Gelled microspheres for the vehiculation and release of therapeutic agents

Every year a wide variety of therapeutic agents are developed and, despite the fast progress in this area, some frequent problems associated to drug development such as poor solubility, high potency, unpleasant organoleptic properties, low stability or inadequate pharmaceutic form, are still not fully resolved.

Nowadays, other sustained release pharmaceutic forms exist (liposomes, bicelles, nanoparticles or microparticles). However, they are intermediate products and require a subsequent vehiculation to constitute the final pharmaceutical form, increasing the production costs. In this sense, there is a need of new transport and delivery methods that are safer, more efficient, simpler, and allow a controlled and sustained release of the drug.

In order to meet this market need, a new method for the synthesis of gelled microspheres has been developed. The microspheres can be used by themselves as therapeutic agents or cosmetics, or to vehiculate bioactive compounds. The microspheres stand out due to their biocompatibility, stability, specificity, even encapsulation, and allow the incorporation of a wide range of biologically active compounds (pharmaceutical, nutraceutical, cosmetics…) for a subsequent sustained release, completely maintaining biological activity.

The production of these microspheres consists of an innovation on the emulsification / internal gelation method wherein the aqueous phase contains an alginate salt or derivative therein, a water-soluble polysaccharide, a calcium salt, and optionally the biologically active compound; the oily phase is made of a mixture of several oils. The aqueous phase is added to the oily phase to form a water-in-oil emulsion, to which is added a fat-soluble acid to generate a dispersion of microparticles.

The resulting microparticles show enhanced organoleptic properties and palatability, an increase of the mucoadhesivity and offer protection to the encapsulated compound from inactivation by external agents.

ADVANTAGES AND BENEFITS

• Homogeneous encapsulation of biologically active compounds, such as drugs, cosmetics or nutraceuticals. This allow to vehiculize these compounds or use them directly as a drug.
• Increased resistance and stability.The microparticles show an enhanced resistance to enzymatic degradation, protecting the encapsulated compound, along with extended stability.
• Biocompatible, safe, enhanced mucoadhesivity, and ideal penetration and rheological properties.
• Sustained release of compoundsduring up to 15 hours after application.
• Enhanced organoleptic properties and palatability.
• Easy formulation of a hydrogel,which allows an improved contact time.
• Easily scalable to industry.
• Reduced production coststhan current suspension and particle systems.
• Useful for the treatment of a wide variety of infections.Preferably, they are used for buccal, nasal, bladder, rectal or vaginal infections.

Current development status

Laboratory prototypes

Applications

Health

Drug delivery

Cosmetics

Biotechnology

Desired business relationship

Patent licensing