Planta Med 2016; 82(S 01): S1-S381
DOI: 10.1055/s-0036-1596239
Abstracts
Georg Thieme Verlag KG Stuttgart · New York

Nanotechnology approach for malaria treatment

L Servat-Medina
1   Faculty of Pharmaceutical Science, University of Campinas, Campinas, SP, Brazil
,
N Durán
2   Biological Chemistry Laboratory, Institute of Chemistry, University of Campinas, Campinas, SP, Brazil
3   Brazilian Nanotechnology National Laboratory (LNNano-CNPEM), Campinas, SP, Brazil
,
AC Lima
4   Urogenital Carcinogenesis: Urogenital and Immunotherapy Laboratory, Institute of Biology, University of Campinas, Campinas, SP, Brazil
,
RT Basting
5   Postgraduate Program in Medical Sciences – Faculty of Medical Science – FCM/University of Campinas, Campinas, SP, Brazil
,
IMO Sousa
1   Faculty of Pharmaceutical Science, University of Campinas, Campinas, SP, Brazil
5   Postgraduate Program in Medical Sciences – Faculty of Medical Science – FCM/University of Campinas, Campinas, SP, Brazil
,
FV Zanutto
6   Institute of Biology, University of Campinas, Campinas, SP, Brazil
,
MA Foglio
1   Faculty of Pharmaceutical Science, University of Campinas, Campinas, SP, Brazil
› Author Affiliations
Further Information

Publication History

Publication Date:
14 December 2016 (online)

 

Malaria is an infectious disease which persist a major cause of morbidity and mortality in tropical and subtropical regions of the world. Artemisinin isolated from Artemisia annua, and the semi-synthetic derivate Artemether (ART), are among the most important class of antimalarial drugs currently available [1]. Pharmaceutical nanotechnology can provide unlimited opportunities for improving the efficacy of the currently used antimalarial drugs [2]. The present work reports the nanonization process of ART. Nanocrystals are nanoparticles of pure drug, without any matrix material, which can be prepared in water media as colloidal nanosuspensions stabilized using polymers. ART in aqueous media was processed by top-down method (nanonization) employed ultrasonic probe. Measurement of the particle size and polydispersity index (PDI) was performed using a Zetasizer Nano ZS. Pluronic® F68, Plantaren 2000® or Carbopol 940® was used as nanosuspension stabilisers. The ART: polymer mass ratios evaluated was 1:0,5; 1:1; 1:2 and 1:4. The average particle size was dependent of polymer mass ratio, as indicated in the Figure 1. The nanocrystals produced showed average size from 290nm, 147nm and 272nm employing Pluronic®, Plantaren® or Carbopol®, respectively. The ART: Plantaren mass ratio of 4 was found as the best condition to achieve the lowest nanocrystals. Nanocrystals were compared to the unprocessed drug by thermal analysis. Cell viability was evaluated in human tumour cells in order to compare the sample's activity. The original drug and nanocrystals showed similar response data, suggesting the nanonization process did not influence in the crystalline nature of ART, as well as did not compromise the biocompatibility (Figure 2). Results, herein reported, support that nanonization technique is a simple and cost-effective approach to produce ART nanocrystals, which can be considered for the preparation of pharmaceutical systems for malaria treatment.

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Fig. 1: Particle size and polydispersity index (PDI values in parentheses) of ART nanosuspension with Pluronic, Plantaren or Carbopol.
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Fig. 2: Cell viability of ART original drug and nanocrystal using human tumour cells panel.

Acknowledgements: Support from CNPq, FAPESP, NanoBioss (MCTI) and Network Braz. Nanotoxicol. (MCTI/CNPq).

Keywords: Nanocrystal, artemether, malaria.

References:

[1] World Malaria Report 2015. http://www.who.int/malaria/visual-refresh/en/

[2] Santos-Magalhães NS, Mosqueira VCF. Nanotechnology applied to the treatment of malaria. Adv Drug Deliv Rev 2010; 62: 560 – 575