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目的考察不同载药方法对介孔二氧化钛纳米粒载药系统载药和溶出速率的影响。方法通过溶剂挥干法、熔融法、吸附平衡法分别将卡维地洛包载于介孔二氧化钛纳米粒中,用扫描电镜和透射电镜观测样品形貌,氮气吸附-解吸法测量载体的比表面积和孔体积,差示扫描量热法分析药物粒子的存在状态,X-射线衍射法进行物相分析,热失重法分析载药量,最后测定载药系统的溶出速率并进行长期稳定性试验。结果三种载药方法均能通过改变药物的存在状态使药物以非晶型存在于载体中而达到提高溶出速率的目的。其中溶剂挥干法所得的载药系统溶出速率提高显著,并且更具有长期稳定性。结论溶剂挥干法为介孔二氧化钛纳米粒载药的首选。
Objective To investigate the effects of different drug loading methods on the drug loading and dissolution rate of mesoporous titania nanoparticle drug delivery system. Methods Carvedilol was encapsulated in mesoporous titania nanoparticles by solvent evaporation, melting and adsorption equilibrium methods respectively. The morphologies of the samples were observed by scanning electron microscopy and transmission electron microscopy. The specific surface area And pore volume, differential scanning calorimetry analysis of the presence of drug particles, phase analysis by X-ray diffraction, thermal loading method analysis of drug loading, and finally measured the dissolution rate of the drug-loaded system and long-term stability test. Results All the three drug-loading methods could achieve the purpose of increasing the dissolution rate by changing the existing state of the drug so that the drug exists in the amorphous form in the carrier. Among them, the dissolution rate of the drug-loading system obtained by solvent evaporation was significantly improved and more stable over the long term. Conclusion Solvent evaporation method is the first choice of drug-loaded titanium dioxide nanoparticles.