Development, Physicochemical Characterization and In Vitro Anti-Inflammatory Activity of Solid Dispersions of α,β Amyrin Isolated from Protium Oilresin

Abstract

α,β Amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has shown a variety of pharmacological properties, including anti-inflammatory effect. ABAM is isolated from Burseraceae oilresins, especially from the Protium species, which is commonly found in the Brazilian Amazon. This work aimed to develop solid dispersions (SD) of ABAM with the following hydrophilic polymers: polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG-6000) and hydroxypropylmethylcellulose (HPMC). The SDs were prepared by physical mixture (PM), kneading (KND) and rotary evaporation (RE) methods. In order to verify any interaction between ABAM and the hydrophilic polymers, physicochemical characterization was performed by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), powder X-ray diffraction (XRD), thermogravimetry (TG) and differential scanning calorimetry (DSC) analysis. Furthermore, an in vitro anti-inflammatory assay was performed with ABAM alone and as SDs with the hydrophilic polymers. The results from the characterization analysis show that the SDs were able to induce changes in the physicochemical properties of ABAM, which suggests interaction with the polymer matrix. In vitro anti-inflammatory assay showed that the SDs improved the anti-inflammatory activity of ABAM and showed no cytotoxicity. In conclusion, this study showed the potential use of SDs as an efficient tool for improving the stability and anti-inflammatory activity of ABAM without cytotoxicity.

Novel Solid Dispersions of Naphthoquinone Using Different Polymers for Improvement of Antichagasic Activity

“…The TG curve of the PVP exhibited two mass losses: the first, in the range of 30 to 100 °C, with a mass variation of 8.77%, corresponding to the presence of water; the second, in the range of 357 to 480 °C, with a mass loss of 83.16%, attributed to the process of thermal polymer degradation, corroborating the literature [35,36]. For SDs with PVP, in the range of 137 to 245 °C, mass variations of 3.53% (IVS320-PVP/RE) and 1% (IVS320-PVP/KN) were found.…”

“…The PEG showed two intense crystalline reflections at 19.30° and 23.43° (Figure 5b), while HPMC and PVP showed an amorphous pattern, with no peak in the diffractogram [30,35].…”

Triterpenoids from Hibiscus sabdariffa L. with PPARδ/γ Dual Agonist Action: In Vivo, In Vitro and In Silico Studies

“…Santos et al reported that a mixture of αand β-amyrin decreased glucose, triglycerides, and cholesterol levels in diabetic mice fed a high-fat diet [25]. Another study demonstrated that these compounds have anti-inflammatory properties in lipopolysaccharidestimulated macrophages, decreasing the production of NO 2 [26], which might be associated with an increase in PPAR expression. Some studies suggest that the activation of PPARδ or PPARγ inhibits the NF-κB pathway, thereby avoiding the synthesis of proinflammatory cytokines [9,27].…”

Review: The Chemistry, Toxicity and Antibacterial Activity of Curcumin and Its Analogues

“…Solid dispersion approach has also been used to enhance the drug dissolution rate and solubility. Solid dispersion allows for the reduction of drug particle size and crystallinity, increases surface area, and enhances wettability by the surrounding hydrophilic carriers [94][95][96]. Several studies showed that solid dispersion using hydrophilic polymers has significantly enhanced curcumin/analogues solubility and potentially improved their bioavailability and pharmacological potentials [87,[97][98][99][100][101][102][103].…”