本文選題：香豆素- + 納米脂質(zhì)載體�。� 參考：《中國(guó)藥科大學(xué)學(xué)報(bào)》2015年04期

【摘要】：利用特色化的中心復(fù)合設(shè)計(jì),以香豆素-6為模型藥物,通過控制特定的因素和指標(biāo),制備粒徑不同而其他性質(zhì)相同的納米脂質(zhì)載體(NLCs),并對(duì)其形態(tài)、Zeta電位和包封率等理化性質(zhì)進(jìn)行研究。通過體外穩(wěn)定性實(shí)驗(yàn)考察NLCs在K-R液和PBS緩沖液中的穩(wěn)定性,同時(shí)以透析法研究制劑的體外釋藥行為特性。采用MTT法研究空白NLCs和載藥NLCs的細(xì)胞毒性,活體成像技術(shù)考察NLCs在小鼠胃腸道中的滯留時(shí)間。結(jié)果顯示:制備所得的粒徑分別為100,200及300 nm的香豆素-6納米脂質(zhì)載體,分散性良好,在K-R液和PBS緩沖液中可以穩(wěn)定存在,并且體外24 h香豆素-6的累積釋放量均不超過總量的7%。MTT實(shí)驗(yàn)表明:空白NLCs和載藥NLCs對(duì)Caco-2毒性較小。小鼠腸內(nèi)滯留試驗(yàn)顯示:NLCs在灌胃給藥6 h后仍然能夠在胃腸道中檢測(cè)到。因此,制備得到的不同粒徑NLCs可以作為模型制劑,用于細(xì)胞水平和動(dòng)物水平上研究NLCs粒徑對(duì)口服吸收的影響。
[Abstract]:Using a specialised central composite design, using coumarin -6 as a model drug, by controlling specific factors and indicators, Nano-lipid carriers (NLCs) with different particle sizes and similar other properties were prepared and their physical and chemical properties such as Zeta potential and encapsulation efficiency were studied. The stability of NLCs in K-R solution and PBS buffer solution was investigated by in vitro stability experiment, and the release behavior of NLCs in vitro was studied by dialysis method. MTT assay was used to study the cytotoxicity of NLCs and drug loaded NLCs. The retention time of NLCs in the gastrointestinal tract of mice was studied by in vivo imaging. The results showed that the coumarin -6 nano-lipids with particle size of 100200 nm and 300nm had good dispersibility and could exist stably in K-R solution and PBS buffer solution. The cumulative release of coumarin -6 in vitro did not exceed 7. MTT. The results showed that the toxicity of NLCs and NLCs to Caco-2 was less than that of NLCs. The intestinal retention test of mice showed that WNLCs could still be detected in the gastrointestinal tract 6 h after intragastric administration. Therefore, the prepared NLCs with different particle sizes can be used as model preparations to study the effects of NLCs particle size on oral absorption at the cellular and animal levels.
【作者單位】： 中國(guó)藥科大學(xué)藥劑學(xué)教研室;中國(guó)藥科大學(xué)新藥研究中心;
【基金】：國(guó)家自然科學(xué)基金資助項(xiàng)目(No.81273467)~~
【分類號(hào)】：R943

【共引文獻(xiàn)】

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