Liposomal Curcumin-Case Study

Background

Curcumin (CUR) is a yellow polyphenol compound derived from the plant turmeric. It is widely used in the treatment of many types of diseases, including cancers of the lung, cervix, prostate, breast, bone and liver. However, its effectiveness is limited by poor water solubility, low bioavailability, and rapid metabolism and systemic elimination. Liposomes are small spherical vesicles composed of a phospholipid bilayer, which have a wide range of applications in pharmaceuticals and dietary supplements. Capable of encapslating hydrophobic drug molecules in the lipid bilayer, while for hydruophilic drug molecules they can be encapsulated in the inner aqueous phase of the liposome, which is the central aqueous cavity of the liposome. Liposomes can be used as delivery systems for drugs and nutrients to improve their stability, bioavailability, targeting and relief release to prolong the duration of action.

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 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 curcumin 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 curcumin are spherical in shape and homogeneous, and the liposome nanosize is around 40 nm. The encapsulation rate was in the range of 20-40%. Curcumin content is between 50-55%. As can be seen from Figure 1C, ordinary curcumin is difficult to dissolve in water and shows obvious stratification, while liposomal curcumin can form a homogeneous and stable system in water and possesses better utilization.

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

• The maximum blood drug concentration Cmax of liposomal curcumin-P2-50% group and liposomal curcumin-P6-50% group were 5.7 and 8.2 times higher than that of the original drug group. The area of the drug-time curve AUC0-t was 3.6 and 2.1 times higher than that of the original drug group, respectively. At the same time, the two groups of liposomes reached the maximum blood concentration at 2 h and 0.125 h, while the original drug group appeared at the peak concentration at 4 h. These indicate that curcumin was prepared into liposomes, which were absorbed into the blood significantly faster than that of the original drug group, and reached the peak concentration in vivo faster, and the bioavailability was significantly improved. (Figure 2)

Figure 2. Pictures of blood concentrations of liposomal curcumin.

• As can be seen from the table 2, the AUC0-12h of both liposomal curcumin-P2-50% and liposomal curcumin-P2-20% were higher than that of the original curcumin group, with the highest RB value of 107.5-fold for liposomal curcumin-P2-50%, suggesting that curcumin was prepared as liposomes and its bioavailability was significantly increased.

Table 1 Blood concentration analysis of curcumin in different groups.

Figure 3. Pictures of relative bioavailability of liposomal curcumin in different groups.

Table 2 Relative bioavailability of curcumin in different groups.

Methods

References

1. Karewicz A, et al.; Curcumin-containing liposomes stabilized by thin layers of chitosan derivatives. Colloids and Surfaces B: Biointerfaces. 2013, 109: 307-316.
2. Hocking A, et al.; The safety and exploration of the pharmacokinetics of intrapleural liposomal curcumin. International Journal of Nanomedicine. 2020,15: 943-952.