Entrapment or microencapsulation of drugs in a polyhydroxyalkano

Details Entrapment or microencapsulation of drugs in a polyhydroxyalkano Entrapment or microencapsulation of drugs in a polyhydroxyalkano

1998-09-09

2000-11-14

Naff, David M.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424489, 435135, 435182, A61K 916, A61K 914, A61K 950, C12P 762, C12N 1104

Patent

active

061466654

ABSTRACT:
A hydrophilic or lipophilic drug is entrapped or microencapsulated in a polyhydroxyalkanoate homopolymer or copolymer. The homopolymer or copolymer is synthesized in an aqueous medium containing a dissolved hydrophilic drug by in vitro enzyme polymerization of a hydroxyalkanoate Coenzyme A monomer to form microporous granules entrapping the drug. The enzyme may be a polyhydroxyalkanoate synthase, and the monomer may be 3-hydroxybutyryl Coenzyme A or 3-hydroxyvalerate Coenzyme A. The monomer is produced by reaction of a carboxylic acid group of a hydroxyalkanoic acid with a thiol group of Coenzyme A. To microencapsulate a lipophilic drug, droplets of oil containing a lipophilic drug are formed dispersed in an aqueous medium such as in the form of an oil-in-water emulsion. The polyhydroxyalkanoate homopolymer or copolymer is formed in the aqueous medium by the enzyme polymerization to form microcapsules having a core of oil containing the drug. The granules or microcapsules containing the drug may be dried.

REFERENCES:
patent: 5229279 (1993-07-01), Peoples et al.
patent: 5250430 (1993-10-01), Peoples et al.
patent: 5451456 (1995-09-01), Marchessault et al.
Juni, et al., Journal of Controlled Release, vol. 4, 1986, pp. 25-32.
Kawaguchi, et al., Journal of Pharmaceutical Sciences, vol. 81, No. 6, Jun. 1992, pp. 508-512.
Bissery, et al., Microspheres and Drug Therapy Pharmaceutical, Immunological and Medical Aspects, 1984, pp. 217-227, edited by S.S. Davis et al, Elsevier Science Publishers.

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