Silymarin-Loaded Nanoparticles Based on Stearic Acid-Modified Bletilla striata Polysaccharide for Hepatic Targeting

Ma, Yan; He, Shaolong; Ma, Xueqin; Hong, Tongtong; Li, Zhifang; Park, Kinam; Wang, Wenping

doi:10.3390/molecules21030265

Cited by 35 publications

(12 citation statements)

References 26 publications

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“…In agreement with results of SEM and DSC analysisis, MTE_mp powder resulted completely amorphous as indicated by PXRD profiles ( Figure 5 ). The diffraction pattern of the MTE raw extract ( Figure 5 , gray line) shows, in the range between 12° and about 50° of 2ϑ, a series of typical reflections of crystalline silymarin complex [ 42 ]. In the MTE_mp pattern, all the peaks of MTE raw extract disappeared.…”

Section: Resultsmentioning

confidence: 99%

Application of Spray Drying Particle Engineering to a High-Functionality/Low-Solubility Milk Thistle Extract: Powders Production and Characterization

et al. 2018

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Many natural compounds having antioxidant and anti-inflammatory activity are a potential target for new therapies against chronic inflammatory syndromes. The oral administration of functional herbal supplements may become a prevention strategy or therapy adjuvant for susceptible patients. A case study is our milk thistle (Silybum marianum) extract rich in silymarin complex. A water-soluble microencapsulated powder system was developed by a spray drying technique to improve the poor silymarin bioactivity after oral administration. Sodium carboxymethylcellulose (NaCMC) was employed as coating/swelling polymer matrix and sodium lauryl sulfate (SLS) as the surfactant (1:1:0.05 w/w/w). A H2O/EtOH/acetone (50/15/35 v/v/v) solvent system was used as liquid feed. The microsystems were capable of improving the in vitro dissolution and permeation rates, suggesting an enhancement of bioactivity after oral administration. The microsystems protect the antioxidant activity of silymarin after harsh storage conditions period and do not affect the anti-inflammatory properties of the raw extract (efficient already at lower concentrations of 0.312 mg/mL) to reduce dendritic cells (DCs) inflammatory cytokine secretion after lipopolysaccharide administration. This approach allows managing particle size, surface properties and release of bioactive agents improving the bioactivity of a herbal supplement and is also possibly applicable to many other similar natural products.

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Section: Resultsmentioning

confidence: 99%

Application of Spray Drying Particle Engineering to a High-Functionality/Low-Solubility Milk Thistle Extract: Powders Production and Characterization

et al. 2018

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“…Ma et al [135] used the Bletilla striata polysaccharide (BSP) modified with SA to encapsulate SLM into self-assembled spherical NPs with a mean diameter of 200 nm. Compared to the drug suspension, the developed formulation with SLM EE of about 80%, was able to improve cytotoxicity and cell uptake in HepG2 cell lines in vitro.…”

Section: Formulation Strategies Designed To Improve the Bioavailabmentioning

confidence: 99%

Formulation Strategies for Enhancing the Bioavailability of Silymarin: The State of the Art

2019

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Silymarin, a mixture of flavonolignan and flavonoid polyphenolic compounds extractable from milk thistle (Silybum marianum) seeds, has anti-oxidant, anti-inflammatory, anti-cancer and anti-viral activities potentially useful in the treatment of several liver disorders, such as chronic liver diseases, cirrhosis and hepatocellular carcinoma. Equally promising are the effects of silymarin in protecting the brain from the inflammatory and oxidative stress effects by which metabolic syndrome contributes to neurodegenerative diseases. However, although clinical trials have proved that silymarin is safe at high doses (>1500 mg/day) in humans, it suffers limiting factors such as low solubility in water (<50 μg/mL), low bioavailability and poor intestinal absorption. To improve its bioavailability and provide a prolonged silymarin release at the site of absorption, the use of nanotechnological strategies appears to be a promising method to potentiate the therapeutic action and promote sustained release of the active herbal extract. The purpose of this study is to review the different nanostructured systems available in literature as delivery strategies to improve the absorption and bioavailability of silymarin.

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“…Ma et al [100] used the Bletilla striata polysaccharide (BSP) modified with stearic acid to encapsulate SIL into self-assembled spherical NPs with a mean diameter of 200 nm. Compared to the drug suspension, the developed formulation with SIL encapsulation efficiency of about 80%, was able to improve cytotoxicity and cell uptake in HepG2 cell lines in vitro.…”

Section: Dendrimers and Polymeric Npsmentioning

confidence: 99%

Advanced Nanotechnologies for Enhancing the Bioavailability of Silymarin: A State of the Art

Costanzo¹,

Angelico²

2019

Preprint

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Silymarin, a mixture of flavonolignan and flavonoid polyphenolic compounds extractable from the milk thistle seed, Silybum marianum, has anti-oxidant, anti-inflammatory, anti-cancer and anti-viral activities potentially useful in the treatment of several liver disorders, such as chronic liver diseases, cirrhosis and hepatocellular carcinoma. Equally promising are the effects of silymarin in protecting the brain from the inflammatory and oxidative stress effects by which metabolic syndrome contributes to neurodegenerative diseases. However, despite clinical trials have proved that silymarin is safe at high doses (>1500 mg/day) in humans, it suffers limiting factors such as low solubility in water (<50 μg/mL), low bioavailability and poor intestinal absorption. To improve its bioavailability and provide a prolonged silymarin release at the site of absorption, the use of nanotechnological strategies appears to be a promising method to potentiate the therapeutic action and promote sustained release of the active herbal extract. The purpose of this study is to review the different nanostructured systems available in literature as delivery strategies to improve the absorption and bioavailability of silymarin.

show abstract

Silymarin-Loaded Nanoparticles Based on Stearic Acid-Modified Bletilla striata Polysaccharide for Hepatic Targeting

Cited by 35 publications

References 26 publications

Application of Spray Drying Particle Engineering to a High-Functionality/Low-Solubility Milk Thistle Extract: Powders Production and Characterization

Application of Spray Drying Particle Engineering to a High-Functionality/Low-Solubility Milk Thistle Extract: Powders Production and Characterization

Formulation Strategies for Enhancing the Bioavailability of Silymarin: The State of the Art

Advanced Nanotechnologies for Enhancing the Bioavailability of Silymarin: A State of the Art

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