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2-Hydroxypropyl-β-cyclodextrin-modified SLN of paclitaxel for overcoming p-glycoprotein function in
Jong-Suep Baek1, Cheong-Weon Cho
1College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Yuseong-gu, Daejeon, South Korea.
Objectives:
This study aimed to evaluate the potential of solid lipid nanoparticles (SLNs) of paclitaxel (PTX) modified with a 2-hydroxypropyl-β-cyclodextrin system to enhance cellular accumulation of PTX into p-glycoprotein (p-gp)-expressing cells.
Methods:
The PTX-loaded-SLNs consisted of lipid (stearic acid) and surfactants (lecithin and poloxamer 188) and were then modified with 2-hydroxypropyl-β-cyclodextrin by a sonication method.
Key Findings:
In terms of cytotoxicity, PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin showed higher cytotoxicity than other formulations. In particular, the cellular uptake of PTX from PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin was about 5.8- and 1.5-fold higher than that from PTX solution and unmodified PTX-loaded SLNs in MCF-7/ADR cells, respectively. After a 4-h incubation, clear fluorescence images inside cells were observed over time. When PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin were incubated with MCF-7/ADR cells for 4 h, cellular uptake of PTX increased 1.7-fold versus that of PTX in the presence of verapamil.
Conclusions:
These results suggest that optimized SLNs modified with 2-hydroxypropyl-β-cyclodextrin may have potential as an oral drug delivery system for PTX.
Insights
Modified solid lipid nanoparticles (SLNs) with 2-hydroxypropyl-β-cyclodextrin significantly enhanced paclitaxel (PTX) cellular uptake in p-glycoprotein-expressing cells, showing improved cytotoxicity and potential for oral drug delivery.
Area of Science:
- Nanotechnology in Drug Delivery
- Pharmaceutical Sciences
- Cancer Therapeutics
Background:
- Paclitaxel (PTX) resistance in cancer cells is often mediated by p-glycoprotein (p-gp) efflux pumps.
- Solid lipid nanoparticles (SLNs) offer a promising platform for drug delivery, but their efficacy can be limited by cellular efflux.
- Modification of drug delivery systems with cyclodextrins can enhance drug solubility and cellular interaction.
Purpose of the Study:
- To evaluate the potential of paclitaxel (PTX)-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin.
- To enhance the cellular accumulation of PTX in p-glycoprotein (p-gp)-expressing cancer cells.
- To assess the impact of this modification on PTX cytotoxicity and cellular uptake.
Main Methods:
- Paclitaxel (PTX)-loaded SLNs were formulated using stearic acid, lecithin, and poloxamer 188.
- The PTX-loaded SLNs were subsequently modified with 2-hydroxypropyl-β-cyclodextrin using a sonication method.
- Cytotoxicity and cellular uptake were evaluated in MCF-7/ADR cells, a p-gp overexpressing cell line.
Main Results:
- PTX-loaded SLNs modified with 2-hydroxypropyl-β-cyclodextrin exhibited significantly higher cytotoxicity compared to other formulations.
- Cellular uptake of PTX was approximately 5.8-fold and 1.5-fold higher from modified SLNs versus PTX solution and unmodified SLNs, respectively.
- Incubation with modified SLNs resulted in a 1.7-fold increase in PTX cellular uptake compared to PTX alone in the presence of verapamil.
Conclusions:
- Optimized SLNs modified with 2-hydroxypropyl-β-cyclodextrin demonstrate enhanced cellular accumulation and cytotoxicity of paclitaxel.
- This formulation holds potential for overcoming p-glycoprotein-mediated drug resistance.
- The modified SLNs may serve as a viable oral drug delivery system for paclitaxel.
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