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Original Articles

Preparation of a novel liver-targeting nanoparticle of norcantharidin derivative and evaluation of its anti-tumour activity

, , , , , , , , & show all
Pages 183-199 | Received 24 Feb 2009, Accepted 19 Apr 2010, Published online: 26 Mar 2011

Figures & data

Figure 1. The synthesis route of Lac-NCTD.

Figure 1. The synthesis route of Lac-NCTD.

Figure 2. Particle size distribution analysis using a Zetasizer Nano particle analyzer.

Figure 2. Particle size distribution analysis using a Zetasizer Nano particle analyzer.

Figure 3. TEM photograph of Lac-NCTD-NPs (×50,000).

Figure 3. TEM photograph of Lac-NCTD-NPs (×50,000).

Figure 4. In vitro release of Lac-NCTD from nanoparticles in various mediums compared to Lac-NCTD. 

, 0.1 mol L−1 HCl for Lac-NCTD-NPs
, physiologic saline for Lac-NCTD
, physiologic saline for Lac-NCTD-NPs
, PBS (pH = 6.0) for Lac-NCTD
, PBS (pH = 6.0) for Lac-NCTD-NPs (− + −), PBS (pH = 7.4) for Lac-NCTD
PBS (pH = 7.4) for Lac-NCTD-NPs
, RPMI1640-10% FBS for Lac-NCTD and
RPMI1640-10% FBS for Lac-NCTD-NPs
.

Figure 4. In vitro release of Lac-NCTD from nanoparticles in various mediums compared to Lac-NCTD. Display full size, 0.1 mol L−1 HCl for Lac-NCTD-NPs Display full size, physiologic saline for Lac-NCTD Display full size, physiologic saline for Lac-NCTD-NPs Display full size, PBS (pH = 6.0) for Lac-NCTD Display full size, PBS (pH = 6.0) for Lac-NCTD-NPs (− + −), PBS (pH = 7.4) for Lac-NCTD Display full size PBS (pH = 7.4) for Lac-NCTD-NPs Display full size, RPMI1640-10% FBS for Lac-NCTD and Display full size RPMI1640-10% FBS for Lac-NCTD-NPs Display full size.

Figure 5. Cytotoxic effects of Lacto-NCTD on various cell lines including (a) HepG2; (b) SMMC-7721; and (c) SGC-7901, at given time points: including 12 h

, 24 h
, 48 h
and 72 h (− × −).

Figure 5. Cytotoxic effects of Lacto-NCTD on various cell lines including (a) HepG2; (b) SMMC-7721; and (c) SGC-7901, at given time points: including 12 h Display full size, 24 h Display full size, 48 h Display full size and 72 h (− × −).

Figure 6. IC50 values of various formulations treated by two different mediums on various cell lines, including (a) HepG2; (b) SMMC-7721; and (c) SGC-7901; NCTD (RPMI-1640 10% FBS)

, NCTD (RPMI-1640 10% Gal-FBS)
, Lac-NCTD (RPMI-1640 10% FBS)
, Lac-NCTD (RPMI-1640 10% Gal-FBS)
, Lac-NCTD-NPs (RPMI-1640 10% FBS)
and Lac-NCTD-NPs (RPMI-1640 10% Gal-FBS) (▪).

Figure 6. IC50 values of various formulations treated by two different mediums on various cell lines, including (a) HepG2; (b) SMMC-7721; and (c) SGC-7901; NCTD (RPMI-1640 10% FBS) Display full size, NCTD (RPMI-1640 10% Gal-FBS) Display full size, Lac-NCTD (RPMI-1640 10% FBS) Display full size, Lac-NCTD (RPMI-1640 10% Gal-FBS) Display full size, Lac-NCTD-NPs (RPMI-1640 10% FBS) Display full size and Lac-NCTD-NPs (RPMI-1640 10% Gal-FBS) (▪).

Figure 7. Determination of Lac-NCTD accumulated in SMMC-7721 cells: (a) blank cell homogenate; (b) Lac-NCTD control aliquot reference substance; and (c) cell homogenate sample with Lac-NCTD; 1.Lac-NCTD.

Figure 7. Determination of Lac-NCTD accumulated in SMMC-7721 cells: (a) blank cell homogenate; (b) Lac-NCTD control aliquot reference substance; and (c) cell homogenate sample with Lac-NCTD; 1.Lac-NCTD.

Figure 8. Half-life of Lac-NCTD in RPM-I1640 medium (without cells).

Figure 8. Half-life of Lac-NCTD in RPM-I1640 medium (without cells).

Figure 9. Tumour growth inhibition by various formulations containing the same mole of effective NCTD in H22-bearing mice (n = 10): PhyS

, NCTD
, Lac-NCTD medium dose
and Lac-NCTD-NPs medium dose
.

Figure 9. Tumour growth inhibition by various formulations containing the same mole of effective NCTD in H22-bearing mice (n = 10): PhyS Display full size, NCTD Display full size, Lac-NCTD medium dose Display full size and Lac-NCTD-NPs medium dose Display full size.

Table 1. Organ coefficients of various formulations in H22-bearing mice (n = 10).

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