ABSTRACT
PURPOSE:
To investigate the in vitro release of octreotide acetate, a somatostatin agonist, from microspheres based on a hydrophilic polyester, poly(D,L-lactide-co-hydroxymethyl glycolide) (PLHMGA).
METHODS:
Spherical and non-porous octreotide-loaded PLHMGA microspheres (12 to 16 μm) and loading efficiency of 60-70% were prepared by a solvent evaporation. Octreotide release profiles were compared with commercial PLGA formulation (Sandostatin LAR(®)); possible peptide modification with lactic, glycolic and hydroxymethyl glycolic acid units was monitored.
RESULTS: PLHMGA microspheres showed burst release (~20%) followed by sustained release for 20-60 days, depending on the hydrophilicity of the polymer. Percentage of released loaded peptide was high (70-90%); > 60% of released peptide was native octreotide. PLGA microspheres did not show peptide release for the first 10 days, after which it was released in a sustained manner over the next 90 days; > 75% of released peptides were acylated adducts.
CONCLUSIONS:
PLHMGA microspheres are promising controlled systems for peptides with excellent control over release kinetics. Moreover, substantially less peptide modification occurred in PLHMGA than in PLGA microspheres.
Free PMC Article
Controlled release of octreotide and assessment of peptide acylation from poly(D,L-lactide-co-hydroxymethyl glycolide) compared to PLGA microspheres
Riferimento:
Pharm Res. 2012 Jan;29(1):110-20.
Autori:
Ghassemi AH, van Steenbergen MJ, Barendregt A, Talsma H, Kok RJ, van Nostrum CF, Crommelin DJ, Hennink WE.
Fonte:
Pharm Res. 2012 Jan;29(1):110-20.
Anno:
2012
Azione:
Profili di rilascio di octreotide da microsfere a base di poliestere idrofilico (D, L-lattide-co-glicolico idrossimetil) sono stati confrontati con la formulazione commerciale PLGA (Sandostatina LAR (®).
Target:
Octreotide microsfere/Sandostatina LAR.
Sostanze: