Drug-nanoencapsulated PLGA microspheres prepared by emulsion electrospray with controlled release behavior.

Drug-nanoencapsulated PLGA microspheres prepared by emulsion electrospray with controlled release behavior.
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DOI:
10.1093/rb/rbw033
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发表时间:
2016-10
影响因子:
6.7
通讯作者:
Wang L
Wang L
中科院分区:
工程技术1区
文献类型:
--
作者:
Yao S;Liu H;Yu S;Li Y;Wang X;Wang L

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现代药物治疗学的发展对药物控释系统提出了更高的要求,即药物控释系统应能有效地包裹药物,并使药物以所需的速率释放,以满足实际系统的需要。本研究采用乳液电喷雾法将两种不同分子量的水性模型药物--刚果红和牛血清白蛋白(BSA)纳米包裹在聚乳酸乙醇酸共聚物(PLGA)微球中。在制备过程中,将药物的水相加入到PLGA的氯仿溶液中形成乳液。然后将乳液电喷雾以制备药物纳米封装的PLGA微球。微球的形态受药物水相与PLGA有机相的体积比(Vw/Vo)和模型药物分子量的影响。共聚焦激光扫描显微镜显示药物相纳米液滴均匀地分散在PLGA微球中,并具有与Vw/Vo相关的不同分布模式。随着药物水相体积比的增加,纳米液滴逐渐增多,形成连续相,加快药物释放速率。与刚果红相比,BSA在PLGA微球中的释药速率较慢,说明BSA的释药速率不仅受Vw/Vo的影响,还受模型药物分子量的影响。总之,采用乳化电喷雾法制备的PLGA微球提供了一种有效、简单的系统,可以实现药物的控制释放,达到满足实际需要的速率。
The development of modern therapeutics has raised the requirement for controlled drug delivery system which is able to efficiently encapsulate bioactive agents and achieve their release at a desired rate satisfying the need of the practical system. In this study, two kind of aqueous model drugs with different molecule weight, Congo red and albumin from bovine serum (BSA) were nano-encapsulated in poly (dl-lactic-co-glycolic acid) (PLGA) microspheres by emulsion electrospray. In the preparation process, the aqueous phase of drugs was added into the PLGA chloroform solution to form the emulsion solution. The emulsion was then electrosprayed to fabricate drug-nanoencapsulated PLGA microspheres. The morphology of the PLGA microspheres was affected by the volume ratio of aqueous drug phase and organic PLGA phase (Vw/Vo) and the molecule weight of model drugs. Confocal laser scanning microcopy showed the nanodroplets of drug phase were scattered in the PLGA microspheres homogenously with different distribution patterns related to Vw/Vo. With the increase of the volume ratio of aqueous drug phase, the number of nanodroplets increased forming continuous phase gradually that could accelerate drug release rate. Moreover, BSA showed a slower release rate from PLGA microspheres comparing to Congo red, which indicated the drug release rate could be affected by not only Vw/Vo but also the molecule weight of model drug. In brief, the PLGA microspheres prepared using emulsion electrospray provided an efficient and simple system to achieve controlled drug release at a desired rate satisfying the need of the practices.
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