Drug delivery platform
Drug delivery platform
Nanologica’s patented technology platform, enables the use of mesoporous silica for tailor-made drug delivery systems for enhanced bioavailability and controlled release.
Nanologica’s drug delivery technology is based on micrometer sized spherical silica particles containing thousands of pores in nanometer size. The nanoporous particles, NPPs, have been designed to enable drug delivery to the lungs. The particle size of these highly porous, spherical particles is tightly controlled (1 – 5µm) to facilitate maximum lung deposition. NPPs are made from amorphous silica which is biosoluble, which means that the particles dissolve in simulated lung fluid.
Drug products for inhalation are made by loading the API into the pores of the particles (excipient), that is encapsulating the drug within the particle. The drug loaded NPPs (drug product) are easily aerosolizable as a dry powder without the need for additional excipients, with fine particle fractions (the share of particles in a size optimum for inhalation) in the range of 70-80 percent, which is a twofold improvement over conventional dry powder inhalation products.
The flow properties of the NPPs are not changed by the drug loading process – the drug product remains freely flowing and can be easily dispensed into a DPI.
A known problem and a real risk in clinical development programs is that the variability in how much drug is delivered to the lung with today’s available technology is great, as a result of patients generating different inhaled flow rates when using dry powder inhalers. Work with budesonide (an inhaled corticosteroid) loaded in NPPs has shown that drug delivery from a commercially available capsule-based DPI is independent of the flow rate used to generate the aerosol cloud. The observation that the company’s NPPs provide consistent drug delivery across a range of clinically relevant inhaled flow rates is hugely significant. In simple terms, this means that Nanologica’s delivery technology is less dependent on the patient’s ability to take a deep breath to get the drug into the lung.
Creating inhaled drug products with NPPs addresses several of the challenges the pharmaceutical industry is faced with today. Common challenges include amorphous and/or poorly soluble APIs and the delivery of biological molecules. Using Nanologica’s NPP delivery technology, these challenges may potentially be addressed.
To provide a chemically stable drug product, The API in DPI formulations is normally crystalline (ordered molecular structure), but for some APIs the solubility of the crystalline form is very low, which can lead to difficulties in reaching the required concentration of the API in the body to elicit a therapeutic response. The alternative is to use the drug in an amorphous form (disordered molecular structure), but this creates significant challenges in terms of chemical and physical stability. When APIs are loaded into NPPs, the drug is captured and stored in an amorphous form within the particle matrix, which has a twofold benefit; the solubility is increased, and the drug is stabilized by being entrapped inside the particle.
Nanologica believes that the NPPs have the potential to also protect biological molecules inside the particles, which may be able to solve the problems of degradation that exist for almost all large molecules. Research in the area of inhaled biologics is at an early stage but is something that the company intends to pursue.
Nanoporous particles (NPPs) for inhalation
- Nanoporous spherical particles
- 1 to 5 µm
- Narrow particle size distribution
- Tuneable particle and pore size
- High loading up to 50%
- Free-flowing powder
Nanologica’s patented drug delivery technology solves problems in pharmaceutical formulations by improving solubility, enhancing bioavailability and protecting APIs from degradation.
Picture: When the API was loaded in Nanologica’s nanoporous particles (named NLAB Spiro™ in the graph), the bioavailability increased significantly compared to the commercial formulation of the API. SLF is simulated lung fluid, PBS is phosphate-buffered saline.
The aerodynamic properties of the particles are perfectly tailored for inhalation. Impactor measurements of Mass Median Aerodynamic Diameter (MMAD) for the NPPs (below refered to NLAB Silica) loaded with three different active ingredients show excellent flow properties
NPPs can solve problems in pharmaceutical formulations by improving solubility, enhancing bioavailability and protecting APIs from degradation.
Graph: Reformulation of the HIV drug Atazanavir (ATV) using NPPs (above refered to NLAB Si-ATV) for improved bioavailability in vivo.
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Benefit of NPPs
• Enhancing dissolution kinetics of poorly soluble compounds
• Controlling release kinetics
• Improving bioavailability
• Stabilizing amorphous form
• Improving handling of APIs
• Applicable for a broad range of API, potentially including inhaled biologics
• Spherical particles
• 1 to 5 µm
• Tuneable particle and pore size
• High loading up to 50%
• Free-flowing powder suitable for inhalation