[Bone-targeted ultradeformable nanoliposomes].
OBJECTIVE
To study the change in vivo distribution change of ultradeformable nanoliposomes (UL) after being modified by poloxamer 407 (P407), Ethylenediaminetetramethylene phosphonic acid (EDTMP) and 1,12-dodecanediaminetetramethylene phosphonic acid (12-DTMP).


METHODS
Pyrene was selected as a model drug. Normal ultradeformable nano-liposomes (N-UL), the ultradeformable nano-liposomes modified by P407 (P-UL), that modified by EDTMP (E-UL) and that modified by 12-DTMP (12-UL) were prepared by the modified dry film ultrasonic method. The biodistributions of pyrene in the four different ULs were studied by fluorescence method.


RESULTS
The encapsulation efficiencies of the three ULs were all over 80%. Compared with N-UL, the peak concentration (c(max)) of pyrene in P-UL, E-UL and 12-UL in bone were increased to 1.51, 1.10 and 1.66 times, the areas under curve (AUC) were increased to 1.83, 1.76 and 3.81 times, the drug targeting efficiencies (DTE) were increase by 277.94%, 203.12% and 653.02%, respectively.


CONCLUSIONS
P-UL, 12-UL and E-UL all showed the ability of targeting at bone, and E-UL reached the significantest targeting effect of the three.
Department of Pharmaceutics, Peking University School of Pharmaceutical Sciences, Beijing 100191, China.
Jia
J
Guo
Miao
M
Zhang
Yun-feng
YF
Li
Peng
P
Zhen
Xin
X
Hu
D001842:Bone and Bones / Q000378:metabolism*; D017886:Durapatite / Q000378:metabolism*; D005029:Ethylenediamines / Q000737:chemistry; D006801:Humans; D008081:Liposomes / Q000737:chemistry* / Q000493:pharmacokinetics; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D063065:Organophosphonates / Q000737:chemistry; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry
D005029:Ethylenediamines; D008081:Liposomes; D063065:Organophosphonates; C418473:ethylenediaminetetrakis(methylphosphonic) acid; D020442:Poloxamer; D017886:Durapatite