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Unicamp granted patent proposes how to obtain enriched extract of natural antimalarial

Invention combines extraction with purification obtaining 2x higher content of the natural antimalarial artemisinin without polluting the environment or leaving toxic solvent residues in the sample

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Research conducted and patented in Campinas State University (Unicamp) managed to obtain enriched and highly purified fractions of artemisinin, a natural antimalarial. The compound is extracted from artemisia (Anniversary Artemisia), a shrub of Asian origin used for centuries to treat malaria fever. The active ingredient and its derivatives are pharmaceutical ingredients recommended by World Health Organization (WHO) and, in Brazil, by Ministry of Health, to combat the disease that still does not have a vaccine. 

The purification technology consists of extracting artemisinin with supercritical carbon dioxide, combined in series with the purification stage in adsorption columns. The unique process of obtaining and pharmaceutical use of refined extract of Anniversary Artemisia gave rise to a patent filing made by Inova Unicamp, with registration granted by the National Institute of Industrial Property (INPI) in July this year. 

“Our objective in the study, which resulted in the technology, was to obtain the maximum amount of artemisinin in the extract with the highest purity, without the use of harmful organic solvents. The process is simultaneous, that is, sequentially. In the end, the solid artemisia material comes out on one side and the concentrated artemisinin on the other”, comments researcher Maria Angela de Almeida Meireles.

According to the researchers, extraction using the conventional method results in a relatively low amount of artemisinin in the extract. These processes also use organic solvents at all stages, which can be toxic and leave traces in the product. Supercritical extraction technology has technological and environmental advantages and one of the team's precautions was, precisely, the use of solvents that do not harm nature, such as (CO2) and ethanol. 

Optimized artemisinin extraction process

With the new process, the researchers obtained an artemisinin content greater than 34% in the enriched fraction of the pharmaceutical compound (double that of other conventional techniques), without generating toxic residues in production or contaminating the sample, that is, with a high degree of purity . An extract with this artemisinin content represents a process yield of 80 to 90%, or even higher, by optimizing the temperature, pressure and solvent flow conditions. They also reduced stages and intermediate steps for manufacturing the input, as supercritical fluids are easier to remove from the sample. 

Extraction with supercritical fluids promotes high mass transfer rates at relatively low temperatures, a fundamental characteristic for choosing the technique for extracting natural products. The system works under high pressure and changing the parameters causes the solvent to go from a supercritical state to a gaseous state, being fully recovered at the end of the process, and can even be reused. Furthermore, the invention allows continuous or semi-continuous configurations.

The process described in the patent for extraction from mugwort using supercritical carbon dioxide comprises at least three steps. In the first, the solid mass of the plant is placed in the extractor and comes into contact with the solvent (carbon dioxide). In the second stage, adsorption, the mixture of substances of interest is retained on the surface of the adsorbent in a fractionated column, arranged in a line in the same circuit. Finally, desorption occurs, which is the separation of the substances of interest from the desorbing solid. Desorption is carried out by adding ethanol to supercritical carbon dioxide. 

Market opportunities for artemisinin

Among the products of greatest interest in technology is the malaria medicine itself. Despite a significant reduction in the disease in Brazil in recent years, the disease, which mainly affects the Amazon region, still represents a public health problem. 164 Brazilian municipalities did not reach the reduction target, defined in the National Malaria Elimination Plan launched in 2015. 

Artemisinin also has anti-inflammatory characteristics that can be applied by the industry in the development of other products. Researchers from Unicamp's Faculty of Food Engineering (FEA) see the technology as an opportunity to produce richer national extracts, explore new and different uses for artemisinin - in injectable forms, tablets and suspensions -, and evaluate the potential of compounds from plants that, today, do not have great commercial value. “Artemisinin has oxygen in the structure of the molecule. We use polarity, that is, its physical affinity for other polar molecules, to enrich the compounds, concentrating the content in the extract and we maintain other compounds that are present in the plant's own metabolism”, explains professor Paulo de Tarso Vieira e Rosa.

Learn more about Purification technology

  • This technology is an Invention Patent (IP) granted by INPI under PI number 0903275-4, this means that Unicamp, as the IP holder, has the exclusivity to license the use/exploitation of the invention to third parties. 
  • For more information about the profile of this and other technologies at the State University of Campinas, visit the Unicamp Patent and Software Portfolio
  • The full Innovation Agency Annual Report is available to download and consultation
  • Also download the Inventores Prize Magazine and read more reports about technologies licensed from Unicamp for the market. 
  • Companies interested in licensing can contact Inova in the area Connection with Companies.

original article published on the Unicamp Innovation Agency website. 

Listen to Repórter Unicamp on the topic produced by Rádio Unicamp.

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Invention combines extraction with purification obtaining 2x higher content of the natural antimalarial artemisinin without polluting the environment or leaving toxic solvent residues in the sample

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