Micronization, What does it do
We are specialized in spray drying micronization of supplements and nutraceuticals for higher bioavailability. We are experts in preclinical studies as permeation studies according ICH and OECD guidelines.
Micronization refers to the reduction of the average particle size of an active compound to the micron scale, which once micronized features:
2. Enhanced solubility
3. Increased bioavailability
4. Improved stability
5. General enhancement of product performance
Welcome to the remarkable world of micronization, a process able to unleash the extraordinary therapeutic potential of the biologically active compounds. Picture this: a microscopic world where micro-scale science reigns supreme and like a meticulous engineer re-assemble supplements and foods in minuscule particles with new incredible therapeutic potential. Micronization operates at the intersection of physics, chemistry, and engineering, utilizing various techniques and technologies to achieve precise particle size reduction in the supplement and food industries:
1. Jet Milling: high-speed jets of compressed gas to reduce particle size.
2. Ball Milling: grinds through balls to achieve particle size reduction through impact and attrition.
3. Spray Drying: micronize and incapsulate in one step, transforming liquids into fine particles.
4. Fluid Energy Milling: high-velocity jets of gas to impact and reduce particle size.
6. Hammer Milling: rotating hammers or knives to break down particles through impact.
7. Cryogenic Milling: extremely low temperatures to embrittle materials followed by grinding.
8. Ultrasonic Milling: high-frequency sound waves to induce cavitation and size reduction.
9. Bead Milling: pearls as grinding media in a liquid suspension to reduce size through shear and impact.
10. Nanomilling: a specialized form of milling used to produce nanoparticles with precise size and distribution.
The Science Behind Micronization
Despite their variety, all the micronization techniques increase the surface area-to-volume ratio (SA:Vr), which is the main responsible for the characteristic advantages of micronization:
The SA:Vr is a measure of how much surface area is exposed for a given volume. It is calculated by dividing the surface area by the volume. When reducing the size, molecules have a higher SA:Vr than the former ones. This is because the surface area of a sphere is proportional to its radius squared, while the volume is proportional to its radius cubed, which means during a scaling down, the surface area decreases less than the volume, resulting in smaller particles with higher surface per unit of volume.
Picture this: a solid particle only made of an active compound, is introduced into a solvent. This particle is nothing more than a number of identical molecules holding together through physical interactions. Now submerged within the solvent is surrounded by solvent molecules starting colliding with the particle surface. During these collisions, the solvent molecules with enough energy can diffuse into the solid and interact with the particles at the molecular level, more frequent are these collisions higher the speed the active compound molecules dissolve into the solvent. This process governs the dissolution speed of the active compound and occurs at the particle-solvent interface, larger is the particle surface per unit of volume faster the active compound dissolves.
Often active compounds are administrated within a dosage form enclosing their molecules within a matrix. Thus, before the dissolution starts, another process needs to take place: the liberation of the active compound from the matrix. This introduces another concept: the liberation rate, which refers to the speed the active compound molecules are released from the dosage form becoming available to dissolve into the solvent. The liberation starts at the matrix-solvent interface where the solvent molecules interact with the matrix leading to its braking down. Also the liberation rate is governed by the SA:Vr, larger the SA:Vr larger the matrix-solvent interface higher the liberation rate.
Both liberation and dissolution rates influence directly solubility, absorption and efficacy of a health product.
When orally administrated, health products find their way into the organisms through absorption across the enteric membranes in the intestine. Enteric membranes are covered by a watery mucus layer called glycocalyx, in which the active compounds need to be dissolved before to interact and cross these membranes.
Now picture the same scenario but with a micronized product, with a high surface-to-volume ratio increasing radically the number of molecules dissolving in the glycocalyx, ready to cross the enteric mucosae, increasing the bioavailability and unlashing the whole therapeutic potential of the product, the patient improves its well-being and the product reputation grows.
The advantages of micronization does not limit to increased efficacy but extend to processes efficiency and product stability.
Dispersibility refers to the ability of a powder to be evenly distributed in a mixture resulting in higher homogeneity, which is important during manufacturing.
Manufacturing flexibility due to higher mixture homogeneity, which allows easy product line segmentation, since the product can be used in a larger verity of dosage forms as: sachets, granulates, tablets, capsules, suspensions, and emulsions. This allows easy .
Suspensions and emulsions of micronized particles are less likely to settle out of the liquid, important for the stability of these products.
The stability and shelf life of products also benefit from micronization. The improved homogeneity previously mentioned also positively affects the stability of micronized products, reducing the risk of segregation and ensuring uniform distribution of active compounds throughout the final dosage form. Additionally, micronized particles exhibit reduced vulnerability to degradation processes, thereby extending the shelf life of products.
Micronization has been proven effective on the coenzyme Q10, grape seed extract, and L-arginine and was found that their stability is significantly improved as the risk of particle segregation is minimized. The authors also discuss the potential advantages for the dietary supplement industry, suggesting how micronization could improve the stability of a wide range of active ingredients, including vitamins, minerals, and botanicals.
Micronization of Active Ingredients in Dietary Supplements: Impact on Stability and Bioavailability.
Journal of Functional Foods, 10, 75-84.
The effect of the enhanced stability of micronized supplements has been also investigated on L-carnitine an amino acid involved in the metabolism of fat and is often taken as for weight loss. The study found that micronization of L-carnitine significantly improved its stability over time.
Effect of Micronization on the Stability and Bioavailability of L-Carnitine in a Dietary Supplement.
Journal of Functional Foods, 16, 310-317
The same findings were reported for curcumin that showed a remarkable 100-fold stability improvement.
Zhang, Y.; Chen, Y.; and Wang, S. (2016).
Effect on Stability, Bioavailability, and In Vitro Anti-Inflammatory Activity.
Journal of Functional Foods, 22, 321-330
a unique micronization technique
Spray drying is a process going far beyond size reduction, capable of micronizing and encapsulating several active compounds within an amorphous matrix in one-step. A process yielding dry powders made of thousands smart microparticles each acting as an independent delivery system designed to govern the liberation of the active compound with precise site and rate release, minimizing dosage waste and maximizing absorption.
This is how it works: controlled delivery systems release the active compounds slowly, maintaining longer the blood levels within the therapeutic window and improving its effectiveness. The delivery system can be also engineered to be smart and use the pH to recognize its location within the gastro-enteric tract behaving accordingly: retaining the active compounds at pH lower than 2 (in the stomach) and releasing them when the pH is higher than 6 (in the intestine). Thus, preventing the unnecessary gastric release and concentrating the therapeutic load in the absorption site, and achieving the following advantages:
Protection: the active compound is preserved from degradation in the stomach.
Higher absorption: of the drug or other substance across the intestinal wall.
Higher efficacy: the controlled release maintains consistent the blood levels within the therapeutic windows increasing the efficacy.
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Micronization a strategic Business Decision
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