Antiplasmodial Activity and Toxicological Assessment of Curcumin PLGA-Encapsulated Nanoparticles
Curcumin is a polyphenolic pigment isolated from the rhizomes of Curcuma longa (turmeric), a medicinal plant widely used in the ancient Indian and Chinese medicine. The antiplasmodial activity of curcumin is often hampered by its fast metabolism and poor water solubility, thus its incorporation into...
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Frontiers Media S.A.
2017-09-01
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| Series: | Frontiers in Pharmacology |
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| Online Access: | http://journal.frontiersin.org/article/10.3389/fphar.2017.00622/full |
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| author | Zulaikha A. Busari Kabiru A. Dauda Olajumoke A. Morenikeji Funmilayo Afolayan Oyetunde T. Oyeyemi Oyetunde T. Oyeyemi Jairam Meena Debasis Sahu Debasis Sahu Amulya K. Panda |
| author_facet | Zulaikha A. Busari Kabiru A. Dauda Olajumoke A. Morenikeji Funmilayo Afolayan Oyetunde T. Oyeyemi Oyetunde T. Oyeyemi Jairam Meena Debasis Sahu Debasis Sahu Amulya K. Panda |
| author_sort | Zulaikha A. Busari |
| collection | DOAJ |
| description | Curcumin is a polyphenolic pigment isolated from the rhizomes of Curcuma longa (turmeric), a medicinal plant widely used in the ancient Indian and Chinese medicine. The antiplasmodial activity of curcumin is often hampered by its fast metabolism and poor water solubility, thus its incorporation into a delivery system could circumvent this problem. This study aimed to evaluate the in vivo antiplasmodial activity and the toxicity assessment of curcumin incorporated into poly (lactic-co-glycolic) acid (PLGA) nanoparticles. Curcumin was loaded with poly (D,L-lactic-co-glycolic acid) (PLGA) using solvent evaporation from oil-in-water single emulsion method. The nanoparticles were characterized and evaluated in vivo for antimalarial activities using Peter’s 4-day suppressive protocol in mice model. Hematological and hepatic toxicity assays were performed on whole blood and plasma, respectively. In vivo anti-parasitic test and toxicity assays for free and encapsulated drug were performed at 5 and 10 mg/kg. In vitro cytotoxicity of free and PLGA encapsulated curcumin (Cur-PLGA) to RAW 264.7 cell line was also determined at varying concentrations (1000–7.8 μg/mL). The size and entrapment efficiency of the nanoparticulate drug formulated was 291.2 ± 82.1 nm and 21.8 ± 0.4 respectively. The percentage parasite suppression (56.8%) at 5 mg/kg was significantly higher than in free drug (40.5%) of similar concentration (p < 0.05) but not at 10 mg/kg (49.5%) at 4-day post-treatment. There were no significant differences in most of the recorded blood parameters in free curcumin and PLGA encapsulated nanoparticulate form (p > 0.05) except in lymphocytes which were significantly higher in Cur-PLGA compared to the free drug (p < 0.05). There were no significant differences in hepatotoxic biomarkers; aspartate aminotransferase and alanine aminotransferase concentrations in various treatment groups (p > 0.05). At higher concentrations (1000 and 500 μg/mL), Cur-PLGA entrapped nanoparticle showed higher toxicity compared with the free drug (p < 0.05) in exposed RAW 264.7 cell line. The cell viability was, however, higher in Cur-PLGA nanoparticles than in free curcumin at lower concentrations (p > 0.05). The antiplasmodial activity and safety of Cur-PLGA was better at lower concentration. |
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| id | doaj.art-3c3d7baaa7054b5b9b852c3ae49a467a |
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| language | English |
| last_indexed | 2024-04-13T18:20:30Z |
| publishDate | 2017-09-01 |
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| spelling | doaj.art-3c3d7baaa7054b5b9b852c3ae49a467a2022-12-22T02:35:28ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122017-09-01810.3389/fphar.2017.00622225923Antiplasmodial Activity and Toxicological Assessment of Curcumin PLGA-Encapsulated NanoparticlesZulaikha A. Busari0Kabiru A. Dauda1Olajumoke A. Morenikeji2Funmilayo Afolayan3Oyetunde T. Oyeyemi4Oyetunde T. Oyeyemi5Jairam Meena6Debasis Sahu7Debasis Sahu8Amulya K. Panda9Department of Zoology, University of IbadanIbadan, NigeriaDepartment of Zoology, University of IbadanIbadan, NigeriaDepartment of Zoology, University of IbadanIbadan, NigeriaDepartment of Zoology, University of IbadanIbadan, NigeriaDepartment of Biological Sciences, University of Medical SciencesOndo, NigeriaProduct Development Cell, National Institute of ImmunologyNew Delhi, IndiaProduct Development Cell, National Institute of ImmunologyNew Delhi, IndiaProduct Development Cell, National Institute of ImmunologyNew Delhi, IndiaDepartment of Biochemistry, School of Bioengineering and Biosciences, Lovely Professional UniversityPhagwara, IndiaProduct Development Cell, National Institute of ImmunologyNew Delhi, IndiaCurcumin is a polyphenolic pigment isolated from the rhizomes of Curcuma longa (turmeric), a medicinal plant widely used in the ancient Indian and Chinese medicine. The antiplasmodial activity of curcumin is often hampered by its fast metabolism and poor water solubility, thus its incorporation into a delivery system could circumvent this problem. This study aimed to evaluate the in vivo antiplasmodial activity and the toxicity assessment of curcumin incorporated into poly (lactic-co-glycolic) acid (PLGA) nanoparticles. Curcumin was loaded with poly (D,L-lactic-co-glycolic acid) (PLGA) using solvent evaporation from oil-in-water single emulsion method. The nanoparticles were characterized and evaluated in vivo for antimalarial activities using Peter’s 4-day suppressive protocol in mice model. Hematological and hepatic toxicity assays were performed on whole blood and plasma, respectively. In vivo anti-parasitic test and toxicity assays for free and encapsulated drug were performed at 5 and 10 mg/kg. In vitro cytotoxicity of free and PLGA encapsulated curcumin (Cur-PLGA) to RAW 264.7 cell line was also determined at varying concentrations (1000–7.8 μg/mL). The size and entrapment efficiency of the nanoparticulate drug formulated was 291.2 ± 82.1 nm and 21.8 ± 0.4 respectively. The percentage parasite suppression (56.8%) at 5 mg/kg was significantly higher than in free drug (40.5%) of similar concentration (p < 0.05) but not at 10 mg/kg (49.5%) at 4-day post-treatment. There were no significant differences in most of the recorded blood parameters in free curcumin and PLGA encapsulated nanoparticulate form (p > 0.05) except in lymphocytes which were significantly higher in Cur-PLGA compared to the free drug (p < 0.05). There were no significant differences in hepatotoxic biomarkers; aspartate aminotransferase and alanine aminotransferase concentrations in various treatment groups (p > 0.05). At higher concentrations (1000 and 500 μg/mL), Cur-PLGA entrapped nanoparticle showed higher toxicity compared with the free drug (p < 0.05) in exposed RAW 264.7 cell line. The cell viability was, however, higher in Cur-PLGA nanoparticles than in free curcumin at lower concentrations (p > 0.05). The antiplasmodial activity and safety of Cur-PLGA was better at lower concentration.http://journal.frontiersin.org/article/10.3389/fphar.2017.00622/fullpolymeric nanoparticlescurcuminantimalarialsafety |
| spellingShingle | Zulaikha A. Busari Kabiru A. Dauda Olajumoke A. Morenikeji Funmilayo Afolayan Oyetunde T. Oyeyemi Oyetunde T. Oyeyemi Jairam Meena Debasis Sahu Debasis Sahu Amulya K. Panda Antiplasmodial Activity and Toxicological Assessment of Curcumin PLGA-Encapsulated Nanoparticles Frontiers in Pharmacology polymeric nanoparticles curcumin antimalarial safety |
| title | Antiplasmodial Activity and Toxicological Assessment of Curcumin PLGA-Encapsulated Nanoparticles |
| title_full | Antiplasmodial Activity and Toxicological Assessment of Curcumin PLGA-Encapsulated Nanoparticles |
| title_fullStr | Antiplasmodial Activity and Toxicological Assessment of Curcumin PLGA-Encapsulated Nanoparticles |
| title_full_unstemmed | Antiplasmodial Activity and Toxicological Assessment of Curcumin PLGA-Encapsulated Nanoparticles |
| title_short | Antiplasmodial Activity and Toxicological Assessment of Curcumin PLGA-Encapsulated Nanoparticles |
| title_sort | antiplasmodial activity and toxicological assessment of curcumin plga encapsulated nanoparticles |
| topic | polymeric nanoparticles curcumin antimalarial safety |
| url | http://journal.frontiersin.org/article/10.3389/fphar.2017.00622/full |
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