Details

Autor(en) / Beteiligte

• Paillard-Giteau, A.
• Tran, V.T.
• Thomas, O.
• Garric, X.
• Coudane, J.
• Marchal, S.
• Chourpa, I.
• Benoît, J.P.
• Montero-Menei, C.N.
• Venier-Julienne, M.C.

Titel

Effect of various additives and polymers on lysozyme release from PLGA microspheres prepared by an s/o/w emulsion technique

Ist Teil von

• European journal of pharmaceutics and biopharmaceutics, 2010-06, Vol.75 (2), p.128-136

Ort / Verlag

Amsterdam: Elsevier B.V

Erscheinungsjahr

2010

Quelle

MEDLINE

Beschreibungen/Notizen

• Incomplete protein release from PLGA-based microspheres due to protein interactions with the polymer is one of the main issues in the development of PLGA protein-loaded microspheres. In this study, a two-dimensional adsorption model was designed to rapidly assess the anti-adsorption effect of formulation components (additives, additives blended with the polymer or modified polymers). Lysozyme was chosen as a model protein because of its strong, non-specific adsorption on the PLGA surface. This study showed that PEGs, poloxamer 188 and BSA totally inhibited protein adsorption onto the PLGA37.5/25 layer. Similarly, it was emphasised that more hydrophilic polymers were less prone to protein adsorption. The correlation between this model and the in vitro release profile was made by microencapsulating lysozyme with a low loading in the presence of these excipients by a non-denaturing s/o/w encapsulation technique. The precipitation of lysozyme with the amphiphilic poloxamer 188 prior to encapsulation exhibited continuous release of active lysozyme over 3 weeks without any burst effect. To promote lysozyme release in the latter stage of release, a PLGA–PEG–PLGA tribloc copolymer was used; lysozyme was continuously released over 45 days in a biologically active form.