Abstract: A non-injectable formulation or formulation for instillation, including self-assembling hydrogels formed of gelators such as the Food and Drug Administration's Generally Regarded as Safe (GRAS) compounds like ascorbyl palmitate, in the form of capsules, tablets, oral suspensions, enemas, and rectal or vaginal suppositories or inserts have been developed. In a preferred embodiment, the formulation contains anti-inflammatories, anti-infectives, or other therapeutic, prophylactic, or diagnostic agents that can be administered orally, especially when lower blood levels relative to tissue levels of agent are preferred. In the most preferred formulation, the composition contains tacrolimus-loaded ascorbyl palmitate gel microfibers containing nanostructures (“hydrogels”).

Abstract: Gels are formed based on generally recognized as safe (GRAS) low molecular weight amphiphilic molecules in a self-assembly process. Therapeutic or prophylactic agents, such as biological macromolecules, are loaded without exposure to temperatures and/or organic solvents which can degrade or destroy the biologic agents and/or their activity. The resulting self-assembled gel composition contains microstructures having pores and aqueous domains at their interior, rendering them permeable to hydrophilic and hydrophobic molecules. This permeability allows sequestration of the biological macromolecules. Once sequestered, the electrostatic, hydrophobic-hydrophobic etc. interactions between the biological macromolecules and the amphiphilic gelators keep the labile payload encapsulated with high stability until the microstructures are degraded.

Abstract: A gel formulation has been developed which provides high loading, e.g., between about 5% and about 50% wt/wt agent/total gel weight, of a wide range of agents, especially amine-containing compounds such as local anesthetic agents that are known to be difficult to encapsulate, and which adhere to charged surfaces. Examples of pharmaceutically important amines include anesthetics, such as lidocaine. Tuning the ionic strength of an aqueous medium during preparation, suspension, and dialysis purification of the hydrogel composition allows for retention and/or control of agent loading contents, as well as a high capacity for adhesion to charged surfaces mimicking inflamed tissue. In some instances, the rheological properties of the gel can be tuned such as to impart thixotropic properties to the gels formed.