Layer-by-layer Polyelectrolytes Coating of Alginate Microgels for Sustained Release of Sodium Benzoate and Zosteric Acid.

The potential of sustaining release of very small (Mw < 250 g/mol) hydrophilic drugs up to several days from layer-by-layer (LbL) polyelectrolyte coated alginate microgels (Alg-Ms) was investigated. One purpose is to minimize post-surgical adhesions, which develop in 12 h to 3 days after surgery. The LbL polyelectrolyte layer would serve as a diffusion barrier for their release. The LbL polyelectrolyte bilayers were prepared using poly(allylamine) (PAH) and poly(styrene sulfonate) (PSS). Sodium benzoate (NaB, Mw = 144 g/mol) and zosteric acid (ZA, Mw = 244 g/mol), two anti-inflammatory and anti-microbial compounds, were used as model drugs. A higher number of PAH/PSS bilayer lead to a greater sustained release of both drugs, and with 4 bilayers, the release of NaB and ZA was prolonged from 24 h to 72 h and 120 h, respectively. Fitting the data to the Ritger-Peppas' equation showed that as the bilayer number increased, the release constant and/or exponent decreased, indicating the LbL PAH/PSS bilayer effectively reduced the permeability of these two very small hydrophilic drugs. The ability to prolong the release of such small hydrophilic molecules, which has rarely been investigated previously, would find broad applications in fields such as anti-adhesion treatment and antifouling coatings.