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Efficient delivery of ursolic acid by poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles for inhibiting the growth of hepatocellular carcinoma in vitro and in vivo.

Zhang H, Zheng D, Ding J, Xu H, Li X, Sun W - Int J Nanomedicine (2015)

Bottom Line: Moreover, UA-NPs significantly delayed tumor growth and localized to the tumor site when compared with the equivalent dose of UA.In addition, both Western blotting and immunohistochemistry suggested that the possible mechanism of the superior efficiency of UA-NPs is mediation by the regulation of apoptosis-related proteins.Therefore, UA-NPs show potential as a promising nanosized drug system for liver cancer therapy.

View Article: PubMed Central - PubMed

Affiliation: Department of Geriatric Gastroenterology, First Affiliated Hospital with Nanjing Medical University, Nanjing, People's Republic of China.

ABSTRACT
Previous reports have shown that ursolic acid (UA), a pentacyclic triterpenoid derived from Catharanthus trichophyllus roots, could inhibit the growth of a series of cancer cells. However, the potential for clinical application of UA is greatly hampered by its poor solubility, whereas the hydrophobicity of UA renders it a promising model drug for nanosized delivery systems. In the current study, we loaded UA into amphiphilic poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles and performed physiochemical characterization as well as analysis of the releasing capacity. In vitro experiments indicated that UA-NPs inhibited the growth of liver cancer cells and induced cellular apoptosis more efficiently than did free UA. Moreover, UA-NPs significantly delayed tumor growth and localized to the tumor site when compared with the equivalent dose of UA. In addition, both Western blotting and immunohistochemistry suggested that the possible mechanism of the superior efficiency of UA-NPs is mediation by the regulation of apoptosis-related proteins. Therefore, UA-NPs show potential as a promising nanosized drug system for liver cancer therapy.

No MeSH data available.


Related in: MedlinePlus

DSC thermograms of UA and UA-NPs.Abbreviations: DSC, differential scanning calorimetry; UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.
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f3-ijn-10-1909: DSC thermograms of UA and UA-NPs.Abbreviations: DSC, differential scanning calorimetry; UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.

Mentions: As shown in Figure 3, pure UA is characterized by an endothermic melting peak at 287°C, while no UA melting peak was found in the DSC curves of UA-NPs. Therefore, the encapsulated UA in the PVP-b-PCL nanoparticles was disorderly dispersed as a crystalline state in the polymer matrix.


Efficient delivery of ursolic acid by poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles for inhibiting the growth of hepatocellular carcinoma in vitro and in vivo.

Zhang H, Zheng D, Ding J, Xu H, Li X, Sun W - Int J Nanomedicine (2015)

DSC thermograms of UA and UA-NPs.Abbreviations: DSC, differential scanning calorimetry; UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4362907&req=5

f3-ijn-10-1909: DSC thermograms of UA and UA-NPs.Abbreviations: DSC, differential scanning calorimetry; UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.
Mentions: As shown in Figure 3, pure UA is characterized by an endothermic melting peak at 287°C, while no UA melting peak was found in the DSC curves of UA-NPs. Therefore, the encapsulated UA in the PVP-b-PCL nanoparticles was disorderly dispersed as a crystalline state in the polymer matrix.

Bottom Line: Moreover, UA-NPs significantly delayed tumor growth and localized to the tumor site when compared with the equivalent dose of UA.In addition, both Western blotting and immunohistochemistry suggested that the possible mechanism of the superior efficiency of UA-NPs is mediation by the regulation of apoptosis-related proteins.Therefore, UA-NPs show potential as a promising nanosized drug system for liver cancer therapy.

View Article: PubMed Central - PubMed

Affiliation: Department of Geriatric Gastroenterology, First Affiliated Hospital with Nanjing Medical University, Nanjing, People's Republic of China.

ABSTRACT
Previous reports have shown that ursolic acid (UA), a pentacyclic triterpenoid derived from Catharanthus trichophyllus roots, could inhibit the growth of a series of cancer cells. However, the potential for clinical application of UA is greatly hampered by its poor solubility, whereas the hydrophobicity of UA renders it a promising model drug for nanosized delivery systems. In the current study, we loaded UA into amphiphilic poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles and performed physiochemical characterization as well as analysis of the releasing capacity. In vitro experiments indicated that UA-NPs inhibited the growth of liver cancer cells and induced cellular apoptosis more efficiently than did free UA. Moreover, UA-NPs significantly delayed tumor growth and localized to the tumor site when compared with the equivalent dose of UA. In addition, both Western blotting and immunohistochemistry suggested that the possible mechanism of the superior efficiency of UA-NPs is mediation by the regulation of apoptosis-related proteins. Therefore, UA-NPs show potential as a promising nanosized drug system for liver cancer therapy.

No MeSH data available.


Related in: MedlinePlus