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Research Article

A novel solid self-nanoemulsifying drug delivery system (S-SNEDDS) for improved stability and oral bioavailability of an oily drug, 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol

, , , , , , , , , , & show all
Pages 1018-1025 | Received 30 Apr 2017, Accepted 15 Jun 2017, Published online: 04 Jul 2017

Figures & data

Figure 1. Effect of carriers on the drug solubility: (A) SLS; (B) HPMC. The drug (1 g), various amounts (0.01–2 g) of SLS and/or various amounts (0.01–1 g) of HPMC were dissolved in 60 mL of 10% ethanol solution, respectively, and then spray-dried. Each value represents the mean ± SD (n = 3).

Figure 1. Effect of carriers on the drug solubility: (A) SLS; (B) HPMC. The drug (1 g), various amounts (0.01–2 g) of SLS and/or various amounts (0.01–1 g) of HPMC were dissolved in 60 mL of 10% ethanol solution, respectively, and then spray-dried. Each value represents the mean ± SD (n = 3).

Figure 2. Effect of antioxidants on the stability of drug in 0.1% H2O2 solution at the accelerated conditions of 40 °C for 4 d. Each value represents the mean ± SD (n = 3).

Figure 2. Effect of antioxidants on the stability of drug in 0.1% H2O2 solution at the accelerated conditions of 40 °C for 4 d. Each value represents the mean ± SD (n = 3).

Figure 3. Scanning electron micrographs (A) and PXRD patterns (B): (a) calcium silicate; (b) SLS; (c) HPMC; (d) S-SNEDDS.

Figure 3. Scanning electron micrographs (A) and PXRD patterns (B): (a) calcium silicate; (b) SLS; (c) HPMC; (d) S-SNEDDS.

Figure 4. Dissolution profile of PLAG in distilled water (A), pH 6.8 buffer solution containing 2.5% SLS (B) and stability at 60 °C for 5 d (C) from S-SNEDDS, commercial soft capsule and drug. Each value represents the mean ± SD (n = 6).

Figure 4. Dissolution profile of PLAG in distilled water (A), pH 6.8 buffer solution containing 2.5% SLS (B) and stability at 60 °C for 5 d (C) from S-SNEDDS, commercial soft capsule and drug. Each value represents the mean ± SD (n = 6).

Figure 5. Mean plasma level–time profiles of PLAG after oral administration of S-SNEDDS, commercial soft capsule and drug at a dose equivalent to 200 mg/kg drug in rats. Each value designates the mean ± SD. (n = 8). The S-SNEDDS was composed of PLAG/SLS/HPMC/BHA/calcium silicate at a weight ratio of 1: 0.25: 0.1: 0.0002: 0.5. *p < .05 compared with drug only and commercial soft capsule.

Figure 5. Mean plasma level–time profiles of PLAG after oral administration of S-SNEDDS, commercial soft capsule and drug at a dose equivalent to 200 mg/kg drug in rats. Each value designates the mean ± SD. (n = 8). The S-SNEDDS was composed of PLAG/SLS/HPMC/BHA/calcium silicate at a weight ratio of 1: 0.25: 0.1: 0.0002: 0.5. *p < .05 compared with drug only and commercial soft capsule.

Table 1. Pharmacokinetic parameters.

Supplemental material

IDRD_Choi_et_al_Supplemental_Content.docx

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