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Enzymatic synthesis and in vitro evaluation of folate-functionalized liposomes

机译:叶酸官能化脂质体的酶促合成及体外评价

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In this study, folate–poly(ethylene glycol)3400–cholesterol conjugates (FA–PEG–Chol) were enzymatically synthesized in one step and incorporated into liposomes to prepare folate (FA)-functionalized liposomes for targeted drug delivery. The FA-functionalized liposomes loaded with betulinic acid (BA) (FA-L-BA) were prepared by thin lipid film method. The FA-L-BA was characterized by their morphology, particle size, zeta potential, encapsulation efficiency (EE), stability, cell cytotoxicity and cellular uptake. The average size of FA-L-BA was 222±8?nm. The spherical particles exhibited a negative electrical charge of -20.12±1.45 mV and high EE of 91.61%±1.16%. The liposomes were taken up selectively by HepG2 cells. FA-L-BA showed enhanced cytotoxicity (50% inhibitory concentration [IC50] =63.07±2.22 μg/mL) compared to nontargeted control normal liposomes loaded with BA (L-BA; IC50 =93.14±2.19 μg/mL) in HepG2 cells in vitro. In?addition, FA-functionalized liposomes loaded with Ir-1 (FA-L-Ir-1) showed significantly higher cellular uptake in HepG2 cells compared to nontargeted control normal liposomes loaded with Ir-1 (L-Ir-1). This novel approach for the liposomes surface modified with FA by a one-step?enzymatic?amidation was expected to provide potential application as a drug carrier for active targeted delivery to tumor cells.
机译:在这项研究中,叶酸-聚(乙二醇) 3400 -胆固醇共轭物(FA-PEG-Chol)一步一步酶法合成,并掺入脂质体中,以制备叶酸(FA)功能化的脂质体药物输送。通过薄脂膜法制备负载有桦木酸(BA)(FA-L-BA)的FA功能化脂质体。 FA-L-BA的特征是其形态,粒径,ζ电势,包封效率(EE),稳定性,细胞细胞毒性和细胞摄取。 FA-L-BA的平均尺寸为222±8μm。球形颗粒的负电荷为-20.12±1.45 mV,高EE为91.61%±1.16%。脂质体被HepG2细胞选择性吸收。与装载BA的非靶向对照正常脂质体(L-BA; IC )相比,FA-L-BA具有增强的细胞毒性(50%抑制浓度[IC 50 ] = 63.07±2.22μg/ mL)。 50 = 93.14±2.19μg/ mL)。此外,与未装载Ir-1(L-Ir-1)的非靶向正常对照脂质体相比,装载有Ir-1(FA-L-Ir-1)的FA功能化脂质体在HepG2细胞中显示出更高的细胞摄取。预期这种通过一步酶酰胺化用FA表面修饰的脂质体的新方法有望作为药物载体用于主动靶向递送至肿瘤细胞。

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