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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

In vivo biodistribution after intraperitoneal administration of (A) UA and (B) UA-NPs in mice.Abbreviations: UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.
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f11-ijn-10-1909: In vivo biodistribution after intraperitoneal administration of (A) UA and (B) UA-NPs in mice.Abbreviations: UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.

Mentions: Figure 11 shows the distribution of free UA and UA-NPs in different tissues at various times. Free UA mainly accumulated in the liver, kidney, and tumor in the initial 12 hours (Figure 11A), then was followed by quick redistribution from these tissues. It is clear that most of the free UA was cleaned up from the major tissues after 48 hours. However, the concentration of UA delivered by nanoparticles gradually accumulated in the liver and tumor over time. At the end of the observation period (48 hours postinjection), the peak UA concentration of UA-NPs was achieved in liver and tumor (Figure 11B). To analyze the potential toxicity of our UA-NPs in vivo, both spleen and liver of mice were harvested during the experiment and investigated via H&E pathological staining, as shown in Figure S3. There was no apparent abnormality or inflammation lesion in any of the four organs, which presents solid evidence to the long term biocompatibility of UA-NPs. These results indicate that delivery of UA by nanoparticles can alter the in vivo biodistribution and prolong the retention time of UA.


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)

In vivo biodistribution after intraperitoneal administration of (A) UA and (B) UA-NPs in mice.Abbreviations: 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

f11-ijn-10-1909: In vivo biodistribution after intraperitoneal administration of (A) UA and (B) UA-NPs in mice.Abbreviations: UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.
Mentions: Figure 11 shows the distribution of free UA and UA-NPs in different tissues at various times. Free UA mainly accumulated in the liver, kidney, and tumor in the initial 12 hours (Figure 11A), then was followed by quick redistribution from these tissues. It is clear that most of the free UA was cleaned up from the major tissues after 48 hours. However, the concentration of UA delivered by nanoparticles gradually accumulated in the liver and tumor over time. At the end of the observation period (48 hours postinjection), the peak UA concentration of UA-NPs was achieved in liver and tumor (Figure 11B). To analyze the potential toxicity of our UA-NPs in vivo, both spleen and liver of mice were harvested during the experiment and investigated via H&E pathological staining, as shown in Figure S3. There was no apparent abnormality or inflammation lesion in any of the four organs, which presents solid evidence to the long term biocompatibility of UA-NPs. These results indicate that delivery of UA by nanoparticles can alter the in vivo biodistribution and prolong the retention time of UA.

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