Particle size, surface hydrophobicity and interaction with serum of parenteral fat emulsions and model drug carriers as parameters related to RES uptake

      This paper is only available as a PDF. To read, Please Download here.


      Fat emulsions for parenteral nutrition, stabilized by egg lecithin, were characterized in terms of parameters relevant to uptake by the reticuloendothelial system (RES), e.g. size distribution, surface hydrophobicity and adsorption of serum components as a measure of the degree of opsonization. Adsorption of serum components was quantified by zeta potential measurement. Fat emulsions for nutrition were compared with emulsions used for drug delivery and model drug carries for intravenous injection. The emulsions for drug delivery were stabilized by the blockcopolymers Poloxamer 188 and 407 (Pluronic F68 and F127) and Poloxamine 908. Model drug carriers were hydrophobic and hydrophilic polystyrene latex particles. Hydrophilic particles were prepared by adsorption of Poloxamine 908 (coating) onto the particle surface. The hydrophobicity and serum protein adsorption decreased from hydrophobic latex particles to egg lecithin emulsions and blockcopolymer emulsions and particles. The data correlated with that in the literature concerning liver uptake in vivo showing complete RES clearance of hydrophobic latex particles, reduced uptake of egg lecithin emulsions and avoidance of RES uptake by Poloxamine 908 coated particles.
      To read this article in full you will need to make a payment
      Subscribe to Clinical Nutrition
      Already a print subscriber? Claim online access
      Already an online subscriber? Sign in
      Institutional Access: Sign in to ScienceDirect


        • Müller RH
        Colloidal Carriers for Controlled Drug Delivery and Targeting.
        Wissenschaftliche Verlagsgesellschaft, Stuttgart, Germany1991 (CRC Press, Boca Raton, Florida)
        • Davis SS
        Colloids as drug-delivery systems.
        Pharmaceutical Technology. 1981; 5: 71-88
        • Senior J
        • Crawley JCW
        • Gregoriadis G
        Tissue distribution of liposomes exhibiting long half-lives in the circulation after intravenous injection.
        Biochemica Biophysica Acta. 1985; 839: 1-8
        • Karino A
        • Hayashi H
        • Yamada K
        • Ozawa Y
        Effect of particle size and emulsifiers on the blood clearance and deposition of injected emulsions.
        Journal of Pharmaceutical Sciences. 1987; 11: 273
        • Schwendener RA
        • Lagocki PA
        • Rahman YE
        The effect of charge and size on the interaction of unilamellar liposomes with macrophages.
        Biochemica Biophysica Acta. 1984; 772: 93-101
        • Wilkins DJ
        • Myers PA
        Studies on the relationship between the electrophoretic properties of colloids and their blood clearance and organ distribution in the rat.
        British Journal of Experimental Pathology. 1966; 47: 568-576
        • Van Oss CJ
        Phagocytosis as a surface phenomenon.
        Annual Review Microbiology. 1978; 32: 19-39
        • Van Oss CJ
        • Absolom DR
        • Neumann HW
        Interaction of phagocytes with other blood cells and with pathogenic and nonpathogenic microbes.
        Annals of the New York Academy of Sciences. 1984; 416: 332-350
        • Van Oss CJ
        • Gillman CF
        • Neumann AW
        Phagocytic Engulfment and Cell Adhesiveness as Cellular Surface Phenomena.
        Dekker, New York1975
        • Edebo L
        • Richardson N
        Enhancement of hydrophobic interaction, negative charge and phagocytosis by dinitrophenyl ligand coupling to Salmonella typhimurium 395 MS.
        International Archives of allergy and Applied Immunology. 1985; 78: 345-352
        • Blunk T
        • Hochstrasser D
        • Rudt S
        • Müller RH
        Two-dimensional gel electrophoresis in the concept of differential opsonization — an approach to drug targeting.
        Archiv der Pharmazie. 1991; 324: 706
        • Wegmuller E
        • Mondandon A
        • Nydegger UE
        • Descoeudres C
        Biocompatibility of different hemodialysis membranes: activation of complement and leukopenia.
        International Journal of Artificial Organs. 1986; 9: 85-92
        • Müller RH
        • Davis SS
        • Illum L
        • Mak E
        Surface characterization of colloidal drug carriers coated with polymers.
        Macromolecular Reprints. 1986; : 161-162
        • Lherm C
        • Müller RH
        • Blunk T
        • Perie M
        • Depraetere P
        • Couvreur P
        Physico-chemical characterization of cyanoacrylate particles.
        Archiv der Pharmazie. 1988; 321: 682
        • Carpentier YA
        • Crabbe V
        • Dahlan W
        • Richelle M
        Reduced phospholipid content of 10% emulsions causes less alterations in plasma lipids of dogs infused for ten days.
        Clinical Nutrition. 1989; 8 (Special Suppl): 99
        • Weidler B
        • von Bormann B
        • Peil J
        • Elmafda I
        • Schwanen N
        • Sommermeyer K
        • Lohmann E
        Welchen Einfluß hat ein Carnitinzusatz auf die pharmakokinetischen Kenngößen einer Fettemulsion?.
        Akt. Ernähr. 1987; 12: 88-92
        • Cummins HZ
        • Pike ER
        Photon Correlation and Light Beating Spectroscopy.
        in: 2nd Edition. Nato Advanced Study Institutes Series B. Plenum Press, New York1974
        • Cummins HZ
        • Pike ER
        Photon Correlation Spectroscopy and Velocimetry.
        in: 2nd Edition. Nato Advanced Study Institutes Series B. Plenum Press, New York1977
        • Müller BW
        • Müller RH
        Particle size analysis of latex suspensions and microemulsions by photon correlation spectroscopy.
        Journal of Pharmaceutical Sciences. 1984; 73: 915-918
        • Koppel DE
        Analysis of macromolecular polydispersity in intensity correlation spectroscopy: The method of cumulants.
        Journal of Chemical Physics. 1976; 57: 4814-4820
        • Müller RH
        • Heinemann S
        • Diederichs JE
        Parenteral fat emulsions II: charge and rigidity of emulsifier film related to long-term stability.
        in: 2nd Edition. Proceed. Intern. Symp. Contr. Rel. Bioact. Mater. 18. 1991: 469
        • Heuer M
        • Leschonski K
        Erfahrungen mit einem neuen Gerät zur Messung von Partikelgrößenverteilungen aus Beugungsspektren.
        in: Preprints Eur. Symp. “Partikelmeßtechnik”. 1984: 515-538
        • James AM
        Electrophoresis of particles in suspensions.
        in: 2nd Edition. Surface and Colloid Science. Vol. 11. Plenum Press, New York1979: 121-185
        • Carstensen H
        • Müller BW
        • Müller RH
        Adsorption of ethoxylated surfactants on nanoparticles. I. Characterization by hydrophobic interaction chromatography.
        International Journal of Pharmaceutics. 1991; 67: 29-37
        • Holley W
        Homogenisieren mit Hochdruck, Niederdruck, Ultraschall und anderen Techniken.
        in: Proc. Annual meeting of the International Pharmaceutical Association (APV), 13–15 April, Strasbourg, France1989: 1-25
        • Heinemann S
        Parenteral fat emulsions — physical stability of emulsions for nutrition and drug delivery.
        in: 2nd Edition. PhD thesis. University of Kiel, Germany1991: 96
        • Vielhaber U
        Genauigkeit der Partikelgrößenanalyse mit Laserbeugungsspektrometern.
        in: Verfahrenstechnick, Interkama Report. 1989
        • Ilum L
        • West P
        • Washington C
        • Davis SS
        The effect of stabilising agent on the organ distribution of lipid emulsions.
        International Journal of Pharmaceuticals. 1989; 54: 41-49
        • Blunk T
        • Müller RH
        Uptake of charged serum components as a selection criterion for i.v. drug carriers avoiding liver/spleen uptake.
        Archiv der Pharmazie. 1989; 322: 755
        • Jeppson R
        • Rössner S
        The influence of emulsifying agents and of lipid soluble drugs on the fractional removal rate of lipid emulsions from the blood stream of the rabbit.
        Acta Pharmacol. Toxicol. 1975; 37: 134-144