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Published on: April 26, 2016
Development of lipid nanoparticles for a histone deacetylases inhibitor as a promising anticancer therapeutic
Tuan Hiep Tran1, Duc Thanh Chu2, Duy Hieu Truong1
1a College of Pharmacy , Yeungnam University , Dae-Dong, Gyeongsan , South Korea and.
Background:
Vorinostat (VRS), a histone deacetylases inhibitor, has significant cytotoxic potential in a large number of human cancer cell lines.
Objective:
To clarify its promising anticancer potential and to improve its drawback related to physical properties and in vivo performance of VRS.
Methods:
VRS was successfully incorporated into nanostructured lipid carriers (NLCs) by the hot microemulsion method using sonication following a homogenization technique.
Results:
After the optimization process, VRS-loaded NLCs (VRS-NLCs) were obtained as ideal quality nanoparticles with a spherical shape, small size (∼150 nm), negative charge (∼-22 mV), and narrow size distribution. In addition, the high entrapment efficiency (∼99%) and sustained drug release profile were recorded. Cytotoxicity study in three different cell lines (A549, MCF-7, and SCC-7) demonstrated higher cytotoxicity of VRS-NLCs than free drug. Finally, the AUC of VRS (118.16 ± 17.35 µgh/mL) was enhanced ∼4.4 times compared with that of free drug (27.03 ± 3.25 µgh/mL).
Conclusion:
These results suggest the potential of NLCs as an oral delivery system for enhancement of cellular uptake, in vitro cytotoxicity in cancer cell lines and the oral bioavailability of VRS.
Insights
Vorinostat (VRS) loaded into nanostructured lipid carriers (NLCs) improved its anticancer effects. This novel formulation enhances drug delivery, leading to increased cytotoxicity and better oral bioavailability for cancer treatment.
Area of Science:
- Pharmaceutical Nanotechnology
- Cancer Therapeutics
- Drug Delivery Systems
Background:
- Vorinostat (VRS), a histone deacetylases inhibitor, exhibits significant cytotoxic potential against various human cancer cell lines.
- Limitations in VRS's physical properties and in vivo performance hinder its clinical application.
Purpose of the Study:
- To enhance the anticancer potential of Vorinostat (VRS).
- To overcome the limitations of VRS related to its physical properties and in vivo performance through advanced formulation.
Main Methods:
- Vorinostat (VRS) was encapsulated into nanostructured lipid carriers (NLCs) using a hot microemulsion method.
- The formulation process involved sonication and homogenization, followed by optimization.
Main Results:
- Optimized VRS-loaded NLCs (VRS-NLCs) were spherical nanoparticles (∼150 nm) with a negative charge (∼-22 mV) and narrow size distribution.
- High entrapment efficiency (∼99%) and sustained drug release were achieved.
- VRS-NLCs demonstrated superior in vitro cytotoxicity compared to free VRS across A549, MCF-7, and SCC-7 cell lines, with a ~4.4-fold increase in AUC for oral bioavailability.
Conclusions:
- Nanostructured lipid carriers (NLCs) show promise as an effective oral delivery system for Vorinostat (VRS).
- NLC formulation enhances cellular uptake, in vitro cytotoxicity, and oral bioavailability of VRS in cancer models.
