PLA stereocomplexes for controlled release of somatostatin analogue

被引：25

作者：

Bishara, A ^{[1
]}

Domb, AJ ^{[1
]}

机构：

[1] Hebrew Univ Jerusalem, IL-91120 Jerusalem, Israel

来源：

JOURNAL OF CONTROLLED RELEASE | 2005年 / 107卷 / 03期

基金：

以色列科学基金会;

关键词：

stereocomplex; poly (lactide); octreotide acetate; peptide release;

D O I：

10.1016/j.jconrel.2005.05.026

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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 mu m 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. (c) 2005 Elsevier B.V. All rights reserved.

引用

页码：474 / 483

页数：10

共 12 条

[1] Sustained delivery of proteins for novel therapeutic products [J].