Effect of Hydration on Physicochemical Properties of End-Capped PLGA

Author:

D’Souza Susan1,Dorati Rossella2ORCID,DeLuca Patrick P.3

Affiliation:

1. Sunovion Pharmaceuticals Inc., Marlborough, MA 01752, USA

2. Department of Drug Sciences, Section of Pharmaceutical Chemistry and Technology, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy

3. University of Kentucky, College of Pharmacy, Lexington, KY 40536, USA

Abstract

The objective of this study was to assess the physicochemical effects of hydrating a hydrophobic end-capped poly(lactide-co-glycolide) (PLGA) polymer in the liquid and vapor state. PLGA RG503 polymer was incubated at 37°C in 0.5% polyvinyl alcohol (PVA) solution and at 90% RH. Samples were withdrawn at predetermined intervals and changes to polymer properties like glass transition temperature (Tg), moisture uptake, molecular weight change, and % acid number were determined using differential scanning calorimetry, Karl Fisher titrimetry, gel permeation chromatography, and acid base titrimetry, respectively. Study results showed that Tg was depressed instantaneously upon hydration, indicating that bulk water acted as a plasticizer of hydrophobic end-capped PLGA. Tg values decreased to levels below the incubation temperature when hydrated in 0.5% PVA solution but not in 90% RH. The drop in Tg exhibited a linear relationship (R2>0.99) to the amount of water uptake by the polymer; higher moisture uptake was noted with liquid water. Removal of moisture from the polymer matrix resulted in recovery of Tg, only up to a period of 14 days. Presence of water in liquid or vapor form caused a reduction in molecular weight of the polymer and a corresponding increase in % acid number over the duration of the study.

Funder

Oakwood Labs

Publisher

Hindawi Limited

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