Abstract：
:This study was aimed at developing a liposome delivery system for a new and potential antitumor lipophilic prodrug of 5-fluorouracil (5-Fu)-N(3)-O-toluyl-fluorouracil (TFu), intended to improve the bioavailability and therapeutic efficacy of 5-Fu by oral and intravenous administration. TFu-loaded liposomes were prepared by a modified film dispersion-homogenization technique, the formulation and manufacture parameters were optimized concerning the drug encapsulation efficiency. TFu-loaded liposomes were characterized according to particle size, size distribution, zeta potential, drug entrapment efficiency, drug loading and physical stability, respectively. In vitro release characteristics, in vivo pharmacokinetic properties and bioavailabilities were also investigated. The formulated liposomes were found to be relatively uniform in size (400.5 +/- 9.6 nm) with a negative zeta potential (-6.4 +/- 0.8 mV). The drug entrapment efficiency and loading were (88.87 +/- 3.25%) and (8.89 +/- 0.19%), respectively. The physical stability experiments results indicated that lyophilized TFu-loaded liposomes were stable for at least 9 months at 4 degrees C. In vitro drug release profile of TFu-loaded liposomes followed the bi-exponential equation. The results of the pharmacokinetic studies in mice indicated that the bioavailability of TFu-loaded liposomes was higher than the suspension after oral administration, and was bioequivalent comparing with TFu 50% alcohol solution after intravenous (i.v.) administration. These results indicated that TFu-loaded liposomes were valued to develop as a practical preparation for oral or i.v. administration.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Sun W,Zhang N,Li A,Zou W,Xu Wdoi
10.1016/j.ijpharm.2007.11.017subject
Has Abstractpub_date
2008-04-02 00:00:00pages
243-50issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(07)00946-5journal_volume
353pub_type
杂志文章abstract：:A substantial drug release from poly(lactic-co-glycolic) acid (PLGA) micro- and nanoparticles can occur in the first hours of immersion, which is referred to as burst release. A strong burst release (when not intentional) is to be avoided as it decreases the efficacy of the treatment and could be dangerous to the host...
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abstract：:Conventional lipid microspheres (LM) were prepared using soybean oil and lipid at a 5.5:1 weight ratio with lipid phase consisting of PC (phosphatidyl choline):CH (cholesterol) (1:0.5) by molar ratio. The average diameter of the particles was 150 nm. Long-circulating microspheres (S-LM) were also prepared similarly bu...
journal_title：International journal of pharmaceutics
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abstract：:Thermal isoeffect dose (TID) is a widely applied concept to evaluate the safety of medical devices that can expose patients to heat. However, it has rarely been used in photothermal therapy (PTT), where nanoparticles are used as light absorbers. Utilizing TID in an appropriate way would make it feasible to compare the...
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
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更新日期：2004-08-20 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.01.046
更新日期：2008-06-05 00:00:00
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journal_title：International journal of pharmaceutics
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更新日期：2013-06-25 00:00:00
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journal_title：International journal of pharmaceutics
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更新日期：2013-08-16 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2019-02-25 00:00:00
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journal_title：International journal of pharmaceutics
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更新日期：2010-03-15 00:00:00
