Characterization of phospholipid vesicles containing lauric acid: physicochemical basis for process and product development. Issue 10 (October 2019)

• Record Type: Journal Article
• Authors: Farkuh, Laura; Hennies, Paulo T.; Nunes, Cláudia; Reis, Salette; Barreiros, Luisa; Segundo, Marcela A.; Oseliero Filho, Pedro L.; Oliveira, Cristiano L.P.; Cassago, Alexandre; Portugal, Rodrigo V.; Muramoto, Rodrigo A.; Carretero, Gustavo P.B.; Schreier, Shirley; Chaimovich, Hernan; Cuccovia, Iolanda M.
• Is Part Of: Heliyon. Volume 5:Issue 10(2019)
• Publication Date: 2019-10
• Subjects: Biotechnology -- Pharmaceutical Science -- Cryo-TEM -- Lauric acid -- DSC -- Lipid Vesicles -- DLS -- Ionizable solute -- SAXS; Research -- Periodicals; Medical sciences -- Periodicals; Natural history -- Periodicals; Social sciences -- Periodicals; Earth sciences -- Periodicals; Physical sciences -- Periodicals; 507.2
• DOI: 10.1016/j.heliyon.2019.e02648
• Languages: English
• ISSNs: 2405-8440

Abstract

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. Abstract : Biotechnology; Pharmaceutical Science; Cryo-TEM; Lauric acid; DSC; Lipid Vesicles; DLS; Ionizable solute; SAXS