Nanocrystal Research and Development

In the growing field of biopharmaceuticals, nanotechnology has become a revolutionary force. Among its various applications, nanocrystals stand out as a key innovation. At BOC Sciences, we are at the forefront of this cutting-edge technology, offering comprehensive nanocrystal research and development services.

What are nanocrystals?

Nanocrystal technology is a novel pharmaceutical technology to increase the solubility of insoluble drugs. Drug nanocrystals refer to drug particles that are directly micro-powdered to nanometer level for the bulk drug, which are carrier-free submicron colloidal dispersion systems. Particle size is 100 ~ 1000 nm, commonly only contains the active pharmaceutical ingredient (APIs)) and stabilizer ( the weight of drugs and the stabilizer systematically than usual to 2:1), the effect of stabilizers is to reduce the accumulation of the drug crystal to improve the stability of the product.

Advantages of nanocrystals

High security: Nanocrystals do not use carrier delivery, so they do not contain a large number of surfactants and carrier materials, will not produce material metabolites, and have high safety.

High bioavailability: The drug particles are reduced to the nanometer level through micro-pulverization, which increases the specific surface area of insoluble drugs, improves solubility and dissolution rate, and has greater surface adhesion, prolongates the action time of drugs in the mucous layer, limits diffusion, increases local concentration of drugs, and promotes drug absorption in the gastrointestinal tract. It has also been reported that nanocrystalline drugs can saturate efflux transporters on biofilms and improve bioavailability.

Improve drug properties: Nanocrystalline technology is suitable for class II and IV drugs in the biological drug classification system (BCS), especially the former, which greatly improves the druggability of insoluble drugs.

High drug load: In addition to the necessary stabilizer, no other excipients are required in the product, and the drug itself is the delivery system with high drug load capacity.

Preparation method of nanocrystals

Nanocrystal (NC) preparation process is divided into top-down, bottom-up and the combination of the two ways. The top-down technology includes medium grinding method and high pressure homogenization method, which is characterized by simple preparation process, strong operability and stable process, and can obtain NC with small average particle size and uniform distribution. Bottom-up technology mainly includes antisolvent precipitation method, supercritical fluid method, solvent evaporation method and spray drying method, which has the advantages of simple operation and low equipment cost. The combination of the two methods can complement the shortcomings of a single preparation method and form a small and uniform particle size NC.

High pressure homogenization

Through high pressure homogenization equipment, the cavitation force is used to convert drugs into nanocrystals, suitable for drugs with poor water solubility and organic solubility. The drug crystals of apigenin, asuracine, baicalein and lutein were prepared by high pressure homogenization.

Pearlmilling technique

The particle size of the milling media in the milling container is in the range of 0.1~20nm, usually ceramic, zirconia, stainless steel, glass, chromium, agate, glass or polystyrene resin coated beads. After the drug, stabilizer and water are mixed in a certain proportion, they are put into a closed milling chamber equipped with milling media. Under high-speed rotation, the drug particles, milling media and the wall collide with each other, generating sustained and strong impact force and shear force to provide the energy required for the micro-pulverization of drug particles, thus producing nanocrystals.

Solvent-antisolvent precipitation

The drug solution (dissolved in an organic solvent that is miscible with water) and the antisolvent (usually water or aqueous medium) are fully mixed to form a water-phase susaturated solution, which nucleates and precipitates the drug, and eventually forms nanoscale drug crystals.

Solvent evaporation method

The drug is dissolved in a volatile solvent, and the drug is precipitated to form nanocrystals by evaporating the solvent. This method can control the crystal growth process and obtain more uniform nanoparticles.

Supercriticalfluid technology

Supercriticalfluid technology is to dissolve drugs in supercriticalfluid (SCF). When supercritical liquid is atomized through a nozzle with a small aperture, the supercritical fluid rapidly vaporizes to crystallize drugs and form drug nanocrystals.

Application of nanocrystals

The versatility of nanocrystals extends to a variety of therapeutic areas, opening up new avenues for treatment and improving patient outcomes. Here are some of the key applications where our nanocrystal research and development services can make a significant impact:

Oral administration: Oral administration is the most convenient and preferred route for patients. However, many drugs face challenges due to poor water solubility and low bioavailability. Nanocrystals can enhance the absorption of such drugs in the gastrointestinal tract, thereby improving treatment effectiveness and patient compliance.

Injection formula: Nanocrystals can be formulated into injectable suspensions or encapsulated in liposomes for targeted delivery to specific tissues or organs. This approach is particularly valuable for the delivery of anti-cancer drugs, where precise targeting can minimize off-target effects and improve therapeutic indices.

Topical and transdermal applications: In traditional forms of drug delivery, the skin is a powerful barrier. Nanocrystals can penetrate the stratum corneum for effective local and transdermal drug delivery. This can be beneficial for treatments ranging from skin diseases to local pain management.

Lung delivery: Inhalation therapy is becoming more and more prominent in the treatment of respiratory diseases. Nanocrystals can be designed as aerosols or dry powder preparations to be inhaled, providing rapid action and improving the deposition of drugs in the lungs.

Central nervous system diseases: The blood-brain barrier (BBB) presents a major challenge to the delivery of drugs to the central nervous system. Nanocrystals are small and able to cross the blood-brain barrier, offering a promising solution for treating neurodegenerative diseases, brain tumors and other central nervous system disorders.

Our expertise in nanocrystal research and development

Our company has assembled a multidisciplinary team of experts with extensive experience in nanotechnology, pharmaceutical science, chemistry and biology. Our teams share a common mission: to unlock the full potential of nanocrystals in prescription medicine and create innovative solutions for unmet medical needs.

Comprehensive formulation development

Our team specializes in designing and optimizing nanocrystal formulations to maximize the solubility and bioavailability of drugs. We employ state-of-the-art technologies such as high pressure homogenization, anti-solvent precipitation and media grinding to produce nanocrystals with precise dimensional control and uniformity. Our goal is to customize each formulation to meet specific therapeutic goals and regulatory requirements.

Nanocrystal characterization and analysis

Understanding the physical and chemical properties of nanocrystals is the basis for their successful development. Our cutting-edge analytical tools, including dynamic light scattering (DLS), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and X-ray diffraction (XRD), allow us to thoroughly characterize nanocrystals. These technologies allow us to evaluate size, shape, surface characteristics and crystallographic information to ensure consistency and quality of the formulation.

Nanocrystal stability and scalability research

The stability of nanocrystals is a key factor in realizing the practical application of nanocrystalline based therapeutics. Our R&D team conducts rigorous stability studies to evaluate the physical and chemical stability of nanocrystals under a variety of conditions.

• Surface modification: Explore different surfactants, polymers or other stabilizers to prevent the aggregation and degradation of nanocrystals.
• Environmental influence: The influence of external factors such as temperature, pH value and light on the stability of nanocrystals was studied.
• Long-term storage: Evaluate the stability of nanocrystals for long-term storage under different conditions, including physical stability (particle size change) and chemical stability (drug degradation).

In addition, we can develop production processes from laboratory to industrial scale to ensure consistent quality and performance of scaled nanocrystals.

Nanocrystal drug release and bioavailability tests

To verify the performance of our nanocrystal formulations, we conducted comprehensive in vitro and in vivo drug release studies. The drug content and drug release curve were determined by high performance liquid chromatography (HPLC) and mass spectrometry (MS). By evaluating parameters such as dissolution rate, permeability and pharmacokinetics, we ensure that the nanocrystals can achieve the desired therapeutic effect. This step is essential to optimize the dosing regimen and maximize patient benefits.

Custom nanocrystal solutions

Each drug and treatment target is unique, and a one-size-fits-all approach is not enough. At our company, we recognize the importance of custom nanomedicine. We work closely with our customers to understand their specific needs and challenges to provide tailored solutions for their drug candidates. Our collaborative approach ensures that our customers receive nanocrystal formulations that are aligned with their project objectives and timelines.

Process of our nanocrystal services

Customer demand analysis and preliminary assessment: Our team of professionals will communicate with you to understand your drug's characteristics, target market, and expected clinical performance. Use our proprietary database and predictive models to conduct in-depth analysis of the physicochemical properties of drugs and evaluate the potential of nanocrystals.

Customized scheme design: According to the characteristics of drug molecules, the most suitable preparation methods for nanocrystals are selected, including but not limited to high pressure homogenization, microjet, solvent evaporation, etc. Design the experimental scheme and determine the best process parameters, including particle size, surface modification, stabilizer selection, etc.

Laboratory development and optimization: Nanocrystals are precisely prepared and characterized in our state-of-the-art laboratory environment using cutting-edge equipment such as nanoparticle size analyzers, transmission electron microscopy (TEM), and dynamic light scattering (DLS). The performance of nanocrystals is optimized through multi-dimensional evaluation such as dissolution curve, stability test and in vivo and in vitro correlation study.

Large-scale production and technology transfer: Once the laboratory stage is successful, we will assist you in scaling up the technology to ensure that the stability and consistency of the nanocrystals are maintained on an industrial scale. Provide comprehensive technical documentation and support to ensure that customers can seamlessly proceed to subsequent clinical trials and production.

Ongoing support and consulting services: Even after the end of the project, we will continue to provide technical support and advisory services to deal with any challenges that may be encountered.

At BOC Sciences, our nanocrystal research and development services represent the convergence of scientific expertise, technological innovation and a strong commitment to improving patient outcomes. By harnessing the power of nanocrystals, we are addressing some of the most pressing challenges in drug formulation and delivery. Our dedication to quality, regulatory compliance and collaborative research ensures that we remain a trusted partner for our customers in the biopharmaceutical industry.

FAQ

1. How do you ensure the stability and efficacy of nanocrystal formulations?

• Dynamic light scattering (DLS) for particle size analysis
• Scanning electron microscopy (SEM) for morphology assessment
• X-ray diffraction (XRD) for crystallinity evaluation

Additionally, we conduct rigorous stability testing under various conditions to ensure long-term stability and integrity of the formulations.

2. Can you scale up nanocrystal formulations for commercial production?

Yes, we provide end-to-end support for scaling up nanocrystal formulations. Our team has extensive experience in transitioning from pilot-scale production to full-scale manufacturing, ensuring seamless integration into your production pipeline.

3. Do you collaborate with other organizations for research and development?

Yes, we actively collaborate with academic institutions, research organizations, and industry partners. These collaborations allow us to stay at the forefront of nanotechnology, continuously exploring new methodologies, materials, and applications for nanocrystals.

4. How do nanocrystals improve drug solubility and bioavailability?

Nanocrystals enhance drug solubility and bioavailability by increasing the surface area available for dissolution. Their small size and high surface energy facilitate faster dissolution rates in biological fluids, allowing for better absorption and improved therapeutic outcomes.

5. What therapeutic areas can benefit from nanocrystal formulations?

Nanocrystal formulations can benefit a wide range of therapeutic areas, including:

• Oncology
• Cardiovascular diseases
• Central nervous system disorders
• Infectious diseases
• Gastrointestinal disorders

Their ability to improve the solubility and bioavailability of drugs makes them applicable to any therapeutic area where poorly water-soluble drugs are a challenge.

6. How do I get started with your nanocrystal research and development services?

To get started, please contact our team through our website or by email. We will arrange an initial consultation to discuss your specific needs and objectives. From there, we can develop a customized plan to create, characterize, and scale up your nanocrystal formulations.