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1.
J Microencapsul ; 20(1): 87-96, 2003.
Article in English | MEDLINE | ID: mdl-12519704

ABSTRACT

A novel solvent-free particle coating process, based on the solvent properties of supercritical fluids (SCF) is described. It consists of dissolving one or more coating materials in supercritical CO(2) and then adjusting T/P conditions in the autoclave so that the coating material becomes insoluble in the CO(2). This insolubilization step causes a coating to deposit on the surface of suspended particles. This process has been applied to bovine serum albumin and sugar granules. Coating was effective, but different morphologies were obtained depending on the coating material used. A discontinuous coating has been made using trimyristin, since this material precipitates as micro-needles. Conversely, a smooth, regular coating has been obtained with a commercially available mixture of glycerides and glyceride esters of PEG (Gelucire 50/02) acting like a film-forming agent.


Subject(s)
Drug Compounding/methods , Drug Delivery Systems , Capsules/chemistry , Carbon Dioxide/chemistry , Serum Albumin, Bovine/administration & dosage , Solubility , Solvents , Sucrose/administration & dosage , Surface Properties , Technology, Pharmaceutical , Temperature , Triglycerides/chemistry
2.
J Microencapsul ; 20(1): 97-109, 2003.
Article in English | MEDLINE | ID: mdl-12519705

ABSTRACT

Solubility measurements of candidate coating materials have been performed in supercritical (SC) CO(2) so as to select appropriate coating materials for implementation of a solvent-free coating process previously described. Solubility of lipidic compounds such as waxes (paraffin, beeswax, Carnauba wax), pure triglycerides (tricaprin, trimyristin, tripalmitin, tristearin) and mixture of glycerides and fatty acid esters (Gelucire) in SC CO(2) were evaluated in a static mode under different temperature and pressure conditions, ranging from 13-52 degrees C and from 50-220 bar, whether the CO(2)was in its liquid or SC state. It was shown that the compounds which are mixtures of various components give rise to a selective extraction of the lower melting point components, as evidenced from thermal analysis of soluble and insoluble fractions of the coating materials.


Subject(s)
Drug Compounding/methods , Drug Delivery Systems , Lipids/chemistry , Capsules/chemistry , Carbon Dioxide/chemistry , Solubility , Surface Properties , Technology, Pharmaceutical , Temperature , Waxes/chemistry
3.
J Microencapsul ; 20(1): 110-28, 2003.
Article in English | MEDLINE | ID: mdl-12519706

ABSTRACT

Solvent-free microparticles, loaded with bovine serum albumin as a model protein, were produced using a novel supercritical (SC) fluid-based coating technology. Coating material consists either of trimyristin (Dynasan 114) or of Gelucire 50-02. Microparticles obtained were characterized as regards their morphology, protein content and in vitro release profile. A discontinuous coating made of micro-needles of trimyristin led to an initial burst release of approximately 70% in 30 min. However, a prolonged release of the BSA could be achieved in a phosphate buffer solution at 37 degrees C over a 24 h period from particles coated with Gelucire 50-02. Furthermore, it was shown that BSA does not undergo any degradation after SC CO(2) treatment under the conditions used in the coating process.


Subject(s)
Drug Delivery Systems , Lipids/chemistry , Serum Albumin, Bovine/administration & dosage , Capsules , Carbon Dioxide/chemistry , Delayed-Action Preparations/administration & dosage , Delayed-Action Preparations/chemistry , Drug Carriers/chemistry , Drug Compounding/methods , Fats/chemistry , Microscopy, Electron, Scanning , Oils/chemistry , Particle Size , Serum Albumin, Bovine/chemistry , Solubility , Surface Properties , Technology, Pharmaceutical , Temperature
4.
Int J Pharm ; 242(1-2): 69-78, 2002 Aug 21.
Article in English | MEDLINE | ID: mdl-12176227

ABSTRACT

Solvent-free microparticles, loaded with a model protein (bovine serum albumin: BSA) have been produced using a novel coating process based on supercritical (SC) fluid technology. Coating material consists of either trimyristin (Dynasan114) or Gelucire50-02, two lipidic compounds having a high melting point. Microparticles were characterized as regards their morphology, protein content and in vitro release profile. A discontinuous coating made of crystalline micro-needles was obtained using Dynasan114. It led to particles with an initial burst release of about 70% in 30 min at 37 degrees C. However, a prolonged release of the protein has been achieved over a 24 h period from particles coated with Gelucire50-02, which produces a more homogeneous, film-forming coating. Furthermore, it was shown that BSA does not undergo any degradation after SCCO2 treatment under the SC conditions used in the coating process.


Subject(s)
Drug Compounding/methods , Proteins/chemistry , Carbon Dioxide/chemistry , Delayed-Action Preparations , Drug Stability , Electrophoresis, Polyacrylamide Gel , Excipients , Kinetics , Lipids/chemistry , Particle Size , Pressure , Proteins/administration & dosage , Serum Albumin, Bovine/chemistry , Solvents , Surface Properties
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