From spray drying to
in vivo studies
for high bioavailability supplements
Spray drying manufactured microparticles possess technological features solving the problems often related to traditionally formulated supplements.
“The health benefits of a nutraceutical will only be realized if it is actually absorbed by our bodies and reaches its intended site of action, such as our bloodstream, livers, lungs or brains.”
J. McClements, Springer Nature Switzerland, Future Food, 2019
Poor absorption and low bioavailability are only some of the problems affecting traditionally formulated supplements with no delivery strategy. After swallowing, a supplement is often weakened by the attack of the lytic enzymes and the acidic pH of the stomach.
The surviving dose is transported to the enteric tract. Here the absorption varies considerably depending on:
- speed of release from the formulation;
- of solubility in H2O;
- and for the lipophilic substances, on the emulsifying properties of the dosage form or on the presence of bile fluids.
The administration of herbal extracts without a strategy optimizing the bioavailability often results in products with little therapeutic impact, leaving the patient’s medical needs unfulfilled.
Spray drying, for botanicals and phytocomplexes with high bioavailability
Spray drying is the micronization technique of choice for thermolabile substances, of which botanicals and phytocomplexes are often rich.
Botanicals and phytocomplexes benefits from Spray drying micronization in which the medicinal substance is dispersed in several nano-compartments embodied within a monolithic matrix. This protect the medicinal substances from degradation, allow the design of the release profile, and an overall increase of the nutraceutical bioavailability and efficacy.
The spray drying micronization allows the design of microdelivery systems protecting botanicals and phytocomplexes from the attack of the lytic enzymes and the acidic pH of the stomach. The dosage is preserved from off-target delivery.
The microdelivery system starts the liberation of the whole dosage only at a planned pH, increasing the on-target delivery, the absorption and bioavailability of the medicinal substance, and featuring:
- controlled speed of release of botanical or phytocomplex;
- High solubility also for lipophilic substances.
A supplement or botanicals when orally administrated is dissipated in an uncontrolled way already in the gastric environment (pH <2, Pure Compound) while, when conveyed within a microdelivery system is effectively concentrated at the absorption site, the enteric mucosa (pH> 6.5, Micro Delivery System).
Spray dryer microparticles features:
Micronization size between 5-30 µm
Spray drying allows the encapsulation of botanicals and phytocomplexes in a modified release vehicle, and therefore means providing patients with a nutraceutical featuring higher bioavailability and therefore therapeutic benefits.
Micro delivery systems are designed to protect, target and control the release rate of botanicals and phytocomplexes in order to increase their bioavailability.
Active molecules protection
Spray drying protects the active components during the micronization processes. Once encapsulated, these are further protected from biological and environmental inactivation such as oxidation, enzymatic and acid degradation.
studies: in vitro, ex vivo,
Permeation studies for solid, semisolid and liquid formulations are a reliable tool for the efficacy validation .
The efficacy evaluation of formulation containing vitamins, botanicals and phytocomplexes benefits from the Franz Cell permeation model, designed to imitate the behaviour of dosage forms when in contact with the absorbing tissue. In the horizontal Franz cells, a membrane separates the donor from the receptor chamber housing a receptor solution and a stirrer. The system is kept at controlled temperature and steady stirring speed.
The test sample is placed in the donor chamber and in contact with the membrane allowing its eventual permeation into the receiving chamber. The permeation is measured collecting the receptor solution through the sampling port.
100 µl aliquots are collected by the sampling port at defined time intervals and analysed by spectroscopic detection, and the increasing accumulation of the diffused compounds are plotted against time.
In vitro tests and cell culture models cannot accurately mimic the complexity of a living animal, to provide a comprehensive insight the supplement or botanical needs a real life conditions test.
In vivo studies
Animal studies incorporate supplements or botanicals into the diet of the animal model, to unravel the biological fate of the nutraceutical, such as absorption, metabolization, distribution, and excretion, as well as its physiological effects such as changes in blood pressure, glucose levels, cholesterol levels, physical activity up to tumour suppression.
More services supporting the nutraceutical innovation
A high impact formula is a mixture of substances protecting and delivering the APIs. To keep high the impact a steady formulation process is required to adjust the formula for novel therapeutic targets and market challenges. We develop standard and unique formulations based on our proprietary know-how including an all-natural ingredients formulation service. We offer formula progress in a broad array of oral, injectable, topical, inhalation, ophthalmic, depot and transmucosal delivery systems. We craft formulas adapting the core parameters of each formulation achieving:
- Protection from the environmental factors decreasing the starting dosage.
- Release in the correct site to maximize the absorption.
- Liberation of the active compound with a suitable dissolution time.
- Enhancing the API absorption mechanism.
An excellent formulation must ensure not only a high API bioavailability levels but also important features as storage stability and lacks of interaction with the packaging, thus preserving safeness and potency. We provide the following stability studies:
- Compatibility Studies between API and container.
- Stress testing.
- Photostability testing.
- Formal stability.
Drug delivery technologies
Understanding the relationship between polymer chemistry and device pharmacokinetics is the drive to guarantee an on-target drug delivery. We develop the following drug delivery technologies for API:
- Polymeric micelles as colloidal drug delivery systems, to increase APIs solubilization, protection and absorption.
- Micro and nanoparticles to help the formulations to reach and maintain a constant API concentration.
- Polymeric gene vectors as self-assembling polycation-DNA complexes provide protection from enzymes allowing the cell entry and transfection.
Analytic & Characterization capacity
Our formulation development is powered by a significant scientific competence and an outstanding technological capacity.
- Zetasizer nano ZSP 2 MALVERN
- HPLC agilent 1200 series AGILENT
- Nano spray dryer B-90 BÜCHI
- HPLC-SEC agilent 1200 series AGILENT
- Microwave reactor discover CEM
- Mini spray drier B-290 BUCHI
- Rheometer DHR2 TA INSTRUMENTS
- Homogenizator at high pressure MICROFLUIDICS