| Formulation of polyiodinated triglyceride analogues in a chylomicron remnant-like liver-selective delivery vehicle. | |
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MedLine Citation:
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PMID: 8792425 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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M A Longino; D A Bakan; J P Weichert; R E Counsell |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Pharmaceutical research Volume: 13 ISSN: 0724-8741 ISO Abbreviation: Pharm. Res. Publication Date: 1996 Jun |
Date Detail:
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Created Date: 1996-12-20 Completed Date: 1996-12-20 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8406521 Medline TA: Pharm Res Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 875-9 Citation Subset: IM |
Affiliation:
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Department of Radiology, University of Michigan, Ann Arbor 48109-0662, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Chylomicrons
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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:
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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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