Rapamycin-Loaded, CapryolTM 90 and Oleic Acid Mediated Nanoemulsions: Formulation Development, Characterization and Toxicity Assessment

Authors

  • Alireza Shafaati Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
  • Hamideh Sobhani Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
  • Nastaran Nafissi-Varcheh Department of Pharmaceutical Biotechnology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
  • Parastoo Tarighi Department of Medical Biotechnology, Faculty of Allied Medicine, Iran University of Medical Sciences, Tehran, Iran.
  • Reza Aboofazeli Department of Pharmaceutics, School of Pharmacy and Protein Technology Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
  • Seyed Naser Ostad Department of Pharmacology and Toxicology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
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/CremophorÒ RH40/TranscutolÒP 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.

Upgrade to premium to download articles

Sign up to access the full text

Already have an account?login

similar resources

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

The aim of this investigation was to design and develop nanoemulsions 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 were investigated by the construction of phase diagrams. Formulations were taken from the o/w NE region of the phase...

full text

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

The aim of this investigation was to design and develop nanoemulsions 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 were investigated by the construction of phase diagrams. Formulations were taken from the o/w NE region of the phase...

full text

formulation development and toxicity assessment of triacetin mediated nanoemulsions as novel delivery systems for rapamycin

the aim of this investigation was to design and develop nanoemulsions 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 were investigated by the construction of phase diagrams. formulations were taken from the o/w ne region of the phase...

full text

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

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 ...

full text

preparation and characterization of rapamycin-loaded nanoemulsions as an approach for increasing anti-proliferative activity. i. phase behavior study

full text

My Resources

Save resource for easier access later

Save to my library Already added to my library

{@ msg_add @}


Journal title

volume 17  issue 3

pages  830- 850

publication date 2018-07-01

{@ msg @}

By following a journal you will be notified via email when a new issue of this journal is published.

Keywords

Hosted on Doprax cloud platform doprax.com

copyright © 2015-2023