Development of lipid nanoparticles for a histone deacetylases inhibitor as a promising anticancer therapeutic

Tuan Hiep Tran; Duc Thanh Chu; Duy Hieu Truong; Jin Wook Tak; Jee Heon Jeong; Van Luong Hoang; Chul Soon Yong; Jong Oh Kim

doi:10.3109/10717544.2014.991432

Development of lipid nanoparticles for a histone deacetylases inhibitor as a promising anticancer therapeutic

Tuan Hiep Tran, Duc Thanh Chu, Duy Hieu Truong, Jin Wook Tak, Jee Heon Jeong, Van Luong Hoang, Chul Soon Yong, Jong Oh Kim

Research output: Contribution to journal › Article › peer-review

21 Scopus citations

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.

Original language	English
Pages (from-to)	1335-1343
Number of pages	9
Journal	Drug Delivery
Volume	23
Issue number	4
DOIs	https://doi.org/10.3109/10717544.2014.991432
State	Published - 3 May 2016
Externally published	Yes

Keywords

Histone deacetylases inhibitor
nanostructured lipid carriers
oral bioavailability
vorinostat

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.3109/10717544.2014.991432

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@article{014602f786c44760a5ef265d21f412a2,

title = "Development of lipid nanoparticles for a histone deacetylases inhibitor as a promising anticancer therapeutic",

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.",

keywords = "Histone deacetylases inhibitor, nanostructured lipid carriers, oral bioavailability, vorinostat",

author = "Tran, \{Tuan Hiep\} and Chu, \{Duc Thanh\} and Truong, \{Duy Hieu\} and Tak, \{Jin Wook\} and Jeong, \{Jee Heon\} and Hoang, \{Van Luong\} and Yong, \{Chul Soon\} and Kim, \{Jong Oh\}",

note = "Publisher Copyright: {\textcopyright} 2014 Informa UK Limited, trading as Taylor \& Francis Group.",

year = "2016",

month = may,

day = "3",

doi = "10.3109/10717544.2014.991432",

language = "English",

volume = "23",

pages = "1335--1343",

journal = "Drug Delivery",

issn = "1071-7544",

publisher = "Taylor and Francis Ltd.",

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TY - JOUR

T1 - Development of lipid nanoparticles for a histone deacetylases inhibitor as a promising anticancer therapeutic

AU - Tran, Tuan Hiep

AU - Chu, Duc Thanh

AU - Truong, Duy Hieu

AU - Tak, Jin Wook

AU - Jeong, Jee Heon

AU - Hoang, Van Luong

AU - Yong, Chul Soon

AU - Kim, Jong Oh

PY - 2016/5/3

Y1 - 2016/5/3

N2 - 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.

AB - 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.

KW - Histone deacetylases inhibitor

KW - nanostructured lipid carriers

KW - oral bioavailability

KW - vorinostat

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DO - 10.3109/10717544.2014.991432

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JF - Drug Delivery

IS - 4

ER -

Development of lipid nanoparticles for a histone deacetylases inhibitor as a promising anticancer therapeutic

Abstract

Keywords

UN SDGs

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