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Molecules 2017, 22(9), 1512; doi:10.3390/molecules22091512

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

1
Pharmacy Department, Health Sciences Center, Universidade Federal do Rio Grande do Norte (UFRN), Natal 59012-570, Rio Grande do Norte (RN), Brazil
2
Department of Pharmacy, Laboratory of Biological Activity, Federal University of Amazonas, Manaus 69077-000, AM, Brazil
3
Department of Chemistry, Institute of Exact Sciences, Federal University of Amazonas, Manaus 69077-000, AM, Brazil
4
Military Institute of Engineering, Rio de Janeiro 22290-270, RJ, Brazil
5
Graduate Program in Biotechnology, Laureate International Universities—UnP, Natal 59056-000, RN, Brazil
*
Author to whom correspondence should be addressed.
Received: 4 August 2017 / Revised: 28 August 2017 / Accepted: 6 September 2017 / Published: 9 September 2017
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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. View Full-Text
Keywords: α,β amyrin; pentacyclic triterpenes; solid dispersions; hydrophilic polymers; anti-inflammatory activity α,β amyrin; pentacyclic triterpenes; solid dispersions; hydrophilic polymers; anti-inflammatory activity
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MDPI and ACS Style

da Silva Júnior, W.F.; Pinheiro, J.G.O.; de Menezes, D.L.B.; e Silva, N.E.S.; de Almeida, P.D.O.; Lima, E.S.; da Veiga Júnior, V.F.; de Azevedo, E.P.; de Lima, Á.A.N. Development, Physicochemical Characterization and In Vitro Anti-Inflammatory Activity of Solid Dispersions of α,β Amyrin Isolated from Protium Oilresin. Molecules 2017, 22, 1512.

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