Doxorubicin loading and eluting characteristics of bioresorbable hydrogel microspheres: In vitro study

Lihui Weng, Hung C. Le, Jingying Lin, Jafar Golzarian

Research output: Contribution to journalArticlepeer-review

40 Scopus citations

Abstract

Non-bioresorbable drug eluting microspheres are being increasingly used for the treatment of unresectable liver tumors, whereas bioresorbable microspheres have not received much attention. In this study, bioresorbable microspheres prepared from chitosan and carboxymethyl cellulose were loaded with doxorubicin (Doxo) via ion-exchange interactions with carboxylic groups in the microspheres. With a 25-40% decrease in the microsphere size depending on their size ranges, the microspheres could load a maximum of 0.3-0.7 mg Doxo/mg dry spheres. As confirmed by confocal microscopy, Doxo was mainly concentrated in the outer 20 ± 5 μm surface layer of the microspheres. The loaded microspheres were stable in aqueous dispersions without aggregation for a prolonged period of time but degradable in a lysozyme solution. Furthermore, the loaded microspheres exhibited a noticeable pH-sensitive behavior with accelerated release of Doxo in acidic environment due to the protonation of carboxylic groups in the microspheres. Compared to commercial non-resorbable drug eluting beads, the loaded bioresorbable microspheres showed a sustained release manner in phosphate buffered saline (PBS). The release data were fitted to an empirical relationship, which reveals a non-Fickian transport mechanism (n = 0.55-0.59). These results demonstrate that the bioresorbable microspheres are promising as attractive carriers for Doxo.

Original languageEnglish (US)
Pages (from-to)185-193
Number of pages9
JournalInternational Journal of Pharmaceutics
Volume409
Issue number1-2
DOIs
StatePublished - May 16 2011
Externally publishedYes

Keywords

  • Bioresorbable
  • Doxorubicin
  • Hydrogel microspheres
  • Ion exchange

ASJC Scopus subject areas

  • Pharmaceutical Science

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