4
views
0
recommends
+1 Recommend
0 collections
    0
    shares
      • Record: found
      • Abstract: found
      • Article: found
      Is Open Access

      Lipids and Lipid-Processing Pathways in Drug Delivery and Therapeutics

      other

      Read this article at

      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          Abstract

          The aim of this work is to analyze relevant endogenous lipid processing pathways, in the context of the impact that lipids have on drug absorption, their therapeutic use, and utilization in drug delivery. Lipids may serve as biomarkers of some diseases, but they can also provide endogenous therapeutic effects for certain pathological conditions. Current uses and possible clinical benefits of various lipids (fatty acids, steroids, triglycerides, and phospholipids) in cancer, infectious, inflammatory, and neurodegenerative diseases are presented. Lipids can also be conjugated to a drug molecule, accomplishing numerous potential benefits, one being the improved treatment effect, due to joined influence of the lipid carrier and the drug moiety. In addition, such conjugates have increased lipophilicity relative to the parent drug. This leads to improved drug pharmacokinetics and bioavailability, the ability to join endogenous lipid pathways and achieve drug targeting to the lymphatics, inflamed tissues in certain autoimmune diseases, or enable overcoming different barriers in the body. Altogether, novel mechanisms of the lipid role in diseases are constantly discovered, and new ways to exploit these mechanisms for the optimal drug design that would advance different drug delivery/therapy aspects are continuously emerging.

          Related collections

          Most cited references76

          • Record: found
          • Abstract: found
          • Article: not found

          Polyunsaturated fatty acids and their metabolites in brain function and disease.

          The brain is highly enriched with fatty acids. These include the polyunsaturated fatty acids (PUFAs) arachidonic acid and docosahexaenoic acid, which are largely esterified to the phospholipid cell membrane. Once PUFAs are released from the membrane, they can participate in signal transduction, either directly or after enzymatic conversion to a variety of bioactive derivatives ('mediators'). PUFAs and their mediators regulate several processes within the brain, such as neurotransmission, cell survival and neuroinflammation, and thereby mood and cognition. PUFA levels and the signalling pathways that they regulate are altered in various neurological disorders, including Alzheimer's disease and major depression. Diet and drugs targeting PUFAs may lead to novel therapeutic approaches for the prevention and treatment of brain disorders.
            Bookmark
            • Record: found
            • Abstract: found
            • Article: not found

            Role of cholesterol and lipid organization in disease.

            Membrane lipids are essential for biological functions ranging from membrane trafficking to signal transduction. The composition of lipid membranes influences their organization and properties, so it is not surprising that disorders in lipid metabolism and transport have a role in human disease. Significant recent progress has enhanced our understanding of the molecular and cellular basis of lipid-associated disorders such as Tangier disease, Niemann-Pick disease type C and atherosclerosis. These insights have also led to improved understanding of normal physiology.
              Bookmark
              • Record: found
              • Abstract: found
              • Article: not found

              Atherogenesis: a postprandial phenomenon.

              The hypothesis that plasma chylomicrons in persons who ingest a cholesterol-rich diet are atherogenic is evaluated. Evidence is presented that in humans, and experimental animals, chylomicron remnants as well as low-density lipoproteins are taken up by arterial cells. In persons who do not have familial hyperlipoproteinemia, atherogenesis may occur during the postprandial period. Research directions that may contribute to the evaluation of chylomicron remnants as a risk factor for atherogenesis are discussed. Lipoprotein studies after administration of a test meal containing fat and cholesterol are urgently needed.
                Bookmark

                Author and article information

                Journal
                Int J Mol Sci
                Int J Mol Sci
                ijms
                International Journal of Molecular Sciences
                MDPI
                1422-0067
                04 May 2020
                May 2020
                : 21
                : 9
                : 3248
                Affiliations
                [1 ]Department of Clinical Pharmacology, School of Pharmacy, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer-Sheva 8410501, Israel; milica@ 123456post.bgu.ac.il (M.M.); sbs@ 123456bgu.ac.il (S.B.-S.)
                [2 ]Department of Chemistry, University of Florida, Gainesville, FL 32603, USA; aponick@ 123456chem.ufl.edu
                [3 ]Department of Medicine, Division of Gastroenterology, University of Florida, Gainesville, FL 32610, USA; Ellen.Zimmermann@ 123456medicine.ufl.edu
                Author notes
                [* ]Correspondence: arikd@ 123456bgu.ac.il
                Author information
                https://orcid.org/0000-0002-3998-1833
                https://orcid.org/0000-0002-4576-638X
                https://orcid.org/0000-0002-3498-3514
                Article
                ijms-21-03248
                10.3390/ijms21093248
                7247327
                32375338
                1015caf5-1d36-4e63-b228-f7374c184405
                © 2020 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 13 April 2020
                : 02 May 2020
                Categories
                Concept Paper

                Molecular biology
                lipid,fatty acid,glyceride,steroid,phospholipid,oral drug absorption,prodrug,phospholipase a2 (pla2)

                Comments

                Comment on this article