Lipid-Drug Conjugates for Oral Bioavailability Enhancement

Hussain, Afzal; Siddique, Mohd Usman Mohd; Singh, Sandeep Kumar; Samad, Abdus; Beg, Sarwar; Wais, Mohammad

doi:10.2174/1877912305666150616220747

Cited by 4 publications

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“…This creates an opportunity for the researchers to come up with different strategies for the enhancement of characterization of phytoconstituent extracts. For enhancing the bioavailability of phytoconstituents, novel solubility enhancement techniques like solid dispersion, complexation, nanocrystals, ultrasonication, and eutectic mixtures provide an alternative approach [4][5][6][7][8]. Silymarin (SL) is the active constituent of Silybum marianum L. Gaertn.…”

Section: Introductionmentioning

confidence: 99%

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

Sherikar

Siddique

et al. 2021

Oxidative Medicine and Cellular Longevity

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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.

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