摘要
目的：制备载有紫杉醇（paclitaxel ，PTX）的多孔硅微球（mesoporous silicon microparticle ，MSM ），并考察MSM对PTX溶出速率以及在人结直肠腺癌细胞（Caco-2）和人结肠癌细胞（HT-29）共培养单层细胞模型中渗透性的影响。方法以“Top-down”的电化学阳极氧化法制备MSM ，用动态光散射法测定粒径，然后采用浸入法装载 PTX以制备紫杉醇多孔硅微球（PTX-MSM）；采用高效液相色谱法测定PTX-MSM的载药量，用透析法测定药物释放度，并用粉末X射线衍射对装载的PTX进行固态分析；考察MSM对PTX的体外释放度及透过Caco-2和 HT-29单层细胞模型能力的影响。结果制备的 MSM 的粒径为1.3～7.1μm ；载药量约为17．46％±1．19％，吸附在MSM的PTX多为无定形态；PTX载入MSM 后体外释放明显加快；MSM使得PTX透过Caco-2和 HT-29共培养单层细胞模型速度显著提高。结论 MSM作为药物载体，可显著提高难溶性药物的释放速率和吸收速度。
Objective To prepare paclitaxel （PTX） loaded mesoporous silicon microparticle （MSM） and to investigate the impact of MSM on the dissolution rate of PTX and its permeability across Caco-2 and HT-29 co-cultured monolayer .Methods The MSM was prepared by the electrochemical anodisation ＂Top-Down＂method .The microparticle size was measured by the dynamic light scattering method ,and then PTX was loaded into the MSM through the immersion method （PTX-MSM ）;loading degree of PTX-MSM was determined by HPLC .MSM release profiles were also studied through putting PTX-MSM into dialysis bags ,and the solid state of loaded PTX inside the MSM was investigated by X-ray powder diffraction ;permeability of PTX across Caco-2 and HT-29 before and after loading into MSM was also investigated .Results Particle size of the MSM was between 1 .3 μm and 7 .1μm ;loading degree of PTX was around 17 .46% ± 1 .19% ;PTX adsorbed onto the surface of MSM was mainly in amorphous phase;release rate of PTX from PTX-MSM was faster than that of bare PTX powder ;MSM also dramatically increased the per-meability of PTX across Caco-2 and HT-29 .Conclusions As the drug carriers ,MSM could significantly enhance the dissolution rate of water-insoluble therapeutics and its permeability .
出处
《西北药学杂志》
CAS
2013年第6期614-616,共3页
Northwest Pharmaceutical Journal
关键词
紫杉醇
多孔硅微球
体外评价
paclitaxel
mesoporous silicon microparticles
in vitro evaluation
