Abstract

The present work focuses on the preparation of alginate-based aerogels in the form of particles for their further study as potential drug delivery systems (solid dosage forms). The dripping method was used to prepare certain gel particles, and supercritical drying was used to obtain final alginate-based aerogel particles. Three model active substances (ketoprofen, nimesulide, loratadine) were impregnated into the obtained aerogels using the supercritical adsorption process. Using the method of X-ray analysis, it was shown that the in the obtained drug-loaded aerogels the corresponding active substances are in an amorphous state, and the stability of this state after six months of storage is confirmed. In vitro dissolution tests for obtained drug-loaded aerogels was performed. For each sample, an appropriate dissolution medium (with certain pH) was determined. In vitro investigations showed the increasing of the release rate for all model active substances. Time was required to release and dissolve 50% of the active drug from drug-loaded aerogels (T1/2), reduced in comparison with pure active drugs in crystalline form. Obtained results provide insight into the application of alginate-based aerogel particles as a drug delivery system to improve pharmacokinetic properties of certain active drugs.

Highlights

  • Aerogels are porous materials with high adsorption capacity, which makes it possible to successfully impregnate various substances into aerogels: Active pharmaceutical ingredients [1,2,3], oils [4], additives for the food industry, etc. [5,6]

  • Organic aerogels in the form of particles can be used in the pharmaceutical industry as drug delivery systems, in medicine as medical products, and in the food industry as a carrier for vitamin supplements or flavors

  • Protein aerogels obtained during this study showed high mechanical strength, as well as good adsorption capacity

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Summary

Introduction

Aerogels are porous materials with high adsorption capacity, which makes it possible to successfully impregnate various substances into aerogels: Active pharmaceutical ingredients [1,2,3], oils [4], additives for the food industry, etc. [5,6]. Organic aerogels in the form of particles can be used in the pharmaceutical industry as drug delivery systems, in medicine as medical products (surgical sorbents), and in the food industry as a carrier for vitamin supplements or flavors. Various polysaccharides (cellulose, starch, alginates, pectin) [7,8,9], as well as various proteins (egg, whey protein, etc.) [10] can be used to prepare organic aerogels. All these substances are united by the ability to form gels either in the presence of water and/or a crosslinking agent, or under the influence of temperature and other factors. One of the most promising materials for the preparation of aerogels that can be used as drug delivery systems is sodium alginate

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