糖基化陶瓷纳米载体用于疏水性药物的口服递送:制剂、优化和评价。
Sugar coated ceramic nanocarriers for the oral delivery of hydrophobic drugs: formulation, optimization and evaluation.
机构信息
Gokaraju Rangaraju College of Pharmacy, Pharmaceutics, Bachupally, Hyderabad, Andhra Pradesh, India.
出版信息
Drug Dev Ind Pharm. 2012 May;38(5):577-86. doi: 10.3109/03639045.2011.617884. Epub 2011 Sep 30.
In order to enhance the delivery of poorly-soluble drugs, we have explored aquasomes (three-layered, ceramic core based, oligosaccharide coated nanoparticles) as potential carriers for the delivery of model hydrophobic drug piroxicam (log P = 3.1). Ceramic nanoparticles were prepared using two techniques; namely, co-precipitation by refluxing and co-precipitation by sonication. Core preparation was finally done using sonication approach; based on the higher % yield (42.4 ± 0.4%) and shorter duration (1 day) compared to the reflux method (27.4 ± 2.05%, 6 days). Lactose loading onto ceramic core was achieved using adsorption. Colorimetric analysis of lactose coating was done using Anthrone method. Optimization of process variables namely, incubation time and core to coat ratio (for sugar loading) was carried out. Optimum time of incubation was 3 h and the core to coat ratio was 4:1. The drug loading was achieved by incubating the sugar loaded cores in different concentrations of piroxicam solution and it was found that 1.5% w/v piroxicam was optimal. Structural characterization using Fourier-Transform Infra Red Spectroscopy (FTIR) confirmed the presence of sugar coating onto the core. Morphological evaluation using transmission electron microscopy (TEM) revealed spherical nanoparticles (size 56.56 ± 5.93 nm for lactose coated core and 184.75 ± 13.78 nm for piroxicam loaded aquasomes) confirming the nanometric dimensions.
为了提高难溶性药物的递送效果,我们探索了水囊(三层、基于陶瓷核、寡糖包裹的纳米颗粒)作为模型疏水性药物吡罗昔康(log P = 3.1)递药的潜在载体。使用两种技术制备陶瓷纳米颗粒;即回流共沉淀和超声共沉淀。最后通过超声法进行核心制备;与回流法(27.4 ± 2.05%,6 天)相比,该方法的产率更高(42.4 ± 0.4%),耗时更短(1 天)。通过吸附作用将乳糖负载到陶瓷核心上。使用蒽酮法对乳糖包衣进行比色分析。优化了工艺变量,即孵育时间和核壳比(用于糖负载)。最佳孵育时间为 3 小时,核壳比为 4:1。通过将负载糖的核在不同浓度的吡罗昔康溶液中孵育来实现药物负载,发现 1.5%w/v 的吡罗昔康是最佳的。使用傅里叶变换红外光谱(FTIR)进行结构表征证实了糖涂层存在于核心上。使用透射电子显微镜(TEM)进行形态评估显示出球形纳米颗粒(乳糖包被核的粒径为 56.56 ± 5.93nm,载吡罗昔康的水囊粒径为 184.75 ± 13.78nm),证实了纳米尺寸。