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Preparation and characterization of lipid emulsions containing styrene maleic acid copolymer for the development of pH-responsive drug carriers.
Chemistry and Physics of Lipids ( IF 3.4 ) Pub Date : 2020-08-20 , DOI: 10.1016/j.chemphyslip.2020.104954
Masafumi Tanaka 1 , Yukimi Fujita 2 , Nao Onishi 2 , Ken-Ichi Ogawara 3 , Hirokazu Nakayama 4 , Takahiro Mukai 2
Affiliation  

Lipid emulsions are potential carriers for poorly water-soluble drugs. Previously, we revealed that lipid nanoparticles complexed with styrene maleic acid copolymer (SMA) disintegrate under acidic pH. In the present study, SMA-containing lipid emulsions (SMA emulsions) were prepared and their physicochemical and biological properties were examined to test whether SMA emulsions could be used as a trigger to facilitate drug release in response to pH reduction. By sonicating lipid and SMA mixtures, homogeneously sized SMA emulsion particles were prepared as verified via dynamic light scattering and transmission electron microscopy. Upon the reduction of solution pH, disintegration of SMA emulsions was observed, which may be utilized for drug release at mildly acidic pH. In addition, the sensitivity to pH changes could be controlled by altering the lipid composition. Serum proteins bound to SMA emulsions were analyzed to predict the metabolic fate upon intravenous injection. Predictably, apolipoproteins were abundantly bound, suggesting that SMA emulsions should avoid being recognized as foreign substances. Furthermore, subcellular distribution studies using a human breast cancer cell line (MDA-MB-231) demonstrated that SMA emulsions localize to lysosomes, which have a lower pH. These results suggest that SMA emulsions could be promising pH-responsive drug carriers.



中文翻译:

包含苯乙烯马来酸共聚物的脂质乳液的制备和表征,用于开发对pH敏感的药物载体。

脂质乳液是水溶性差的药物的潜在载体。以前,我们发现脂质纳米颗粒与苯乙烯马来酸共聚物(SMA)络合在酸性pH下会崩解。在本研究中,制备了含SMA的脂质乳剂(SMA乳剂),并对其理化和生物学特性进行了测试,以测试SMA乳剂是否可以用作引发剂以响应pH降低而释放药物。通过超声处理脂质和SMA混合物,制备了均一大小的SMA乳液颗粒,通过动态光散射和透射电子显微镜进行了验证。在溶液pH降低时,观察到SMA乳液的崩解,其可用于在弱酸性pH下释放药物。此外,通过改变脂质组成可以控制对pH变化的敏感性。分析与SMA乳剂结合的血清蛋白,以预测静脉注射后的代谢命运。可以预见,载脂蛋白被充分结合,表明SMA乳液应避免被识别为异物。此外,使用人类乳腺癌细胞系(MDA-MB-231)进行的亚细胞分布研究表明,SMA乳剂定位于pH值较低的溶酶体。这些结果表明SMA乳液可能是有希望的pH响应药物载体。此外,使用人类乳腺癌细胞系(MDA-MB-231)进行的亚细胞分布研究表明,SMA乳剂定位于pH值较低的溶酶体。这些结果表明SMA乳液可能是有希望的pH响应药物载体。此外,使用人类乳腺癌细胞系(MDA-MB-231)进行的亚细胞分布研究表明,SMA乳剂定位于pH值较低的溶酶体。这些结果表明SMA乳液可能是有希望的pH响应药物载体。

更新日期:2020-08-26
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