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Original Research

A novel folate-modified self-microemulsifying drug delivery system of curcumin for colon targeting

, , , , , , , & show all
Pages 151-162 | Published online: 09 Jan 2012

Figures & data

Table 1 Solubility of curcumin in various vehicles

Table 2 Actual and transformed values, mean particle size, and solubility of seven different formulations per Simplex–Lattice design

Figure 1 Ternary phase diagrams studies for selecting of oil, surfactant, and cosurfactant.

Figure 1 Ternary phase diagrams studies for selecting of oil, surfactant, and cosurfactant.

Figure 2 The contour plots of response for the contour plot of mean particle size (A), the contour plot of solubility (B), and the mixed contour plot of mean particle size and solubility (C).

Abbreviations: S, surfactant; CoS, cosurfactant.

Figure 2 The contour plots of response for the contour plot of mean particle size (A), the contour plot of solubility (B), and the mixed contour plot of mean particle size and solubility (C).Abbreviations: S, surfactant; CoS, cosurfactant.

Table 3 The predicted values and the experimental results of the curcumin-loaded self-microemulsifying drug delivery system prepared under the optimum conditions

Figure 3 Transmission electron microscope micrographs of curcumin-loaded self-microemulsifying drug delivery system with the scale bar for the image representing 50 nm.

Figure 3 Transmission electron microscope micrographs of curcumin-loaded self-microemulsifying drug delivery system with the scale bar for the image representing 50 nm.

Table 4 The absorption percentage of curcumin in different formulations with the established in situ colon perfusion method in rats for 6 hours

Table 5 Mean particle size and zeta potential of different self-microemulsifying drug delivery system formulations

Figure 4 Dissolution profiles of curcumin from curcumin-loaded folate-modified self-microemulsifying drug delivery system colon-targeted capsules in stimulated gastrointestinal fluids of different pH at a speed of 50 rpm.

Note: Results are represented by mean ± standard deviation (n = 3).

Figure 4 Dissolution profiles of curcumin from curcumin-loaded folate-modified self-microemulsifying drug delivery system colon-targeted capsules in stimulated gastrointestinal fluids of different pH at a speed of 50 rpm.Note: Results are represented by mean ± standard deviation (n = 3).

Table 6 Cytotoxicities of various curcumin to Hela and HT-29 cells

Figure 5 Fluorescence microscopy images showcasing the time dependent (0.5, 1, 2, 5, and 24 hours) intracellular uptake of Coumarin 6 from Coumarin 6-loaded self-microemulsifying drug delivery system, Coumarin 6-loaded folate-modified self-microemulsifying drug delivery system, and Coumarin 6-loaded folate-modified self-microemulsifying drug delivery system+1mM folic acid by HT-29 (human colon carcinoma cell line) (A) and Hela (human uterine cervix cancer line) cells (B), the concentration of Coumarin 6 is 15 μg/mL.

Abbreviations: FA, folic acid; FSMEDDS, folate-modified self-microemulsifying drug delivery system; h, hours; SMEDDS, self-microemulsifying drug delivery system.

Figure 5 Fluorescence microscopy images showcasing the time dependent (0.5, 1, 2, 5, and 24 hours) intracellular uptake of Coumarin 6 from Coumarin 6-loaded self-microemulsifying drug delivery system, Coumarin 6-loaded folate-modified self-microemulsifying drug delivery system, and Coumarin 6-loaded folate-modified self-microemulsifying drug delivery system+1mM folic acid by HT-29 (human colon carcinoma cell line) (A) and Hela (human uterine cervix cancer line) cells (B), the concentration of Coumarin 6 is 15 μg/mL.Abbreviations: FA, folic acid; FSMEDDS, folate-modified self-microemulsifying drug delivery system; h, hours; SMEDDS, self-microemulsifying drug delivery system.

Figure 6 Flow cytometry results of HT-29 (human colon carcinoma cell line) (A) and Hela (human uterine cervix cancer cell line) (B) cells incubated with Coumarin 6-loaded folate-modified self-microemulsifying drug delivery system + 1 mM folate (black), Coumarin 6-loaded folate-modified self-microemulsifying drug delivery system (green), Coumarin 6-loaded self-microemulsifying drug delivery system (blue) at an equivalent Coumarin 6 concentration of 15 μg/mL for 2 hours at 37°C.

Figure 6 Flow cytometry results of HT-29 (human colon carcinoma cell line) (A) and Hela (human uterine cervix cancer cell line) (B) cells incubated with Coumarin 6-loaded folate-modified self-microemulsifying drug delivery system + 1 mM folate (black), Coumarin 6-loaded folate-modified self-microemulsifying drug delivery system (green), Coumarin 6-loaded self-microemulsifying drug delivery system (blue) at an equivalent Coumarin 6 concentration of 15 μg/mL for 2 hours at 37°C.