Development of an oral suspension containing dry extract of Aleurites moluccanus with anti-inflammatory activity

Abstract

Aleurites moluccanus L. (Willd.), Euphorbiaceae, is a tree that is native to Indonesia and India. Various parts of this tree are commonly used in traditional medicine to treat pain, fever, inflammation, hepatitis, gastric ulcer and other ailments. An oral suspension containing dried extract of A moluccanus was developed and in vivo anti-inflammatory activity was evaluated. Extract 100 and 50mg/ml loaded oral suspensions were prepared using different suspending agents. The formulations were analysed by their appearance, pH, density, redispersion time, rate of settling, Theological behaviour, distribution of particle size and zeta potential. The dose uniformity was determined by measuring the content of total phenolic compounds expressed in swertisin by a validated HPLC method, as well as the dissolution profile. The stability of oral suspensions was analysed in accelerated studies (40 °C for 6 months). The anti-inflammatory activity was analysed using an in vivo paw oedema model. The taste and odour of the suspensions were shown to be characteristic of the extract. Carmellose sodium (CS; 0.5%) and microcrystalline cellulose and carmellose sodium mixture (MCCS; 1%) showed better physical behaviour. The content of total phenolic compounds was 1.6 mg/ml and approximately 100% of the total phenolic compounds dissolved within 10 min. During the stability study, the formulations were approved by their physical-chemical properties and were shown to lose 12–14% of total phenolic compounds at 40 °C after 6 months. Suspensions containing 50mg/ml of standardised dried extract inhibited around 35 ± 7.6% of paw oedema. Formulations containing CS showed more anti-inflammatory activity. Suspensions containing dry extract of A. moluccanus were successfully obtained and showed physical and physical-chemistry properties that were appropriate and characteristic of this dosage form, suitable for administration in paediatric and elderly populations, making this an alternative to tablets.

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Acknowledgements

The authors wish to thank the Laboratório Farmacêutico Eurofarma (São Paulo, Brazil), FINEP/MCT (Financiadora de Estudos e Projetos/Ministério da Ciência e Tecnologia) (no. 01.05.0812.00), Fundação de Amparo a Pesquisa e Inovação no Estado de Santa Catarina, CNPq, MS/DECIT (Ministério da Saúde/Departamento de Ciência e Tecnologia da Secretaria de Ciência, Tecnologia e Insumos Estratégicos), CT-BIOTEC (Fundos Setoriais de Biotecnologia) and CT-Saúde (Fundos Setoriais de Saúde, Edital Bioinova No. 551023/2007-4) for their financial support during this study. RMD is M.Sc. students in Pharmaceutical Science supported by grants from the Eurofarma/Univali.

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RMD and SSC carried out the laboratory work, data analysis and writing of the manuscript. NLMQ supervised the pharmacological studies and contributed to critical writing and reading of the manuscript. CMS and VCF contributed to botanical, phytochemistry and analytical studies. TMBB and RMLS contributed to designed the study, supervised the analytical and technological studies and contributed to critical writing and reading of the manuscript. All the authors have read the final manuscript and approved the submission.

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Correspondence to Ruth Meri Lucinda-Silva.

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Mac Donald, R., Camargo, S.S., Meyre-Silva, C. et al. Development of an oral suspension containing dry extract of Aleurites moluccanus with anti-inflammatory activity. Rev. Bras. Farmacogn. 26, 68–76 (2016). https://doi.org/10.1016/j.bjp.2015.06.011

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Keywords

  • Aleurites moluccanus
  • Anti-inflammatory
  • Phytomedicine
  • Oral suspension