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Articles

Hydrophilically modified self-assembling α-tocopherol derivative as niosomal nanocarrier for improving clarithromycin oral bioavailability

, , , , , , & show all
Pages 568-578 | Received 02 Dec 2016, Accepted 16 May 2017, Published online: 25 May 2017

Figures & data

Figure 1. Synthesis scheme of hydrophilically modified α-tocopherol product “E1CLK”.

Figure 1. Synthesis scheme of hydrophilically modified α-tocopherol product “E1CLK”.

Figure 2. EI-MS mass spectra of synthesized amphiphilic carrier E1CLK.

Figure 2. EI-MS mass spectra of synthesized amphiphilic carrier E1CLK.

Figure 3. 1H NMR spectra of synthesized amphiphilic carrier (E1CLK).

Figure 3. 1H NMR spectra of synthesized amphiphilic carrier (E1CLK).

Figure 4. AFM images of clarithromycin-loaded E1CLK-based niosomal vesicles.

Figure 4. AFM images of clarithromycin-loaded E1CLK-based niosomal vesicles.

Table 1. Characterization of E1CLK-based niosomal formulation (composition, particle size, PD, EE% and zeta potential).

Figure 5. In-vitro release study of drug-loaded E1CLK niosomal vesicles at pH 7.4, 4.0 and 2.0 (n = 3, mean ± SEM).

Figure 5. In-vitro release study of drug-loaded E1CLK niosomal vesicles at pH 7.4, 4.0 and 2.0 (n = 3, mean ± SEM).

Figure 6. In-vitro haemolysis study of synthesized amphiphilic carrier (E1CLK) at different concentrations (n = 3, mean ± SEM).

Figure 6. In-vitro haemolysis study of synthesized amphiphilic carrier (E1CLK) at different concentrations (n = 3, mean ± SEM).

Figure 7. Cell cytotoxicity study of synthesized surfactant (E1CLK), where (A) and (B) show percent cell viability against NIH/3T3 cell line after 24 and 48 h, respectively, while (C) and (D) show percent cell viability against HeLa cell line after 24 and 48 h, respectively. (n = 3, mean ± SEM). Poly-L-lysine and Tween 80 are used as reference standard and positive control, respectively.

Figure 7. Cell cytotoxicity study of synthesized surfactant (E1CLK), where (A) and (B) show percent cell viability against NIH/3T3 cell line after 24 and 48 h, respectively, while (C) and (D) show percent cell viability against HeLa cell line after 24 and 48 h, respectively. (n = 3, mean ± SEM). Poly-L-lysine and Tween 80 are used as reference standard and positive control, respectively.

Table 2. In-vivo acute toxicity of E1CLK in mice.

Figure 8. Plasma drug concentration of clarithromycin when given orally as E1CLK niosomal formulation, commercial suspension and tablets at 15 mg/kg body weight dose (n = 6, mean ± SE).

Figure 8. Plasma drug concentration of clarithromycin when given orally as E1CLK niosomal formulation, commercial suspension and tablets at 15 mg/kg body weight dose (n = 6, mean ± SE).

Table 3. In-vivo oral pharmacokinetics of clarithromycin when administered as E1CLK-based niosomal formulation, commercial suspension and tablets.

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