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Formulation Development and Toxicity Assessment of Triacetin Mediated Nanoemulsions as Novel Delivery Systems for Rapamycin.

Sobhani H, Tarighi P, Ostad SN, Shafaati A, Nafissi-Varcheh N, Aboofazeli R - Iran J Pharm Res (2015)

Bottom Line: Maximum drug release was observed in case of 4 formulations prepared with Tween 80 and Tween 20.MTT test results revealed different toxicity of NEs for SKBR-3 cell line and TEER demonstrated that formulations containing Tween 20 caused a more considerable decrease in cell integrity in comparison with those prepared with Tween 80.The results obtained from cellular uptake experiments were in consistent with those obtained from TEER and cytotoxicity experiments.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

ABSTRACT
The aim of this investigation was to design and develop nanoemulsions (NEs) as novel delivery systems for rapamycin. Phase behavior of quaternary systems composed of Traicetin (as oil), various surfactants and co-surfactants and water at different surfactant/co-surfactant weight ratios was investigated by the construction of phase diagrams. Formulations were taken from the o/w NE region of the phase diagrams, depending upon the extent of NE domain. The spontaneous emulsification method was used to prepare various formulations containing 1 mg/mL of the drug. The NEs were characterized and subjected to stability tests at various temperatures over 9-12 months. Cumulative drug release from the selected formulations was determined for a period of 48 h using a dialysis sac. The assay of rapamycin was carried out using an HPLC technique. The effect of NEs on the viability of SKBR-3 cells was evaluated by MTT assay. The integrity of Caco-2 cell monolayers was measured by Transepithelial Electrical Resistance (TEER) and the transport of rapamycin-loaded NEs across Caco-2 cell monolayers was then assessed. The uptake of NEs by SKBR-3 cells was also investigated using florescence microscopy. Maximum drug release was observed in case of 4 formulations prepared with Tween 80 and Tween 20. MTT test results revealed different toxicity of NEs for SKBR-3 cell line and TEER demonstrated that formulations containing Tween 20 caused a more considerable decrease in cell integrity in comparison with those prepared with Tween 80. The results obtained from cellular uptake experiments were in consistent with those obtained from TEER and cytotoxicity experiments.

No MeSH data available.


Related in: MedlinePlus

Transmission electron microscopy image of a rapamycin containing nanoemulsion
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Figure 5: Transmission electron microscopy image of a rapamycin containing nanoemulsion

Mentions: The droplet size in NEs must be in a nanometer range. In this study, the particle size of the selected drug-loaded NEs was measured using photon correlation spectroscopy to confirm the formation of nanoparticles. In addition, PDI was also determined to provide information about the deviation from the average size. Table 2 depicts the droplet size and PDI values of the selected formulations. It was observed that in all cases, the average size of the emulsions was less than 50 nm. As indicated in Table 2, formulation F6 containing Tween 20/Transcutol at the Rsm of 2:1 yielded a nanoparticle diameter of 13.68 nm with a PDI of 0.434, whereas F39 containing Labrasol/iso-propanol at the Rsm of 2:1 showed a nanoparticle diameter of 47.17 with a PDI of 0.152 which suggests the uniformity of droplet size (47.17 nm) in the formulation. The result of transmission electron microscopy can be observed in Figure 5 which reveals that the lipid emulsion droplets are almost spherical and that the droplet is in the nanometer range.


Formulation Development and Toxicity Assessment of Triacetin Mediated Nanoemulsions as Novel Delivery Systems for Rapamycin.

Sobhani H, Tarighi P, Ostad SN, Shafaati A, Nafissi-Varcheh N, Aboofazeli R - Iran J Pharm Res (2015)

Transmission electron microscopy image of a rapamycin containing nanoemulsion
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4499422&req=5

Figure 5: Transmission electron microscopy image of a rapamycin containing nanoemulsion
Mentions: The droplet size in NEs must be in a nanometer range. In this study, the particle size of the selected drug-loaded NEs was measured using photon correlation spectroscopy to confirm the formation of nanoparticles. In addition, PDI was also determined to provide information about the deviation from the average size. Table 2 depicts the droplet size and PDI values of the selected formulations. It was observed that in all cases, the average size of the emulsions was less than 50 nm. As indicated in Table 2, formulation F6 containing Tween 20/Transcutol at the Rsm of 2:1 yielded a nanoparticle diameter of 13.68 nm with a PDI of 0.434, whereas F39 containing Labrasol/iso-propanol at the Rsm of 2:1 showed a nanoparticle diameter of 47.17 with a PDI of 0.152 which suggests the uniformity of droplet size (47.17 nm) in the formulation. The result of transmission electron microscopy can be observed in Figure 5 which reveals that the lipid emulsion droplets are almost spherical and that the droplet is in the nanometer range.

Bottom Line: Maximum drug release was observed in case of 4 formulations prepared with Tween 80 and Tween 20.MTT test results revealed different toxicity of NEs for SKBR-3 cell line and TEER demonstrated that formulations containing Tween 20 caused a more considerable decrease in cell integrity in comparison with those prepared with Tween 80.The results obtained from cellular uptake experiments were in consistent with those obtained from TEER and cytotoxicity experiments.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

ABSTRACT
The aim of this investigation was to design and develop nanoemulsions (NEs) as novel delivery systems for rapamycin. Phase behavior of quaternary systems composed of Traicetin (as oil), various surfactants and co-surfactants and water at different surfactant/co-surfactant weight ratios was investigated by the construction of phase diagrams. Formulations were taken from the o/w NE region of the phase diagrams, depending upon the extent of NE domain. The spontaneous emulsification method was used to prepare various formulations containing 1 mg/mL of the drug. The NEs were characterized and subjected to stability tests at various temperatures over 9-12 months. Cumulative drug release from the selected formulations was determined for a period of 48 h using a dialysis sac. The assay of rapamycin was carried out using an HPLC technique. The effect of NEs on the viability of SKBR-3 cells was evaluated by MTT assay. The integrity of Caco-2 cell monolayers was measured by Transepithelial Electrical Resistance (TEER) and the transport of rapamycin-loaded NEs across Caco-2 cell monolayers was then assessed. The uptake of NEs by SKBR-3 cells was also investigated using florescence microscopy. Maximum drug release was observed in case of 4 formulations prepared with Tween 80 and Tween 20. MTT test results revealed different toxicity of NEs for SKBR-3 cell line and TEER demonstrated that formulations containing Tween 20 caused a more considerable decrease in cell integrity in comparison with those prepared with Tween 80. The results obtained from cellular uptake experiments were in consistent with those obtained from TEER and cytotoxicity experiments.

No MeSH data available.


Related in: MedlinePlus