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Research Article

Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems: in vitro, in vivo and in situ intestinal permeability studies

, , , , , , , & show all
Pages 740-747 | Received 13 Jan 2014, Accepted 21 Feb 2014, Published online: 27 Mar 2014

Figures & data

Table 1. Blank formulations compatibility test (vehicle compositions for screening SEDDS formulations, with the proportion of oil 30%, surfactant 50%, cosurfactant 20%).

Table 2. Solubility of piperine in various vehicles at 25 °C (n = 3, mean ± SD; mg/ml).

Figure 1. Pseudo-ternary phase diagrams indicating the efficient self-emulsification region with ethyl oleate as oil, Tween 80 as surfactant, and Transcutol P as the cosurfactant, with a drug loading of 2.5%. The solid outline represents the area explored for nano-emulsion region; and the filled squares represent the compositions which were evaluated.

Figure 1. Pseudo-ternary phase diagrams indicating the efficient self-emulsification region with ethyl oleate as oil, Tween 80 as surfactant, and Transcutol P as the cosurfactant, with a drug loading of 2.5%. The solid outline represents the area explored for nano-emulsion region; and the filled squares represent the compositions which were evaluated.

Figure 2. Size distribution of Piperine (Pip) SEDDS in water.

Figure 2. Size distribution of Piperine (Pip) SEDDS in water.

Figure 3. Dissolution profiles of Pip from SEDDS and self-prepared capsule (n = 6).

Figure 3. Dissolution profiles of Pip from SEDDS and self-prepared capsule (n = 6).

Figure 4. Plasma concentration-time profiles of Pip from SEDDS and self-prepared capsule following oral administrations in rats. Each value is mean ± SE (n = 6).

Figure 4. Plasma concentration-time profiles of Pip from SEDDS and self-prepared capsule following oral administrations in rats. Each value is mean ± SE (n = 6).

Table 3. Main pharmacokinetic parameters of piperine after a single oral dose of SEDDS or self-prepared capsules in rats (n = 6, mean ± SE, **p < 0.01; *p < 0.05).

Figure 5. (A) Comparison of Peff and Ka of different concentration perfusion solutions determined by SPIP study in rat duodenum; (B) Effect of different intestine segments on compounds absorption; (C) Effect of adjuvant on absorption parameters of Pip solution. (n = 5, mean ± SD, #p < 0.05, ##p < 0.01 represented for Peff, *p < 0.05, **p < 0.01 represented for Ka).

Figure 5. (A) Comparison of Peff and Ka of different concentration perfusion solutions determined by SPIP study in rat duodenum; (B) Effect of different intestine segments on compounds absorption; (C) Effect of adjuvant on absorption parameters of Pip solution. (n = 5, mean ± SD, #p < 0.05, ##p < 0.01 represented for Peff, *p < 0.05, **p < 0.01 represented for Ka).

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