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Tailor-Made Microcapsules

 

Microencapsulation is a widely used process in the food and pharmaceutical industries with many different aims. In the pharmaceutical industry, the technique is mostly used to protect the active ingredient against degradation due to environmental conditions – such as light, oxidation, pH and microbial degradation – to control the drug release profile, or for taste masking purposes.

The microencapsulation process can be described as the formation of a capsule (wall) of coating material around the active pharmaceutical ingredient, the core of the composite particle, resulting in solid particles of micrometer size constituted by at least two components.

There are several techniques used to produce microencapsulated materials. These include chemical methods, which typically involve a polymerisation reaction to form the wall, and physical methods based in solvent evaporation, melt cooling or coacervation. The selection of the technique to use in a particular application is mainly based in the properties of the materials to be processed – such as the stability of the drug during the microencapsulation process – the reproducibility of the drug product’s attributes, and the ease of process scale-up.

Among the solvent evaporation methods, spray drying is probably the most versatile technology available. In a single step, it allows the production of the microcapsules as well as the manipulation of particle or powder properties such as particle size distribution, morphology and powder density. This in turn can be of paramount importance to downstream processing of the pharmaceutical formulation, whether it comprises capsule or sachet filling, tabletting, or any other final process.

COATING MATERIALS

While the active substance to encapsulate is not a matter of choice, the encapsulating materials can be chosen from a wide variety of approved products. The selection should take into account the lipo- and hydrophilic character of the active substance, the target role of the encapsulating agent, encapsulation efficiency, product stability during storage, and the pharmacokinetic profile (for immediate or controlled release). These materials are most often divided into the following categories:

  • Polysaccharides, such as starches, maltodextrins and arabic gum
  • Lipids, such as stearic acid, mono and diglycerides, among others
  • Proteins, such as gelatins, casein and soy

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Marco Gil, PhD, is an Engineer at R&D Particle Design Discipline at Hovione FarmaCiencia SA, Loures, Portugal. He is currently focused on the application of particle design technologies such as jet and wet milling and spray drying to enhance the properties of pharmaceutical materials. He received his Chemical Engineering degree and PhD from the Technical University of Lisbon, Portugal. After teaching in two Portuguese universities, he joined Hovione at the Particle Design Discipline, where he started working in the development of spray drying processes. Later on, he gained a special interest in the development and production of solid dispersions and microencapsulated materials by spray drying and spray congealing.

Filipe Gaspar, PhD, is the Director of R&D Particle Design Discipline at Hovione FarmaCiencia SA, Loures, Portugal. The focus of his work is on novel particle engineering technologies (bridging API synthesis with formulation). He received his Chemical Engineering degree from the Technical University of Lisbon, Portugal and his PhD from the University of Birmingham, UK. After receiving his PhD, he worked for three years as a Research Fellow at the University of Birmingham and as a consultant in the field of supercritical fluids. He joined Hovione in 2003 as a Process Engineer, where he participated in the commissioning of the first large-scale spray dryer. In 2004, he joined the R&D group and two years later become Head of the Particle Design Discipline.

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Marco Gil
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Filipe Gaspar
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