Pharmos Corporation

Joseph Schwarz

Doron Friedman

Shimon Amselem

The invention relates to novel methods for making oil-in-water emulsions having mucoadhesive properties which are primarily intended for administration of biologically active compounds to mucosal surfaces. The emulsion has an aqueous continuous phase and a plurality of submicron particles having an average particle diameter of from 10 nm to 600 nm, with the particles having a hydrophobic phase of a fat or oil which forms a hydrophobic core that is surrounded by a surfactant layer. The emulsion further includes a mucoadhesive polymer which is a polymer or copolymer of acrylic acid or methacrylic acid, a poly (methyl vinyl ether/maleic anhydride) copolymer, pectin, alginic acid, hyaluronic acid, chitosan, gum tragacanth, karaya gum or carboxymethylcellulose surrounding the hydrophobic one. A biologically active compound may also be included, if desired. The hydrophobic core has less than 1% (w/w) protein, relative to the weight of the hydrophobic core, and the emulsion contains less than 5% (w/w) surfactant, relative to the weight of the hydrophobic phase.

Bioadhesive emulsion preparations for enhanced drug delivery

The present invention provides emulsions comprising a plurality of submicron particles, a bioactive peptide, and an aqueous continuous phase or that effect enhanced oral bioavailability of the peptide. Another aspect of the invention provides compositions and methods of administering peptides in an emulsion comprising a plurality of submicron particles, a mucoadhesive macromolecule, a bioactive peptide, and an aqueous continuous phase, which promotes absorption of the bioactive peptide through mucosal surfaces by achieving mucoadhesion of the emulsion particles. Mucous surfaces suitable for application of the emulsions of the present invention may include corneal, conjunctival, buccal, sublingual, nasal, vaginal, pulmonary, stomachic, intestinal, and rectal routes of administration.

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Rehovot, Israel

Joseph Schwarz