Method for the synthesis of gelled microspheres for the homogeneous vehiculation and release of biologically active compounds.
A new method for the synthesis of gelled microspheres that can homogeneously carry biologically active compounds has been developed. The microspheres become of special interest for their use by themselves or as a vehicle. Unlike other common excipients, these microspheres are resistant to enzymatic degradation, stable, biocompatible, safe, mucoadhesive, and allow a controlled and sustained release of active compounds.
Every year a wide variety of therapeutic agents are developed and, despite the fast progress in this area, some frequent problems associated with 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 subsequent vehiculation to constitute the final pharmaceutical form, increasing the production costs. In this sense, there is a need for 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, and 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 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 mucoadhesive, and offer protection to the encapsulated compound from inactivation by external agents.