Evaluation of Blood Clearance Rates and Biodistribution of Poly(2-oxazoline)-Grafted Liposomes
Two amphipatic polymers of the poly(2-oxazoline) family, poly(2-methyl-2-oxazoline) (PMOZ) and poly(2-ethyl-2-oxazoline) (PEOZ), were synthesized with the carboxylic group positioned at either the initiation or termination ends of the polymer chains. Distearoylphosphatidyletha-nolamine was covalentl...
Saved in:
Published in | Journal of pharmaceutical sciences Vol. 85; no. 2; pp. 133 - 137 |
---|---|
Main Authors | , , , |
Format | Journal Article |
Language | English |
Published |
New York
Elsevier Inc
01.02.1996
John Wiley & Sons, Inc Wiley American Pharmaceutical Association |
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | Two amphipatic polymers of the poly(2-oxazoline) family, poly(2-methyl-2-oxazoline) (PMOZ) and poly(2-ethyl-2-oxazoline) (PEOZ), were synthesized with the carboxylic group positioned at either the initiation or termination ends of the polymer chains. Distearoylphosphatidyletha-nolamine was covalently linked to the carboxyl groups of the polymers, resulting in conjugates which incorporate readily into liposomes. Systematic evaluation of plasma clearance kinetics and biodistribution of liposomes containing hydrogenated soy phosphatidylcholine, cholesterol, and 5 mol % the polymer-lipid conjugates in mice revealed the following. Both polymers, PMOZ and PEOZ, exhibited long plasma lifetimes and low hepatosplenic uptake. PMOZ was more effective at decreasing blood clearance rates than PEOZ. The best results, which were quantitatively comparable to the results obtained with the optimized preparations of methoxypolyethylene glycol(PEG)-2000-grafted liposomes, were obtained with formulations containing PMOZ of molecular weight 3260. |
---|---|
Bibliography: | ArticleID:JPS2 istex:EBC69402084F14DA0F3C8F8EC57AAE2393608821 MPS, mononuclear phagocyte system ; PL, phospho-lipid; POZ, poly(2-oxazoline); PMOZ, poly(2-methyl-2-oxazoline); PEOZ, poly(2-ethyl-2-oxazoline); PEG, polyethylene glycol; mPEG, methoxy-PEG; DSPE, distearoylphosphatidylethanolamine; HSPC, hydrogenated soy phosphatidylcholine; CHOL, cholesterol; DP, dgree of polymerization; TI, tyraminylinulin, GPC, gel permeation chromatography, DMF, N,N′-dimethylformamide. ark:/67375/WNG-WX8DV123-1 MPS, mononuclear phagocyte system ; PL, phospho‐lipid; POZ, poly(2‐oxazoline); PMOZ, poly(2‐methyl‐2‐oxazoline); PEOZ, poly(2‐ethyl‐2‐oxazoline); PEG, polyethylene glycol; mPEG, methoxy‐PEG; DSPE, distearoylphosphatidylethanolamine; HSPC, hydrogenated soy phosphatidylcholine; CHOL, cholesterol; DP, dgree of polymerization; TI, tyraminylinulin, GPC, gel permeation chromatography, DMF , dimethylformamide. N ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0022-3549 1520-6017 |
DOI: | 10.1021/js9504043 |