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      Liposomes containing lipids from Sulfolobus islandicus withstand intestinal bile salts: An approach for oral drug delivery?

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          Abstract

          In an attempt to design an oral drug delivery system, suited to protect labile drug compounds like peptides and proteins against the harsh environment in the stomach and upper intestine, we have prepared liposomes from phospholipids, cholesterol and archaeal lipids. As source for the archaeal lipids we used Sulfolobus islandicus, a hyperthermophilic archaeon, whose lipids have not been used in liposomes before. Culturing conditions and extraction protocols for its membrane lipids were established and the lipid composition of the crude lipid extract was characterized. The extracted membrane lipid fraction of S. islandicus consisted primarily of diether lipids with only a small fraction of tetraether lipids. Small unilamellar liposomes with 18% (mol/mol) of crude archaeal lipid extract were from S. islandicus were produced, for the first time and proven to be stabilized against aggressive bile salts as determined by loss of entrapped marker (calcein). At 4.4mM taurocholate (physiological taurocholate level) liposomes containing archaeal lipids retained entrapped marker better than liposomes made of egg phosphatidylcholine (PC) alone and to an extent similar to liposomes made of egg PC and cholesterol. Our findings showed that crude archaeal lipid extracts have, to a certain extent, stabilizing effects on liposomes similar to purified tetraether lipid fractions tested previously.

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          Author and article information

          Journal
          Int J Pharm
          International journal of pharmaceutics
          Elsevier BV
          1873-3476
          0378-5173
          Sep 30 2015
          : 493
          : 1-2
          Affiliations
          [1 ] Department of Biology and Nordic Center for Earth Evolution, University of Southern Denmark, Odense, Denmark; Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Odense, Denmark.
          [2 ] Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Odense, Denmark.
          [3 ] Department of Biology and Nordic Center for Earth Evolution, University of Southern Denmark, Odense, Denmark.
          [4 ] Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Odense, Denmark. Electronic address: mmb@sdu.dk.
          Article
          S0378-5173(15)30045-4
          10.1016/j.ijpharm.2015.07.026
          26192627
          250ece3c-25cb-4597-ab2a-4d768ff4b3da
          History

          Archaeal lipids,Bile salt,Ether lipid,Lipid structure,Liposome,Oral delivery system,Structure elucidation

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