Semaglutide Microspheres-Case Study

Background

Semaglutide is a hypoglycemic agent used in the treatment of type 2 diabetes mellitus, which is a glucagon-like peptide-1 (GLP-1) receptor agonist that works by mimicking GLP-1 in the human body. It is able to reduce the risk of major adverse cardiovascular events (MACE), including cardiovascular death, nonfatal myocardial infarction, and nonfatal stroke in adult patients with type 2 diabetes with concomitant cardiovascular disease. However, simepaglutide typically requires injectable administration, which may lead to decreased patient compliance, especially in patients with chronic diseases requiring long-term treatment, and frequent injections may compromise the continuity of therapy. Making simepaglutide into microsphere formulations can achieve long-lasting effects, reduce the frequency of administration, and improve patient compliance. In addition, the microsphere formulation can protect the stability of the drug during the transmission process in the body, avoid rapid degradation, and ensure that the active ingredients of the drug can reach the site of action.

Challenge

• Drug stabilization: Peptide drugs are susceptible to factors such as pH, temperature and enzymatic degradation, leading to degradation.
• Encapsulation efficiency and drug loading
• Microsphere size homogeneity
• Drug release kinetics: stable and long-lasting release
• Scale-up production

Solution

Utilizing our microsphere sustained-release platform, we can provide microsphere sustained-release formulations to extend the duration of drug action. In addition, we can ensure the industrialization of microspheres on the ground with a production capacity, and can help customers to do the FDA registration.

Results

• As shown in Figure 1, the experimental results showed that the drug-loaded microspheres had a homogeneous morphology of about 50 μm.

Fig. 1 TEM picture of semaglutide microspheres for injection.

• The test results show that semaglutide microsphere products have been released in the human body for more than 30 days. (As shown in Figure 2)

Fig. 2 Time curve of AUCO-/AUCNE percentage in plasma of SD rats after single intramuscular injection.

Table 1 Comparative experimental results of various formulations of Semaglutide Microspheres in rats.

Methods

Reference

1. Zeng H, et al.; Effect of hydroxyethyl starch on drug stability and release of semaglutide in PLGA microspheres. International Journal of Pharmaceutics. 2024, 654: 123991-124001.