Development of chrysin loaded poloxamer micelles and toxicity evaluation in fish embryos

Sassa-deepaeng, Tanongsak; Pikulkaew, Surachai; Okonogi, Siriporn

doi:10.5582/ddt.2016.01039

Cited by 13 publications

(7 citation statements)

References 30 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Nanoemulsion is a classical type of nanoformulations and generally comprises oil, water, surfactant, cosurfactant, and target drug . Nanoemulsion and other types of nanoformulations (e.g., micelles and nanoparticles) have been widely used to improve the oral absorption of poorly soluble drugs due to their great ability to enhance drug dissolution. − Several recent studies have explored the potential of nanoformulations for intestinal absorption improvement of presystemically metabolized drugs. − The nanoemulsions containing pharmaceutical excipients (PEs) capable of inhibiting enzyme activities (e.g., labrasol and cremophor EL) can greatly enhance the oral absorption of drugs by decreasing their metabolism. , This PE strategy for the bioavailability enhancement is feasible and advantageous because (1) many commonly used PEs are potent activity modifiers of drug-metabolizing enzymes; − and (2) commonly used PEs are considered safe in humans without significant toxicity concerns . Therefore, enzyme inhibitory PE-based nanoemulsions represent a promising approach to overcome the poor bioavailability of presystemically metabolized drugs.…”

Section: Introductionmentioning

confidence: 99%

Sodium Oleate-Based Nanoemulsion Enhances Oral Absorption of Chrysin through Inhibition of UGT-Mediated Metabolism

et al. 2016

View full text Add to dashboard Cite

Oral bioavailability of flavonoids (and many phenolic drugs) is severely limited by extensive first-pass glucuronidation. Here we aimed to determine the modulatory effects of commonly used pharmaceutical excipients (PEs) on UDP-glucuronosyltransferase (UGT) activities and to evaluate the potential of nanoemulsions containing a UGT-inhibitory PE for oral absorption enhancement of chrysin, a model flavonoid. The effects of PEs on glucuronidation were determined using tissue (liver and intestine) microsomes, expressed UGT1A1 enzyme, and UGT1A1-overexpressing HeLa cells. Nanoemulsions were prepared using a modified emulsification technique and subsequently characterized by particle size, zeta-potential, morphology, and in vitro drug release. Pharmacokinetic studies were performed with rats to assess the effects of nanoemulsions on the metabolism and pharmacokinetics of chrysin. Of 21 PEs, five (i.e., Brij 35, Brij 58, labrasol, sodium oleate, and Tween 20) significantly inhibited chrysin glucuronidation. Of note, sodium oleate was the most potent inhibitor of glucuronidation. Eight PEs including Tween 80 had no effects on glucuronidation of chrysin. The chrysin nanoemulsions prepared with sodium oleate (named SO-NE) were spherical or near-spherical (particle size, 83.2 nm; zeta-potential, -43.7 mV; entrapment efficiency, 89.5%). The reference nanoemulsions prepared with Tween 80 (T80-NE) were highly similar to SO-NE in terms of particle size, zeta-potential, and drug release. It was demonstrated in pharmacokinetic studies that SO-NE led to a 4.3-fold increase in systemic exposure of chrysin and a 3.5-fold increase in C value, whereas T80-NE did not cause any changes in chrysin pharmacokinetics. In conclusion, sodium oleate-based nanoemulsions greatly enhanced oral absorption of chrysin. Oral absorption enhancement of chrysin was attained through targeted inhibition of first-pass glucuronidation by sodium oleate.

show abstract

Section: Introductionmentioning

confidence: 99%

Sodium Oleate-Based Nanoemulsion Enhances Oral Absorption of Chrysin through Inhibition of UGT-Mediated Metabolism

et al. 2016

View full text Add to dashboard Cite

show abstract

“…19 They can therefore be used as drug carriers to the brain. 20 Another interesting work has pointed out the use of naturally occurring flavonoid chrysin. It has been reported to prevent cognitive decline mediated by decreasing oxidative stress by regulating BDNF levels.…”

Section: ■ Introductionmentioning

confidence: 99%

“…Originating from a natural source, they are less toxic and provide additional immunostimulatory properties . They can therefore be used as drug carriers to the brain . Another interesting work has pointed out the use of naturally occurring flavonoid chrysin.…”

Section: Introductionmentioning

confidence: 99%

Chrysin-Loaded Chitosan Nanoparticle-Mediated Neuroprotection in Aβ_1–42-Induced Neurodegenerative Conditions in Zebrafish

Saleem

Banerjee²,

Kannan

2022

ACS Chem. Neurosci.

View full text Add to dashboard Cite

Amyloid β plaques and neurofibrillary tangles are the characteristic features of Alzheimer's disease (AD). Plaques of amyloid β play a pivotal role in affecting cognitive functions and memory. Alzheimer's disease is a progressive neurodegenerative disease and is one of the leading causes of dementia worldwide. Several treatment strategies focusing on the amyloid cascade have been implemented to treat AD. The blood−brain barrier (BBB) poses the main obstructive barrier by refraining drugs from penetrating the brain. Nanotechnology is a promising research field for brain drug delivery using nanosized particles. Zebrafish is emerging as a model of interest to elaborate on brain targeting and nanotechnology-based therapeutics for neurodegenerative diseases.In the current study, we have synthesized and characterized chrysin-loaded chitosan nanoparticles (Chr-Chi NPs) and evaluated them for neuroprotection against amyloid-β-induced toxicity. We find that treatment with Chr-Chi NPs helps to retain memory, cognition, and synaptic connections, which are otherwise compromised due to Aβ 1−42 toxicity. The NPs further help in reducing aggregates of amyloid β, thus decreasing neuronal death and generation of reactive oxygen species (ROS). Taken together, our study brings to light a novel strategy for treating AD by a combined action on the neurons and amyloid aggregates mediated by chrysin and chitosan, respectively. Chr-Chi NPs, therefore, have the potential to provide a beneficial combinatorial treatment strategy for AD.

show abstract

“…Doxorubicin has been used as an anticancer drug by intercalating DNA strands and inhibiting the growth of cancer cells. The application of nanomicelles led to drug delivery improvement at therapeutic sites with enhanced drug action, increased availability thanks to solubilizing the hydrophobic drugs, and also high thermodynamic stability, prolonged circulation in the blood stream, preferential accumulation in tumor target tissues and overcoming the multiple drug resistance effect . Carriers with structures sensitive to pH and temperature increase drug release power and therapeutic efficacy at disease sites .…”

Section: Introductionmentioning

confidence: 99%

“…The application of nanomicelles led to drug delivery improvement at therapeutic sites with enhanced drug action, increased availability thanks to solubilizing the hydrophobic drugs, and also high thermodynamic stability, prolonged circulation in the blood stream, preferential accumulation in tumor target tissues and overcoming the multiple drug resistance effect. [21][22][23][24][25] Carriers with structures sensitive to pH and temperature increase drug release power and therapeutic efficacy at disease sites. [26][27][28][29] Polymeric micelles have become important for enhancing therapeutic efficiency due to high biocompatibility and drug loading capacity, low toxicity and also highly efficient drug delivery.…”

Section: Introductionmentioning

confidence: 99%

An in vitro focus on doxorubicin hydrochloride delivery of novel pH‐responsive poly(2‐succinyloxyethylmethacrylate) and poly[(N‐4‐vinylbenzyl),N,N‐diethylamine] diblock copolymers

Ghamkhari

Massoumi

Agbolaghi

2018

Polymer International

View full text Add to dashboard Cite

Novel pH‐responsive poly(2‐succinyloxyethylmethacrylate)‐b‐poly[(N‐4‐vinylbenzyl),N,N‐diethylamine] [poly(SEMA‐b‐VEA)] diblock copolymers were synthesized via reversible addition fragmentation transfer (RAFT) polymerization to investigate their self‐assembly micellar behavior. The self‐assembly behaviors of synthesized diblock copolymers with distinct molecular weights (labeled (1) to) were confirmed by 1H NMR spectroscopy, TEM and dynamic light scattering measurements. Doxorubicin hydrochloride (DOX) loading capacity was evaluated, and the in vitro cytotoxicity effect of DOX‐loaded diblock copolymer was also studied by assessing the survival rate of the breast cancer cell line MCF‐7 with 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) assay. The results exhibited remarkable controlled release in the MTT assay. The DOX encapsulation efficiency was calculated to be 96.4%. The size and zeta potential of DOX‐loaded poly(SEMA‐b‐VEA) diblock copolymers were 204 nm and +5.7 mV at a pH of 7.4. DOX release values after 440 h at pH 7.4, 5.4 and 4 were 22.15%, 31.43% and 47.06%, respectively. The released values of DOX‐loaded poly(SEMA‐b‐VEA) and at pH 7.4 were 22.15%, 20.5% and 17.5%, respectively. Cell survival ratios were 18.9%, 23.16% and 16.92% after 72 h. Poly(SEMA‐b‐VEA) copolymers can be considered in nanomedicine applications due to their excellent pH‐responsive micellar behavior. © 2017 Society of Chemical Industry

show abstract

Development of chrysin loaded poloxamer micelles and toxicity evaluation in fish embryos

Cited by 13 publications

References 30 publications

Sodium Oleate-Based Nanoemulsion Enhances Oral Absorption of Chrysin through Inhibition of UGT-Mediated Metabolism

Sodium Oleate-Based Nanoemulsion Enhances Oral Absorption of Chrysin through Inhibition of UGT-Mediated Metabolism

Chrysin-Loaded Chitosan Nanoparticle-Mediated Neuroprotection in Aβ_1–42-Induced Neurodegenerative Conditions in Zebrafish

An in vitro focus on doxorubicin hydrochloride delivery of novel pH‐responsive poly(2‐succinyloxyethylmethacrylate) and poly[(N‐4‐vinylbenzyl),N,N‐diethylamine] diblock copolymers

Contact Info

Product

Resources

About

Development of chrysin loaded poloxamer micelles and toxicity evaluation in fish embryos

Cited by 13 publications

References 30 publications

Sodium Oleate-Based Nanoemulsion Enhances Oral Absorption of Chrysin through Inhibition of UGT-Mediated Metabolism

Sodium Oleate-Based Nanoemulsion Enhances Oral Absorption of Chrysin through Inhibition of UGT-Mediated Metabolism

Chrysin-Loaded Chitosan Nanoparticle-Mediated Neuroprotection in Aβ1–42-Induced Neurodegenerative Conditions in Zebrafish

An in vitro focus on doxorubicin hydrochloride delivery of novel pH‐responsive poly(2‐succinyloxyethylmethacrylate) and poly[(N‐4‐vinylbenzyl),N,N‐diethylamine] diblock copolymers

Contact Info

Product

Resources

About

Chrysin-Loaded Chitosan Nanoparticle-Mediated Neuroprotection in Aβ_1–42-Induced Neurodegenerative Conditions in Zebrafish