Antimalarial Activity of Ethyl Acetate Extract and Fraction of Bidens pilosa against Plasmodium berghei (ANKA)

Background. Malaria is one of the most critical diseases causing about 219 million cases worldwide in developing countries. The spread and development of resistance against chemical antimalarial drugs is one of the major problems associated with malaria control. The present study was to investigate the antimalarial efficacy of ethyl acetate extract and one fraction of Bidens pilosa in vivo in order to support the usage of this plant by traditional healers to treat malaria. Methods. The extracts were prepared by maceration of B. pilosa leaf powder in ethyl acetate. The liquid filtrate of the extract and the best in vitro antiplasmodial fraction using HPLC were concentrated and evaporated using a rotavapor under vacuum to dryness. The antimalarial activity of B. pilosa plant products were evaluated in vivo against Plasmodium berghei infected mice according to the Peter and Rane test. The antimalarial efficacy of the a selected crude extract (ethyl acetate extract) was evaluated at 125, 250, and 500 mg/kg, while a selected fraction from ethyl acetate extract (fraction 12) was evaluated at 62.5 and 125 mg/kg. Blood from experimental animals was collected to assess hematological parameters. Results. The crude extract of ethyl acetate and fraction 12 demonstrated 100% in vivo parasite suppressive activity at doses of 500 mg/kg and 125 mg/kg, respectively, for the crude extract and fraction 12. The mice treated with 250 and 500 mg/kg had their parasitemia (intraerythrocytic phase of P. Berghei) drop considerably, disappearing by the 8th day in mice receiving 500 mg/kg. The ethyl acetate extract of B. pilosa, fraction 12 showed an even higher antiplasmodial activity. By the 5th day of the experiment, the treatment led to a modification of hematological parameters in mice. The chloroquine (5 mg/kg), fraction 12 (125 mg/kg), and the crude extract (500 mg/kg) groups all survived the 30 days of the experiment, while the negative control group registered 100% of the deaths. Conclusion. This study scientifically supports the use of Bidens pilosa leaves in the traditional treatment of malaria. However, the mode of action and in vivo toxicity of the plant still need to be assessed.

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Antimalarial Effect of the Total Glycosides of the Medicinal Plant, Ranunculus japonicus

Pathogens ◽

10.3390/pathogens10050532 ◽

2021 ◽

Vol 10 (5) ◽

pp. 532

Author(s):

Hae-Soo Yun ◽

Sylvatrie-Danne Dinzouna-Boutamba ◽

Sanghyun Lee ◽

Zin Moon ◽

Dongmi Kwak ◽

...

Keyword(s):

Chinese Medicine ◽

Traditional Chinese Medicine ◽

Plasmodium Berghei ◽

Antimalarial Activity ◽

Hematological Parameters ◽

Significant Inhibition ◽

Ic50 Values ◽

The Republic

In traditional Chinese medicine, Ranunculus japonicus has been used to treat various diseases, including malaria, and the young stem of R. japonicus is consumed as a food in the Republic of Korea. However, experimental evidence of the antimalarial effect of R. japonicus has not been evaluated. Therefore, the antimalarial activity of the extract of the young stem of R. japonicus was evaluated in vitro using both chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) strains; in vivo activity was evaluated in Plasmodium berghei-infected mice via oral administration followed by a four-day suppressive test focused on biochemical and hematological parameters. Exposure to extracts of R. japonicus resulted in significant inhibition of both chloroquine-sensitive (3D7) and resistant (Dd2) strains of P. falciparum, with IC50 values of 6.29 ± 2.78 and 5.36 ± 4.93 μg/mL, respectively. Administration of R. japonicus also resulted in potent antimalarial activity against P. berghei in infected mice with no associated toxicity; treatment also resulted in improved hepatic, renal, and hematologic parameters. These results demonstrate the antimalarial effects of R. japonicus both in vitro and in vivo with no apparent toxicity.

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Antimalarial Effect of the Root of Silene macrosolen A. Rich (Caryophyllaceae) on Plasmodium-berghei-Infected Mice

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2021/8833865 ◽

2021 ◽

Vol 2021 ◽

pp. 1-11

Author(s):

Gebru Hagos Atsbha ◽

Rajkapoor Balasubramanian ◽

Abadi Kahsu Gebre

Keyword(s):

Acute Toxicity ◽

Ethyl Acetate ◽

Crude Extract ◽

Plasmodium Berghei ◽

Antimalarial Activity ◽

Public Health Problem ◽

New Drugs ◽

Major Public Health Problem ◽

Traditional Use

Background. Malaria remains a major public health problem globally. Poor access to antimalarial drugs compounded with rapidly evolving drug resistance encourages researchers to continuously look for new drugs. Of importance, traditionally used medicines of plant origin are the highest priority as the ethnobotanical claim can be used as an important clue for its safety and efficacy profiles. Silene macrosolen A. Rich (Caryophyllaceae) has been traditionally used for malaria treatment in Ethiopia. Therefore, this study was aimed to evaluate the in vivo antimalarial activity of the plant against Plasmodium-berghei-infected (ANKA strain) Swiss albino mice. Methods. The dried powdered root of Silene macrosolen was extracted using 80% methanol. The crude extract was fractionated using chloroform, ethyl acetate, and distilled water that have different affinities to plant phytoconstituents. The in vivo antimalarial activities of the crude extract were evaluated using 4-day suppressive, prophylactic, and curative tests. The antimalarial activity of the solvent fractions was evaluated in a 4-day suppressive test. The oral acute toxicity of the crude extract was also determined according to the OECD guidelines. Results. The percentage of parasite suppression on the crude extract was 31.02%, 35.82%, and 39.23% in prophylactic, curative, and 4-day suppressive tests, respectively, at the tested dose level of 400 mg/kg. The percentages of chemosuppression of the solvent fractions (400 mg/kg) were 43.07%, 42.61%, and 38.38% in aqueous, ethyl acetate, and chloroform fractions, respectively. Both the crude extract and solvent fractions also significantly prolonged survival time except in the prophylactic test. In addition, prevention of weight loss and reduction in temperature and packed cell volume (PCV) were observed in crude extract as well as solvent fractions. The acute toxicity test of the plant extract also exhibited no sign of toxicity. Conclusion. The result indicated that Silene macrosolen has a significant antimalarial activity, justifying the traditional use of the plant material for treatment of malaria.

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Evaluation of antimalarial and antioxidant activities of the methanol seed extract of Adenanthera pavonina (Linn) in Plasmodium berghei infected mice

Asian Journal of Medical Sciences ◽

10.3126/ajms.v5i4.9107 ◽

2014 ◽

Vol 5 (4) ◽

pp. 44-51 ◽

Cited By ~ 3

Author(s):

Aduragbenro Deborah Adedapo ◽

Juliet N Olayinka ◽

Oyindamola O. Abiodun ◽

Ademola A Oyagbemi ◽

Odunayo Azeez ◽

...

Keyword(s):

Oxidative Stress ◽

Crude Extract ◽

Plasmodium Berghei ◽

Antioxidant Activities ◽

Antimalarial Activity ◽

Seed Extract ◽

Control Group ◽

Untreated Control Group ◽

Adenanthera Pavonina

Objectives: Malaria and oxidative stress are major health problems in the world in general. The goal of the study is to investigate the antimalarial and antioxidant activities of the methanol seed extract of Adenanthera pavonina linn (ADP) in Plasmodium berghei infected mice. Methods: Thirty five mice distributed into seven groups of five animals each were used in this study. Plasmodium berghei, was inoculated into Swiss albino mice intraperitoneally with an innoculum size of 1x107 on day zero (D0). The vehicle (1% DMSO), ADP (100, 200, 400, 600 and 800 mg/kg dose) or chloroquine (10 mg/kg) were thereafter administered from D0 – D3. At the end of the antimalarial studies, the blood samples from these animals were collected through cardiac puncture for biochemical assay. The effect of the ADP on the biomakers of oxidative stress was determined in infected mice. In addition in vitro antioxidant activities of ADP were assessed using the 1, 1-diphenyl-2-picrylhydrazyl (DPPH) based assay. Results: The percentage parasitemia decreased significantly in the parasitized treated group with the crude extract (p < 0.001) compared to the parasitized untreated control group. Also the crude extract, at a dose of 800 mg/kg exerted an antimalarial activity (92.11%) higher than that of chloroquine (88.73%). In the in vitro antioxidant studies, the extract had an IC50> 400 μg/ml which was significantly higher than the standard antioxidant drug, ascorbic acid (IC50 = 1.20 μg/ml). In the case of biochemical and in vivo assay, there was no statistical significant difference (p >0.05) in plasma total protein, malondialdehyde (MDA) and hydrogen peroxide (H2O2) levels in all the treated groups compared to the parasite control group but, there was a statistical significant decrease (p < 0.05) in glutathione (GSH) levels at doses of 400 and 800 mg/kg compared to the parasitized untreated control group. Conclusions: Methanol seed extract of Adenanthera pavonina demonstrated a significant antimalarial activity but did not exert any antioxidant effect over the parasitized treated mice. DOI: http://dx.doi.org/10.3126/ajms.v5i4.9107 Asian Journal of Medical Sciences 2014 Vol.5(4); 44-51

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Evaluation of Antimalarial Activity of Methanolic Root Extract of Myrica salicifolia A Rich (Myricaceae) Against Plasmodium berghei–Infected Mice

Journal of Evidence-Based Integrative Medicine ◽

10.1177/2515690x20920539 ◽

2020 ◽

Vol 25 ◽

pp. 2515690X2092053 ◽

Cited By ~ 2

Author(s):

Zemene Demelash Kifle ◽

Getnet Mequanint Adinew ◽

Mestayet Geta Mengistie ◽

Abyot Endale Gurmu ◽

Engidaw Fentahun Enyew ◽

...

Keyword(s):

Crude Extract ◽

Plasmodium Berghei ◽

Antimalarial Activity ◽

Effective Vaccine ◽

Root Extract ◽

Honestly Significant Difference ◽

Significant Difference ◽

And Control

Background. The management and control of malaria has become gradually challenging due to the spread of drug-resistant parasites, lack of effective vaccine, and the resistance of vector to insecticides. Consequently, novel agents are urgently needed from different sources including from medicinal plants. In Ethiopia and Uganda, Myrica salicifolia root is traditionally claimed for the treatment of malaria. The aim of this study was to evaluate the in vivo antimalarial activity of root crude extract of M salicifolia. Methods. The parasite, Plasmodium berghei was used in this study since it is an appropriate parasite that is most commonly used because of its higher accessibility. A 4-day suppressive test was employed to evaluate the antimalarial effect of crude extract against early infection. The curative and prophylactic effect of the crude extract was further tested by Rane’s test and residual infection procedure. Parasitemia, survival time, packed cell volume, body weight, and rectal temperature of mice were used as evaluation parameters. Windows SPSS version 24 was used to analyze the data and analysis of variance followed by Tukey’s honestly significant difference to compare results between groups. Results. The root crude extract of M salicifolia significantly ( P < .05-.0001) suppressed parasitemia. The crude extract exhibited a chemosuppression of 40.90. Conclusion. The development of new antimalarial agents and the finding supports the traditional claims and previous in vitro studies.

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Antimalarial Activity ofCocos nuciferaHusk Fibre: Further Studies

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2013/742476 ◽

2013 ◽

Vol 2013 ◽

pp. 1-9 ◽

Cited By ~ 8

Author(s):

J. O. Adebayo ◽

E. A. Balogun ◽

S. O. Malomo ◽

A. O. Soladoye ◽

L. A. Olatunji ◽

...

Keyword(s):

Body Weight ◽

Ethyl Acetate ◽

Ethyl Acetate Extract ◽

Antimalarial Activity ◽

Cocos Nucifera ◽

Normal Liver ◽

Creatinine Concentration ◽

Extract Fraction

In this study, the antimalarial and toxicity potentials of husk fibre extracts of five Nigerian varieties ofCocos nuciferawere evaluatedin vitro. The only active extract fraction, West African Tall (WAT) ethyl acetate extract fraction, was then evaluated for its phytochemical constituents, antimalarial and toxicity potentials at varying doses (31.25–500 mg/kg body weight) using various organ function indices. The results revealed that WAT ethyl acetate extract fraction (WATEAEF) contained alkaloids, tannins, and flavonoids and was active againstPlasmodium falciparumW2 strain maintained in continuous culture, with a selectivity index of 30.3. The same extract fraction was activein vivoagainstPlasmodium bergheiNK65, causing more than 50% reduction in parasitaemia on days 4 and 6 after inoculation at various doses administered. WATEAEF did not significantly alter (P>0.05) function indices of the liver and cardiovascular system at all doses administered but significantly increased (P<0.05) plasma creatinine concentration at 250 and 500 mg/Kg body weight compared to controls. The results of this study suggest that WATEAEF possesses antimalarial activity and may not adversely affect normal liver function nor predispose subjects to cardiovascular diseases but may impair normal kidney function at higher doses. Further studies are underway to isolate the active principles.

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Antimalarial Activity of the 80% Methanol Leaf Extract and Solvent Fractions of Stephania abyssinica (Dill. & A. Rich.) Walp. against Plasmodium berghei Infection in Mice

Ethiopian Pharmaceutical Journal ◽

10.4314/epj.v36i2.4 ◽

2021 ◽

Vol 36 (2) ◽

pp. 109-120

Author(s):

Mekuanent Zemene ◽

Mestayet Geta ◽

Solomon Assefa Huluka ◽

Eshetie Melese Birru

Keyword(s):

Ethyl Acetate ◽

Plasmodium Berghei ◽

Antimalarial Activity ◽

Treated Group ◽

Chloroform Fraction ◽

Global Public Health ◽

African Countries ◽

Hydroalcoholic Extract

Malaria continues to be a global public health threat. In Africa, malaria accounts for a substantial morbidity and mortality. The emergence of drug resistant malaria parasites and subsequent decrement in effectiveness of current antimalarial medications have complicated malaria control. This urged developing an effective alternative antimalarial agent. Leaves and root of Stephania abyssinica (Dill. & A. Rich.) Walp. is traditionally used for the treatment of malaria in east African countries such as Ethiopia and proved for its in vitro antimalarial efficacy. Hence, this study aimed at evaluating the antimalarial activity of S. abyssinica. Cold maceration technique was employed to prepare the 80% methanol crude extract followed by fractionation using n-hexane, chloroform and ethyl acetate. The in vivo antimalarial property of different dose levels (100, 200 and 400 mg/kg/day) of the hydroalcoholic extract and solvent fractions were investigated using prophylactic and 4-day suppressive mice models, against Plasmodium berghei (ANKA strain). Highest (400 mg/kg) doses of the hydroalcoholic extract and solvent fractions (hexane, chloroform and ethyl acetate) exhibited a statistically significant (p < 0.001) chemosuppressive activities. The chloroform fraction revealed the highest chemosuppresion (55.80%) and chemoprophylactic (57.59%) potency in 4-day suppressive and prophylactic tests, respectively, at 400 mg/kg dose level. Furthermore, 400 mg dose of the chloroform fraction significantly prevented malaria associated haemolysis as compared to vehicle treated group in both prophylactic (p < 0.05) and suppressive (p < 0.01) models. In conclusion, the current study gave evidence that the plant has a potential antimalarial activity against P. berghei, which upholds traditional claims and justifies a need to undertake advanced pharmacological and toxicological investigations.

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Antimalarial Activity of Hydromethanolic Crude Extract and Chloroform Fraction of Brucea antidysenterica Leaves in Plasmodium berghei-Infected Mice

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2021/2089114 ◽

2021 ◽

Vol 2021 ◽

pp. 1-14

Author(s):

Tezera Jemere Aragaw ◽

Kefyalew Ayalew Getahun

Keyword(s):

Crude Extract ◽

Plasmodium Berghei ◽

Antimalarial Activity ◽

Negative Control ◽

Chloroform Fraction ◽

Curative Effect ◽

Antimalarial Agents ◽

Different Doses

Background. Different parts of Brucea antidysenterica are used in traditional and alternative medicine in Ethiopia for the treatment of different health problems including malaria and have good in vitro antimalarial activity. However, no in vivo study was conducted to substantiate the claim. Our study planned to determine the antimalarial effect of B. antidysenterica extract. Methods. Swiss albino mice (6–8 weeks old, 20–28 g) were inoculated with Plasmodium berghei. Different doses of both hydromethanolic extract and chloroform fraction were orally given at 100, 200, and 400 mg/kg/day. Results. The parasitemia suppression percent of hydromethanolic crude extract and chloroform fraction in chemosuppressive tests ranged between 33.48 and 75.93% and 38.32 and 76.64%, respectively. The hydromethanolic crude extract and chloroform fraction exhibited the curative effect of 46.75–70.91% and 50.30–80.06% parasitemia suppression, respectively ( p < 0.001), compared with negative control. Conclusion. From our study, it is concluded that the hydromethanolic crude extract and chloroform fraction of B. antidysenterica leaves showed promising antiplasmodial effects against Plasmodium berghei. This upholds the folkloric use of B. antidysenterica leaves and the thought of as a possible source to develop new antimalarial agents.

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Assessment of Antiplasmodial Activity and Toxicity of Crude Extracts and Isolated Compounds from Oncoba spinosa (Flacourtiaceae)

Journal of Advances in Medical and Pharmaceutical Sciences ◽

10.9734/jamps/2019/v21i130124 ◽

2019 ◽

pp. 1-14

Author(s):

Kodi Philip ◽

Peter Kiplagat Cheplogoi ◽

Mwangi Muthoni Elizabeth ◽

M. Akala Hoseah ◽

Moses K. Langat

Keyword(s):

Acute Toxicity ◽

Ethyl Acetate ◽

Crude Extract ◽

Antimalarial Activity ◽

Local Communities ◽

Antiplasmodial Activity ◽

Isolation And Purification ◽

Crude Extracts

Aims: The medicinal plant Oncoba spinosa is used by the local communities in Butebo County in Eastern Uganda for treatment of malaria and other diseases. In vitro antiplasmodial activities of the crude extracts and isolated compounds were screened against chloroquine sensitive 3D7 and resistant Dd2 strains. In vivo acute toxicity of the extracts and structure elucidation were also determined in the study. Experimental: Crude extracts of: n-hexane, dichloromethane, ethyl acetate and methanol were prepared. Isolation and purification of these extracts were done using chromatographic techniques which consisted of column and thin layer chromatography. The structures were elucidated on the basis of spectroscopic evidence. In vitro antiplasmodial activity was performed on chloroquine sensitive 3D7 and resistant Dd2 strains of Plasmodium falciparum using SYBR Green 1 assay technique. Lorke’s method of acute toxicity was used to determine the in vivo acute toxicity of the crude extracts in mice. Results: The root ethyl acetate crude extract had highest antiplasmodial activity of IC50:4.69 ± 0.01 µg/mL and 3.52 ± 0.02 µg/mL against 3D7 and Dd2 strains respectively while the remaining three were inactive against both strains of Plasmodium. Isolation resulted in the identification of three known compounds which included: β-sitosterol, benzoic acid and chaulmoogric acid. Among the tested compounds β-sitosterol showed the highest activity of IC50 3D7: 5.51 µM. Dichloromethane and hexane extracts were non-toxic with LD50 > 5000 mg/kg while the EtOAc and MeOH extracts were slightly toxic with LD50 of 547.72 mg/kg. Statistically significance existed between the antiplasmodial activity of the crude extracts and compounds when compared with the controls at (p < 0.05). Extracts and compounds exerted a significant (P < 0.05) decrease in antiplasmodial activity compared to the positive controls. Conclusion: The findings confirm the ethnobotanical use of O. spinosa by the local communities in Butebo County for the treatment of malaria. The results also suggest that the crude extract of this plant is safe and possesses antimalarial activity which can be used as a basis for in vivo and clinical studies to be done. Therefore the plant can offer a potential drug lead for developing a safe, effective and affordable antimalarial.

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Antimalarial Activities of Hydromethanolic Crude Extract and Chloroform Fraction of Gardenia ternifolia Leaves in Plasmodium berghei Infected Mice

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2020/6674002 ◽

2020 ◽

Vol 2020 ◽

pp. 1-11

Author(s):

Tezera Jemere Aragaw ◽

Dessie Tegegne Afework ◽

Kefyalew Ayalew Getahun

Keyword(s):

Crude Extract ◽

Plasmodium Berghei ◽

Antimalarial Activity ◽

Negative Control ◽

Malaria Treatment ◽

Species Variation ◽

Chloroform Fraction ◽

Post Hoc

Background. Gardenia ternifolia is utilized in traditional medicine of Ethiopia for malaria treatment and possessing in vitro antimalarial activity. However, no in vivo study was conducted to substantiate the claim. The aim of this study was to judge the antimalarial activity of Gardenia ternifolia extract in vivo in Plasmodium berghei-infected mice. Methods. Plasmodium berghei was inoculated to healthy mice, and hydromethanolic crude extract and chloroform fraction of G. ternifolia leaves at 100 mg/kg/day, 200 mg/kg/day, and 400 mg/kg/day were administered. Percent parasitemia inhibition, percent change in bodyweight, hemoglobin level, and mean survival time were determined. Data were analyzed using one-way ANOVA followed by post hoc Tukey HSD test with IBM SPSS software version 20.0 statistical package and P < 0.05 considered as statistically significant. Results. The chemosuppressive test of hydromethanolic crude extract at 100 mg/kg/day, 200 mg/kg/day, and 400 mg/kg/day ranged from 27.09% to 67.72%, and chloroform fraction had 35.21%–78.19% parasitemia suppression, respectively. For curative test on day 5, hydromethanolic crude extract at 100 mg/kg/day, 200 mg/kg/day, and 400 mg/kg/day ranged from 25.58% to 48.76%, chloroform fraction at 100 mg/kg/day, 200 mg/kg/day, and 400 mg/kg/day and chloroquine base at 10 mg/kg showed 46.36%–74.42% and 92.87% percent parasitemia inhibition, respectively, and also the results to both tests were highly significant ( P < 0.001 ) compared to the negative control. Maximum effects on chemosuppressive, curative, prevention of weight loss, and reduction in hemoglobin were observed at higher doses of the hydromethanolic crude extract and chloroform fraction. Conclusion. From this study, hydromethanolic crude extract and chloroform fraction of G. ternifolia leaves have shown promising antimalarial activity. The findings support the traditional claim of G. ternifolia leaves for malaria treatment; however, species variation could also limit such a straightforward extrapolation of the findings of this study in humans.

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Antimalarial Activity of Bidens pilosa Root Extract Co-spray Dried in the Presence of β-Cyclodextrin or Aerosil:Microcrystalline Cellulose Blend

Planta Medica International Open ◽

10.1055/a-1348-5707 ◽

2021 ◽

Vol 8 (01) ◽

pp. e1-e9

Author(s):

Diego F. Cortés-Rojas ◽

Thales Lira de Medeiros ◽

Claudio Bruno Silva de Oliveira ◽

Ywlliane da Silva Rodrigues Meurer ◽

Valter Ferreira de Andrade-Neto ◽

...

Keyword(s):

Spray Drying ◽

Crude Extract ◽

Antimalarial Activity ◽

In Vitro Toxicity ◽

Root Extract ◽

Bidens Pilosa ◽

Pharmaceutical Excipients ◽

Spray Dried

AbstractThe purpose of this work was to evaluate if the antimalarial activity of Bidens pilosa L. root extract could be enhanced by co-spray drying with the pharmaceutical excipients blend of colloidal silicon dioxide:microcrystalline cellulose and β-cyclodextrin. The in vivo antimalarial activity of the products was evaluated in mice infected with Plasmodium berghei. Acute in vivo and in vitro toxicity in S5 HeLa cells were also carried out. B. pilosa L. root extract was lyophilized and used as a control. The spray-dried preparations enhanced the survival of the infected mice compared to the lyophilized crude root extract. The Bidens extract formulations were able to inhibit up to 71% of the growth of the parasite in the lowest tested dose, being about five times more active than the crude extract, thus showing significant partial antiplasmodial activity. The dried preparations did not show signals of toxicity in both the in vitro and in vivo assays. The results showed strong evidence that the co-spray drying of B. pilosa root extract with the selected pharmaceutical excipients might stabilize the bioactive compounds and enhance its antimalarial activity compared with the lyophilized crude extract.

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