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用于透皮给药的盐酸格拉司琼纳米凝胶的设计、优化与表征

Design, Optimization and Characterization of Granisetron HCl Loaded Nano-gel for Transdermal Delivery.

作者信息

Aggarwal Geeta, Kumar Vikash, Chaudhary Hema

机构信息

PDM University, PDM College of Pharmacy, B'garh, India.

出版信息

Pharm Nanotechnol. 2017;5(4):317-328. doi: 10.2174/2211738505666170915151118.

Abstract

BACKGROUND & OBJECTIVE: Our research objective was to design, develop, optimize and characterize Granisetron HCl transdermal gel in order to minimize side effects associated with oral delivery.

METHOD

A statistical design was practically applied for further optimization and preparation of transfersomal gel using Box-Behnken methodology at three levels. The selected independent and dependent variables were Lipoid, surfactant and sonication time and encapsulation efficiency, size and flux correspondingly.

RESULT

The optimized formulation (GTV-16) morphology, shape, size, potential, encapsulation capacity and flux (using Franz-diffusion cell assembly via animal skin barricade medium) were determined. Then, GTV-16 incorporated into gel and during evaluation nano-transformal gel has good particle size of 127.7±1.08 nm, better entrapment efficiency of 83.0 ± 3.22 % and flux of 20.0 ± 1.88µgcm-2/h.

CONCLUSION

The results demonstrated that Granisetron Hydrochloride loaded nano-gel was significantly superior with 8.5 fold enhancement in bioavailability as compared with drug solution.

摘要

背景与目的

我们的研究目标是设计、开发、优化并表征盐酸格拉司琼透皮凝胶,以尽量减少口服给药相关的副作用。

方法

实际应用一种统计设计,采用三水平的Box-Behnken方法进一步优化和制备传递体凝胶。选定的自变量和因变量分别为类脂、表面活性剂和超声处理时间,以及包封率、粒径和通量。

结果

确定了优化配方(GTV-16)的形态、形状、尺寸、电位、包封能力和通量(通过动物皮肤屏障介质使用Franz扩散池装置)。然后,将GTV-16加入凝胶中,在评估过程中,纳米传递体凝胶具有良好的粒径,为127.7±1.08nm,包封率更高,为83.0±3.22%,通量为20.0±1.88µgcm-2/h。

结论

结果表明,与药物溶液相比,载有盐酸格拉司琼的纳米凝胶生物利用度显著提高了8.5倍。

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