[Preparation of cardiomyocyte-targeting liposomes and their targeting ability in vitro].
OBJECTIVE
To prepare the cardiomyocyte-targeting liposomes and investigate their cardiomyocyte targetability in vitro.


METHODS
Liposomes modified with compound PAC were prepared (PAC-L); The uptake of PAC-L by cardiomyocytes was studied by incubating fluorescence labeled liposomes with cardiomyocytes in vitro and measuring the association of liposomes by a fluorescence spectrophotometer.


RESULTS
A high affinity of PAC-L to the cardiomyocytes was observed, the amount of cell uptake of PAC-L by cardiomyocytes was higher than that by nonmyocyte (P < 0.001); The amount of cardiomyocyte uptake of PAC-L on the normoxia condition 2 h was 2.9-fold higher than that of plain-L, and the increase was 5.2-fold when hypoxia occured; The form of liposome uptake changed, the amount of cardiomyocyte uptake of Plain-L by internalization was only 11%, while that of PAC-L was 56%.


CONCLUSIONS
It is indicated that PAC-L was a potential drug carrier for targeting to ischemic myocardium.
Chen
Yan
Y
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
Deng
Ying-Jie
YJ
Hao
Yan-Li
YL
Wang
Zhen-Yuan
ZY
Sheng
Jun
J
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000818:Animals; D000831:Animals, Newborn; D015687:Cell Hypoxia; D002478:Cells, Cultured; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005233:Fatty Alcohols / Q000737:chemistry / Q000378:metabolism*; D008081:Liposomes; D051379:Mice; D015394:Molecular Structure; D032383:Myocytes, Cardiac / Q000187:drug effects / Q000378:metabolism*; D011412:Propanolamines / Q000494:pharmacology
C522389:3-(4-(2-hydroxy-(1-methylethylamino)propyl-oxy)phenyl)hexadecanol ester; D000319:Adrenergic beta-Antagonists; D004337:Drug Carriers; D005233:Fatty Alcohols; D008081:Liposomes; D011412:Propanolamines; C036604:esmolol