Abstract Title:

Lactic acid triggers, in vitro, thiomersal to degrade protein in the presence of PLGA microspheres.

Abstract Source:

Int J Pharm. 2004 Apr 1 ;273(1-2):1-8. PMID: 15010124

Abstract Author(s):

Jocimara A M Namur, Célia S Takata, Ana M Moro, Mário J Politi, P Soares De Araujo, Iolanda M Cuccovia, M H Bueno Da Costa

Article Affiliation:

Jocimara A M Namur


Microspheres of polymers like poly(lactic-co-glycolic acid) (PLGA) have been studied as a vehicle for controlled release vaccines. They require materials and processes that might change the protein antigenicity. Lactic acid is produced during microsphere degradation that occurs in tandem with protein liberation. In addition, most of the proteins that have been used in microencapsulation studies contain Thimerosal((R))(TM) and this can introduce another undesirable effect for their stability. We demonstrated in vitro that the thiosalycilic acid (TSA), produced after the reduction of TM by lactic acid, reduces the S-S bridge of the previously incubated diphtheric toxoid (Dtxd). This reduction is immediately followed by blocking the two -SH formed by the same TSA molecules. In the light of these conclusions it is necessary now, to reinterpret the in vitro protein degradation-stabilization data in the presence of PLGA microspheres, mainly for those proteins which contain S-S. We propose that all the PLGA microspheres microencapsulation studies and protein structural considerations should be done in the absence of TM as preservative.

Study Type : In Vitro Study
Additional Links
Problem Substances : Thimerosal : CK(799) : AC(190)

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