PLA stereocomplexes for controlled release of somatostatin analogue

Ashgan Bishara, Abraham J. Domb

Research output: Contribution to journalArticlepeer-review

25 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

Bibliographical note

Funding Information:
This work was supported in post by The US-Israel Binational Fund, BSF, and a grant form the Israeli of Science Foundation (ISF).

Funding

This work was supported in post by The US-Israel Binational Fund, BSF, and a grant form the Israeli of Science Foundation (ISF).

FundersFunder number
US–Israel Binational Fund
United States-Israel Binational Science Foundation
Israel Science Foundation

    Keywords

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

    Fingerprint

    Dive into the research topics of 'PLA stereocomplexes for controlled release of somatostatin analogue'. Together they form a unique fingerprint.

    Cite this