Enhancement of Bioavailability and Pharmacodynamic Effects of Thymoquinone Via Nanostructured Lipid Carrier (NLC) Formulation

Elmowafy, Mohammed; Samy, Ahmed M.; Raslan, Mohamed A.; Salama, Ayman; Said, Ragab; Abdelaziz, Abdelaziz E.; El‐Eraky, Wafaa I.; Awdan, Sally A. El; Viitala, Tapani

doi:10.1208/s12249-015-0391-0

Cited by 105 publications

(57 citation statements)

References 32 publications

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“…of TQ have been identified that are somehow involved in tumorigenesis or development of drug resistance (Kundu et al, 2014b) (Figure 1). Though treatment with TQ alone has shown antitumor efficacy in several in vitro and in vivo studies as mentioned in details in a recent review (Majdalawieh et al, 2017), the lower efficacy (Effenberger et al, 2010) and poor bioavailability (Ganea et al, 2010; Elmowafy et al, 2016) of TQ is the primary bottleneck for considering it as the primary therapeutic agent. Therefore, in this review, we proposed the potential role of TQ as an adjuvant therapy with different types of conventional cancer treatments namely surgery, radiotherapy, chemotherapy, and immunotherapy either to prevent carcinogenesis or to potentiate the efficiency of conventional therapeutic modalities.…”

Section: Introductionmentioning

confidence: 99%

Thymoquinone as a Potential Adjuvant Therapy for Cancer Treatment: Evidence from Preclinical Studies

et al. 2017

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Thymoquinone (TQ), the main bioactive component of Nigella sativa, has been found to exhibit anticancer effects in numerous preclinical studies. Due to its multitargeting nature, TQ interferes in a wide range of tumorigenic processes and counteracts carcinogenesis, malignant growth, invasion, migration, and angiogenesis. Moreover, TQ can specifically sensitize tumor cells toward conventional cancer treatments (e.g., radiotherapy, chemotherapy, and immunotherapy) and simultaneously minimize therapy-associated toxic effects in normal cells. In this review, we summarized the adjuvant potential of TQ as observed in various in vitro and in vivo animal models and discussed the pharmacological properties of TQ to rationalize its supplementary role in potentiating the efficacy of standard therapeutic modalities namely surgery, radiotherapy, chemotherapy, and immunotherapy. Altogether, we suggest further comprehensive evaluation of TQ in preclinical and clinical levels to delineate its implied utility as a novel complementary adjuvant therapy for cancer treatment.

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Section: Introductionmentioning

confidence: 99%

Thymoquinone as a Potential Adjuvant Therapy for Cancer Treatment: Evidence from Preclinical Studies

et al. 2017

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“…This study was designed for quantification and evaluation of pharmacokinetics of TQ in layer chickens following PO and IV administration. The PO dose was selected according to previous study in rats (Elmowafy et al, ) while IV dose was established based on study conducted in rabbits (Alkharfy et al, ). For this purpose, a sensitive and selective HPLC system was utilized for pharmacokinetic analysis.…”

Section: Discussionmentioning

confidence: 99%

“…This study was designed for quantification and evaluation of pharmacokinetics of TQ in layer chickens following PO and IV administration. The PO dose was selected according to previous study in rats (Elmowafy et al, 2016) Khan, & Alkharfy, 2015). In this study, a combination of sodium di-hydrogen phosphate buffer and acetonitrile was utilized as mobile phase.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of thymoquinone in layer chickens following oral and intravenous administration

Iqbal

Javeed

Sattar

et al. 2019

Vet Pharm & Therapeutics

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Thymoquinone (TQ) is the major constituent of Nigella sativa and known to possess a variety of pharmacological effects. This study was designed to evaluate the pharmacokinetic profile of TQ following oral (PO) and intravenous (IV) administration in layer chickens. The layer chickens were equally divided into two groups (six chickens in each group, total 12 chickens), and TQ was administered via PO and IV routes. For PO route, the dose was 20 mg/kg b.w. and for IV route, 5 mg/kg b.w. was administered, respectively. A sensitive and accurate High‐Performance Liquid Chromatography (HPLC) technique was validated for the quantification of TQ from plasma. The limit of detection (LOD) and limit of quantification (LOQ) were 0.02 µg/ml and 0.05 µg/ml, respectively with >80% recovery. Maximum plasma concentration (Cmax) following PO and IV administration was 8.805 and 4.497 µg/ml, respectively, while time to reach at maximum concentration (Tmax) was 1 and 0.1 hr, respectively. The elimination half‐lives were recorded as 1.02 and 0.978 hr, whereas the mean residence times were 1.79 and 1.036 hr following both PO and IV administration, respectively. The 85% PO bioavailability was indicative that TQ could be used for various therapeutic purposes in layer chickens.

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“…The absolute oral bioavailability of both DIM-10 and DIM-14 was found to be approximately <20%. Because many studies demonstrated the promising role of different nanoformulations in overcoming poor aqueous solubility [25,31,5,28], we chose NLC formulation approach [17,32,6,24]. Initially, prepared NLC formulation were subjected to in vitro drug release profiles and found that both DIM-10 and DIM-14 release were significantly increased in NLC formulations compared to free drugs; this increased drug release is due to increase solubility of DIMs in nanocarrier systems.…”

Section: Discussionmentioning

confidence: 99%

Novel diindolylmethane derivatives based NLC formulations to improve the oral bioavailability and anticancer effects in triple negative breast cancer

Godugu

Doddapaneni

Safe

et al. 2016

European Journal of Pharmaceutics and Biopharmaceutics

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The present study demonstrates the promising anticancer effects of novel C-substituted diindolylmethane (DIM) derivatives DIM-10 and DIM-14 in aggressive TNBC models. In vitro studies demonstrated that these compounds possess strong anticancer effects. Caco-2 permeability studies resulted in poor permeability and poor oral bioavailability was demonstrated by pharmacokinetic studies. Nano structured lipid carrier (NLC) formulations were prepared to increase the clinical acceptance of these compounds. Significant increase in oral bioavailability was observed with NLC formulations. Compared to DIM-10, DIM-10 NLC formulation showed increase in Cmax and AUC values by 4.73 and 11.19-folds, respectively. Similar pattern of increase was observed with DIM-14 NLC formulations. In dogs DIM-10 NLC formulations showed an increase of 2.65 and 2.94-fold in Cmax and AUC, respectively. The anticancer studies in MDA-MB-231 orthotopic TNBC models demonstrated significant reduction in tumor volumes in DIM-10 and DIM-14 NLC treated animals. Our studies suggest that NLC formulation of both DIM-10 and 14 is effective in TNBC models.

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Enhancement of Bioavailability and Pharmacodynamic Effects of Thymoquinone Via Nanostructured Lipid Carrier (NLC) Formulation

Cited by 105 publications

References 32 publications

Thymoquinone as a Potential Adjuvant Therapy for Cancer Treatment: Evidence from Preclinical Studies

Thymoquinone as a Potential Adjuvant Therapy for Cancer Treatment: Evidence from Preclinical Studies

Pharmacokinetics of thymoquinone in layer chickens following oral and intravenous administration

Novel diindolylmethane derivatives based NLC formulations to improve the oral bioavailability and anticancer effects in triple negative breast cancer

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