Curcumin-loaded solid lipid nanoparticles have prolonged in vitro antitumour activity, cellular uptake and improved in vivo bioavailability

Sun, Jiabei; Bi, Chao; Chan, Ho-Leung; Sun, Song Yung; Zhang, Qingwen; Zheng, Ying

doi:10.1016/j.colsurfb.2013.06.032

Cited by 240 publications

(128 citation statements)

References 43 publications

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“…SLNs showed a sustained the release of curcumin, as opposed to spontaneous diffusion of free curcumin control, dissolved only in 10 mM Tween 60 . A biphasic release pattern was observed: the sustained release profile showed an initial burst release 20,22 . The release processes of all the systems were analyzed up to 100 h. There was an initial burst release of 20-25 of curcumin within 9-10 h, which was due to the weakly adsorbed curcumin.…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

Effects of Fatty Acids on the Interfacial and Solution Behavior of Mixed Lipidic Aggregates Called Solid Lipid Nanoparticles

et al. 2016

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Section: In Vitro Release Studiesmentioning

confidence: 99%

Effects of Fatty Acids on the Interfacial and Solution Behavior of Mixed Lipidic Aggregates Called Solid Lipid Nanoparticles

et al. 2016

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“…The previous findings of Sharma et al (2004) showed that the oral dosing of curcumin (3.6 g) produced the plasma curcumin level of 11.1 nmol/l after an hour of dosing in a human clinical trial . Furthermore, intravenous administration of unformulated curcumin (2 mg/kg) via the tail vain to rats showed better availability of curcumin 6.6 µg/ml in the blood plasma concentration (Sun et al 2013).…”

Section: Pharmacokinetics Of Curcuminmentioning

confidence: 99%

Curcumin and its allied analogues: epigenetic and health perspectives - a review

Imran¹,

Nadeem²,

Khan³

et al. 2017

Czech J. Food Sci.

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Curcumin (diferuoyl methane) is a yellow active ingredient present in turmeric. It is a homodimer of feruloylmethane that comprises a hydroxyl and methoxy group (heptadiene with two Michael acceptors), and α-, β-diketone. It contains various metabolites, i.e. hexahydrocurcumin (HHC), tetrahydrocurcumin (THC), octahydrocurcumin (OHC), dihydrocurcumin (DHC), curcumin sulphate, and curcumin glucuronide. Curcumin has been proven the most effective histone deacetylase (HDAC) inhibitor in HeLa nuclear extracts. It has the ability to affect the Akt, growth factors, NF-kB, and metastatic and angiogenic pathways. Curcumin has a strong therapeutic or preventive potential against several major human ailments, i.e. suppression of inflammation, cardiovascular, diabetes, tumorigenesis, chronic fatigue, antidepressant and neurological activities, depression, loss of muscle and bone, and neuropathic pain. In future, higher utilisation of curcumin as an active agent in food based products is required to curtail the human health disorders.

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“…In an effort to address these limitations, various curcumin delivery systems have been investigated, including solid dispersion, liposomes, polymeric nanoparticles (Grama et al, 2011;Verderio et al, 2013). These systems suffer from several drawbacks, such as poor physical stability, drug leakage, and the potential toxicity of the excipients (Sun et al, 2013). Solid lipid nanoparticles (SLNs) have recently been under consideration for drug delivery because they offer the possibility of modulating drug release and provide both stability and compatibility while avoiding the shortcomings of liposomes, including undesired stability problems and the potential toxicity of the materials such as polymeric nanoparticles (Saupe & Rades, 2006;Vaghasiya et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improvedin vivooral bioavailability andin situintestinal absorption of curcumin

Tang

et al. 2014

Drug Delivery

134

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Purpose: The present study was to formulate curcumin solid lipid nanoparticles (Cur-SLNs) with P-gp modulator excipients, TPGS and Brij78, to enhance the solubility and bioavailability of curcumin. Methods: The formulation was optimized by Plackett-Burman screening design and Box-Behnken experiment design. Then physiochemical properties, entrapment efficiency and in vitro release of Cur-SLNs were characterized. In vivo pharmacokinetics study and in situ single-pass intestinal perfusion were performed to investigate the effects of Cur-SLNs on the bioavailability and intestinal absorption of curcumin. Results: The optimized formulations showed an average size of 135.3 ± 1.5 nm with a zeta potential value of À24.7 ± 2.1 mV and 91.09% ± 1.23% drug entrapment efficiency, meanwhile displayed a sustained release profile. In vivo pharmacokinetic study showed AUC 0!t for Cur-SLNs was 12.27-folds greater than curcumin suspension and the relative bioavailability of Cur-SLNs was 942.53%. Meanwhile, T max and t 1/2 of curcumin for Cur-SLNs were both delayed comparing to the suspensions (p50.01). The in situ intestinal absorption study revealed that the effective permeability (P eff ) value of curcumin for SLNs was significantly improved (p50.01) comparing to curcumin solution. Conclusion: Cur-SLNs with TPGS and Brij78 could improve the oral bioavailability and intestinal absorption of curcumin effectively. KeywordsCurcumin, in situ intestinal absorption, oral bioavailability, P-glycoprotein, solid lipid nanoparticles History

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Curcumin-loaded solid lipid nanoparticles have prolonged in vitro antitumour activity, cellular uptake and improved in vivo bioavailability

Cited by 240 publications

References 43 publications

Effects of Fatty Acids on the Interfacial and Solution Behavior of Mixed Lipidic Aggregates Called Solid Lipid Nanoparticles

Effects of Fatty Acids on the Interfacial and Solution Behavior of Mixed Lipidic Aggregates Called Solid Lipid Nanoparticles

Curcumin and its allied analogues: epigenetic and health perspectives - a review

Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improvedin vivooral bioavailability andin situintestinal absorption of curcumin

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