Silymarin-laden PVP-PEG polymeric composite for enhanced aqueous solubility and dissolution rate: Preparation and in vitro characterization

Yousaf, Abid Mehmood; Rasheed, Usman; Shahzad, Yasser; Mahmood, Tariq; Hussain, Talib

doi:10.1016/j.jpha.2018.09.003

Cited by 54 publications

(40 citation statements)

References 42 publications

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“…One of the recently published research reports a formulation composed by SLM-PVP-PEG (0.25:1.5:1.5, on weight basis) in form of polymeric composite, which promotes an increase in SLM solubility of more than 24 mg/mL and an excellent dissolution profile [124]. The enhancement in drug solubility and dissolution has been attributed to a better SLM wetting driven by the hydrophilic polymers, complete conversion of the crystalline components into the amorphous state and molecular level homogeneousness of SLM, PVP and PEG in the resulting polymeric composite.…”

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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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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“…19,37 That is the why, the formulations VI and VII with higher polymer concentrations showed apparently decreased solubility of bezafibrate. 37,38 Formulation V, consisting of bezafibrate, PVP K30 and cremophor ELP (1/12/1.5, w/w/w), showed apparently the highest solubility of bezafibrate (27.59 ± 4.90 mg/mL) which was about fivefold than that of the corresponding physical mixture. The physical mixture was obtained by simply triturating bezafibrate, PVP K30 and cremophor ELP (1/12/1.5, w/w/w) using a pestle and mortar.…”

Section: Resultsmentioning

confidence: 97%

<p>Electrosprayed Polymeric Nanospheres for Enhanced Solubility, Dissolution Rate, Oral Bioavailability and Antihyperlipidemic Activity of Bezafibrate</p>

Sun¹,

Shen²,

Shafique³

et al. 2020

IJN

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Background: Bezafibrate is a BCS class II drug as it presents very low solubility in water; therefore, its bioavailability after oral administration is very poor. The aim of this work was to enhance solubility and dissolution rate of bezafibrate in water in order to enhance its oral bioavailability. Methods: Several formulations were prepared using PVP K30 and Cremophor ELP employing the solvent-evaporation method and the electrospraying technique. Solubility, release rate, bioavailability in male Sprague Dawley rats, and lipid profile attributes in Wistar rats were assessed in comparison with bezafibrate plain powder. Solid-state characterization was carried out using X-ray diffraction (XRD) analysis, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy and scanning electron microscopy (SEM). Results: All the formulations exerted positive effect towards the desired goal. In particular, the optimized formulation furnished about 14-fold enhanced solubility and 85.48 ± 10.16% drug was released in 10 min as compared with bezafibrate alone (4.06 ± 2.59%). The drug existed in the amorphous state in the prepared sample as confirmed by XRD and DSC, whilst no drug-excipient interactions were observed through FTIR analysis. Moreover, SEM revealed smooth-surfaced spherical particles of the optimized formulation. A 5.5-fold higher oral bioavailability was achieved with the optimized formulation in comparison with bezafibrate plain powder. Also, TG, LDL and TC were decreased, and HDL was increased considerably in HFD-treated rats. Conclusion: The optimized formulation consisting of bezafibrate, PVP K30 and cremophor ELP (1/12/1.5, w/w/w) might be a capable drug delivery system for orally administering poorly water-soluble bezafibrate with improved bioavailability and antihyperlipidemic effects.

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“…One of the recently published research reports a formulation composed by SIL-PVP-PEG (0.25 : 1.5 : 1.5, on weight basis) in form of polymeric composite, which promotes an increase in the SIL solubility of more than 24 mg / ml and an excellent dissolution profile [90]. The enhancement in drug solubility and dissolution has been attributed to a better SIL wetting driven by the hydrophilic of 27…”

Section: Inclusion In Polymeric Matricesmentioning

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-laden PVP-PEG polymeric composite for enhanced aqueous solubility and dissolution rate: Preparation and in vitro characterization

Cited by 54 publications

References 42 publications

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

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

<p>Electrosprayed Polymeric Nanospheres for Enhanced Solubility, Dissolution Rate, Oral Bioavailability and Antihyperlipidemic Activity of Bezafibrate</p>

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

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