Document Detail


Formulation of polyiodinated triglyceride analogues in a chylomicron remnant-like liver-selective delivery vehicle.
MedLine Citation:
PMID:  8792425     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
PURPOSE: A formulation methodology for the incorporation of polyiodinated triglyceride (ITG) analogues into a protein-free chylomicron remnant-like emulsion was developed to provide a vehicle for the selective hepatic delivery of these agents for contrast-enhanced X-ray computed tomography (CECT). METHODS: Triglyceride emulsions (10% w/v) were prepared at various processing pressures, temperatures and times with a Microfluidizer 110-S using different emulsion component proportions to establish processing and compositional parameters in order to afford stable ITG emulsions (ITG-LE) approaching 200 nm mean diameter. RESULTS: Preliminary data indicated that with a formulation composed of 2.4% dioleoyl PC with a cholesterol:DOPC mole ratio of 0.4 emulsified at 14,700 psi, 35 degrees C for 10 min routinely afforded ITG-LE in the desired size range. The elimination of salt and amino acid from the bulk phase enhanced the stability of the ITG-LE. Incorporation of cholesterol into the monolayer was of critical importance in generating a stable emulsion near the targeted size, with a C:DOPC mole ratio of 0.4 producing a size minimum relative to higher or lower C:DOPC values. CONCLUSIONS: The ITG analogues can be readily incorporated into stable remnant-like emulsions of relatively uniform particle size. Combination of the unique ITG contrast agent with the remnant-like delivery vehicle demonstrates a high degree of hepatic selectivity in biodistribution studies and offers significant potential for selective hepatic CECT.
Authors:
M A Longino; D A Bakan; J P Weichert; R E Counsell
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Pharmaceutical research     Volume:  13     ISSN:  0724-8741     ISO Abbreviation:  Pharm. Res.     Publication Date:  1996 Jun 
Date Detail:
Created Date:  1996-12-20     Completed Date:  1996-12-20     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8406521     Medline TA:  Pharm Res     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  875-9     Citation Subset:  IM    
Affiliation:
Department of Radiology, University of Michigan, Ann Arbor 48109-0662, USA.
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MeSH Terms
Descriptor/Qualifier:
Chylomicrons / chemistry*
Contrast Media / administration & dosage,  chemical synthesis*
Drug Compounding
Drug Delivery Systems*
Emulsions
Liver / metabolism*
Particle Size
Surface Properties
Temperature
Triglycerides / administration & dosage,  chemical synthesis*
Chemical
Reg. No./Substance:
0/Chylomicrons; 0/Contrast Media; 0/Emulsions; 0/Triglycerides

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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