Technology
journals. OMICS Group has been instrumental in taking the
knowledge on Science & technology to the doorsteps of ordinary
men and women. Research Scholars, Students, Libraries, Educational
Institutions, Research centers and the industry are main
stakeholders that benefitted greatly from this knowledge
dissemination. OMICS Group also organizes 300 International
conferences annually across the globe, where knowledge transfer
takes place through debates, round table discussions, poster
presentations, workshops, symposia and exhibitions.
About OMICS Group Conferences
OMICS Group International is a pioneer and leading science event
organizer, which publishes around 400 open access journals and
conducts over 300 Medical, Clinical, Engineering, Life Sciences,
Phrama scientific conferences all over the globe annually with the
support of more than 1000 scientific associations and 30,000 editorial
board members and 3.5 million followers to its credit.
OMICS Group has organized 500 conferences, workshops and national
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Bengaluru and Mumbai.
Aqueous Solubility and
Degradation Kinetics of the
Phytochemical Anticancer
Thymoquinone; Probing the
Effects of Solvents, pH and Light
JUMAH M. M. SALMANI, Ph.D
CHINA PHARMACEUTICAL UNIVERSITY
Background
Cancers account for 20-25% of deaths in clinical
practices.
Attempts to cure or palliate cancer employ 3
basic methods:

Surgery

Radiotherapy

Chemotherapy.
Cancer Chemotherapy
It is the use of drugs to inhibit or kill
proliferating cancer cells, while leaving host
cells unaffected.
The optimum achievement of this goal is still far
from reality.
Limitations of Chemotherapy
Is there any Alternatives?
Naturally
occurring phytochemical
compounds with anticancer activity.
Nigella Sativa
Why?
Long History, thousands of years of use
in folk medicine.
 Readily Available in low cost.
 High Safety profile.
 Contain many bioactive products among
them “Thymoquinone” whose anticancer
effects has been recently documented.

Thymoquinone
It is the Bioactive component of Nigella
Sativa with documented:
Anti-inflammatory
Anti-histaminic
Anti-diabetic
Analgesic
Anticancer
Thymoquinone Anticancer Effects:
TQ
exerts its pharmacologic effects through
the modulation of the physiological and
biochemical events responsible for the
generation of ROS.
In normal tissues, TQ behave as a powerful
antioxidant.
In cancer tissue it works as Pro-oxidant.
Play regulatory role
Inhibition of cancer Hallmarks
Literature Survey
 Hundreds
of reports documented the activity
of TQ most particularly in cancer therapy
mediated by different mechanisms.
 It has protective effect for normal tissue.
 It has augmenting effect for other anticancer
agents.
 It can repair the damage caused by other
Chemotherapeutics agents.
 Yet very few reports about the formulations
were found.
Previous Formulations Drawbacks
Low
Drug Loading & Encapsulation
Efficiency
Burst
No
Release Pattern
Stability Study
The Goals of current Study

In vitro quantitative analysis of
Thymoquinone in order to perform
Aqueous Solubility and Stability study
and the role of solvents, pH and light is
to be elucidated as well.
Quantitative Analysis of Thymoquinone
HPLC
Forced
Degradation
study
 Acid
 Base
 UV
 Oxidation
HPLC Validation as per ICH

Linearity (0.5-10 μg/mL , R2=0.9999)

Specificity

Precision (RSD% < 2%)

LOD and LOQ (0.081 and 0.246 µg/mL )
TQ peak 10 min
Main UV
degradation
peaks
Acid
degradation
peaks
Main base Degradation
peaks
Oxidation degradation
peaks
Summary

Our developed HPLC method for
detection and quantification of TQ was
proved to be as a Stability Indicating
Method.
Solubility study
Performed
using excess of TQ in
different Aqueous solvents for 72
hours in closed dark conditions to
exclude the effect of light.
Results of solubility study
The values represent the concentration of TQ ± SD in μg/ml
Aqueous Stability Study
 TQ
in Series of aqueous solvents.
 Dark to avoid light
 Tightly closed container
 fixed temp.
HPLC.
Results of stability study:
120
residual TQ conc.%
100
80
0h
24 h
60
48 h
72 h
96 h
40
20
0
Water
Saline
P.B pH5
P.B pH7.4
P.B pH9
0.1NHCL
Effect of Light

The effect of light was studied for TQ
solutions in organic solvents (in which the
drug was shown to be stable for at least 7
days in dark to exclude the effect of
solvent).

The study performed in light illumination
chamber at 750 lux at 25°C.
Results:
Severe degradation of TQ within 24 h
regardless the solvent type.
 Kinetics of light degradation of TQ
follow 2nd Order.
 In absence of light TQ is stable in ethanol
and 1:1 ratio ethanol :water/buffer.

Initial TQ
chromatogram
in ethanol
After 48 h
subjected to
light
Initial TQ
UV spectrum
After 48
subjected to
light
Conclusion





TQ aqueous solubility compromised by
stability
TQ is unstable in all aqueous solvents with
direct effect of pH on the degradation.
In dark TQ stable in ethanol and ethanol:
water/buffer mixture of 1:1 ratio.
Light has severe effect on TQ stability.
Stability issue of TQ in aqueous solvents for
the first time to be studied, and previous
formulation discrepancies may be correlated
to this issue.
Upcoming studies (unpublished yet)
Thermodynamic analysis
of TQ.
Investigating the role of Physicochemical
properties of TQ and the formulation
strategies on developing successful
formulation.
Finding the solution then carrying out
thorough evaluation both in vitro and in
vivo.
Latest Findings:
 We
got promising results that
may have a role in the near future
clinical use of the valuable drug
in cancer therapy.
Thank you
Lets Meet again at Pharmacognosy-2015
3rd International Conference and Exhibition
on Pharmacognosy, Phytochemistry and
Natural Products
October 26-28, 2015 Hyderabad, India
Theme: Advanced trends for the future of Herbal Drugs and
Products
Website: http://pharmacognosy-phytochemistry-naturalproducts.pharmaceuticalconferences.com/