Preparation and Evaluation of Silymarin-Loaded Solid Eutectic for Enhanced Anti-Inflammatory, Hepatoprotective Effect: In Vitro–In Vivo Prospect

Solubility of phytochemicals is a major concern for drug delivery, permeability, and their biological response. However, advancements in the novel formulation technologies have been helping to overcome these challenges. The applications of these newer technologies are easy for commercialization and...

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Autores principales: Abdulla Sherikar, Mohd Usman Mohd Siddique, Mahesh More, Sameer N. Goyal, Milan Milivojevic, Saad Alkahtani, Saud Alarifi, Md Saquib Hasnain, Amit Kumar Nayak
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Publicado: Hindawi Limited 2021
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spelling oai:doaj.org-article:16cc38a9421a4b678f0f3e970cbf0abb2021-11-22T01:09:51ZPreparation and Evaluation of Silymarin-Loaded Solid Eutectic for Enhanced Anti-Inflammatory, Hepatoprotective Effect: In Vitro–In Vivo Prospect1942-099410.1155/2021/1818538https://doaj.org/article/16cc38a9421a4b678f0f3e970cbf0abb2021-01-01T00:00:00Zhttp://dx.doi.org/10.1155/2021/1818538https://doaj.org/toc/1942-0994Solubility of phytochemicals is a major concern for drug delivery, permeability, and their biological response. However, advancements in the novel formulation technologies have been helping to overcome these challenges. The applications of these newer technologies are easy for commercialization and high therapeutic outcomes compared to conventional formulations. Considering these facts, the present study is aimed to prepare a silymarin-loaded eutectic mixture with three different ratios of Polyvinylpyrrolidone K30 (PVP K30) and evaluating their anti-inflammatory, and hepatoprotective effects. The preliminary phytochemical and characterization of silymarin, physical mixture, and solid dispersions suggested and successfully confirmed the formation of solid dispersion of silymarin with PVP K30. It was found that the solubility of silymarin was increased by 5-fold compared to pure silymarin. Moreover, the in vitro dissolution displayed that 83% of silymarin released within 2 h with 2.8-fold increase in dissolution rate compared to pure silymarin. Also, the in vivo study suggested that the formulation significantly reduced the carbon tetrachloride- (0.8620±0.05034∗∗ for 1 : 3 ratio), paracetamol- (0.7300±0.01517∗∗ for 1 : 3 ratio), and ethanol- (0.8100±0.04037∗∗ for 1 : 3 ratio) induced hepatotoxicity in rats. Silymarin solid dispersion was prepared using homogenization methods that have prominent anti-inflammatory effect (0.6520±0.008602∗∗ with 8.33%) in carrageenan-induced rat paw model.Abdulla SherikarMohd Usman Mohd SiddiqueMahesh MoreSameer N. GoyalMilan MilivojevicSaad AlkahtaniSaud AlarifiMd Saquib HasnainAmit Kumar NayakHindawi LimitedarticleCytologyQH573-671ENOxidative Medicine and Cellular Longevity, Vol 2021 (2021)
institution DOAJ
collection DOAJ
language EN
topic Cytology
QH573-671
spellingShingle Cytology
QH573-671
Abdulla Sherikar
Mohd Usman Mohd Siddique
Mahesh More
Sameer N. Goyal
Milan Milivojevic
Saad Alkahtani
Saud Alarifi
Md Saquib Hasnain
Amit Kumar Nayak
Preparation and Evaluation of Silymarin-Loaded Solid Eutectic for Enhanced Anti-Inflammatory, Hepatoprotective Effect: In Vitro–In Vivo Prospect
description Solubility of phytochemicals is a major concern for drug delivery, permeability, and their biological response. However, advancements in the novel formulation technologies have been helping to overcome these challenges. The applications of these newer technologies are easy for commercialization and high therapeutic outcomes compared to conventional formulations. Considering these facts, the present study is aimed to prepare a silymarin-loaded eutectic mixture with three different ratios of Polyvinylpyrrolidone K30 (PVP K30) and evaluating their anti-inflammatory, and hepatoprotective effects. The preliminary phytochemical and characterization of silymarin, physical mixture, and solid dispersions suggested and successfully confirmed the formation of solid dispersion of silymarin with PVP K30. It was found that the solubility of silymarin was increased by 5-fold compared to pure silymarin. Moreover, the in vitro dissolution displayed that 83% of silymarin released within 2 h with 2.8-fold increase in dissolution rate compared to pure silymarin. Also, the in vivo study suggested that the formulation significantly reduced the carbon tetrachloride- (0.8620±0.05034∗∗ for 1 : 3 ratio), paracetamol- (0.7300±0.01517∗∗ for 1 : 3 ratio), and ethanol- (0.8100±0.04037∗∗ for 1 : 3 ratio) induced hepatotoxicity in rats. Silymarin solid dispersion was prepared using homogenization methods that have prominent anti-inflammatory effect (0.6520±0.008602∗∗ with 8.33%) in carrageenan-induced rat paw model.
format article
author Abdulla Sherikar
Mohd Usman Mohd Siddique
Mahesh More
Sameer N. Goyal
Milan Milivojevic
Saad Alkahtani
Saud Alarifi
Md Saquib Hasnain
Amit Kumar Nayak
author_facet Abdulla Sherikar
Mohd Usman Mohd Siddique
Mahesh More
Sameer N. Goyal
Milan Milivojevic
Saad Alkahtani
Saud Alarifi
Md Saquib Hasnain
Amit Kumar Nayak
author_sort Abdulla Sherikar
title Preparation and Evaluation of Silymarin-Loaded Solid Eutectic for Enhanced Anti-Inflammatory, Hepatoprotective Effect: In Vitro–In Vivo Prospect
title_short Preparation and Evaluation of Silymarin-Loaded Solid Eutectic for Enhanced Anti-Inflammatory, Hepatoprotective Effect: In Vitro–In Vivo Prospect
title_full Preparation and Evaluation of Silymarin-Loaded Solid Eutectic for Enhanced Anti-Inflammatory, Hepatoprotective Effect: In Vitro–In Vivo Prospect
title_fullStr Preparation and Evaluation of Silymarin-Loaded Solid Eutectic for Enhanced Anti-Inflammatory, Hepatoprotective Effect: In Vitro–In Vivo Prospect
title_full_unstemmed Preparation and Evaluation of Silymarin-Loaded Solid Eutectic for Enhanced Anti-Inflammatory, Hepatoprotective Effect: In Vitro–In Vivo Prospect
title_sort preparation and evaluation of silymarin-loaded solid eutectic for enhanced anti-inflammatory, hepatoprotective effect: in vitro–in vivo prospect
publisher Hindawi Limited
publishDate 2021
url https://doaj.org/article/16cc38a9421a4b678f0f3e970cbf0abb
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