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Title: Optimization of Doxorubicin Loading for Superabsorbent Polymer Microspheres: in vitro Analysis

Journal Article · · Cardiovascular and Interventional Radiology
 [1];  [2];  [3]; ;  [4];  [5]
  1. University Hospital Basel, Institute of Radiology (Switzerland)
  2. Vancouver General Hospital, University of British Columbia, Hepatobiliary Section, Department of Surgery (Canada)
  3. University of California Los Angeles, Angio/Interventional Section, UCLA Department of Radiological Sciences, David Geffen School of Medicine (United States)
  4. Vancouver General Hospital, University of British Columbia, Department of Radiology (Canada)
  5. British Columbia Institute of Technology, School of Health Sciences (Canada)

Purpose: This study was designed to establish the ability of super-absorbent polymer microspheres (SAP) to actively uptake doxorubicin and to establish the proof of principle of SAP's ability to phase transfer doxorubicin onto the polymer matrix and to elute into buffer with a loading method that optimizes physical handling and elution characteristics. Methods: Phase I: 50-100 {mu}m SAP subject to various prehydration methods (normal saline 10 cc, hypertonic saline 4 cc, iodinated contrast 10 cc) or left in their dry state, and combined with 50 mg of clinical grade lyophilized doxorubicin reconstituted with various methods (normal saline 10 cc and 25 cc, sterile water 4 cc, iodinated contrast 5 cc) were placed in buffer and assessed based on loading, handling, and elution utilizing high-performance liquid chromatography (HPLC). Phase II: top two performing methods were subject to loading of doxorubicin (50, 75, 100 mg) in a single bolus (group A) or as a serial loading method (group B) followed by measurement of loading vs. time and elution vs. time. Results: Phase I revealed the most effective loading mechanisms and easiest handling to be dry (group A) vs. normal saline prehydrated (group B) SAP with normal saline reconstituted doxorubicin (10 mg/mL) with loading efficiencies of 83.1% and 88.4%. Phase II results revealed unstable behavior of SAP with 100 mg of doxorubicin and similar loading/elution profiles of dry and prehydrated SAP, with superior handling characteristics of group B SAP at 50 and 75 mg. Conclusions: SAP demonstrates the ability to load and bulk phase transfer doxorubicin at 50 and 75 mg with ease of handling and optimal efficiency through dry loading of SAP.

OSTI ID:
21608564
Journal Information:
Cardiovascular and Interventional Radiology, Vol. 35, Issue 2; Other Information: DOI: 10.1007/s00270-011-0168-0; Copyright (c) 2012 Springer Science+Business Media, LLC and the Cardiovascular and Interventional Radiological Society of Europe (CIRSE); Country of input: International Atomic Energy Agency (IAEA); ISSN 0174-1551
Country of Publication:
United States
Language:
English