Rapamycin-Loaded, Capryol<sup>TM</sup> 90 and Oleic Acid Mediated Nanoemulsions: Formulation Development, Characterization and Toxicity Assessment
| Author | Hamideh Sobhani | en |
| Author | Parastoo Tarighi | en |
| Author | Seyed Nasser Ostad | en |
| Author | Alireza Shafaati | en |
| Author | Nastaran Nafissi-Varcheh | en |
| Author | Reza Aboofazeli | en |
| Issued Date | 2018-07-31 | en |
| Abstract | This study was planned to explore the capability of nanoemulsions (NEs) consisting of CapryolTM 90 and oleic acid for the delivery of rapamycin (RAP). Permeability and cytotoxicity of RAP-loaded NEs were also inspected. Pseudo-ternary phase diagrams were created with oleic acid and CapryolTM 90 (as oil phase) and four surfactants and co-surfactants at various weight ratios (Rsm). Selected NEs from O/W region on the phase diagrams with the drug concentration of 1 mg/mL, were prepared via the spontaneous emulsification technique, characterized for particle size and subjected to stability tests at various temperatures over 9-12 months. Cumulative drug release was determined for a period of 48 h using a dialysis sac. The assay of RAP was determined using HPLC technique. Cytotoxicity of NEs was evaluated by MTT assay on breast cancer cell line, namely SKBR-3. The permeability of RAP-loaded NEs across Caco-2 monolayers was assessed by measurement of TEER (transepithelial electrical resistance) value. The intracellular uptake of coumarin 6-loaded NEs by SKBR-3 cells was also investigated using florescence microscopy. NEs containing oleic acid/Tween 20/propylene glycol, CapryolTM 90/Tween 20/iso-propanol, and CapryolTM 90/Cremophor® RH40/Transcutol® P showed more cytotoxicity and permeability compared with the RAP methanolic solution. The minimum toxic concentration of RAP in NE formulations was found to be 7.5 µg/mL. The highest intracellular uptake was observed for the NE composed of CapryolTM 90/Tween 20/iso-propanol which was in consistent with the results obtained from cytotoxicity and permeability tests. The overall results implicated that this novel carrier was effective for enhancing RAP permeation in Caco-2 cell membrane along with enhancement of cytotoxicity. | en |
| DOI | https://doi.org/10.22037/ijpr.2018.2274 | en |
| URI | https://brieflands.com/journals/ijpr/articles/124785 | en |
| Keyword | Rapamycin | en |
| Keyword | Nanoemulsion | en |
| Keyword | Phase diagram | en |
| Keyword | MTT | en |
| Keyword | TEER | en |
| Publisher | Brieflands | en |
| Title | Rapamycin-Loaded, Capryol<sup>TM</sup> 90 and Oleic Acid Mediated Nanoemulsions: Formulation Development, Characterization and Toxicity Assessment | en |
| Type | Original Article | en |
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