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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: 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.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

The tumor protein expression of COX-2, Caspase-3, Bax, and Bcl-2 in H22-transplanted mice treated with empty NPs, UA, and UA-NPs.Notes: (A) The gel image of Western blot analysis. (B) The histogram representing the semiquantification of gel image normalizing the band with the GAPDH control. **P<0.01 versus control. #P<0.05 versus the equivalent dose of UA. Data are presented as mean ± SD (n=3).Abbreviations: NP, nanoparticle; SD, standard deviation; UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.
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f9-ijn-10-1909: The tumor protein expression of COX-2, Caspase-3, Bax, and Bcl-2 in H22-transplanted mice treated with empty NPs, UA, and UA-NPs.Notes: (A) The gel image of Western blot analysis. (B) The histogram representing the semiquantification of gel image normalizing the band with the GAPDH control. **P<0.01 versus control. #P<0.05 versus the equivalent dose of UA. Data are presented as mean ± SD (n=3).Abbreviations: NP, nanoparticle; SD, standard deviation; UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.

Mentions: The expressions of COX-2, Bcl-2, Bax, and Caspase-3 in H22 cells or tumor tissues were examined by Western blotting and immunohistochemical staining. The subcutaneous hepatocellular carcinoma tumor models were treated with empty nanoparticles, UA, and UA-NPs, respectively. UA and UA-NPs upregulated the expressions of Caspase-3 and Bax, but downregulated the expressions of Bcl-2 and COX-2 (Figure 8). Most importantly, there were significant differences between the protein expressions in cells treated with UA-NPs and free UA (P<0.05). In other words, UA-NPs had a more significant effect on protein expression than did free UA. The results from the tumor tissues were in accordance with the results from cells (Figure 9).


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)

The tumor protein expression of COX-2, Caspase-3, Bax, and Bcl-2 in H22-transplanted mice treated with empty NPs, UA, and UA-NPs.Notes: (A) The gel image of Western blot analysis. (B) The histogram representing the semiquantification of gel image normalizing the band with the GAPDH control. **P<0.01 versus control. #P<0.05 versus the equivalent dose of UA. Data are presented as mean ± SD (n=3).Abbreviations: NP, nanoparticle; SD, standard deviation; 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

f9-ijn-10-1909: The tumor protein expression of COX-2, Caspase-3, Bax, and Bcl-2 in H22-transplanted mice treated with empty NPs, UA, and UA-NPs.Notes: (A) The gel image of Western blot analysis. (B) The histogram representing the semiquantification of gel image normalizing the band with the GAPDH control. **P<0.01 versus control. #P<0.05 versus the equivalent dose of UA. Data are presented as mean ± SD (n=3).Abbreviations: NP, nanoparticle; SD, standard deviation; UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.
Mentions: The expressions of COX-2, Bcl-2, Bax, and Caspase-3 in H22 cells or tumor tissues were examined by Western blotting and immunohistochemical staining. The subcutaneous hepatocellular carcinoma tumor models were treated with empty nanoparticles, UA, and UA-NPs, respectively. UA and UA-NPs upregulated the expressions of Caspase-3 and Bax, but downregulated the expressions of Bcl-2 and COX-2 (Figure 8). Most importantly, there were significant differences between the protein expressions in cells treated with UA-NPs and free UA (P<0.05). In other words, UA-NPs had a more significant effect on protein expression than did free UA. The results from the tumor tissues were in accordance with the results from cells (Figure 9).

Bottom Line: 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.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