Excipient-excipient interactions in the development of nanocarriers: an innovative statistical approach for formulation decisions

Autor(es)

Beraldo-de-Araujo, Viviane Lucia ^{[1, 2]} ; Beraldo-de-Araujo, Anderson ^[3] ; Ribeiro Costa, Juliana Souza ^{[1, 2]} ; Martins Pelegrine, Ana Carolina ^[2] ; Moraes Ribeiro, Ligia Nunes ^[1] ; de Paula, Eneida ^[1] ; Oliveira-Nascimento, Laura ^[2]

Afiliação do(s) autor(es)

^[1] Univ Estadual Campinas, Biol Inst, Dept Biochem & Tissue Biol, Rua Monteiro Lobato 255, BR-13083862 Campinas, SP - Brazil

^[2] Univ Estadual Campinas, Pharmaceut Technol Lab, Fac Pharmaceut Sci, Rua Candido Portinari 200, BR-13083871 Campinas, SP - Brazil

^[3] Fed Univ ABC, Ctr Nat & Human Sci, BR-05508090 Santo Andre - Brazil

• Tipo de documento: Artigo Científico
• Fonte: SCIENTIFIC REPORTS; v. 9, JUL 24 2019.
• Citações Web of Science: 0

Resumo

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. (AU)

• Processo FAPESP: 14/14457-5 - Carreadores baseados em lipídios (SLN/NLC e lipossomas com gradiente iônico) como estratégia para aumentar a encapsulação e a potência de anestésicos locais
• Beneficiário: Eneida de Paula
• Modalidade de apoio: Auxílio à Pesquisa - Temático