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

Autor: Laura Farkuh, Paulo T. Hennies, Cláudia Nunes, Salette Reis, Luisa Barreiros, Marcela A. Segundo, Pedro L. Oseliero Filho, Cristiano L.P. Oliveira, Alexandre Cassago, Rodrigo V. Portugal, Rodrigo A. Muramoto, Gustavo P.B. Carretero, Shirley Schreier, Hernan Chaimovich, Iolanda M. Cuccovia
Jazyk: angličtina
Rok vydání: 2019
Předmět:
Zdroj: Heliyon, Vol 5, Iss 10, Pp e02648- (2019)
Druh dokumentu: article
ISSN: 2405-8440
DOI: 10.1016/j.heliyon.2019.e02648
Popis: 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.
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