With the deepening of research on small molecule drugs, the structural design of drug molecules is becoming more and more complex, and the poor solubility of drugs has become an important problem in the development of new drugs. About 40% of the small molecule drugs currently on the market are refractory compounds, and the proportion of refractory candidate compounds in the research and development stage is close to 90%. Therefore, improving drug solubility and bioavailability has become one of the urgent problems in the development of new drugs. BOC Sciences is committed to developing cutting-edge drug solubility enhancement technologies for insoluble drugs and providing innovative solutions to customers around the world.
Nanotechnology is used to cleverly control the microstructure of nanoparticles, such as size, shape and surface characteristics, so that drug molecules can be accurately embedded or adsorbed to nanocarriers to build a stable nanomedicine delivery system. These exquisite nanocarriers can not only greatly increase the contact area between drugs and biological fluids, accelerate the dissolution rate of drugs, but also effectively avoid drug degradation in the body, achieve precise targeted delivery, thereby optimizing the therapeutic effect while minimizing potential side effects.
Key innovations:
Engineering design and synthesis of nanoparticles: Using polymer materials, inorganic nanoparticles or liposomes as carriers, using self-assembly, emulsified-solvent volatilization, spray drying and other advanced technologies to carefully create nanocarriers.
Surface functional modification: Hydrophilic polymers such as polyethylene glycol (PEG) are used to modify the surface of nanoparticles to enhance their stability and biocompatibility.
Drug loading and intelligent release control: Through physical adsorption, chemical bonding or encapsulation technology, drugs are loaded inside the nanoparticles, and smart release mechanisms such as pH sensitive, temperature sensitive or enzyme response are designed to ensure accurate drug delivery.
Drug nanocrystals and nanoparticles are also commonly used solubilization methods. The drug is crushed or milled into nano-sized particles by mechanical energy, so that it is uniformly dispersed in the medium and forms a stable state, which can be widely used in various pharmaceutical preparations, including tablets, capsules and injections.
Solid dispersion technology creates a solid complex by highly dispersing drug molecules in a suitable carrier material, similar in principle to how a solution or suspension behaves in a liquid environment. We use a variety of technological paths such as melting, solvent evaporation or mechanical dispersion to significantly increase the dissolution rate of drugs and thus enhance their bioavailability.
Hot melt extrusion (HME): With the help of the HME process, a solid dispersion with better solubility is produced. This process involves melting and mixing the active pharmaceutical ingredient (API) with a polymer carrier, which is subsequently extruded to form a solid matrix to achieve efficient dissolution of the drug.
Spray drying: Our spray drying technology is good at converting liquid preparations into dry powder preparations with significantly improved solubility. It is particularly suitable for the treatment of heat-sensitive drugs and can effectively form amorphous solid dispersions to further enhance the bioavailability of drugs.
Lipid-based preparations, with their unique chemical and physical properties, are very effective in improving the solubility and bioavailability of insoluble drugs and have become the savior of insoluble drugs. Their core lies in utilizing the unique properties of lipids to create a favorable microenvironment that promotes the dissolution and absorption of drugs.
Self-emulsifying drug delivery systems (SEDDS): This is an innovative formulation in which oils, surfactants and co-solvents are carefully blended to form a uniform mixture. Once in the gastrointestinal tract, SEDDS immediately spontaneously form tiny milk droplets, greatly enhancing the solubility of the drug while promoting its absorption across the intestinal wall.
Lipid nanoparticles: We work on the development of lipid nanoparticles such as solid lipid nanoparticles (SLNS) and nanostructured lipid carriers (NLC). These particles can not only efficiently encapsulate insoluble drugs, but also significantly improve their solubility while ensuring drug stability, demonstrating excellent biopharmaceutical properties.
Cyclodextrins, as a unique class of cyclic oligosaccharides, are ideal partners for insoluble drugs due to their hydrophilic outer surface and hydrophobic inner cavity. By forming clathrates with drug molecules, cyclodextrins not only improve the solubility of the drug, but may also promote drug absorption by changing the lipid barrier at the absorption site, thus significantly improving bioavailability. This process involves the interaction of cyclodextrins with cell membrane components such as cholesterol, phospholipids, and proteins to adjust the permeability of the lipid barrier.
Inclusion compound development: We use many types of cyclodextrins, including alpha, beta and gamma cyclodextrins, to carefully design inclusion compounds to optimize the solubility and bioavailability of active pharmaceutical ingredients (APIs).
Modified cyclodextrin applications: Our team of experts is skilled in the use of modified cyclodextrins, such as hydroxypropyl beta-cyclodextrin, which have greater dissolution capabilities and open up new paths for drug delivery.
Micro-pulverization technology pulverizes drug particles to the micron level through the principle of fluid dynamics, significantly enlarges the specific surface area of the drug, and improves the porosity and surface energy. This process greatly improves the solubility and bioavailability of insoluble drugs, providing strong support for drug delivery.
Jet grinding: We use cutting-edge jet grinding technology to generate micro-pulverized drug particles with uniform particle size distribution and significantly improved solubility to ensure efficient drug delivery.
Spray drying: In addition to solid dispersion technology, our spray drying technology is also applied to micro-pulverization to produce ultra-fine powders with higher solubility, creating favorable conditions for drug absorption and distribution.
By changing the chemical form of the drug, such as the formation of drug salts or eutectic, the solubility of the drug can be significantly improved. Our salt and eutectic technologies not only provide a stable form of the drug, but also optimize its biopharmaceutical properties to ensure optimal absorption in the body.
Microemulsion preparation is an ideal carrier for insoluble drugs because of its unique microstructure. They can effectively accommodate different fat-soluble drugs, improve drug stability, and promote the absorption of macromolecules of water-soluble drugs, significantly improving the bioavailability of drugs in the body. The micro particle size and uniform distribution of the microemulsion greatly improve the dispersion of the drug and show a broad application prospect. Our microemulsions and self-microemulsification systems rapidly form microemulsions in the gastrointestinal environment, ensuring effective absorption of drugs and providing patients with a more efficient and safer treatment experience.
Particle size analysis: Use laser diffraction and dynamic light scattering to accurately measure particle size and distribution to optimize solubility.
Thermal analysis: Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) are used to evaluate the thermal properties of formulations to ensure stability and performance.
X-ray powder diffraction (XRPD): XRPD is used to study the crystal structure of apis and formulations, providing insight into solubility and stability.
Dissolution testing: Rigorous dissolution testing is performed to assess the solubility and release of our formulations under a variety of conditions.
Improve bioavailability: The increase in solubility improves bioavailability and ensures that the therapeutic agent is more effective in achieving the desired goal. This can lower doses, reduce side effects and improve patient compliance.
Accelerate drug discovery: By overcoming solubility challenges early in the development process, we help accelerate the progress of drug candidates from discovery to clinical trials and commercialization.
The versatility of the formulation: We have a wide range of solubility enhancement technologies that allow us to develop a variety of formulations tailored to the specific needs of each API. This flexibility allows us to create a wide range of dosage forms, including oral, injectable and topical formulations.
Enhance patentability: Innovative solubility enhancement strategies can provide new intellectual property opportunities, strengthen pharmaceutical companies' patent portfolios and extend the market exclusivity of their products.
1. What is solubility enhancement, and why is it important?
Solubility enhancement refers to the methods and technologies used to increase the solubility of poorly soluble drugs. Solubility is crucial because it directly affects a drug's bioavailability, or how well it can be absorbed into the bloodstream. Enhanced solubility ensures that drugs are more effective at lower doses, reducing side effects and improving patient outcomes.
2. What types of drugs typically require solubility enhancement?
Poorly soluble drugs include a wide range of therapeutic agents such as certain anti-cancer drugs, antibiotics, antifungals, and drugs used for chronic conditions like cardiovascular diseases and diabetes. Many new chemical entities (NCEs) discovered during drug development also suffer from poor solubility.
3. What are the main technologies used for solubility enhancement?
4. How do nanotechnology-based solutions improve solubility?
Nanotechnology-based solutions improve solubility by reducing the particle size of poorly soluble drugs to the nanoscale. This increases the surface area, which enhances the dissolution rate and bioavailability. Examples include nanosuspensions, which are stable suspensions of drug nanoparticles, and nanocrystals, which are crystalline nanoparticles with superior solubility.
5. Can lipid-based formulations be used for all types of drugs?
Lipid-based formulations are particularly effective for lipophilic (fat-loving) drugs. These formulations enhance solubility by creating emulsions or encapsulating the drug in lipid matrices, improving absorption in the gastrointestinal tract.
6. How can we start a project with your solubility enhancement services?
To start a project, simply contact us through our website or customer service. We will schedule an initial consultation to discuss your specific needs and challenges. Our team of experts will then develop a customized plan to enhance the solubility of your drug compounds, ensuring optimal results for your development projects.