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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

In vitro cytotoxicity of Ccn-sus, Ccn-BNPs, Ccn-BNP-GA, and GA + Ccn-BNP-GA against HepG2 cells for 24 hours.Notes: Each point represents the mean ± standard deviation (n=6). *P<0.05 compared with Ccn-BNPs, #P<0.05 compared with Ccn-BNP-GA.Abbreviations: Ccn-sus, curcumin suspension; Ccn-BNPs, curcumin-loaded albumin nanoparticles; Ccn-BNP-GA, curcumin-loaded albumin nanoparticles surface-functionalized with GA; GA, glycyrrhetinic acid.
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f6-ijn-10-5475: In vitro cytotoxicity of Ccn-sus, Ccn-BNPs, Ccn-BNP-GA, and GA + Ccn-BNP-GA against HepG2 cells for 24 hours.Notes: Each point represents the mean ± standard deviation (n=6). *P<0.05 compared with Ccn-BNPs, #P<0.05 compared with Ccn-BNP-GA.Abbreviations: Ccn-sus, curcumin suspension; Ccn-BNPs, curcumin-loaded albumin nanoparticles; Ccn-BNP-GA, curcumin-loaded albumin nanoparticles surface-functionalized with GA; GA, glycyrrhetinic acid.

Mentions: As shown in Figure 6, when the Ccn-loaded formulations at various concentrations were added to the incubated cells for 24 hours, a dramatic decrease in cell viability could be observed. The anticancer activity of Ccn-BNP-GA was significantly higher than that of the other formulations, which could be ascribed to GA receptor-mediated specific endocytosis. Moreover, a competitive binding assay was conducted by adding free GA prior to application of Ccn-BNP-GA. The inhibition rate gradually manifested a decreased pattern, and the results revealed that free GA competed with Ccn-BNP-GA to bind with GA receptors on the HepG2 cell surface, thus leading to saturation of GA receptors and inhibiting the delivery of Ccn-BNP-GA into cells. Generally, more Ccn-BNP-GA was internalized by GA receptor-mediated endocytosis than undecorated Ccn-BNPs, and the Ccn-loaded formulations inhibited HepG2 cells in a concentration-dependent manner.


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)

In vitro cytotoxicity of Ccn-sus, Ccn-BNPs, Ccn-BNP-GA, and GA + Ccn-BNP-GA against HepG2 cells for 24 hours.Notes: Each point represents the mean ± standard deviation (n=6). *P<0.05 compared with Ccn-BNPs, #P<0.05 compared with Ccn-BNP-GA.Abbreviations: Ccn-sus, curcumin suspension; Ccn-BNPs, curcumin-loaded albumin nanoparticles; Ccn-BNP-GA, curcumin-loaded albumin nanoparticles surface-functionalized with GA; GA, glycyrrhetinic acid.
© Copyright Policy
Related In: Results  -  Collection

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

f6-ijn-10-5475: In vitro cytotoxicity of Ccn-sus, Ccn-BNPs, Ccn-BNP-GA, and GA + Ccn-BNP-GA against HepG2 cells for 24 hours.Notes: Each point represents the mean ± standard deviation (n=6). *P<0.05 compared with Ccn-BNPs, #P<0.05 compared with Ccn-BNP-GA.Abbreviations: Ccn-sus, curcumin suspension; Ccn-BNPs, curcumin-loaded albumin nanoparticles; Ccn-BNP-GA, curcumin-loaded albumin nanoparticles surface-functionalized with GA; GA, glycyrrhetinic acid.
Mentions: As shown in Figure 6, when the Ccn-loaded formulations at various concentrations were added to the incubated cells for 24 hours, a dramatic decrease in cell viability could be observed. The anticancer activity of Ccn-BNP-GA was significantly higher than that of the other formulations, which could be ascribed to GA receptor-mediated specific endocytosis. Moreover, a competitive binding assay was conducted by adding free GA prior to application of Ccn-BNP-GA. The inhibition rate gradually manifested a decreased pattern, and the results revealed that free GA competed with Ccn-BNP-GA to bind with GA receptors on the HepG2 cell surface, thus leading to saturation of GA receptors and inhibiting the delivery of Ccn-BNP-GA into cells. Generally, more Ccn-BNP-GA was internalized by GA receptor-mediated endocytosis than undecorated Ccn-BNPs, and the Ccn-loaded formulations inhibited HepG2 cells in a concentration-dependent manner.

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