Abstract:
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.
journal_name
Drug Delivjournal_title
Drug deliveryauthors
Tran TH,Chu DT,Truong DH,Tak JW,Jeong JH,Hoang VL,Yong CS,Kim JOdoi
10.3109/10717544.2014.991432subject
Has Abstractpub_date
2016-05-01 00:00:00pages
1335-43issue
4eissn
1071-7544issn
1521-0464journal_volume
23pub_type
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