Author(s): Perera G, Barthelmes J, BernkopSchnrch A
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Abstract Within this study metronidazole-containing microparticles based on a pectin-4-aminothiophenol (Pec-ATP) conjugate were developed and investigated regarding their potential for colon-specific drug delivery. Microparticles were produced by spray-drying and subsequent processing. Posteriorly, they were investigated regarding their disintegration behavior, particle size, drug load, release behavior and impact on viability of Caco-2 cells. Microparticles with a mean diameter of 5.16+/-2.41 microm and a drug load of 1.15+/-0.03\% metronidazole were prepared. Disintegration studies revealed that the stability of Pec-ATP microparticles was significantly improved compared to control microparticles based on unmodified pectin. In vitro release studies without potential colonic release-inducers revealed that 34.4-fold more metronidazole is retarded in Pec-ATP microparticles within 6h compared to control particles. It could be demonstrated that the retarded amount of metronidazole can be released rapidly under the influence of pectinolytic enzymes or a reducing agent, simulating the colonic environment. Cell viability studies did not reveal a significant difference between native and modified pectin, neither as a solution nor as microparticle suspension. From the improved stability, the described release features and the low toxicity of the investigated microparticles can be concluded that these particles are a promising carrier for colon-specific drug delivery. Copyright (c) 2010 Elsevier B.V. All rights reserved.
This article was published in J Control Release
and referenced in Biology and Medicine