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Fabrication of genistein-loaded biodegradable TPGS-b-PCL nanoparticles for improved therapeutic effects in cervical cancer cells.

Zhang H, Liu G, Zeng X, Wu Y, Yang C, Mei L, Wang Z, Huang L - Int J Nanomedicine (2015)

Bottom Line: The TPGS-b-PCL NPs were found to have higher cellular uptake efficiency than PCL NPs.Furthermore, compared with pristine genistein and genistein-loaded PCL NPs, the genistein-loaded TPGS-b-PCL NPs at the same dose were more effective in inhibiting tumor growth in the subcutaneous HeLa xenograft tumor model in BALB/c nude mice.In conclusion, the results suggested that genistein-loaded biodegradable TPGS-b-PCL nanoparticles could enhance the anticancer effect of genistein both in vitro and in vivo, and may serve as a potential candidate in treating cervical cancer.

View Article: PubMed Central - PubMed

Affiliation: School of Life Sciences, Tsinghua University, Beijing, People's Republic of China ; The Shenzhen Key Laboratory of Gene and Antibody Therapy, Center for Biotechnology and Biomedicine and Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen, Guangdong, People's Republic of China.

ABSTRACT
Genistein is one of the most studied isoflavonoids with potential antitumor efficacy, but its poor water solubility limits its clinical application. Nanoparticles (NPs), especially biodegradable NPs, entrapping hydrophobic drugs have promising applications to improve the water solubility of hydrophobic drugs. In this work, TPGS-b-PCL copolymer was synthesized from ε-caprolactone initiated by d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) through ring-opening polymerization and characterized by Fourier transform infrared spectroscopy, proton nuclear magnetic resonance spectroscopy, gel permeation chromatography, and thermogravimetric analysis. The genistein-loaded NPs were prepared by a modified nanoprecipitation method and characterized in the aspects of particle size, surface charge, morphology, drug loading and encapsulation efficiency, in vitro drug release, and physical state of the entrapped drug. The TPGS-b-PCL NPs were found to have higher cellular uptake efficiency than PCL NPs. MTT and colony formation experiments indicated that genistein-loaded TPGS-b-PCL NPs achieved the highest level of cytotoxicity and tumor cell growth inhibition compared with pristine genistein and genistein-loaded PCL NPs. Furthermore, compared with pristine genistein and genistein-loaded PCL NPs, the genistein-loaded TPGS-b-PCL NPs at the same dose were more effective in inhibiting tumor growth in the subcutaneous HeLa xenograft tumor model in BALB/c nude mice. In conclusion, the results suggested that genistein-loaded biodegradable TPGS-b-PCL nanoparticles could enhance the anticancer effect of genistein both in vitro and in vivo, and may serve as a potential candidate in treating cervical cancer.

No MeSH data available.


Related in: MedlinePlus

FESEM image (A), TEM image (B), and DLS spectra (C) of genistein-loaded TPGS-b-PCL NPs.Abbreviations: DLS, dynamic light scattering; FESEM, field emission scanning electron microscopic; NPs, nanoparticles; PCL, poly(ε-caprolactone); TEM, transmission electron microscopic; TPGS, d-α-tocopheryl polyethylene glycol 1000 succinate.
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f6-ijn-10-2461: FESEM image (A), TEM image (B), and DLS spectra (C) of genistein-loaded TPGS-b-PCL NPs.Abbreviations: DLS, dynamic light scattering; FESEM, field emission scanning electron microscopic; NPs, nanoparticles; PCL, poly(ε-caprolactone); TEM, transmission electron microscopic; TPGS, d-α-tocopheryl polyethylene glycol 1000 succinate.

Mentions: A high-resolution image of genistein-loaded TPGS-b-PCL NPs was obtained using FESEM and TEM. As shown in Figure 6A (FESEM image) and 6B (TEM image), the genistein-loaded TPGS-b-PCL NPs were in moderate uniformity with a nearly spherical shape and smooth surface. Moreover, the particle size was around 170 nm, which was slightly smaller than that obtained from the dynamic light scattering method (Figure 6C) because of lack of hydration shell when particle size was determined by FESEM and TEM.


Fabrication of genistein-loaded biodegradable TPGS-b-PCL nanoparticles for improved therapeutic effects in cervical cancer cells.

Zhang H, Liu G, Zeng X, Wu Y, Yang C, Mei L, Wang Z, Huang L - Int J Nanomedicine (2015)

FESEM image (A), TEM image (B), and DLS spectra (C) of genistein-loaded TPGS-b-PCL NPs.Abbreviations: DLS, dynamic light scattering; FESEM, field emission scanning electron microscopic; NPs, nanoparticles; PCL, poly(ε-caprolactone); TEM, transmission electron microscopic; TPGS, d-α-tocopheryl polyethylene glycol 1000 succinate.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4383221&req=5

f6-ijn-10-2461: FESEM image (A), TEM image (B), and DLS spectra (C) of genistein-loaded TPGS-b-PCL NPs.Abbreviations: DLS, dynamic light scattering; FESEM, field emission scanning electron microscopic; NPs, nanoparticles; PCL, poly(ε-caprolactone); TEM, transmission electron microscopic; TPGS, d-α-tocopheryl polyethylene glycol 1000 succinate.
Mentions: A high-resolution image of genistein-loaded TPGS-b-PCL NPs was obtained using FESEM and TEM. As shown in Figure 6A (FESEM image) and 6B (TEM image), the genistein-loaded TPGS-b-PCL NPs were in moderate uniformity with a nearly spherical shape and smooth surface. Moreover, the particle size was around 170 nm, which was slightly smaller than that obtained from the dynamic light scattering method (Figure 6C) because of lack of hydration shell when particle size was determined by FESEM and TEM.

Bottom Line: The TPGS-b-PCL NPs were found to have higher cellular uptake efficiency than PCL NPs.Furthermore, compared with pristine genistein and genistein-loaded PCL NPs, the genistein-loaded TPGS-b-PCL NPs at the same dose were more effective in inhibiting tumor growth in the subcutaneous HeLa xenograft tumor model in BALB/c nude mice.In conclusion, the results suggested that genistein-loaded biodegradable TPGS-b-PCL nanoparticles could enhance the anticancer effect of genistein both in vitro and in vivo, and may serve as a potential candidate in treating cervical cancer.

View Article: PubMed Central - PubMed

Affiliation: School of Life Sciences, Tsinghua University, Beijing, People's Republic of China ; The Shenzhen Key Laboratory of Gene and Antibody Therapy, Center for Biotechnology and Biomedicine and Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen, Guangdong, People's Republic of China.

ABSTRACT
Genistein is one of the most studied isoflavonoids with potential antitumor efficacy, but its poor water solubility limits its clinical application. Nanoparticles (NPs), especially biodegradable NPs, entrapping hydrophobic drugs have promising applications to improve the water solubility of hydrophobic drugs. In this work, TPGS-b-PCL copolymer was synthesized from ε-caprolactone initiated by d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) through ring-opening polymerization and characterized by Fourier transform infrared spectroscopy, proton nuclear magnetic resonance spectroscopy, gel permeation chromatography, and thermogravimetric analysis. The genistein-loaded NPs were prepared by a modified nanoprecipitation method and characterized in the aspects of particle size, surface charge, morphology, drug loading and encapsulation efficiency, in vitro drug release, and physical state of the entrapped drug. The TPGS-b-PCL NPs were found to have higher cellular uptake efficiency than PCL NPs. MTT and colony formation experiments indicated that genistein-loaded TPGS-b-PCL NPs achieved the highest level of cytotoxicity and tumor cell growth inhibition compared with pristine genistein and genistein-loaded PCL NPs. Furthermore, compared with pristine genistein and genistein-loaded PCL NPs, the genistein-loaded TPGS-b-PCL NPs at the same dose were more effective in inhibiting tumor growth in the subcutaneous HeLa xenograft tumor model in BALB/c nude mice. In conclusion, the results suggested that genistein-loaded biodegradable TPGS-b-PCL nanoparticles could enhance the anticancer effect of genistein both in vitro and in vivo, and may serve as a potential candidate in treating cervical cancer.

No MeSH data available.


Related in: MedlinePlus