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Published on: December 1, 2016
Synergistic Combination of Sodium Aescinate-Stabilized, Polymer-Free, Twin-Like Nanoparticles to Reverse Paclitaxel
Juan Li1, Lei Zheng2, Rongmei Wang1
1Department of Clinical Pharmacy, The Second Hospital, Cheeloo College of Medicine, Shandong University, Jinan, Shandong 250033, People's Republic of China.
Background:
The development of paclitaxel (PTX) resistance seriously restricts its clinical efficacy. An attractive option for combating resistance is inhibiting the expression of P-glycoprotein (P-gp) in tumor cells. We have reported that flavokawain A (FKA) inhibited P-gp protein expression in PTX-resistant A549 (A549/T) cells, indicating that FKA combined with PTX may reverse PTX resistance. However, due to the variable pharmacokinetics of FKA and PTX, the conventional cocktail combination in clinics may cause uncertainty of treatment efficacy in vivo.
Materials And Methods:
To synergistically elevate the anti-cancer activity of PTX and FKA in vivo, the national medical products administration (NMPA) approved sodium aescinate (Aes) was utilized to stabilize hydrophobic PTX and FKA to form polymer-free twin like PTX-A nanoparticles (NPs) and FKA-A NPs.
Results:
The resulting nanoparticles prepared simply by nanoprecipitation possessed similar particle size, good stability and ultrahigh drug loadings of up to 50%. With the aid of Aes, these two drugs accumulated in tumor tissue by passive targeting and were efficiently taken up by A549/T cells; this resulted in significant suppression of tumor growth in A549/T homograft mice at a low PTX dose (2.5 mg·kg-1). Synergistic effects and reversed PTX resistance were achieved by the combination of PTX-A NPs and FKA-A NPs by inhibiting P-gp expression in tumor cells.
Conclusion:
Using NMPA-approved Aes to prepare twin-like nanoparticles without introducing any new materials provides an efficient platform for combination chemotherapy and clinical translation.
Insights
This study developed novel nanoparticles combining paclitaxel (PTX) and flavokawain A (FKA) using sodium aescinate (Aes) to overcome PTX resistance. The Aes-stabilized nanoparticles effectively suppressed tumor growth and reversed resistance by inhibiting P-glycoprotein (P-gp).
Area of Science:
- Nanotechnology
- Drug Delivery Systems
- Cancer Therapeutics
Background:
- Paclitaxel (PTX) resistance in cancer limits clinical effectiveness.
- Inhibiting P-glycoprotein (P-gp) is a strategy to combat PTX resistance.
- Flavokawain A (FKA) showed potential to inhibit P-gp and reverse PTX resistance.
Purpose of the Study:
- To synergistically enhance the anti-cancer activity of PTX and FKA in vivo.
- To develop a stable nanoparticle formulation for combination chemotherapy.
- To overcome the pharmacokinetic variability of conventional PTX and FKA combinations.
Main Methods:
- Formulation of polymer-free, twin-like PTX-Aes (PTX-A) and FKA-Aes (FKA-A) nanoparticles using sodium aescinate (Aes).
- Characterization of nanoparticles for particle size, stability, and drug loading.
- In vivo evaluation in A549/T homograft mice to assess tumor suppression and P-gp inhibition.
Main Results:
- Nanoparticles exhibited good stability and high drug loading (up to 50%).
- Aes-aided nanoparticles achieved passive tumor targeting and efficient cellular uptake.
- Significant tumor growth suppression was observed at a low PTX dose, demonstrating synergistic effects and reversed PTX resistance via P-gp inhibition.
Conclusions:
- Sodium aescinate (Aes) effectively stabilized PTX and FKA into twin-like nanoparticles.
- This Aes-based nanoparticle platform offers an efficient strategy for combination chemotherapy.
- The approach shows promise for clinical translation in overcoming drug resistance.
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