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Characterization of phospholipid vesicles containing lauric acid: physicochemical basis for process and product development

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Autor(es):
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Farkuh, Laura [1] ; Hennies, Paulo T. [2] ; Nunes, Claudia [3] ; Reis, Salette [3] ; Barreiros, Luisa [3] ; Segundo, Marcela [3] ; Oseliero Filho, Pedro L. [4] ; Oliveira, Cristiano L. P. [4] ; Cassago, Alexandre [5] ; Portugal, V, Rodrigo ; Muramoto, Rodrigo A. [1] ; Carretero, Gustavo P. B. [1] ; Schreier, Shirley [1] ; Chaimovich, Hernan [1] ; Cuccovia, Iolanda M. [1]
Número total de Autores: 15
Afiliação do(s) autor(es):
[1] Univ Sao Paulo, Inst Chem, Dept Biochem, Sao Paulo - Brazil
[2] Libera Tecnol & Inovacao Ltda, Sao Paulo - Brazil
[3] Univ Porto, Fac Pharm, REQUIMTE, LAQV, Porto - Portugal
[4] Univ Sao Paulo, Inst Phys, Dept Expt Phys, Sao Paulo - Brazil
[5] V, Brazilian Ctr Res Energy & Mat CNPEM, Brazilian Nanotechnol Natl Lab LNNano, Campinas, SP - Brazil
Número total de Afiliações: 5
Tipo de documento: Artigo Científico
Fonte: HELIYON; v. 5, n. 10 OCT 2019.
Citações Web of Science: 0
Resumo

Lauric acid (LAH) strongly inhibits the growth of acne-causing bacteria. LAH is essentially water-insoluble and the solubility of laurate (LA) salts are medium and temperature dependent. Hence, LAH/LA preparations are difficult to formulate. Here we fully characterized phospholipid vesicles containing up to 50 mol% LAH. Vesicles of dipalmitoylphosphatidylcholine (DPPC) containing LAH, at pHs 7.4 and 5.0, were characterized measuring size, charge, bilayer phase transition temperature (Tm) and permeability of water-soluble probes. Small angle X-ray scattering and cryotransmission electron microscopy showed multilamellar vesicles at low LAH %. Increasing LAH % had a negligible effect on particle size. An internal aqueous compartment in all vesicle's preparations, even at equimolar DPPC: LAH fractions, was demonstrated using water-soluble probes. At pH 5.0, the interaction between DPPC and LAH increased the Tm and phase transition cooperativity showing a single lipid phase formed by hydrogen-bonded DPPC: LAH complexes. At pH 7.4, vesicles containing 50 mol% LAH exhibited distinct phases, ascribed to complex formation between LAH and LA or LAH and DPPC. LAH incorporated in the vesicles minimally permeated a skin preparation at both pHs, indicating that the primary sites of LAH solubilization were the skin layers. These results provide the foundations for developing processes and products containing DPPC: LAH. (AU)

Processo FAPESP: 13/08166-5 - Química em interfaces: interações de fármacos, peptídios e enzimas com membranas modelos
Beneficiário:Iolanda Midea Cuccovia
Linha de fomento: Auxílio à Pesquisa - Temático
Processo FAPESP: 14/50983-3 - INCT 2014: fluidos complexos
Beneficiário:Antonio Martins Figueiredo Neto
Linha de fomento: Auxílio à Pesquisa - Temático