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

Author(s):Show less -

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]

Affiliation

^[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

• Document type: Journal article
• Source: HELIYON; v. 5, n. 10 OCT 2019.
• Web of Science Citations: 0

Abstract

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)

• FAPESP's process: 13/08166-5 - Interfacial chemistry: drugs, peptides and ezymes interactions with membrane models
• Grantee: Iolanda Midea Cuccovia
• Support Opportunities: Research Projects - Thematic Grants
• FAPESP's process: 14/50983-3 - INCT 2014: complex fluids
• Grantee: Antonio Martins Figueiredo Neto
• Support Opportunities: Research Projects - Thematic Grants