چکیده (انگلیسی):

Various biotin-modified liposomes incorporated with docetaxel (DTX) were prepared to study
the effect of surface biotin density on the pharmacokinetic profile of the liposome. Four types
of liposomes such as PEG modified liposome (PDL), 0.5% (mol) biotin modified liposome
(0.5BDL), 1% (mol) biotin modified liposome (1BDL) and 2% (mol) biotin modified liposome
(2BDL) were prepared using thin film dispersion method.The prepared liposomes were characterized
by measuring encapsulation efficiency (EE), particle size, Zeta-potential, physical
stability and drug release profiles in vitro. MTT assay was performed to elevate the cytotoxicity
of liposomes on MCF-7 cells. In vivo evaluation was further performed to investigate
the effect of biotin surface density on the pharmacokinetic profiles. All the prepared liposomes
exhibited high encapsulation efficiency, small particle size, narrow particle distribution
and sustained release profiles in vitro. In MTT assay, 0.5BDL showed largest tumor cell toxicity,
compared with DTX solution. All liposomes containing DTX showed prolonged blood
circulation in vivo, and 0.5BDL showed the longest circulation time among the biotin modified
liposome. Surface modification of liposome had a negative impact on the circulation
of liposomes in the blood, which needs to be considered when designing the ligand mediated
targeting delivery systems. A proper amount of biotin liposome with 0.5% molar ratio
is expected to produce the best anti-tumor effect.