Top ten considerations in the development of parenteral emulsions.

The development of parenteral emulsions continues to play an important role in the formulation and delivery of many drugs. In addition to solubilization and stabilization applications, appropriately designed parenteral emulsions are effective delivery systems for sustained release and targeting of drugs. Control of the strict requirements of globule size and surface charge is important in the design and ultimate stability of the formulation. This review highlights the important issues and suggests strategies to assist the scientist in the development, manufacture and stability of this essential dosage form.

[1]  M. Tripp,et al.  Stability of total nutrient admixtures in a dual-chamber flexible container. , 1990, American journal of hospital pharmacy.

[2]  B. Lundberg,et al.  Preparation of drug-carrier emulsions stabilized with phosphatidylcholine-surfactant mixtures. , 1994, Journal of pharmaceutical sciences.

[3]  P. Carl,et al.  Pregnanolone emulsion , 1987, Anaesthesia.

[4]  C. Washington.  The electrokinetic properties of phospholipid-stabilized fat emulsions: III. Interdroplet potentials and stability ratios in monovalent electrolytes , 1990 .

[5]  R. Haskell.  Characterization of submicron systems via optical methods. , 1998, Journal of pharmaceutical sciences.

[6]  A. Tibell,et al.  Cyclosporin A in fat emulsion carriers: experimental studies on pharmacokinetics and tissue distribution. , 1995, Pharmacology & toxicology.

[7]  Arvid Wretlind,et al.  Invited Review: Development of Fat Emulsions , 1981 .

[8]  C. Washington.  Stability of lipid emulsions for drug delivery , 1996 .

[9]  J. Riess,et al.  Highly fluorinated amphiphiles and colloidal systems, and their applications in the biomedical field. A contribution. , 1998, Biochimie.

[10]  M. Groves,et al.  Hydrolysis Kinetics of Phospholipids in Thermally Stressed Intravenous Lipid Emulsion Formulations , 1992, The Journal of pharmacy and pharmacology.

[11]  N. Niederle,et al.  Hypersensitivity reactions to parenteral lipid solutions , 1997, Supportive Care in Cancer.

[12]  M. Weinstock,et al.  Pharmacological evaluation of an injectable prolonged release emulsion of physostigmine in rabbits , 1986, The Journal of pharmacy and pharmacology.

[13]  M. Kearney,et al.  Compatibility and stability of additives in parenteral nutrition admixtures. , 1998, Nutrition.

[14]  Recollections of pioneers in nutrition: landmarks in the development of parenteral nutrition. , 1992, Journal of the American College of Nutrition.

[15]  Zuck Tf,et al.  Current status of injectable oxygen carriers. , 1994 .

[16]  B. Müller,et al.  The effect of oil components and homogenization conditions on the physicochemical properties and stability of parenteral fat emulsions , 1998 .

[17]  C. Washington,et al.  The electrokinetic properties of phospholipid stabilized fat emulsions. IV. The effect of glucose and of pH , 1990 .

[18]  M. Hashida,et al.  Prolonged release of bleomycin from parenteral gelatin sphere-in-oil-in-water multiple emulsion. , 1982, Chemical & pharmaceutical bulletin.

[19]  S. Benita,et al.  Submicron emulsions as colloidal drug carriers for intravenous administration: comprehensive physicochemical characterization. , 1993, Journal of pharmaceutical sciences.

[20]  John P. Grant,et al.  Invited Review: Intravenous Lipid Emulsions , 1987 .

[21]  B. Lundberg.  A Submicron Lipid Emulsion Coated with Amphipathic Polyethylene Glycol for Parenteral Administration of Paclitaxel (Taxol) , 1997, The Journal of pharmacy and pharmacology.

[22]  S. Davis,et al.  The electrokinetic properties of phospholipid-stabilized fat emulsions , 1990 .

[23]  M. Laval-jeantet,et al.  Effect of Particle Size on the Tissue Distribution of Iodized Emulsified Fat Following Intravenous Administration , 1982, Investigative radiology.

[24]  D. Maki,et al.  Total nutrient admixtures appear safer than lipid emulsion alone as regards microbial contamination: growth properties of microbial pathogens at room temperature. , 1998, JPEN. Journal of parenteral and enteral nutrition.

[25]  Gilbert S. Banker,et al.  Pharmaceutical Dosage Forms: Disperse Systems , 1988 .

[26]  J. Gallelli,et al.  Formulation and evaluation of ethiodized oil emulsion for intravenous hepatography. , 1979, Journal of pharmaceutical sciences.

[27]  C. Washington.  The electrokinetic properties of phospholipid stabilized fat emulsions VI. Zeta potentials of Intralipid 20% in TPN mixtures , 1992 .

[28]  S. Yalkowsky,et al.  Evaluation of in vitro precipitation methods. , 1998, Journal of pharmaceutical sciences.

[29]  L. Zarif,et al.  Novel fluorocarbon-based injectable oxygen-carrying formulations with long-term room-temperature storage stability. , 1994, Advances in experimental medicine and biology.

[30]  H. Ogata,et al.  Effect of phospholipid emulsifiers on physicochemical properties of intravenous fat emulsions and/or drug carrier emulsions , 1990, The Journal of pharmacy and pharmacology.

[31]  J. Sibert,et al.  Hypernatraemic dehydration and necrotizing enterocolitis. , 1985, Postgraduate medical journal.

[32]  C. Washington.  The electrokinetic properties of phospholipid-stabilized fat emulsions. II. Droplet mobility in mixed electrolytes , 1990 .

[33]  C. Washington,et al.  THE ELECTROKINETIC PROPERTIES OF PHOSPHOLIPID STABILIZED FAT EMULSIONS.V.THE EFFECT OF AMINO ACIDS ON EMULSION STABILITY , 1991 .

[34]  J. Sunamoto,et al.  Polysaccharide-coated oil droplets in oil-in-water emulsions as targetable carriers for lipophilic drugs. , 1991, Journal of pharmaceutical sciences.

[35]  D. L. Gilbert,et al.  Compatibility of propofol injectable emulsion with selected drugs during simulated Y-site administration. , 1997, American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists.

[36]  I. Hakansson,et al.  Physical and biological changes in an artificial fat emulsion during storage , 1964, The Journal of pharmacy and pharmacology.

[37]  A. A. Hincal,et al.  Preparation and properties of a stable intravenous lorazepam emulsion , 1997, Journal of clinical pharmacy and therapeutics.

[38]  G. Hardy,et al.  The stability of ascorbic acid in TPN mixtures stored in a multilayered bag. , 1992, Clinical nutrition.

[39]  Taizo Kimura,et al.  The pharmacokinetics of water-in-oil-in-water-type multiple emulsion of a new tacrolimus formulation , 1997, Lipids.

[40]  A. Kurihara,et al.  Lipid emulsions of palmitoylrhizoxin: effects of particle size on blood dispositions of emulsion lipid and incorporated compound in rats. , 1996, Biopharmaceutics & drug disposition.

[41]  L. Pelham.  Rational use of intravenous fat emulsions. , 1981, American journal of hospital pharmacy.

[42]  W. Yu,et al.  A novel approach to the preparation of injectable emulsions by a spontaneous emulsification process , 1993 .

[43]  S. Benita,et al.  Emulsions as drug carriers for ophthalmic use , 1994 .

[44]  M. Y. Levy,et al.  Design and characterization of a submicronized o/w emulsion of diazepam for parenteral use , 1989 .

[45]  Rainer H. Müller,et al.  Effect of light and temperature on zeta potential and physical stability in solid lipid nanoparticle (SLN) dispersions , 1998 .

[46]  C. Washington,et al.  Reduction of absorption of drugs into TPN plastic containers by phospholipids and fat emulsions , 1988 .

[47]  L. Allen,et al.  Studies on microemulsions using Brij 96 as surfactant and glycerin, ethylene glycol and propylene glycol as cosurfactants , 1989 .

[48]  T. Fujita,et al.  Fluorocarbon emulsion as a candidate for artificial blood. Correlation between particle size of the emulsion and acute toxicity. , 1971, European surgical research. Europaische chirurgische Forschung. Recherches chirurgicales europeennes.

[49]  W. Steffee,et al.  Microbial growth comparisons of five commercial parenteral lipid emulsions. , 1984, JPEN. Journal of parenteral and enteral nutrition.

[50]  S. Davis,et al.  The production of parenteral feeding emulsions by microfluidizer , 1988 .

[51]  H. Talsma,et al.  Particle size in parenteral fat emulsions, what are the true limitations? , 1996 .

[52]  D. Lichtenberg,et al.  Lipid infusion with different triglyceride cores (long-chain vs medium-chain/long-chain triglycerides): effect on plasma lipids and bilirubin binding in premature infants. , 1991, JPEN. Journal of parenteral and enteral nutrition.

[53]  S. Venkatesh,et al.  Compositional heterogeneity in parenteral lipid emulsions after sedimentation field flow fractionation. , 1998, Journal of pharmaceutical sciences.

[54]  S. Mühlebach,et al.  Lipid peroxidation of i.v. lipid emulsions in TPN bags: the influence of tocopherols. , 1998, Nutrition.

[55]  C. Washington.  The stability of intravenous fat emulsions in total parenteral nutrition mixtures , 1990 .

[56]  W. S. Singleton,et al.  Chromatographically homogeneous egg lecithin as stabilizer of emulsions for intravenous nutrition , 1964 .

[57]  B. Müller,et al.  The stabilization of parenteral fat emulsion using non-ionic ABA copolymer surfactant , 1998 .

[58]  Raymond C Rowe,et al.  Handbook of Pharmaceutical Excipients , 1994 .

[59]  H. Kaş,et al.  Naproxen incorporated lipid emulsions. I. Formulation and stability studies , 1998, Journal of clinical pharmacy and therapeutics.