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Reducing Demand for Formulation Additives through Surface Control: Controlling Bioadhesive Container Properties

Ponche A, Sarrailh S, Grosjean B, Brouet G.

Respiratory Drug Delivery 2016. Volume 1, 2016: 157-164.

Abstract:

Additives are present in numerous formulations to confer specific properties or stability to active compounds. Lubricants, surfactants, fillers, or binders are used to modify interfacial interactions with surfaces, improve handling of particles, or avoid their coagulation. Surface active agents are required in amounts above a minimally active concentration, which tends to result in higher than optimal concentrations included in formulations. Surface chemical engineering is a way to reduce the number and/or concentration of additives to comply with evolving international standards. Surface engineering and chemical grafting of active coupounds are two ways to reduce concentration or reduce leachables in pharmaceutical formulations. The need for “smart surfaces” has never been so present and it begins with a better understanding of molecule-surface interactions. Monolayers are molecular coatings with versatile chemistry that can be used as a model platform to investigate interactions. These autoorganized nanolayers can easily be converted into antibacterial coatings and be effective with considerably lower surface concentration than in solution. Engineering the surface by physical treatments including ion bombardment or polymerized grafted additives is also a good strategy for manufacturers to modify the surface and reduce production steps (like washing for elastomer gaskets for example, or improving siliconization of metering valve). The compliance with pharmaceutical quality or manufacturing standards is then improved by reducing number of additives or lowering their concentrations.