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Synthesis, characterization, and in vitro evaluation of curcumin-loaded albumin nanoparticles surface-functionalized with glycyrrhetinic acid.

Li J, Chen T, Deng F, Wan J, Tang Y, Yuan P, Zhang L - Int J Nanomedicine (2015)

Bottom Line: Ccn-BNP-GA also appeared to be taken up to a greater extent by HepG2 cells than undecorated groups, which might be due to the high affinity of GA for GA receptors on the HepG2 cell surface.Further, Ccn-BNP-GA showed an approximately twofold higher rate of cell apoptosis than the other groups.Moreover, proliferation of HepG2 cells was arrested in G2/M phase based on cell cycle analysis.

View Article: PubMed Central - PubMed

Affiliation: Chongqing Medicine Engineering Research Center, Chongqing Key Laboratory of Biochemistry and Molecular Pharmacology, School of Pharmacy, Chongqing Medical University, Chongqing, People's Republic of China.

ABSTRACT
We have designed and developed curcumin (Ccn)-loaded albumin nanoparticles (BNPs) surface-functionalized with glycyrrhetinic acid (Ccn-BNP-GA) for GA receptor-mediated targeting. Ccn-BNP-GA was prepared by conjugating GA as a hepatoma cell-specific binding molecule onto the surface of BNPs. Ccn-BNP-GA showed a narrow distribution with an average size of 258.8±6.4 nm, a regularly spherical shape, an entrapment efficiency of 88.55%±5.54%, and drug loading of 25.30%±1.58%. The density of GA as the ligand conjugated to BNPs was 140.48±2.784 μg/g bovine serum albumin. Cytotoxicity assay results indicated that Ccn-BNP-GA was significantly more cytotoxic to HepG2 cells and in a concentration-dependent manner. Ccn-BNP-GA also appeared to be taken up to a greater extent by HepG2 cells than undecorated groups, which might be due to the high affinity of GA for GA receptors on the HepG2 cell surface. These cytotoxicity assay results were corroborated by analysis of cell apoptosis and the cell cycle. Further, Ccn-BNP-GA showed an approximately twofold higher rate of cell apoptosis than the other groups. Moreover, proliferation of HepG2 cells was arrested in G2/M phase based on cell cycle analysis. These results, which were supported by the GA receptor-mediated endocytosis mechanism, indicate that BNPs surface-functionalized with GA could be used in targeted cancer treatment with high efficacy, sufficient targeting, and reduced toxicity.

No MeSH data available.


Related in: MedlinePlus

Effect of 24 hours of treatment with curcumin on the cell cycle in HepG2 cells.Notes: (A) Control, (B) curcumin suspension, (C) curcumin-loaded albumin nanoparticles, (D) curcumin-loaded albumin nanoparticles surface-functionalized with GA, and (E) GA + curcumin-loaded albumin nanoparticles surface-functionalized with GA.Abbreviation: GA, glycyrrhetinic acid.
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f10-ijn-10-5475: Effect of 24 hours of treatment with curcumin on the cell cycle in HepG2 cells.Notes: (A) Control, (B) curcumin suspension, (C) curcumin-loaded albumin nanoparticles, (D) curcumin-loaded albumin nanoparticles surface-functionalized with GA, and (E) GA + curcumin-loaded albumin nanoparticles surface-functionalized with GA.Abbreviation: GA, glycyrrhetinic acid.

Mentions: The FCM procedure (BD FACS Vantage SE) was used to further analyze how the involvement of Ccn-BNP-GA changed the distribution of HepG2 cells present in different phases of the cell cycle. As seen in Figure 10, treatment of HepG2 cells with the Ccn suspension led to a gradual increment in G2/M phase cells compared with the control. Moreover, treatment with Ccn-BNPs or Ccn-BNP-GA resulted in changes ranging from 9.59% to 14.12% in G2/M phase; Ccn-BNP-GA differed from the control group by 4.52% and the Ccn suspension group by 6.88%. Further, a dramatic decrease in the G2/M phase was observed in the competitive binding experiment. These data confirm that Ccn-BNP-GA can induce cell cycle arrest in the G2/M phase.


Synthesis, characterization, and in vitro evaluation of curcumin-loaded albumin nanoparticles surface-functionalized with glycyrrhetinic acid.

Li J, Chen T, Deng F, Wan J, Tang Y, Yuan P, Zhang L - Int J Nanomedicine (2015)

Effect of 24 hours of treatment with curcumin on the cell cycle in HepG2 cells.Notes: (A) Control, (B) curcumin suspension, (C) curcumin-loaded albumin nanoparticles, (D) curcumin-loaded albumin nanoparticles surface-functionalized with GA, and (E) GA + curcumin-loaded albumin nanoparticles surface-functionalized with GA.Abbreviation: GA, glycyrrhetinic acid.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4556296&req=5

f10-ijn-10-5475: Effect of 24 hours of treatment with curcumin on the cell cycle in HepG2 cells.Notes: (A) Control, (B) curcumin suspension, (C) curcumin-loaded albumin nanoparticles, (D) curcumin-loaded albumin nanoparticles surface-functionalized with GA, and (E) GA + curcumin-loaded albumin nanoparticles surface-functionalized with GA.Abbreviation: GA, glycyrrhetinic acid.
Mentions: The FCM procedure (BD FACS Vantage SE) was used to further analyze how the involvement of Ccn-BNP-GA changed the distribution of HepG2 cells present in different phases of the cell cycle. As seen in Figure 10, treatment of HepG2 cells with the Ccn suspension led to a gradual increment in G2/M phase cells compared with the control. Moreover, treatment with Ccn-BNPs or Ccn-BNP-GA resulted in changes ranging from 9.59% to 14.12% in G2/M phase; Ccn-BNP-GA differed from the control group by 4.52% and the Ccn suspension group by 6.88%. Further, a dramatic decrease in the G2/M phase was observed in the competitive binding experiment. These data confirm that Ccn-BNP-GA can induce cell cycle arrest in the G2/M phase.

Bottom Line: Ccn-BNP-GA also appeared to be taken up to a greater extent by HepG2 cells than undecorated groups, which might be due to the high affinity of GA for GA receptors on the HepG2 cell surface.Further, Ccn-BNP-GA showed an approximately twofold higher rate of cell apoptosis than the other groups.Moreover, proliferation of HepG2 cells was arrested in G2/M phase based on cell cycle analysis.

View Article: PubMed Central - PubMed

Affiliation: Chongqing Medicine Engineering Research Center, Chongqing Key Laboratory of Biochemistry and Molecular Pharmacology, School of Pharmacy, Chongqing Medical University, Chongqing, People's Republic of China.

ABSTRACT
We have designed and developed curcumin (Ccn)-loaded albumin nanoparticles (BNPs) surface-functionalized with glycyrrhetinic acid (Ccn-BNP-GA) for GA receptor-mediated targeting. Ccn-BNP-GA was prepared by conjugating GA as a hepatoma cell-specific binding molecule onto the surface of BNPs. Ccn-BNP-GA showed a narrow distribution with an average size of 258.8±6.4 nm, a regularly spherical shape, an entrapment efficiency of 88.55%±5.54%, and drug loading of 25.30%±1.58%. The density of GA as the ligand conjugated to BNPs was 140.48±2.784 μg/g bovine serum albumin. Cytotoxicity assay results indicated that Ccn-BNP-GA was significantly more cytotoxic to HepG2 cells and in a concentration-dependent manner. Ccn-BNP-GA also appeared to be taken up to a greater extent by HepG2 cells than undecorated groups, which might be due to the high affinity of GA for GA receptors on the HepG2 cell surface. These cytotoxicity assay results were corroborated by analysis of cell apoptosis and the cell cycle. Further, Ccn-BNP-GA showed an approximately twofold higher rate of cell apoptosis than the other groups. Moreover, proliferation of HepG2 cells was arrested in G2/M phase based on cell cycle analysis. These results, which were supported by the GA receptor-mediated endocytosis mechanism, indicate that BNPs surface-functionalized with GA could be used in targeted cancer treatment with high efficacy, sufficient targeting, and reduced toxicity.

No MeSH data available.


Related in: MedlinePlus