Long-acting Controlled-release Injection Technologies

For drugs with long therapeutic cycles, long-acting injectables are an option to reduce the frequency of injections and improve patient compliance. CD Formulation can provide our clients with long-acting formulation technologies. Our pharmacologists can provide strategies to extend the duration of action of a drug after injection by (1) modifying the drug structure to extend the half-life of the drug's degradation in the body, (2) forming a drug reservoir at the injection site, such as subcutaneously or intramuscularly, to slowly release the drug through formulation methods, and (3) modifying the physicochemical properties of the drug to adjust the dissolution rate of the drug.

Why Long-acting Protein Drugs are Needed

Protein drugs have a short half-life due to the presence of proteases in large quantities in tissues, which can hydrolyze protein drugs and render them inactive, and due to the filtration effect of the glomerulus, molecules with a molecular weight of less than 69 kDa are easily cleared during metabolism, and the liver also has an important role in the drug metabolism process. In order to maintain a certain efficacy, high doses of drugs need to be administered frequently, and long-term repeated injections not only increase the pain of patients but also cause a series of side effects. Therefore, there is a clinical need to develop long-acting protein drugs.

Long-acting Injectables - Technology Solutions

• Long-acting injection protocols with extended drug half-life reconfiguration

Technologies to improve the half-life of protein drugs include: chemical modification of protein drugs, protein fusion, glycosylation, construction of anti-protease mutants, etc.

• Long-acting regimens for sustained release formulations with reservoir formation at the injection site

Long-acting extended-release formulations that form a drug reservoir include: microspheres, DepoFoam technology, and in situ gels. Sustained release formulations provide longer cycles of activity with a single injection, even with reduced injection frequency, while improving therapeutic efficacy by placing a more constant blood concentration.

• Long-acting injection protocols that alter the physicochemical properties of the drug

Technologies that alter the nature of the drug and thus achieve long-lasting injections include: injectable implants, and refractory salt technology. Refractory salt technology, which converts water-soluble drugs into insoluble salts to control the release of the drug and prolong its duration of action. Polymers are usually mixed with a solvent and then injected for drug delivery. The solvent diffuses rapidly from the injection site and the polymer is transformed into a precipitate, forming a biodegradable implant. The mechanism of drug release differs from that of microspheres in that implants control drug release by diffusion.

Below is a table of long-acting injectable technologies.

CD Formulation focuses on the development of long-acting injectable technologies. Through years of development, we can provide our customers with a series of core technologies that reduce production costs, improve production efficiency and enhance product quality. Our technologies and services are constantly being updated. If you are interested in our technologies or if the technologies and services you want are not on the list, please feel free to contact us and we will provide you with exclusive solutions.