Moisture-Activated Rheological Structuring of Nonaqueous Poloxamine- Poly(Acrylic Acid) Systems Designed as Novel Biomedical Implants

作者：Jones David S^*; Muldoon Brendan C O; Woolfson A David; Andrews Gavin P; McCoy Colin P; Sanderson F Dominic

来源：Journal of Pharmaceutical Sciences, 2010, 99(4): 1838-1854.

DOI：10.1002/jps.21956

• polyacrylic acid
• Tetronic
• rheology
• mucoadhesion
• rheological structuring

This study reports the formulation/characterisation of novel polymeric platforms designed to behave as low-viscosity systems in the nonaqueous state, however, following uptake of aqueous fluids, exhibit rheological structuring and mucoadhesion. The rheological/mechanical and mucoadhesive properties of platforms containing poly(acrylic acid) (PAA, 1%, 3%, 5%, w/w) and poloxamines (Tetronic 904, 901, 704, 701, 304), both in the absence and presence of phosphate buffered saline (PBS, pH 7.4) are described. With the exception of Tetronic 904, all formulations exhibited Newtonian flow in the nonaqueous state, whereas, all aqueous formulations displayed pseudoplastic flow. The consistency and viscoelastic properties were dependent on the concentrations of PAA and PBS and Tetronic grade. PBS significantly increased the consistency, viscoelasticity and mucoadhesion, reaching a maximum at a defined concentration of PBS that was dependent on PAA concentration and Tetronic grade. Formulations containing Tetronic 904 exhibited greatest consistency and elasticity both prior to and after dilution with PBS. Increasing PAA concentration enhanced the mucoadhesive properties. Prolonged drug release of metronidazole was observed from formulations containing 10% (w/w) PBS, 3% and, particularly, 5% (w/w) PAA. It is suggested that the physicochemical properties of formulations containing 3% or 5% (w/w) PAA and Tetronic 904, would render them suitable platforms for administration to body cavities.

• 出版日期2010-4