Thymoquinone-loaded nanostructured lipid carriers: preparation, gastroprotection, in vitro toxicity, and pharmacokinetic properties after extravascular administration

Abdelwahab, Siddig Ibrahim; Sheikh, Bassem Y.; Taha, Manal Mohamed Elhassan; How, Chee Wun; Abdullah, Rasedee; Yagoub, Umar; El-Sunousi, Rashad; Eid, Eltayeb E M

doi:10.2147/ijn.s44108

Cited by 104 publications

(58 citation statements)

References 38 publications

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“…4 Active principles from natural sources with anti cancer properties exhibit their activities via apoptotic and cell-signaling pathways, and act Although natural products have strong therapeutic values, many of their derivatives have poor water solubility and bioavailability, which severely limit their use in medicine. 6 The nanoparticle delivery systems are newly introduced methods to overcome these limitations, turning potential but poorly soluble drugs into effective therapeutic agents. 7 Among the nanoparticles, lipid nanoparticles are particularly compatible for use in humans and animals.…”

Section: Introductionmentioning

confidence: 99%

Antileukemic effect of zerumbone-loaded nanostructured lipid carrier in WEHI-3B cell-induced murine leukemia model

Rahman¹,

Abdullah²,

How³

et al. 2015

IJN

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Cancer nanotherapy is progressing rapidly with the introduction of many innovative drug delivery systems to replace conventional therapy. Although the antitumor activity of zerumbone (ZER) has been reported, there has been no information available on the effect of ZER-loaded nanostructured lipid carrier (NLC) (ZER-NLC) on murine leukemia cells. In this study, the in vitro and in vivo effects of ZER-NLC on murine leukemia induced with WEHI-3B cells were investigated. The results from 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide, Hoechst 33342, Annexin V, cell cycle, and caspase activity assays showed that the growth of leukemia cells in vitro was inhibited by ZER-NLC. In addition, outcomes of histopathology, transmission electron microscopy, and Tdt-mediated dUTP nick-end labeling analyses revealed that the number of leukemia cells in the spleen of BALB/c leukemia mice significantly decreased after 4 weeks of oral treatment with various doses of ZER-NLC. Western blotting and reverse-transcription quantitative polymerase chain reaction assays confirmed the antileukemia effects of ZER-NLC. In conclusion, ZER-NLC was shown to induce a mitochondrial-dependent apoptotic pathway in murine leukemia. Loading of ZER in NLC did not compromise the anticancer effect of the compound, suggesting ZER-NLC as a promising and effective delivery system for treatment of cancers.

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Section: Introductionmentioning

confidence: 99%

Antileukemic effect of zerumbone-loaded nanostructured lipid carrier in WEHI-3B cell-induced murine leukemia model

Rahman¹,

Abdullah²,

How³

et al. 2015

IJN

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“…Thymoquine's free-radical binding activity can protect the tissue and prevent the formation of ethanol-induced gastric ulcers. 61 Finally, paeonol, which is found in the plant genus Paeonia, has protective action against ultraviolet B (UVB)-induced melanogenesis. Paeonol has been shown to inhibit tyrosinase, which is activated by UVB and produces melanin.…”

Section: Application To Bacterial Infectionmentioning

confidence: 99%

“…65 Thymoquinone, the main bioactive component in Nigella sativa, when encapsulated in a lipid nanocarrier, had a six-fold increase in bioavailability compared to that of free thymoquinone and it showed an increase in gastrointestinal protective properties. 61,82 Natamycin, an antifungal agent produced by the bacterium Streptomyces natalensis, is commercially available for the treatment of corneal fungal infections. Bhatta et al 83 used lecithin mucosal adhesive nanoparticles to deliver natamycin and compared it to the commercially available natamycin ophthalmic suspension (USP Natamet).…”

mentioning

confidence: 99%

Natural product-based nanomedicine: recent advances and issues

Watkins¹,

Wu²,

Zhang³

et al. 2015

IJN

163

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Natural products have been used in medicine for many years. Many top-selling pharmaceuticals are natural compounds or their derivatives. These plant- or microorganism-derived compounds have shown potential as therapeutic agents against cancer, microbial infection, inflammation, and other disease conditions. However, their success in clinical trials has been less impressive, partly due to the compounds’ low bioavailability. The incorporation of nanoparticles into a delivery system for natural products would be a major advance in the efforts to increase their therapeutic effects. Recently, advances have been made showing that nanoparticles can significantly increase the bioavailability of natural products both in vitro and in vivo. Nanotechnology has demonstrated its capability to manipulate particles in order to target specific areas of the body and control the release of drugs. Although there are many benefits to applying nanotechnology for better delivery of natural products, it is not without issues. Drug targeting remains a challenge and potential nanoparticle toxicity needs to be further investigated, especially if these systems are to be used to treat chronic human diseases. This review aims to summarize recent progress in several key areas relevant to natural products in nanoparticle delivery systems for biomedical applications.

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“…The trend of using palm oil based materials for the development of polymeric drug vehicles is growing due to the natural polymer's biocompatibility compared to the petrochemical-based polymers [6][7][8][9][10][11]. In addition, the synthetic polymers commonly use chemicals that emits greenhouse gases (GHGs), utilizes high energy during the products preparation and processing and most importantly generates toxic by-products [12].…”

Section: Introductionmentioning

confidence: 99%

Palm Oil-Based Precursors for Development of Polymeric Delivery System

Tajau

Rohani²,

Isahak³

et al. 2017

MJAS

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The use of precursors from natural based polymers offer a more biocompatible and biodegradable properties in producing polymer drug vehicle compared to drug vehicles made from synthetic polymer precursors, which normally found in high molecular weight (MW). High MW polymer will lead to immunologic inflammatory responses due to their lower biodegradability and higher cytotoxicity compared to low MW that could give smaller particle size, higher solubility, higher release efficiency, non-immunogenic, better biodegradability and lower cytotoxicity. Therefore, this study is aimed to produce valuable precursors, particularly to produce epoxidized palm olein (EPOo) and diol, to be used in the development of a new polymeric drug vehicle with low MW. An EPOo was synthesized via in-situ epoxidizing of palm olein (POo) with peracid and sulfuric acid (H 2 SO 4 ) catalyst. Meanwhile the diol was synthesized using hydroxylation of palm oil-based oleic acid via esterification of oleic acid (OA) with glycerol and 4-dodecylbenzyl sulfonic acid catalyst (DBSA). It was found that both palm oil-based precursors have been successfully synthesized from natural resources of palm oil. Physico-chemical properties of the synthesized precursors showed that the EPOo and the diol possess average molecular weight (MW) between 900-1500 g/mol and hydroxyl functionality between 2 and 3, based on the presence of hydroxyl (O-H) group functionality, showed in the Infra-red (IR) spectra in the range of 3200-3600 cm -1 . These low MW palm oil based-precursors have potential uses for the design and development of new properties of polymeric drug vehicle such as acrylated palm olein (APOo) and polyol polyester, which will produce particle size in the range of 100 -200 nm or smaller with high efficiency drug loading and controlled release profiles.Keywords: drug delivery system, palm oil, polymeric nanoparticle Abstrak Penggunaan pelopor dari polimer semulajadi bagi menghasilkan penyampai ubat polimer mempunyai kelebihan tertentu iaitu ianya bersifat bioserasi dan biodegradasi berbanding sistem penyampai ubat yang dibuat daripada pelopor polimer sintetik, kebiasaannya mempunyai berat molekul (MW) yang tinggi. Polimer dengan MW yang tinggi boleh menyebabkan gerak balas keradangan keimunan akibat kurang keterbiodegradasikan dan kesitotoksikan yang tinggi dibandingkan MW yang rendah yang boleh menghasilkan partikel bersaiz lebih kecil, keterlarutan dan kecekapan perlepasan yang tinggi, tidak imunogen, terbiodegradasi dengan lebih baik dan sitotoksiti yang rendah. Oleh itu, kajian ini bertujuan menghasilkan pelopor yang bersifat istimewa, terutamanya minyak sawit olein terepoksida (EPOo) dan diol yang digunakan dalam membangunkan sistem penyampaian ubat dengan MW yang rendah. EPOo telah disintesis menggunakan pengepoksidaan in-situ minyak sawit olein (POo) dengan perasid dan pemangkin asid sulfurik (H 2 SO 4 ). Sementara itu, diol disintesis menggunakan penghidroksilan minyak sawit oleik menggunakan pengesteran asid oleik (OA) dengan gliserol dan p...

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Thymoquinone-loaded nanostructured lipid carriers: preparation, gastroprotection, in vitro toxicity, and pharmacokinetic properties after extravascular administration

Cited by 104 publications

References 38 publications

Antileukemic effect of zerumbone-loaded nanostructured lipid carrier in WEHI-3B cell-induced murine leukemia model

Antileukemic effect of zerumbone-loaded nanostructured lipid carrier in WEHI-3B cell-induced murine leukemia model

Natural product-based nanomedicine: recent advances and issues

Palm Oil-Based Precursors for Development of Polymeric Delivery System

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