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

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*

*Corresponding author

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

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.
OriginalsprogEngelsk
Artikelnummere02648
TidsskriftHeliyon
Vol/bind5
Udgave nummer10
Antal sider10
ISSN2405-8440
DOI
StatusUdgivet - okt. 2019
Udgivet eksterntJa

Bibliografisk note

Funding Information:
L. Farkuh thanks Ph.D. Bárbara Bianca Gerbelli (IF-USP), CNPq, FAPESP (Proc. 2013/08166-5), Santander Universidades (COPGRAD.01 - 044/2014). I.M.Cuccovia thanks the National Council for Scientific and Technological Development (CNPq – 465259/2014-6), the Coordination for the Improvement of Higher Education Personnel (CAPES), the National Institute of Science and Technology Complex Fluids (INCT-FCx), and the São Paulo Research Foundation (FAPESP – 2014/50983-3). We acknowledge the Brazilian Nanotechnology National Laboratory (LNNano), CNPEM, for the use of cryo-TEM facilities. This work was supported by The European Union ( FEDER funds) and National Funds ( FCT / MEC , Fundação para a Ciência e a Tecnologia and Ministério da Educação e Ciência) under the Partnership Agreement PT2020 UID/QUI/50006/2013 - POCI/01/0145/FEDER/007265. L. Barreiros thanks FCT and POPH (Programa Operacional Potencial Humano) for her Post-Doc grant (SFRH/BPD/89668/2012). C. Nunes thanks FCT for her Investigator Grant (IF/00293/2015). G.P.B.Carretero acknowledges the Programa CAPES: INCT -Institutos Nacionais de Ciência e Tecnologia (Proc. 88887.137085/2017-00), R.A. Muramoto acknowledges CNPq. I.M. Cuccovia, H. Chaimovich, and S. Schreier are research fellows of CNPq.

Emneord

  • Biotechnology
  • Cryo-TEM
  • DLS
  • DSC
  • Ionizable solute
  • Lauric acid
  • Lipid Vesicles
  • Pharmaceutical Science
  • SAXS

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