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Title: Excipient-excipient interactions in the development of nanocarriers: an innovative statistical approach for formulation decisions
Author: Beraldo-de-araújo, Viviane Lucia; Beraldo-de-araújo, Anderson; Costa, Juliana Souza Ribeiro; Pelegrine, Ana Carolina Martins; Ribeiro, Lígia Nunes Moraes; Paula, Eneida De; Oliveira-nascimento, Laura
Year: 2019
Is part of: Scientific Reports, v. 9, p. 1 - 10
DOI: https://doi.org/10.1038/s41598-019-47270-w

Citation: Beraldo-de-araújo, Viviane Lucia; Beraldo-de-araújo, Anderson; Costa, Juliana Souza Ribeiro; Pelegrine, Ana Carolina Martins; Ribeiro, Lígia Nunes Moraes; Paula, Eneida De; Oliveira-nascimento, Laura; Excipient-excipient interactions in the development of nanocarriers: an innovative statistical approach for formulation decisions. Scientific Reports, v.9, p. 1-10, 2019

Abstract: Excipient interaction has become essential knowledge for rational formulation design of nanoparticles. Nanostructured lipid carriers (NLCs) include at least three types of excipient, which enhance excipient interaction possibilities and relevance. The present article introduces an alternative approach for evaluating a great number of excipients with few samples, using NLC as a model delivery system. This approach is based on two sequential experiments using Hall-2 experimental design and analysis of excipient interactions in respect to their physicochemical properties by multilevel statistics. NLCs were prepared using a hot emulsification-ultrasonication method with lidocaine and nine excipients (solid lipids, oils and surfactants). The evaluated parameters were z-average size (DLS), dispersity (DLS), zeta potential (electrophoretic mobility) and entrapment efficiency (HPLC). Cetyl palmitate, beeswax, castor oil, capric/caprylic acid and polysorbate 80 all presented larger effects amongst the studied factors as well as a clear pattern of synergistic interactions. Following the verified trends, we produced an optimized NLC that exhibited all desirable physicochemical characteristics and a modified drug release profile. Our results demonstrate the methodology's robustness, which can be applied to other nanoparticles and establish a cost-effective excipient evaluation.

Keywords: drug delivery systems; nanostructed lipid carriers;
Subjects: CIENCIAS_DA_SAUDE;


Funding: This study was financed in part by the Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior - Brasil (CAPES) - Finance Code 001 and Sao Paulo Research Foundation (FAPESP) grant number 14/14457-5. The authors thank Espaco da Escrita - Pro-Reitoria de Pesquisa - UNICAMP - for the language services provided.
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