【摘要】：目的制備載紫杉醇固體脂質(zhì)納米粒,并對其理化性質(zhì)、體外釋藥特性及體外抗腫瘤活性進行初步研究。方法矩形微通道內(nèi)制備載藥納米粒,正交實驗篩選最優(yōu)處方;動態(tài)光散射法測定其粒徑;高效液相色譜法測定其載藥量和包封率;透析法測定其體外釋藥特性;四甲基偶氮唑藍(MTT)法測定其體外抗腫瘤活性。結(jié)果最優(yōu)處方制備的納米粒為規(guī)整球形,無明顯團聚現(xiàn)象,平均粒徑為(129.73±2.41)nm,載藥量和包封率分別為(3.11±1.90)%和(43.67±0.55)%;體外釋放藥物分為突釋和持續(xù)釋放兩個階段,120 h累計釋藥率為87.3%;體外抗腫瘤活性明顯高于紫杉醇原藥。結(jié)論微通道法制備紫杉醇納米粒簡便可行,制劑質(zhì)量符合要求,該方法在藥學(xué)領(lǐng)域應(yīng)用前景廣闊。
[Abstract]:Aim to prepare paclitaxel-loaded solid lipid nanoparticles and to study their physicochemical properties in vitro release characteristics and antitumor activity in vitro. Methods the drug-loaded nanoparticles were prepared in rectangular microchannel, the optimal prescription was screened by orthogonal experiment, the particle size was measured by dynamic light scattering, the drug loading and entrapment efficiency were measured by high performance liquid chromatography (HPLC), the drug release characteristics in vitro were determined by dialysis. The antineoplastic activity in vitro was determined by (MTT) method with tetramethylazo blue. Results the nanoparticles prepared by the optimal prescription were regular spherical and had no obvious agglomeration. The average particle size was (129.73 鹵2.41) nm, and entrapment efficiency was (3.11 鹵1.90)% and (43.67 鹵0.55)%, respectively, and the drug loading and entrapment efficiency of the nanoparticles were (129.73 鹵2.41)% and (43.67 鹵0.55)%, respectively. Drug release in vitro was divided into two stages: sudden release and sustained release, the cumulative release rate was 87.3% at 120 h, and the antitumor activity in vitro was significantly higher than that of paclitaxel. Conclusion the preparation of paclitaxel nanoparticles by microchannel method is simple and feasible, and the quality of the preparation meets the requirements. This method has a wide application prospect in pharmaceutical field.
【作者單位】： 臺州市立醫(yī)院;浙江工業(yè)大學(xué)藥學(xué)院;
【基金】：國家自然科學(xué)基金資助項目(21376223)
【分類號】：R944

【參考文獻】

相關(guān)期刊論文 前4條

1 許海玉;張鐵軍;趙平;朱雪瑜;許浚;;中藥緩控釋制劑的研究現(xiàn)狀及研發(fā)思路[J];藥物評價研究;2010年01期

2 陳潔;李博;吳定偉;金一;;多烯紫杉醇納米乳的研制和質(zhì)量評價[J];中國藥學(xué)雜志;2010年07期

3 喻經(jīng)緯;魯智豪;高靜;沈琳;;紫杉醇耐藥機制研究進展及研究方向[J];中國藥學(xué)雜志;2013年14期

4 鄭楠楠;吳琳華;唐景玲;;聚乙二醇維生素E琥珀酸酯在藥劑學(xué)中的應(yīng)用進展[J];中國藥學(xué)雜志;2014年16期

【共引文獻】

相關(guān)期刊論文 前10條

1 王艷明;杜守穎;翟永松;陸洋;王文峰;;自制益智方滲透泵片的體外釋放度考察[J];中華中醫(yī)藥雜志;2012年06期

2 閆軍;王曉東;唐文照;賈獻慧;;丹皮酚脂質(zhì)體凝膠的質(zhì)量控制研究[J];現(xiàn)代藥物與臨床;2011年02期

3 張洪兵;朱雪瑜;張鐵軍;;納米技術(shù)應(yīng)用于中藥制劑的研究進展[J];現(xiàn)代藥物與臨床;2011年03期

4 黃濤;孫燕燕;林宏;張鐵軍;;中藥口服滲透泵制劑的研究進展[J];現(xiàn)代藥物與臨床;2012年06期

5 李艷萍;張志榮;;納米乳的研究進展及其應(yīng)用[J];華西藥學(xué)雜志;2010年04期

6 楊小敏;王躍武;;中藥漂浮劑的研究進展[J];內(nèi)蒙古中醫(yī)藥;2013年31期

7 晏子俊;李萬玉;萬坤;張景R，

本文編號：2436393