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AAPS PharmSciTech

, 20:78 | Cite as

Development and Characterization of a Self-Nanoemulsifying Drug Delivery System Comprised of Rice Bran Oil for Poorly Soluble Drugs

  • Georgios K. Eleftheriadis
  • Panagiota Mantelou
  • Christina Karavasili
  • Paschalina Chatzopoulou
  • Dimitrios Katsantonis
  • Maria Irakli
  • Aggeliki Mygdalia
  • Ioannis S. Vizirianakis
  • Dimitrios G. FatourosEmail author
Research Article Theme: Lipid-Based Drug Delivery Strategies for Oral Drug Delivery
Part of the following topical collections:
  1. Theme: Lipid-Based Drug Delivery Strategies for Oral Drug Delivery

Abstract

Poor aqueous solubility and low bioavailability are limiting factors in the oral delivery of lipophilic drugs. In a formulation approach to overcome these limitations, rice bran (RB) oil was evaluated as drug carrier in the development of self-nanoemulsifying drug delivery systems (SNEDDS). The performance of RB in formulations incorporating Kolliphor RH40 or Kolliphor EL as surfactants and Transcutol HP as cosolvent was compared to a common oil vehicle, corn oil (CO). Serial dilutions of the preconcentrates were performed in various media [distilled water and simulated intestinal fluids mimicking fasted state (FaSSIF) and fed state (FeSSIF)] and at different dilution ratios to simulate the in vivo droplets’ behavior. The developed SNEDDS were assessed by means of phase separation, droplet size, polydispersity index, and ζ-potential. Complex ternary diagrams were constructed to identify compositions exhibiting monophasic behavior, droplet size < 100 nm, and polydispersity index (PDI) < 0.25. Multifactor analysis and response surface areas intended to determine the factors significantly affecting droplet size. The oil capacity to accommodate lipophilic drugs was assessed via fluorescence spectroscopy based on the solvatochromic behavior of Nile Red. Solubility studies were performed to prepare fenofibrate- and itraconazole-loaded SNEDDS and assess their droplet size, whereas dissolution experiments were conducted in simulated intestinal fluids. Caco-2 cell viability studies confirmed the safety of the SNEDDS formulations at 1:100 and 1:1000 dilutions after cell exposure in culture for 4 h. The obtained results showed similar performance between RB and CO supporting the potential of RB as oil vehicle for the effective oral delivery of lipophilic compounds.

KEY WORDS

rice bran oil SNEDDS poorly soluble drugs multifactor analysis simulated intestinal fluids 

Notes

Acknowledgements

The current work has received financial support within the project “Sustainable techno-economic solutions for the agricultural value chain” Waste-7-2015 topic H2020 690142 project (AGROCYCLE). Gattefosse (France) and BASF (Germany) are greatly acknowledged for the generously gifted formulation excipients.

Supplementary material

12249_2018_1274_MOESM1_ESM.docx (686 kb)
ESM 1 (DOCX 686 kb)

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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  • Georgios K. Eleftheriadis
    • 1
  • Panagiota Mantelou
    • 1
  • Christina Karavasili
    • 1
  • Paschalina Chatzopoulou
    • 2
  • Dimitrios Katsantonis
    • 3
  • Maria Irakli
    • 2
  • Aggeliki Mygdalia
    • 3
  • Ioannis S. Vizirianakis
    • 4
  • Dimitrios G. Fatouros
    • 1
    Email author
  1. 1.Laboratory of Pharmaceutical Technology, Department of PharmacyAristotle University of ThessalonikiThessalonikiGreece
  2. 2.Hellenic Agricultural Organization DemeterPlant Breeding and Genetic Resources InstituteThessalonikiGreece
  3. 3.Hellenic Agricultural Organization DemeterCereal InstituteThessalonikiGreece
  4. 4.Laboratory of Pharmacology, School of PharmacyAristotle University of Thessaloniki GRThessalonikiGreece

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