Bioadhesive emulsion preparations for enhanced drug delivery

A method for making an oil-in-water emulsion having mucoadhesive properties which comprises the steps of:

• preparing an oil-in-water emulsion comprising a hydrophobic phase in an aqueous phase and an acidic mucoadhesive macromolecule, said emulsion being in the form of a plurality of submicron particles having a hydrophobic core surrounded by the mucoadhesive macromolecule;
• adjusting the pH of said emulsion to a first pH value which promotes substantial ionization of the mucoadhesive macromolecule in order to avoid breakdown of the emulsion;
• and
• providing the emulsion with a final pH of between 3 and 8 to enhance biocompatability or to provide a stable storage environment for the emulsion;
• wherein the mucoadhesive macromolecule 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.

A method for making an oil-in-water emulsion having mucoadhesive properties comprising the steps of:

• preparing an oil-in-water emulsion comprising a hydrophobic phase in an aqueous phase and a basic mucoadhesive macromolecule, said emulsion being in the form of a plurality of submicron particles having a hydrophobic core surrounded by the mucoadhesive macromolecule;
• adjusting the pH of said emulsion to a first pH value which promotes substantial ionization of the mucoadhesive macromolecule in order to avoid breakdown of the emulsion;
• and
• providing the emulsion with a final pH of between 3 and 8 to enhance biocompatability or to provide a stable storage environment for the emulsion;
• wherein the mucoadhesive macromolecule 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.

A method for making an oil-in-water emulsion having mucoadhesive properties which comprises the steps of:

• emulsifying a hydrophobic phase with sufficient amounts of a surfactant and an aqueous solution to form an oil-in-water emulsion having a plurality of submicron particles that have a hydrophobic core surrounded by the surfactant in a continuous aqueous phase;
• adding a mucoadhesive macromolecule to the emulsion to coat the submicron particles;
• and
• providing the emulsion with a final pH of between 3 and 8 to enhance biocompatability or to provide a stable storage environment for the emulsion;
• wherein the mucoadhesive macromolecule 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.