Research: ZHANG and COLLEAGUES,

Listed in Issue 268

Abstract

ZHANG and COLLEAGUES, 1. Department of Hospital Pharmacy, The First Hospital of Suqian, Suqian, People's Republic of China studied how ginsenoside compound K (CK) mixed micellar delivery system could enhance tumour targeting and antitumour effects.

Background

The roles of ginsenoside compound K (CK) in inhibiting tumour have been widely recognized in recent years. However, low water solubility and significant P-gp [P-glycoprotein] efflux have restricted its application.

Methodology

In this study, CK ascorbyl palmitate (AP)/d-α-tocopheryl polyethylene glycol 1000 succinate monoester (TPGS) mixed micelles were prepared as a delivery system to increase the absorption and targeted antitumour effect of CK.

Results

Consequently, the solubility of CK increased from 35.2±4.3 to 1,463.2±153.3 μg/mL. Furthermore, in an in vitro A549 cell model, CK AP/TPGS mixed micelles significantly inhibited cell growth, induced G0/G1 phase cell cycle arrest, induced cell apoptosis, and inhibited cell migration compared to free CK, all indicating that the developed micellar delivery system could increase the antitumour effect of CK in vitro. Both in vitro cellular fluorescence uptake and in vivo near-infrared imaging studies indicated that AP/TPGS mixed micelles can promote cellular uptake and enhance tumour targeting. Moreover, studies in the A549 lung cancer xenograft mouse model showed that CK AP/TPGS mixed micelles are an efficient tumour-targeted drug delivery system with an effective antitumour effect. Western blot analysis further confirmed that the marked antitumour effect in vivo could likely be due to apoptosis promotion and P-gp efflux inhibition.

Conclusion

Therefore, these findings suggest that the AP/TPGS mixed micellar delivery system could be an efficient delivery strategy for enhanced tumour targeting and antitumor effects.

References

Zhang Y1, Tong D1, Che D1, Pei B1, Xia X1, Yuan G1, Jin X1. Ascorbyl palmitate/d-α-tocopheryl polyethylene glycol 1000 succinate monoester mixed micelles for prolonged circulation and targeted delivery of compound K for antilung cancer therapy in vitro and in vivo. Int J Nanomedicine. 12:605-614. Jan 16 2017. DOI: 10.2147/IJN.S119226 . eCollection 2017.

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