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AAPS PharmSciTech

, Volume 19, Issue 1, pp 123–133 | Cite as

Anticancer Efficacy of Self-Nanoemulsifying Drug Delivery System of Sunitinib Malate

  • Saad M. AlshahraniEmail author
  • Abdullah S. Alshetaili
  • Ahmed Alalaiwe
  • Bader B. Alsulays
  • Md. Khalid Anwer
  • Ramadan Al-Shdefat
  • Faisal Imam
  • Faiyaz Shakeel
Research Article

Abstract

Sunitinib malate (SM) is reported as a weakly soluble drug in water due to its poor dissolution rate and oral bioavailability. Hence, in the current study, various “self-nanoemulsifying drug delivery systems (SNEDDS)” of SM were prepared, characterized and evaluated for the enhancement of its in vitro dissolution rate and anticancer efficacy. On the basis of solubilization potential of SM in various excipients, “Lauroglycol-90 (oil), Triton-X100 (surfactant) and Transcutol-P (cosurfactant)” were selected for the preparation of SM SNEDDS. SM-loaded SNEDDS were developed by spontaneous emulsification method, characterized and evaluated for “thermodynamic stability, self-nanoemulsification efficiency, droplet size, polydispersity index (PDI), zeta potential (ZP), surface morphology, refractive index (RI), the percent of transmittance (% T) and drug release profile.” In vitro dissolution rate of SM was significantly enhanced from an optimized SNEDDS in comparison with SM suspension. The optimized SNEDDS of SM with droplet size of 42.3 nm, PDI value of 0.174, ZP value of −36.4 mV, RI value of 1.339, % T value of 97.3%, and drug release profile of 95.4% (after 24 h via dialysis membrane) was selected for in vitro anticancer efficacy in human colon cancer cells (HT-29) by MTT assay. MTT assay indicated significant anticancer efficacy of optimized SM SNEDDS against HT-29 cells in comparison with free SM. The results of this study showed the great potential of SNEDDS in the enhancement of in vitro dissolution rate and anticancer efficacy of poorly soluble drug such as SM.

KEY WORDS

anticancer efficacy dissolution droplet size SNEDDS sunitinib malate 

Notes

Acknowledgements

“This project was supported by Deanship of Scientific Research, Prince Sattam Bin Abdulaziz University, Al-Kharj, Saudi Arabia (Project No.5657/03/2016)”.

Compliance with Ethical Standards

Conflict of Interest

The authors declare that they have no conflict of interest.

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Copyright information

© American Association of Pharmaceutical Scientists 2017

Authors and Affiliations

  • Saad M. Alshahrani
    • 1
    Email author
  • Abdullah S. Alshetaili
    • 1
  • Ahmed Alalaiwe
    • 1
  • Bader B. Alsulays
    • 1
  • Md. Khalid Anwer
    • 1
  • Ramadan Al-Shdefat
    • 1
    • 2
  • Faisal Imam
    • 3
  • Faiyaz Shakeel
    • 4
    • 5
  1. 1.Department of Pharmaceutics, College of PharmacyPrince Sattam Bin Abdulaziz UniversityAl-KharjSaudi Arabia
  2. 2.Department of Pharmaceutical Sciences, Faculty of PharmacyJadara UniversityIrbidJordan
  3. 3.Department of Pharmacology and Toxicology, College of PharmacyKing Saud UniversityRiyadhSaudi Arabia
  4. 4.Department of Pharmaceutics, College of PharmacyKing Saud UniversityRiyadhSaudi Arabia
  5. 5.Center of Excellence in Biotechnology Research (CEBR)King Saud UniversityRiyadhSaudi Arabia

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