Potential of Cationic-Polymeric Nanoparticles for Oral Delivery of Naringenin: In Vitro and In Vivo Investigations

Chaurasia, Sundeep; Patel, Ravi R.; Prasad, Vure; Mishra, Brahmeshwar

doi:10.1016/j.xphs.2017.10.006

Cited by 35 publications

(10 citation statements)

References 67 publications

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“…Zhang et al [94] aimed to improve the oral absorption of baicalin, which has low solubility and poor permeability, by using a micellar formulation comprised of the carriers Pluronic P123 copolymer and sodium taurocholate. Sustained release profile of baicalin-loaded mixed micelles, in in vitro drug release experiment, held in several pH conditions, showed 14% drug released after 2 h in gastric conditions and 54% release within 48 h in intestinal conditions, compared to 34% and 79% release [105], nanoparticles [106][107][108][109][110], phytosome [111], nanoliposome [112], mixed micelles [113,114], SNEDDS [115,116], nanocarrier [117,118], nanoemulsion [119], nanosuspension [ Mixed micelles [129,130], nanoparticles [131,132], solid dispersion [133,134] , SNEDDS [135] , SMEDDS [136], lipid carrier [137], copolymeric micelles [138], exosomes [139] Naringenin DENV, HCV SNEDDS [140], solid dispersion [141], nanoparticles [142,143] , liposome [144], nanosuspension [145,146] In vitro uptake studies, carried out with a caco-2 cell line, determined the absorption of baicalin within the mixed micelles and verified their internalization ability. Baicalin-loaded ST-P123-MMs formulation achieved high oral bioavailability (Fig.…”

Section: Delivery Of Herbal Extracts and Phytochemicalsmentioning

confidence: 99%

Antiviral effect of phytochemicals from medicinal plants: Applications and drug delivery strategies

Ben‐Shabat

Yarmolinsky²,

Porat

et al. 2019

Drug Deliv. and Transl. Res.

287

184

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Viral infections affect three to five million patients annually. While commonly used antivirals often show limited efficacy and serious adverse effects, herbal extracts have been in use for medicinal purposes since ancient times and are known for their antiviral properties and more tolerable side effects. Thus, naturally based pharmacotherapy may be a proper alternative for treating viral diseases. With that in mind, various pharmaceutical formulations and delivery systems including micelles, nanoparticles, nanosuspensions, solid dispersions, microspheres and crystals, self-nanoemulsifying and self-microemulsifying drug delivery systems (SNEDDS and SMEDDS) have been developed and used for antiviral delivery of natural products. These diverse technologies offer effective and reliable delivery of medicinal phytochemicals. Given the challenges and possibilities of antiviral treatment, this review provides the verified data on the medicinal plants and related herbal substances with antiviral activity, as well as applied strategies for the delivery of these plant extracts and biologically active phytochemicals.

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Section: Delivery Of Herbal Extracts and Phytochemicalsmentioning

confidence: 99%

Antiviral effect of phytochemicals from medicinal plants: Applications and drug delivery strategies

Ben‐Shabat

Yarmolinsky²,

Porat

et al. 2019

Drug Deliv. and Transl. Res.

287

184

View full text Add to dashboard Cite

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“…Naringenin has very limited water solubility (46 ± 6.0 μg/mL), gastrointestinal degradation, and low bioavailability, thus providing a major hurdle for its development as a drug and limiting its therapeutic use [ 12 ]. Several approaches have been undertaken to increase its solubility using nanotechnology [ 13 , 14 , 15 , 16 , 17 ]. Kumar et al synthesized chitosan-encapsulated naringenin nanoparticles with antioxidant and anticancer activities [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

Formulation Design, Statistical Optimization, and In Vitro Evaluation of a Naringenin Nanoemulsion to Enhance Apoptotic Activity in A549 Lung Cancer Cells

et al. 2020

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Naringenin (NAR), a flavonoid mainly found in citrus and grapefruits, has proven anti-cancer activities. However, the poor water solubility and low bioavailability of NAR limits its use as a therapeutic agent. The aim of this study was to develop and optimize stable naringenin nanoemulsions (NAR-NE) using a Box–Behnken experimental design to obtain a formulation with a higher efficiency. Anticancer activity of optimized NAR-NE was evaluated in A549 lung cancer cells using cell viability, flow-cytometric assays, and enzyme-linked immunosorbent assay. The stabilized nanoemulsion, which showed a spherical surface morphology, had a globule size of 85.6 ± 2.1 nm, a polydispersity index of 0.263 ± 0.02, a zeta potential of −9.6 ± 1.2 mV, and a drug content of 97.34 ± 1.3%. The NAR release from the nanoemulsion showed an initial burst release followed by a stable and controlled release for a longer period of 24 h. The nanoemulsion exhibited excellent thermodynamic and physical stability against phase separation and storage. The NAR-NE showed concentration-dependent cytotoxicity in A549 lung cancer cells, which was greater than that of free NAR. The percentage of apoptotic cells and cell cycle arrest at the G2/M and pre-G1 phases induced by NAR-NE were significantly higher than those produced by free NAR (p < 0.05). NAR-NEs were more effective than the NAR solution in reducing Bcl2 expression, while increasing pro-apoptotic Bax and caspase-3 activity. Therefore, stabilized NAR-NE could be a suitable drug delivery system to enhance the effects of NAR in the treatment of lung cancer.

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“…Among various physicochemical properties, surface charges have been reported playing a critical role in determining the in vivo behaviors of nanoparticles following oral administration. − Particles with cationic surfaces interact with the negatively charged residues in mucin and are trapped within the mucus, belonging to what is generally called mucus-adhesive particles (MAPs). − Despite reports on the enhancement of oral absorption by MAPs, recent studies suggested that MAPs are not preferred for systemic drug delivery because MAPs may be trapped in the exterior mucus layer and cleared gradually without absorption following the turning over of the mucus . On the contrary, mucus-penetrating particles are able to facilitate the penetration of particles across the mucus layer. − Interestingly, particles with net neutral charges gained attraction for the design of mucus-penetrating particles due to superior mucus-penetrating abilities. , Moreover, surface charges affect the internalization of particles by the intestinal epithelial cells, with cationic surfaces favoring significant and fast internalization. , Nevertheless, there are controversies over the exact role the surface charges play in oral delivery, which is partially ascribed to a lack of understanding of the transport process of intact particles.…”

Section: Introductionmentioning

confidence: 99%

Effect of Surface Charges on Oral Absorption of Intact Solid Lipid Nanoparticles

et al. 2019

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Surface charge is a crucial factor that determines the in vivo behaviors of drug nanocarriers following administration via different routes. However, there is still a lack of comprehensive knowledge of how surface charges affect the in vivo behaviors of particles, especially for oral delivery. In this study, solid lipid nanoparticles (SLNs), as model drug nanocarriers, are modified to bear either anionic, cationic, or net neutral surface charges. The effect of surface charges on oral absorption of intact SLNs was investigated by tracking the in vivo transport of the particles. The fluorescent bioimaging strategy exploits the aggregation-caused quenching property to discriminate the particles. Both in vitro and in vivo lipolysis studies confirm slowed-down lipolysis by anionic charges in comparison with both unmodified and net neutral SLNs but accelerated degradation by cationic charges. The scanning of ex vivo tissues and organs reveals limited absorption of unmodified SLNs into the circulation. Nevertheless, all three types of surface charge modifications are able to enhance the oral absorption of intact SLNs with the fastest and highest absorption observed for net neutral SLNs, possibly owing to promoted mucus penetration. Anionic SLNs, though repulsed by the mucus layer, show the second highest absorption owing to enhanced lymphatic transport. The efficacy of cationic charge modification is less significant due to entrapment and retention in mucus layers as well as increased lability to lipolysis. In conclusion, surface charges may serve as initiators to guide the in vivo behaviors and enhance the oral absorption of intact SLNs.

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Potential of Cationic-Polymeric Nanoparticles for Oral Delivery of Naringenin: In Vitro and In Vivo Investigations

Cited by 35 publications

References 67 publications

Antiviral effect of phytochemicals from medicinal plants: Applications and drug delivery strategies

Antiviral effect of phytochemicals from medicinal plants: Applications and drug delivery strategies

Formulation Design, Statistical Optimization, and In Vitro Evaluation of a Naringenin Nanoemulsion to Enhance Apoptotic Activity in A549 Lung Cancer Cells

Effect of Surface Charges on Oral Absorption of Intact Solid Lipid Nanoparticles

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