Oral bioavailability enhancement and hepatoprotective effects of thymoquinone by self-nanoemulsifying drug delivery system

Kalam, Mohd Abul; Raish, Mohammad; Ahmed, Ali; Alkharfy, Khalid M.; Kazi, Mohsin; Alshamsan, Aws; Al-Jenoobi, Fahad I.; Al-Mohizea, Abdullah M.; Shakeel, Faiyaz

doi:10.1016/j.msec.2017.03.088

Cited by 77 publications

(79 citation statements)

References 47 publications

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“…Developed SNEDDS of DOX HCl were subjected to different stability testings in order to discard unstable SNEDDS for further studies. These tests were carried out through the following methods like heating and cooling, centrifugation and freeze-thaw cycles by following the method reported in the literature [32].…”

Section: Stability Studies Of Selected Snedds Via Thermodynamic Methodsmentioning

confidence: 99%

“…Each experiment was repeated in triplicate. All the excipients selected for SNEDDS formulation were generally regarded as a safe category (GRAS) and finally, excipients were selected on the basis of the highest solubility and miscibility of drug and oil in different excipients [32,33].…”

Section: Solubility Studiesmentioning

confidence: 99%

“…Suitable nanoemulsions of DOX and Nigella were developed by phase titration method. While the ratio of Smix, oil and aqueous medium of SNEDDS was selected on the basis of the emulsifying regions obtained from the pseudo-ternary phase diagrams [32]. Finally, Labrafil, Kolliphor RH 40 and glycerol was selected as oil, surfactant and co-surfactant, respectively and were added into the oil phase in the chosen concentration, further deionized water was added drop by drop till the sample become clear and transparent liquid with continuous vortexing.…”

Section: Development Of Sneddsmentioning

confidence: 99%

“…Heating-cooling cycles involved six cycles of storage at 40 C and 40 C for 48 h. The formulations were evaluated either for any drug precipitation or phase separation. Thereafter, the formulations were diluted with distilled water up to 1:25 and the resulting SNEDDS were evaluated for any instability issues [32]. Passed formulations were selected for further stability studies like centrifugation.…”

Section: Heating-cooling Cyclementioning

confidence: 99%

“…The emulsification times and appearances after dilution with an aqueous phase are listed in Table 2. The blank SNEDDS (F2, F3, F5-F8) showed transparent appearances after dilution and found that emulsification times less than 180 s, which indicated they could disperse quickly and completely when subjected to aqueous dilution under mild agitation [32]. After the drug loading, the emulsification time of F1, F4 increased from 110 s to 178 s, representing that the drug had a strong influence on the flow ability of the interfacial film [45].…”

Section: Emulsification Efficacymentioning

confidence: 99%

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Development and evaluation of doxorubicin self nanoemulsifying drug delivery system with Nigella Sativa oil against human hepatocellular carcinoma

Usmani

Mishra

Ali

et al. 2019

Artificial Cells, Nanomedicine, and Biotechnology

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Objective: The development of self nano emulsifying co-delivery system of doxorubicin and Nigella sativa oil for potentiating the anticancer effects against HepG2 cell lines. Materials and methods: SNEDDS were formulated by using Labrafil and N. sativa oil (3:2% w/w), Kolliphor RH40 (15% w/w), glycerol (5% w/w) as oil phase, surfactant and co-surfactant while deionized water (75% v/v) used as an aqueous phase. Optimized SNEDDS was evaluated for drug release and in vitro anticancer efficacy in liver cancer (HepG2) cell line. Results and discussion: The selected formulation (F6) has a mean particle size of 79.7 nm with PDI 0.098 and the minimum viscosity of 16.42 cps with % transmittance of 1.332 with maximum drug release of 96.968% in 32 h as compared to DOX alone. Stability data showed stable emulsion in both 25 0 C and-4 0 C. F6 showed improved efficacy in HepG2 cells by cytotoxicity, showed significant results p<.05 with 2.5 lg/ml of (inhibitory concentration) IC50. Conclusion: The overall study displayed that co-delivery of DOX and Nigella sativa oil in the form of SNEDDS may be an efficient carrier for further in vivo studies using oral delivery in human hepatocellular carcinoma in mammals.

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Section: Stability Studies Of Selected Snedds Via Thermodynamic Methodsmentioning

confidence: 99%

Section: Solubility Studiesmentioning

confidence: 99%

Section: Development Of Sneddsmentioning

confidence: 99%

Section: Heating-cooling Cyclementioning

confidence: 99%

Section: Emulsification Efficacymentioning

confidence: 99%

See 3 more Smart Citations

Development and evaluation of doxorubicin self nanoemulsifying drug delivery system with Nigella Sativa oil against human hepatocellular carcinoma

Usmani

Mishra

Ali

et al. 2019

Artificial Cells, Nanomedicine, and Biotechnology

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Protective effect of thymoquinone nanoemulsion in reducing the cardiotoxic effect of 5‐fluorouracil in rats

Karim,

Arabameri,

Alimoradi

et al. 2024

Drug Development Research

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Abstract5‐Fluorouracil (5‐FU), which is one of the most widely used chemotherapy drugs, has various side effects on the heart. Thymoquinone (TMQ), the main bioactive component of Nigella sativa, has antioxidant and protective effects against toxicity. In this study, we investigated the protective effect of thymoquinone against cardiotoxicity caused by 5‐FU in vitro and in vivo models. H9C2 cells were exposed to 5‐FU and TMQ, and cell viability was evaluated in their presence. Also, 25 male Wistar rats were divided into five control groups, 5‐FU, 2.5, and 5 mg TMQ in nanoemulsion form (NTMQ) + 5‐FU and 5 mg NTMQ. Cardiotoxicity was assessed through electrocardiography, cardiac enzymes, oxidative stress markers, and histopathology. 5‐FU induced cytotoxicity in H9c2 cells, which improved dose‐dependently with NTMQ cotreatment. 5‐FU caused body weight loss, ECG changes (increased ST segment, prolonged QRS, and QTc), increased cardiac enzymes (aspartate aminotransferase [AST], creatine kinase‐myocardial band [CK‐MB], and lactate dehydrogenase [LDH]), oxidative stress (increased malondialdehyde, myeloperoxidase, nitric acid; decreased glutathione peroxidase enzyme activity), and histological damage such as necrosis, hyperemia, and tissue hyalinization in rats. NTMQ ameliorated these 5‐FU‐induced effects. Higher NTMQ dose showed greater protective effects. Thus, the results of our study indicate that NTMQ protects against 5‐FU cardiotoxicity likely through antioxidant mechanisms. TMQ warrants further research as an adjuvant to alleviate 5‐FU chemotherapy side effects.

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Green NP‐HPTLC and green RP‐HPTLC methods for the determination of thymoquinone: A contrast of validation parameters and greenness assessment

Foudah

Shakeel

Alqarni

et al. 2021

Phytochemical Analysis

Self Cite

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Introduction Thymoquinone (TQ) is a naturally derived bioactive compound with several therapeutic effects. Objective The highly sensitive, rapid and green normal‐phase (NP)/reversed‐phase (RP) high‐performance thin‐layer chromatography (HPTLC) densitometry technique was developed for the determination of TQ in various plant extracts of different geographical regions, commercial capsules, creams and essential oils. Methodology The NP densitometry estimation of TQ was performed using a cyclohexane–ethyl acetate (90:10, v/v) green solvent system, while, the RP‐densitometry estimation of TQ was performed using an ethanol–water (80:20, v/v) green solvent system. The estimation of TQ was conducted at 259 nm. Results The NP and RP densitometry techniques were observed linear in the range of 25–1000 and 50–600 ng/band, respectively. All validation parameters such as accuracy, precision, robustness and sensitivity of NP/RP densitometry were observed within the limit of regulatory requirements and hence found to be suitable for the determination of TQ. The TQ contents were found to be highest in the Saudi Arabian extract followed by the Syrian extract, Indian extract, commercial capsules, commercial creams, Jordanian extract, Egyptian extract, Palestinian extract and commercial essential oils using NP densitometry. The TQ contents were found in same order using RP densitometry, but they were much lower than those recorded using NP densitometry. The Analytical GREEnness (AGREE) scores of NP and RP densitometry were found to be 0.82 and 0.84, respectively, suggesting an excellent greenness profile. Conclusions Based on these results, NP/RP densitometry was found to be suitable for the pharmaceutical assay of TQ.

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Oral bioavailability enhancement and hepatoprotective effects of thymoquinone by self-nanoemulsifying drug delivery system

Cited by 77 publications

References 47 publications

Development and evaluation of doxorubicin self nanoemulsifying drug delivery system with Nigella Sativa oil against human hepatocellular carcinoma

Development and evaluation of doxorubicin self nanoemulsifying drug delivery system with Nigella Sativa oil against human hepatocellular carcinoma

Protective effect of thymoquinone nanoemulsion in reducing the cardiotoxic effect of 5‐fluorouracil in rats

Green NP‐HPTLC and green RP‐HPTLC methods for the determination of thymoquinone: A contrast of validation parameters and greenness assessment

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