Liposomal Resveratrol-Case Study

Background

Resveratrol is a natural compound with a wide range of biological activities, including antioxidant, anti-inflammatory, anti-tumor, anti-aging, and neuroprotective and cardioprotective effects. However, resveratrol has low water solubility, resulting in poor oral absorption and poor chemical stability. Therefore, finding effective delivery systems to overcome solubility, stability and bioavailability issues is a major challenge. Liposomes, as one of the nanocarriers, have been successfully incorporated with resveratrol to improve its bioactivity and stability under UV irradiation.

Challenge

• Low solubility & 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 to enhance the absorption and distribution of resveratrol in the body and to enhance its pharmacological effects while reducing potential side effects. CD Bioparticles has extensive experience in developing liposomes over the years and has the capability for stable batch production and industrialization. Liposomal resveratrol 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 resveratrol are spherical in shape and homogeneous, and the liposome nanosize is around 45 nm. The resveratrol content is between 5-50%. As can be seen from Figure 1B, ordinary resveratrol is difficult to dissolve in water and shows obvious stratification, while liposomal resveratrol can form a homogeneous and stable system in water and possesses better utilization.

Figure 1. (A) TEM picture of liposomal resveratrol; (B) Plain resveratrol on the left and liposomal resveratrol on the right.

• The maximal blood concentrations of liposomal resveratrol-P2-50%, liposome resveratrol-P6-50%, and liposome resveratrol-P6-5% were 1.53 ± 0.77 μg/mL, 7.21 ± 2.65 μg/mL, and 11.88 ± 4.23 μg/mL, respectively, which were significantly higher than that of the resveratrol prodrug group (0.83 ± 0.45 μg/mL). Meanwhile, the area of the drug-time curve AUC0-1 of these three groups of liposomal resveratrol was 2.3, 2.4 and 4.2 times higher than that of the original resveratrol group, respectively, indicating that the bioavailability of resveratrol was significantly increased after it was prepared into liposomes. (Figure 2)

Figure 2. Pictures of blood concentrations of Liposomal Resveratrol.

• As can be seen from the table 2, the AUC0-12h of both liposomal resveratrol-P2-35% and liposomal resveratrol-P2-50% were higher than that of resveratrol prodrug group. Among them, liposomal resveratrol-P2-50% showed the highest RB value of 14.02-fold. It indicated that the bioavailability of resveratrol was significantly increased after it was prepared into liposomes and microencapsulated powder.

Table 1 Blood concentration analysis of resveratrol in different groups.

Figure 3. Pictures of relative bioavailability of liposomal resveratrol.

Table 2 Relative bioavailability of resveratrol in different groups.

Methods

Reference

1. Hou J, et al.; Liposomal resveratrol alleviates platelet storage lesion via antioxidation and the physical buffering effect. ACS Applied Materials & Interfaces, 2023, 15(39): 45658-45667.