Thymoquinone Loaded in Nanostructured Lipid Carrier Showed Enhanced Anticancer Activity in 4T1 Tumor-Bearing Mice

Ong, Yong Sze; Yazan, Latifah Saiful; Ng, Wei Keat; Abdullah, Rasedee; Mustapha, Noordin Mohamed; Sapuan, S. M.; Foo, Jhi Biau; Tor, Yin Sim; How, Chee Wun; Rahman, Napsiah Abd; Ansar, Fatin Hannani Zakarial

doi:10.2217/nnm-2017-0322

Cited by 32 publications

(19 citation statements)

References 45 publications

(51 reference statements)

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“…However, this is not always true as it has been shown that the capacity of NLCs loaded with chemotherapeutic agents in demonstrating higher anticancer activity compared to the free drug is of question. For instance, optimized thymoquinone-loaded NLCs exhibited lower anticancer activity compared to free thymoquininone after oral administration in 4T1 mammary carcinoma in mice although animals treated with drug-loaded NLCs showed higher survival rates than those treated with free DOX [97]. These findings suggest that the enhancement of the physiochemical and pharmacokinetic properties by NLCs may not always be accompanied with a higher anticancer activity in vivo.…”

Section: Applications Of Nlcs In Delivery Of Chemotherapeutic Agentsmentioning

confidence: 98%

Nanostructured Lipid Carriers for Delivery of Chemotherapeutics: A Review

et al. 2020

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The efficacy of current standard chemotherapy is suboptimal due to the poor solubility and short half-lives of chemotherapeutic agents, as well as their high toxicity and lack of specificity which may result in severe side effects, noncompliance and patient inconvenience. The application of nanotechnology has revolutionized the pharmaceutical industry and attracted increasing attention as a significant means for optimizing the delivery of chemotherapeutic agents and enhancing their efficiency and safety profiles. Nanostructured lipid carriers (NLCs) are lipid-based formulations that have been broadly studied as drug delivery systems. They have a solid matrix at room temperature and are considered superior to many other traditional lipid-based nanocarriers such as nanoemulsions, liposomes and solid lipid nanoparticles (SLNs) due to their enhanced physical stability, improved drug loading capacity, and biocompatibility. This review focuses on the latest advances in the use of NLCs as drug delivery systems and their preparation and characterization techniques with special emphasis on their applications as delivery systems for chemotherapeutic agents and different strategies for their use in tumor targeting.

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Section: Applications Of Nlcs In Delivery Of Chemotherapeutic Agentsmentioning

confidence: 98%

Nanostructured Lipid Carriers for Delivery of Chemotherapeutics: A Review

et al. 2020

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“…50,51 Hence, based on the particles size, PDI, zeta potential and encapsulation efficiency, TQ-NLC can be classified as an ideal nanoformulation with ideal characteristics such as small mean diameter (less than 50 nm), low polydispersity index (less than 0.2), excellent encapsulation and reduced toxicity. 21,22,52 The distribution of the nanoparticles within the body is mainly influenced by these characteristics. 53 The release profile of TQ-NLC showed that the concentration of TQ released by NLC was not equivalent to the concentration of TQ alone even after 72 h. Hence, in contrast to pure TQ solution (which showed the burst release profile), the absence of concentration spike was anticipated when the cells were treated with TQ-NLC.…”

Section: Discussionmentioning

confidence: 99%

<p>Pharmacokinetics and Biodistribution of Thymoquinone-loaded Nanostructured Lipid Carrier After Oral and Intravenous Administration into Rats</p>

Ansar¹,

Latifah²,

Kamal³

et al. 2020

IJN

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Background: Thymoquinone (TQ), an active compound isolated from Nigella sativa, has been proven to exhibit various biological properties such as antioxidant. Although oral delivery of TQ is valuable, it is limited by poor oral bioavailability and low solubility. Recently, TQ-loaded nanostructured lipid carrier (TQ-NLC) was formulated with the aim of overcoming the limitations. TQ-NLC was successfully synthesized by the high-pressure homogenization method with remarkable physiochemical properties whereby the particle size is less than 100 nm, improved encapsulation efficiency and is stable up to 24 months of storage. Nevertheless, the pharmacokinetics and biodistribution of TQ-NLC have not been studied. This study determined the bioavailability of oral and intravenous administration of thymoquinone-loaded nanostructured lipid carrier (TQ-NLC) in rats and its distribution to organs. Materials and Methods: TQ-NLC was radiolabeled with technetium-99m before the administration to the rats. The biodistribution and pharmacokinetics parameters were then evaluated at various time points. The rats were imaged at time intervals and the percentage of the injected dose/gram (%ID/g) in blood and each organ was analyzed. Results: Oral administration of TQ-NLC exhibited greater relative bioavailability compared to intravenous administration. It is postulated that the movement of TQ-NLC through the intestinal lymphatic system bypasses the first metabolism and therefore enhances the relative bioavailability. However, oral administration has a slower absorption rate compared to intravenous administration where the AUC 0-∞ was 4.539 times lower than the latter. Conclusion: TQ-NLC had better absorption when administered intravenously compared to oral administration. However, oral administration showed greater bioavailability compared to the intravenous route. This study provides the pharmacokinetics and biodistribution profile of TQ-NLC in vivo which is useful to assist researchers in clinical use.

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“…This work overcame the limitation of applying the CEO to aqueous-based foods. 26 Currently, various novel and innovative NLC have been produced as a carrier to target anticancer functions such as zerumbone, 27 thymoquinone 28,29 and citral 30 and as a worthy drug observably increased antitumor activity in leukemia and breast tumor cells in vitro and in vivo. More examples of compounds loaded NLC are presented in Table 1.…”

Section: Nanocarriermentioning

confidence: 99%

<p>Novel Drug Delivery Systems for Loading of Natural Plant Extracts and Their Biomedical Applications</p>

Rahman

Othman

Hammadi

et al. 2020

IJN

128

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Many types of research have distinctly addressed the efficacy of natural plant metabolites used for human consumption both in cell culture and preclinical animal model systems. However, these in vitro and in vivo effects have not been able to be translated for clinical use because of several factors such as inefficient systemic delivery and bioavailability of promising agents that significantly contribute to this disconnection. Over the past decades, extraordinary advances have been made successfully on the development of novel drug delivery systems for encapsulation of plant active metabolites including organic, inorganic and hybrid nanoparticles. The advanced formulas are confirmed to have extraordinary benefits over conventional and previously used systems in the manner of solubility, bioavailability, toxicity, pharmacological activity, stability, distribution, sustained delivery, and both physical and chemical degradation. The current review highlights the development of novel nanocarrier for plant active compounds, their method of preparation, type of active ingredients, and their biomedical applications.

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Thymoquinone Loaded in Nanostructured Lipid Carrier Showed Enhanced Anticancer Activity in 4T1 Tumor-Bearing Mice

Cited by 32 publications

References 45 publications

Nanostructured Lipid Carriers for Delivery of Chemotherapeutics: A Review

Nanostructured Lipid Carriers for Delivery of Chemotherapeutics: A Review

<p>Pharmacokinetics and Biodistribution of Thymoquinone-loaded Nanostructured Lipid Carrier After Oral and Intravenous Administration into Rats</p>

<p>Novel Drug Delivery Systems for Loading of Natural Plant Extracts and Their Biomedical Applications</p>

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