期刊
SCIENCE BULLETIN
卷 61, 期 8, 页码 622-631出版社
SCIENCE PRESS
DOI: 10.1007/s11434-016-1046-6
关键词
Drug delivery system; Liposome; Sodium tanshinone II-A sulfonate; BKCa channel; Vasodilatation
资金
- National Natural Science Foundation of China [30670763, 81173661, 31300948]
- Sichuan Technology and Education Committee [2011FZ0106, XYTD201005, 09ZZ010]
Some drugs exert curative effects intracellularly, but their hydrophilic property prohibits the membrane-penetrating process and thus limits the curative efficacies, although this property guarantee their solubility in aqueous phase. An example is sodium tanshinone II-A sulfonate (DS-201), a derivative of Chinese medical herb Danshen (Salvia miltiorrhiza) which is a BKCa channel opener and a vasodilator. This study established and optimized a liposome delivery system which could pack and deliver DS-201 into HEK293 cells transfected with BKCa channels, and DS-201 given this way significantly increased the open probability of BKCa channel from baseline 0.013 +/- 0.004 to 0.036 +/- 0.011 at +40 mV membrane potential (P < 0.05) in single-channel attached study, and also increased the current density from baseline 23.2 +/- 4.4 to 66.0 +/- 15.2 pA/pF at +40 mV membrane potential (P < 0.05), compared with the direct extracellular administration of this drug. Moreover, showing a similar to 60 % inhibition of the PE or PGF2a induced vascular constriction, the DS-201 liposomes did posses significantly enhanced vasorelaxant effect on rat mesenteric artery, compared with similar to 20 % inhibition of the directly administration of this drug (P < 0.05), suggesting that DS-201 delivered by liposomes significantly improved the drug's vasorelaxing effect. Taken together, the optimized DS-201 liposomes in our study successfully delivered DS-201 into cells and thus significantly activated BKCa channels to reverse the contraction induced by PE and PGF2 alpha, attesting the enhanced bioavailability.
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