Sterically stabilized liposomes as a potent carrier for shikonin

被引:24
|
作者
Kontogiannopoulos, K. N. [1 ]
Tsermentseli, S. K. [1 ]
Assimopoulou, A. N. [1 ]
Papageorgiou, V. P. [1 ]
机构
[1] Aristotle Univ Thessaloniki, Dept Chem Engn, Organ Chem Lab, Thessaloniki 54124, Greece
关键词
Alkannin; cancer; quinones; stability study; stealth liposomes; STEALTH LIPOSOMES; ANTITUMOR-ACTIVITY; CIRCULATION TIME; IN-VITRO; PHARMACOKINETICS; DOXORUBICIN; ALKANNINS; RELEASE; ISOHEXENYLNAPHTHAZARINS; POLYMERIZATION;
D O I
10.3109/08982104.2014.891233
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The ability of pegylated liposomes (sterically stabilized liposomes-SSL) to localize in solid tumors via the enhanced permeability and retention (EPR) effect, partly depends on their long circulating properties which can be achieved by grafting polyethylene glycol (PEG) to the liposomes' surface. Alkannin and shikonin (A/S) are naturally occurring hydroxynaphthoquinones with a well-established spectrum of wound healing, antimicrobial, anti-inflammatory, antioxidant, and recently established antitumor activity. The purpose of this work was to prepare and characterize shikonin-loaded pegylated liposomes as a new drug carrier for shikonin, as a continuation of authors' previous work on conventional shikonin-loaded liposomal formulations. Three new pegylated liposomal formulations of shikonin (DSPC-PEG(2000), EPC-PEG(2000), and DPPC-PEG(2000)) were prepared and characterized in terms of physicochemical characteristics, pharmacokinetics, and stability (at 4 degrees C, for 28 d) and compared with the corresponding conventional ones. Particle size distribution, zeta-potential, entrapment efficiency, and release profile of the entrapped drug were measured. Results indicated the successful incorporation of shikonin into liposomes alongside with their good physicochemical characteristics, high entrapment efficiency, satisfactory in vitro release profile, and good physical stability. The results are considered promising and could be used as a road map for designing further in vivo experiments.
引用
收藏
页码:230 / 240
页数:11
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