Liposomal Vitamin C-Case Study

Background

Vitamin C is a nutrient that is essential to the human body but cannot be synthesized by the body itself. It is a strong water-soluble antioxidant, which has various physiological effects in the human body, and plays a vital role in maintaining the normal life activities of the human body. It can antioxidize, regulate immune function, enhance immunity and improve the ability to fight infections. In addition vitamin C can increase the absorption of non-heme iron (iron in plant foods), which has a positive effect on the prevention of anemia. Studies have shown that the vitamin also protects cardiovascular health, regulates blood pressure, and is anti-inflammatory. However, the stability of vitamin C is poor, easy to be affected by the external environment and oxidative decomposition (light, high temperature, etc.). In addition, the alkaline environment of the intestinal tract and metal ions can also lead to vitamin C destruction. In order to achieve certain efficacy and replenish the body's vitamin C content, some commercially available products recommend higher daily dosages (1,000mg), which can result in about 50% of the vitamin C not being absorbed and utilized.

Challenge

• Low bioavailability
• Chemical stability issues
• Biological stability issues
• Imprecise controlled release technology

Solution

This encapsulation property of liposomes makes them an effective drug delivery system that can improve drug stability and bioavailability while reducing toxic side effects and enabling targeted delivery. CD Bioparticles has extensive experience in developing liposomes over the years and has the capability for stable batch production and industrialization. Liposomal vitamin C prepared using high-pressure homogenization technology exhibit the following properties:

Results

Note: P2 is a special process formulation 1. P6 is a special process formulation 2.

• As shown in Figure 1 , the experimental results indicate that liposomal vitamin C are spherical in shape and homogeneous, and the liposome nanosize is around 30 nm. The encapsulation rate was in the range of 20- 40%.

Figure 1. (A) TEM picture of liposomal vitamin C; (B) DLS of liposomal vitamin C.

• As can be seen from the table 1, the relative bioavailability of liposomal vitamin C-P2-50%, liposomal vitamin C-P6-50%, liposomal vitamin C-P2-70%, liposomal vitamin C-P6-70% and 20% LVC (liquid) was higher than that of vitamin C original group. The highest of 20% LVC (liquid) was 8.79-fold, indicating that the bioavailability of vitamin C was significantly increased when it was prepared as liposomes.

Figure 2. Pictures of relative bioavailability of liposomal vitamin C.

Table 1 Relative bioavailability of vitamin C in different groups.

Methods

Reference

1. Gopi S, et al.; Evaluation and clinical comparison studies on liposomal and non-liposomal ascorbic acid (vitamin C) and their enhanced bioavailability. Journal of Liposome Research. 2020, 31(4): 356-364.