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Critical attributes of formulation and of elaboration process of PLGA-protein microparticles.

Abstract：

:Low drug loading, burst effect during release and drug inactivation account for the main drawbacks of protein microencapsulation in poly(d,l-lactic-co-glycolic) acid (PLGA) matrix by the water-in oil-in water (W/O/W) solvent evaporation method. Thus, the current study was set to invest the critical attributes of formulation and of elaboration process which determine protein loading into microparticles as well as its further release, using albumin as protein model. NaCl concentration in the external aqueous phase, poly(vinyl alcohol) (PVA) concentration and mostly viscosity of both the internal aqueous phase and the organic phase were critical attributes for improving drug loading, with polymer molecular weight and hydrophobicity likewise directly related to albumin loading. In such a way, when using 0.5% PVA as internal aqueous phase the highest albumin loading was achieved. Optimized microparticles exhibited a sustained in vitro release of albumin over 130 days. The influence of the microencapsulation process on albumin stability and biological activity was evaluated by carrying out cell proliferation assays on PC12 cells with albumin released from microparticles. Such assay demonstrated that the microencapsulation procedure optimized in this study did not affect the biological stability of the microencapsulated protein.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Martín-Sabroso C,Fraguas-Sánchez AI,Aparicio-Blanco J,Cano-Abad MF,Torres-Suárez AI

doi

10.1016/j.ijpharm.2015.01.008

subject

Has Abstract

pub_date

2015-03-01 00:00:00

pages

27-36

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(15)00010-1

journal_volume

480

pub_type

杂志文章

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