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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

Antitumor effect of UA-NPs in H22 subcutaneous tumor bearing mouse model.Notes: Changes in (A) tumor volume, (B) relative tumor volume, (C) therapeutic group/control group (T/C)%, and (D) body weight of H22-transplanted imprinting control region mice receiving different therapy treatments. *P<0.05 versus control; **P<0.01 versus control. #P<0.05 versus the equivalent dose of UA. Data in (A) and (D) are presented as mean ± SD.Abbreviations: SD, standard deviation; NP, nanoparticle; UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.
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f6-ijn-10-1909: Antitumor effect of UA-NPs in H22 subcutaneous tumor bearing mouse model.Notes: Changes in (A) tumor volume, (B) relative tumor volume, (C) therapeutic group/control group (T/C)%, and (D) body weight of H22-transplanted imprinting control region mice receiving different therapy treatments. *P<0.05 versus control; **P<0.01 versus control. #P<0.05 versus the equivalent dose of UA. Data in (A) and (D) are presented as mean ± SD.Abbreviations: SD, standard deviation; NP, nanoparticle; UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.

Mentions: Figure 6A indicates the tumor growth curves of mice treated with different agents. Both free UA and UA-NPs delayed tumor growth in a dose-dependent manner, while UA-NPs led to a more retarded growth from day 5. There was a significant difference between the tumor volumes of mice treated with UA-NPs and free UA (P<0.05). The curves of derived parameters from tumor volume, including RTV and T/C%, demonstrated the superior antitumor effects of UA-NPs compared with free UA by showing the similar trends of tumor volume (Figure 6B and C). As shown in Figure 6D, bodyweight change curves show that UA induced severe weight loss by the end of the experiment. We noticed that two mice in the UA group had necropsy at the centers of their tumor, and they were in a very weak state (mobility and “color of fur”). This was not very obvious until the second week of the experiment. These results partially indicate that free UA led to more toxicity than UA-NPs at the equivalent administered dose.


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)

Antitumor effect of UA-NPs in H22 subcutaneous tumor bearing mouse model.Notes: Changes in (A) tumor volume, (B) relative tumor volume, (C) therapeutic group/control group (T/C)%, and (D) body weight of H22-transplanted imprinting control region mice receiving different therapy treatments. *P<0.05 versus control; **P<0.01 versus control. #P<0.05 versus the equivalent dose of UA. Data in (A) and (D) are presented as mean ± SD.Abbreviations: SD, standard deviation; NP, nanoparticle; 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

f6-ijn-10-1909: Antitumor effect of UA-NPs in H22 subcutaneous tumor bearing mouse model.Notes: Changes in (A) tumor volume, (B) relative tumor volume, (C) therapeutic group/control group (T/C)%, and (D) body weight of H22-transplanted imprinting control region mice receiving different therapy treatments. *P<0.05 versus control; **P<0.01 versus control. #P<0.05 versus the equivalent dose of UA. Data in (A) and (D) are presented as mean ± SD.Abbreviations: SD, standard deviation; NP, nanoparticle; UA, ursolic acid; UA-NPs, UA-loaded poly(N-vinylpyrrolidone)-block-poly (ε-caprolactone) nanoparticles.
Mentions: Figure 6A indicates the tumor growth curves of mice treated with different agents. Both free UA and UA-NPs delayed tumor growth in a dose-dependent manner, while UA-NPs led to a more retarded growth from day 5. There was a significant difference between the tumor volumes of mice treated with UA-NPs and free UA (P<0.05). The curves of derived parameters from tumor volume, including RTV and T/C%, demonstrated the superior antitumor effects of UA-NPs compared with free UA by showing the similar trends of tumor volume (Figure 6B and C). As shown in Figure 6D, bodyweight change curves show that UA induced severe weight loss by the end of the experiment. We noticed that two mice in the UA group had necropsy at the centers of their tumor, and they were in a very weak state (mobility and “color of fur”). This was not very obvious until the second week of the experiment. These results partially indicate that free UA led to more toxicity than UA-NPs at the equivalent administered dose.

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