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.
Highlights
The Burseraceae family has 18 genres and around 700 species that are distributed throughout three different tribes: Canarieae, Protieae and Bursereae
According to the Fourier transform infrared (FTIR) spectrum for ABAM (Figure 1A), the high intensity band found at approximately 2800 cm−1 is associated with axial deformation of the C-H bonds in aliphatic chains
The band at the 3250–3400 cm−1 region is attributed to a hydroxyl group (O-H) linked to an aliphatic carbon chain, and the one at the 1031–1100 cm−1 region is due to the vibration of the C-O bond
Summary
The Burseraceae family has 18 genres and around 700 species that are distributed throughout three different tribes: Canarieae, Protieae and Bursereae. A common tree found in Brazilian Amazon, is one of the most widely studied species. It is popularly known as almecegueira, breu-branco verdadeiro, almecegueira-cheirosa, almecegueira-de-cheiro and almecegueiro-bravo [2]. An oilresin is either produced when the trunk of Protium heptaphyllum is injured or naturally exuded. It is generally used in popular medicine for its anti-inflammatory, analgesic, expectorant and wound healing properties [3]. Several studies have shown the presence of secondary metabolites in Protium heptaphyllum, especially triterpenes such as α,β amyrin (ABAM) [4]
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