【摘要】：目的制備紫杉醇納米粒-微球系統(tǒng)(taxol nanoparticals-in-microsphere system,TAX-NiMS),并考察其體外釋放特性。方法以聚乳酸-羥基乙酸共聚物(poly(lactic-co-glycolic acid),PLGA)為載體,采用乳化溶劑揮發(fā)法制備紫杉醇納米粒(taxol nanoparticals,TAX-NPs)。以包封率、載藥量及粒徑為考察指標(biāo),采用單因素試驗法優(yōu)化處方。采用內(nèi)源乳化凝膠法,以海藻酸鈣為包裹材料,制備包覆TAX-NPs的微球系統(tǒng)。在掃描電鏡和透射電鏡下觀察TAX-NiMS的表面和內(nèi)部形態(tài),并測定其粒徑及體外釋放特性。結(jié)果納米粒優(yōu)化處方:PLGA質(zhì)量濃度為100 g·L-1,聚乙烯醇質(zhì)量濃度為10 g·L-1,油相與水相體積比為1∶10,超聲功率為300 W。微球優(yōu)化處方:海藻酸鈉(NaALG)質(zhì)量濃度為15 g·L-1,Span-80質(zhì)量濃度為10 g·L-1,Ca CO3與Na ALG質(zhì)量比為1∶3,油相與水相體積比為1∶5。此條件下制備的TAX-NiMS的包封率、載藥量和平均粒徑分別為(84.33±1.11)%、(1.12±0.15)%和(2.678±0.014)μm。TAX-NiMS的12h釋放量僅達(dá)到16.51%。結(jié)論 TAX-NiMS的制備方法穩(wěn)定可控,且突釋效應(yīng)顯著減小,為藥物新劑型的開發(fā)提供了思路。
[Abstract]:Objective to prepare paclitaxel nanoparticles-microspheres system (taxol nanoparticals-in-microsphere system,TAX-NiMS) and investigate its release characteristics in vitro. Methods the paclitaxel nanoparticles (taxol nanoparticals,TAX-NPs) were prepared by emulsifying solvent volatilization with polylactic acid-glycolic acid copolymer (poly (lactic-co-glycolic acid) as the carrier. The encapsulation efficiency, drug loading and particle size were used to optimize the formulation. The microspheres coated with TAX-NPs were prepared using calcium alginate as encapsulation material by internal emulsifying gel method. The surface and internal morphology of TAX-NiMS were observed by SEM and TEM, and its particle size and release characteristics in vitro were measured. Results the optimized formulation was 100 g / L ~ (-1), 10 g / L ~ (-1) of polyvinyl alcohol, 1: 10 of volume ratio of oil to water, and 300 W of ultrasonic power. The optimized formulation of microspheres was as follows: the mass concentration of sodium alginate (NaALG) was 15 g / L ~ (-1) Span-80, the mass ratio of Ca CO3 to Na ALG was 1: 3, and the volume ratio of oil phase to water phase was 1: 5. The encapsulation efficiency, drug loading and average particle size of TAX-NiMS prepared under these conditions were (84.33 鹵1.11) and (1.12 鹵0.15)% and (2.678 鹵0.014) 渭 m.TAX-NiMS, respectively. Conclusion the preparation method of TAX-NiMS is stable and controllable, and the effect of sudden release is significantly reduced, which provides a way for the development of new dosage forms of TAX-NiMS.
【作者單位】： 河北科技大學(xué)化學(xué)與制藥工程學(xué)院;
【基金】：河北省杰出青年科學(xué)基金項目(H2014208004)
【分類號】：R943

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