Preparation and stabilization of heparin/gelatin complex coacervate microcapsules. 1997

M Tsung, and D J Burgess
Department of Pharmaceutical Sciences, School of Pharmacy, University of Connecticut, Storrs 06269-2092, USA.

The aims of this study are to optimize conditions for the preparation, stabilization, and harvesting of heparin/gelatin microcapsules prepared by complex coacervation. Microelectrophoresis and dry coacervate weight were used to determine the optimum conditions of pH and ionic strength for maximum heparin/gelatin coacervate yield. Heparin/gelatin microcapsules were formed by complex coacervation in the presence and absence of poly(1-vinyl-2-pyrrolidone) (PVP), which was used as a stabilizer. The microcapsules were collected using a spray-drying technique. Microcapsule particle size was analyzed using an AccuSizer optical sizer. Optimized conditions for maximum coacervate yield were pH 2.6, ionic strength 10 mM, and a 1:2 heparin/gelatin A ratio. PVP stabilized the heparin/gelatin coacervate droplets and reduced droplet aggregation during spray-drying. The mean particle diameter of the spray-dried coacervate droplets was lower in the presence of PVP and was unaffected by PVP concentration (in the range 0.5-2.0% w/w). Heparin/gelatin microcapsules, prepared under conditions optimized for maximum coacervate yield, were stabilized without the use of chemical cross-linking agents. Stabilization was achieved by a combination of the addition of PVP and spray-drying.

UI MeSH Term Description Entries
D008956 Models, Chemical Theoretical representations that simulate the behavior or activity of chemical processes or phenomena; includes the use of mathematical equations, computers, and other electronic equipment. Chemical Models,Chemical Model,Model, Chemical
D010316 Particle Size Relating to the size of solids. Particle Sizes,Size, Particle,Sizes, Particle
D004337 Drug Carriers Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers. Drug Carrier
D004586 Electrophoresis An electrochemical process in which macromolecules or colloidal particles with a net electric charge migrate in a solution under the influence of an electric current. Electrophoreses
D005780 Gelatin A product formed from skin, white connective tissue, or bone COLLAGEN. It is used as a protein food adjuvant, plasma substitute, hemostatic, suspending agent in pharmaceutical preparations, and in the manufacturing of capsules and suppositories. Gelafusal
D006493 Heparin A highly acidic mucopolysaccharide formed of equal parts of sulfated D-glucosamine and D-glucuronic acid with sulfaminic bridges. The molecular weight ranges from six to twenty thousand. Heparin occurs in and is obtained from liver, lung, mast cells, etc., of vertebrates. Its function is unknown, but it is used to prevent blood clotting in vivo and vitro, in the form of many different salts. Heparinic Acid,alpha-Heparin,Heparin Sodium,Liquaemin,Sodium Heparin,Unfractionated Heparin,Heparin, Sodium,Heparin, Unfractionated,alpha Heparin

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