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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

Appearance of nanoemulsion formulations following a) 9 months storage at 4 °C, and b,c) 12 months storage at 40 °C
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Figure 8: Appearance of nanoemulsion formulations following a) 9 months storage at 4 °C, and b,c) 12 months storage at 40 °C

Mentions: To evaluate the NEs stability, the droplet size, PDI and drug content were monitored over 9-12 months storage at 4, 25 and 40 °C. As can be observed in Table 5, at 4 and 25 °C, the NEs presented an increase in mean droplet size (still less than 50 nm) which may be attributed to a good particle stabilization. No phase separation or turbidity was observed. The PDI remained relatively unchanged for all formulations. At 40 °C, none of the formulations survived the stability test and turned to two-phase systems (Figure 8). Stability studies with respect to the assay of RAP in NEs kept at 25 °C (for 12 months) and 4 °C (for 9 months) were analyzed individually (Table 5). The minimum percentage of undecomposed RAP remaining in NE formulations was 21% and 81% at 25 °C and 4 °C, respectively.


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)

Appearance of nanoemulsion formulations following a) 9 months storage at 4 °C, and b,c) 12 months storage at 40 °C
© Copyright Policy
Related In: Results  -  Collection

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

Figure 8: Appearance of nanoemulsion formulations following a) 9 months storage at 4 °C, and b,c) 12 months storage at 40 °C
Mentions: To evaluate the NEs stability, the droplet size, PDI and drug content were monitored over 9-12 months storage at 4, 25 and 40 °C. As can be observed in Table 5, at 4 and 25 °C, the NEs presented an increase in mean droplet size (still less than 50 nm) which may be attributed to a good particle stabilization. No phase separation or turbidity was observed. The PDI remained relatively unchanged for all formulations. At 40 °C, none of the formulations survived the stability test and turned to two-phase systems (Figure 8). Stability studies with respect to the assay of RAP in NEs kept at 25 °C (for 12 months) and 4 °C (for 9 months) were analyzed individually (Table 5). The minimum percentage of undecomposed RAP remaining in NE formulations was 21% and 81% at 25 °C and 4 °C, respectively.

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