PLA stereocomplexes for controlled release of somatostatin analogue

Ashgan Bishara, Abraham J. Domb

Research output: Contribution to journalArticlepeer-review

26 Scopus citations

Abstract

Reversible stereoselective complexes were spontaneously formed from mixing acetonitrile solutions of enantiomeric d-poly(lactide) (d-PLA), l-poly(lactide) (l-PLA), and octreotide (an octapeptide, somatostatin analogue). Hetero-stereocomplexes of poly (d-lactide) and l-octreotide were obtained by spray freezing of solution of d-PLA and octreotide. An additional transition temperature close to the melting point of enantiomeric PLA was observed in DSC thermogram. The same phenomenon was observed in stereocomplex of d-PLA/l-PLA and octreotide. The enthalpy of both transition temperatures correlate with peptide content in the hetero-stereocomplex. The spray method produced compact and smooth micro particles compared to particles formed by precipitation in acetonitrile solution. The particle size of stereocomplexes was in the range of 1.5 to 4 μm for all formations. Increasing peptide concentration in the stereocomplex increases the release rate of the peptide, and increases polymer degradation rate as monitored by lactic acid release form stereocomplexes.

Original languageEnglish
Pages (from-to)474-483
Number of pages10
JournalJournal of Controlled Release
Volume107
Issue number3
DOIs
StatePublished - 20 Oct 2005
Externally publishedYes

Keywords

  • Octreotide acetate
  • Peptide release
  • Poly (lactide)
  • Stereocomplex

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