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Design of experiments for the development of poly(d,l-lactide-co-glycolide) nanoparticles loaded with Uncaria tomentosa

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Abstract

Polymeric nanoparticles have been shown to be effective carriers for natural substances that possess anticancer properties. Incorporation of these natural substances into polymeric nanoparticles increases targeting of these drugs, thus reducing side effects. Uncaria tomentosa (UT) is a Peruvian Amazon plant (existing in the Brazilian Amazon rainforest) that possesses promising anti-tumor activity. This paper describes the development of poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles loaded with UT extract. The emulsion solvent evaporation method was utilized and the initial conditions were determined for the organic phase (OP) and the aqueous phase (AP). The influence of surfactant (type and concentration), PLGA concentration and AP volume on nanoparticle size, polydispersity index (PI), and entrapment efficiency (EE) was determined using a fractional factorial design (FFD). In addition, the formulation was optimized using a Box–Behnken design. After the conditions were optimized, UT nanoparticles were obtained using an OP composed of an ethyl acetate:acetone (3:2) mixture which contained the UT alkaloids and PLGA, and an AP composed of a buffered solution of Poloxamer 188 (pH 7.5). The optimized formulation produced an EE of 64.6 %, a particle size of 107.4 nm and a PI of 0.163. The preliminary experiments provided important information regarding the behavior of the nanoparticulate system and the FFD used in this study greatly facilitated the selection of the most optimal conditions for formulation development.

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Acknowledgments

This work was supported by FAPERJ and CAPES Edital CAPES Nanobiotecnologia 2008. The authors wish to thank the Herbarium Laboratório Botânico Ltda., IFRJ, LADEQ/UFRJ, and EngePol/COPPE/UFRJ.

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The authors declare no conflicts of interest.

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Authors and Affiliations

  1. Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil

    Ana Ferreira Ribeiro, Lúcio Mendes Cabral & Valéria Pereira de Sousa

  2. Faculty of Pharmacy, Federal Institute of Education, Science and Technology of Rio de Janeiro, R. Prof. Carlos Wenceslau 343, Realengo, Rio de Janeiro, RJ, 25715-000, Brazil

    Ana Ferreira Ribeiro, Carina Torres Garruth Ferreira & Juliana Fernandes dos Santos

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  1. Ana Ferreira Ribeiro
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  2. Carina Torres Garruth Ferreira
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  5. Valéria Pereira de Sousa
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Correspondence to Ana Ferreira Ribeiro.

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Ribeiro, A.F., Ferreira, C.T.G., dos Santos, J.F. et al. Design of experiments for the development of poly(d,l-lactide-co-glycolide) nanoparticles loaded with Uncaria tomentosa . J Nanopart Res 17, 69 (2015). https://doi.org/10.1007/s11051-015-2883-y

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