Various polymers

Three polymers have been used to encapsulate a hydrophobic drug (Seiyaku, 1980). For example, polystyrene was dissolved in an organic solvent which was immiscible with water. A hydrophobic drug was then incorporated into the solution and then this core material was dissolved in an enteric high-polymer electrolyte; for example, methylacrylate. Coacerva-tion was then carried out with a solution of gelatin at an appropriate pH and cooling. Thus the drug is surrounded by the high-polymer and a coacérvate wall film of gelatin and the polymer electrolyte.

Mathiowitz etal. (1988) prepared polyanhydrides of the following diacids: sebacic, bis (p-carboxy phenoxy) propane and dodecanedioic acid. The polymers were characterized by infrared spectroscopy, X-ray diffrac tion, viscosity, differential scanning calorimetry and scanning electron microscopy. Microspheres were prepared by dissolving the polymer in methylene chloride, adding the core and then the mixture was dropped into silicone oil containing Span 85 and varying amounts of methylene chloride, depending on the polymer. After stirring for 1 h, petroleum ether was added, and after further stirring the microcapsules were isolated. Several modifications of the above procedure were tested. In general, the surface of the microspheres was smooth with no pores. The porosity of the microcapsules depended upon the polymer and the proportions of the polymer used to prepare the microspheres. It was proposed that the process used with low molecular weight polymers took place slowly, resulting in relatively non-porous microspheres, whereas the process used for high molecular weight polymers was rapid and resulted in spheres with significant internal porosity. Drug release was affected by polymer composition, physical properties of the microspheres and the type of drug. Microspheres loaded with insulin showed good urine and serum glucose control in diabetic rats.

Bodmeier and Chen (1989) encapsulated three anti-inflammatory agents, namely indomethacin, ibuprofen and ketoprofen, by solvent evaporation using various polymers: ethylcellulose, poly(e-caprolactone), poly(methyl methacrylate), polystyrene and Eudragit RS and RL. The polymer and drug were codissolved in a water-immiscible organic solvent. This solution was then poured into the aqueous phase containing a low concentration of poly (vinyl alcohol). The resulting o/w emulsion was then agitated for 90 min at room temperature. The microspheres were filtered, washed with water and dried. The encapsulation efficiency into ethylcellulose was highest for indomethacin followed by ibuprofen and ketoprofen. This order was inversely correlated to the aqueous solubility. All drugs were encapsulated because of their low water solubility and the efficiency of encapsulation was improved by increasing the drug loading and the polymer: organic solvent ratio. The drug release in aqueous solution at pH 7.4, 37°C under sink conditions was governed by microsphere size, drug loading and polymer composition. The release of indomethacin from ethylcellulose microcapsules was too slow and could be increased by using more permeable polymers or polymers blends. The rates of polymer and drug precipitation during microsphere formation depended upon the organic solvent selected. When chloroform was used as the solvent, the drug precipitated before the polymer and indomethacin crystals were observed on the microsphere surface. With methylene chloride, the polymer precipitated before the drug and no drug crystals were seen.

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