【摘要】：本文擬構(gòu)建整合素配體c RGDyk修飾的三甲基殼聚糖納米給藥系統(tǒng),以期提高胰島素的口服生物利用度。采用單因素篩選法對(duì)其處方進(jìn)行優(yōu)化,篩選最優(yōu)處方制得非配體修飾納米粒(TMC NPs)和配體修飾納米粒(C-TMC NPs),粒徑分別為(240.3±4.2)和(259.5±3.3)nm;電位分別為(33.5±0.8)和(25.7±1.6)m V;包封率分別為(76.0±2.2)%和(74.4±2.0)%;載藥量分別為(50.1±2.1)%和(26.1±1.0)%。以Caco-2細(xì)胞為模型,考察了TMC NPs和C-TMC NPs的細(xì)胞攝取、跨膜及相關(guān)轉(zhuǎn)運(yùn)機(jī)制。C-TMC NPs的攝取及藥物累計(jì)透過量較TMC NPs分別提高了1.98倍和2.84倍。研究發(fā)現(xiàn),TMC NPs和C-TMC NPs的細(xì)胞攝取均由網(wǎng)格蛋白、小窩蛋白介導(dǎo)的主動(dòng)轉(zhuǎn)運(yùn)及大胞飲參與,且游離的c RGDyk可顯著抑制C-TMC NPs的細(xì)胞攝取。
[Abstract]:In order to improve the oral bioavailability of insulin, a trimethyl chitosan nano-delivery system modified with c RGDyk integrin ligands was constructed in this paper. The single factor screening method was used to optimize the formulation of (TMC NPs) and ligand modified nanoparticles (C-TMC NPs), = (240.3 鹵4. 2) and (259.5 鹵3. 3) nm;, respectively). The potential was (33.5 鹵0.8) and (25.7 鹵1.6) m V; entrapment efficiency was (76.0 鹵2.2)% and (74.4 鹵2.0)%, the drug loading was (50.1 鹵2.1)% and (26.1 鹵1.0)%, respectively. The cellular uptake, transmembrane and related transport mechanisms of TMC NPs and C-TMC NPs were investigated using Caco-2 cells as a model. The uptake of C-TMC NPs and the cumulative drug transmittance of C-TMC NPs were 1.98 and 2.84 times higher than those of TMC NPs, respectively. It was found that the cellular uptake of both, TMC NPs and C-TMC NPs was mediated by grid protein, fossa protein mediated active transport and large cell drink, and free c RGDyk could significantly inhibit the cellular uptake of C-TMC NPs.
【作者單位】： 四川大學(xué)華西藥學(xué)院;
【基金】：國家自然科學(xué)基金資助項(xiàng)目(81173010)
【分類號(hào)】：R96

【共引文獻(xiàn)】

相關(guān)期刊論文 前10條

1 Bahman Rahimi-Esboei;Mahdi Fakhar;Aroona Chabra;Mahboobeh Hosseini;;In vitro treatments of Echinococcus granulosus with fungal chitosan,as a novel biomolecule[J];Asian Pacific Journal of Tropical Biomedicine;2013年10期

2 鐘萌;楊林;楊梅;胡雪原;張景R，

本文編號(hào)：2409296