摘要
一直以来,研究人员不断寻求改善药物溶解性能的技术或策略,以提高药物的生物利用度,增进疗效,降低毒性。这些技术或策略基本上可概括为两类：一类是化学方法,通过改变难溶解药物的理化性能,提高其水溶性,增强其透膜性能,如药物改性PEG化、糖化、合成水溶性前体药物、合成磷脂等各种复合物;另一类是物理方法,即尽可能减小药物颗粒的粒径或物理存在状态,如微粉化、通过环糊精包合、制备固体分散体等。
The improving effect of electrospun drug-loaded nanofibers on the solubility of poorly water-soluble drug was investigated in the present research.Drug-loaded nanofibers were successfully prepared using electrospinning process with helicid as the poorly water-soluble model drug and polyvinylpyrrolidone K60（PVP K60） as the filament-forming matrix.Scanning electron microscopy observation demonstrated that the nanofibers had a three-dimensional continuous web structure,and had well smooth surface and a diameter between 400-600 nm.X-ray diffraction results suggested that helicid lost its original crystal structure but highly distributed into the nanofibers in an amorphous state,resulting from the hydrogen bonding interactions between the carboxylic group of PVP K60 and the hydroxyl groups of helicid.The drug-loaded nanofibers obviously improved helicid＇s solubility,and were able to completely release the whole drug in 60 s.Electrospun drug-loaded nanofibers can improve the solubility and release profiles of poorly water-soluble drug.
出处
《药学学报》
CAS
CSCD
北大核心
2009年第10期1179-1182,共4页
Acta Pharmaceutica Sinica
基金
上海市科委基金资助项目(08JC1400600)
中国博士后基金资助项目(20080440565)
中英药用纺织品联合实验室提供资助
关键词
电纺
纳米纤维
难溶药物
聚乙烯吡咯烷酮
速溶
electrospinning
nanofibers
poorly water-soluble drug
polyvinylpyrrolidone
fast dissolving
