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Pharmaceutical Research

, Volume 31, Issue 8, pp 2022–2034 | Cite as

Computed Tomography-Guided Screening of Surfactant Effect on Blood Circulation Time of Emulsions: Application to the Design of an Emulsion Formulation for Paclitaxel

  • Eun-Hye Lee
  • Soon-Seok Hong
  • So Hee Kim
  • Mi-Kyung Lee
  • Joon Seok Lim
  • Soo-Jeong Lim
Research Paper

ABSTRACT

Purpose

In an effort to apply the imaging techniques currently used in disease diagnosis for monitoring the pharmacokinetics and biodisposition of particulate drug carriers, we sought to use computed tomography (CT) scanning methodology to investigate the impact of surfactant on the blood residence time of emulsions.

Methods

We prepared the iodinated oil Lipiodol emulsions with different compositions of surfactants and investigated the impact of surfactant on the blood residence time of emulsions by CT scanning.

Results

The blood circulation time of emulsions was prolonged by including Tween 80 or DSPE-PEG (polyethylene glycol 2000) in emulsions. Tween 80 was less effective than DSPE-PEG in terms of prolongation effect, but the blood circulating time of emulsions was prolonged in a Tween 80 content-dependent manner. As a proof-of-concept demonstration of the usefulness of CT-guided screening in the process of formulating drugs that need to be loaded in emulsions, paclitaxel was loaded in emulsions prepared with 87 or 65% Tween 80–containing surfactant mixtures. A pharmacokinetics study showed that paclitaxel loaded in 87% Tween 80 emulsions circulated longer in the bloodstream compared to those in 65% Tween 80 emulsions, as predicted by CT imaging.

Conclusions

CT-visible, Lipiodol emulsions enabled the simple evaluation of surfactant composition effects on the biodisposition of emulsions.

KEY WORDS

lipiodol emulsion pharmacokinetics computed tomography paclitaxel 

Notes

ACKNOWLEDGMENTS AND DISCLOSURES

This study was supported by grants from the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (Nos. 2010-0008838, 2012R1A2A2A01046171).

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Copyright information

© Springer Science+Business Media New York 2014

Authors and Affiliations

  1. 1.Department of Bioscience and BioengineeringSejong UniversitySeoulRepublic of Korea
  2. 2.College of Pharmacy Research Institute of Pharmaceutical Science and TechnologyAjou UniversitySuwonRepublic of Korea
  3. 3.College of PharmacyWoosuk UniversityWanju-gunRepublic of Korea
  4. 4.Department of RadiologyYonsei University Health SystemSeoulRepublic of Korea

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