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粗提物在非离子表面活性剂囊泡和固体脂质纳米粒中的局部递送

Topical Delivery of Crude Extracts in Niosomes and Solid Lipid Nanoparticles.

作者信息

Chinembiri Tawona N, Gerber Minja, du Plessis Lissinda H, du Preez Jan L, Hamman Josias H, du Plessis Jeanetta

机构信息

Centre of Excellence for Pharmaceutical Sciences, Faculty of Health Sciences, North-West University, Potchefstroom, South Africa.

出版信息

Pharmacogn Mag. 2017 Oct;13(Suppl 3):S663-S671. doi: 10.4103/pm.pm_489_16. Epub 2017 Oct 11.

Abstract

BACKGROUND

is a medicinal plant native to India and is known to have anticancer properties. It has been investigated for its anti-melanoma properties, and since melanoma presents on the skin, it is prudent to probe the use of in topical formulations. To enhance topical drug delivery and to allow for controlled release, the use of niosomes and solid lipid nanoparticles (SLNs) as delivery vesicles were explored.

OBJECTIVE

The objective of this study is to determine the stability and topical delivery of crude extracts encapsulated in niosomes and SLNs.

MATERIALS AND METHODS

Water, ethanol, and 50% ethanol crude extracts of were prepared using 24 h soxhlet extraction which were each encapsulated in niosomes and SLNs. Franz cell diffusion studies were conducted with the encapsulated extracts to determine the release and skin penetration of the phytomolecules, withaferin A, and withanolide A.

RESULTS

The niosome and SLN formulations had average sizes ranging from 165.9 ± 9.4 to 304.6 ± 52.4 nm with the 50% ethanol extract formulations having the largest size. A small particle size seemed to have correlated with a low encapsulation efficiency (EE) of withaferin A, but a high EE of withanolide A. There was a significant difference ( < 0.05) between the amount of withaferin A and withanolide A that were released from each of the formulations, but only the SLN formulations managed to deliver withaferin A to the stratum corneum-epidermis and epidermis-dermis layers of the skin.

CONCLUSION

SLNs and niosomes were able to encapsulate crude extracts of and release the marker compounds, withaferin A, and withanolide A, for delivery to certain layers in the skin.

SUMMARY

crude extracts were prepared using ethanol, water, and 50% ethanol as solvents. These three extracts were then incorporated into niosomes and solid lipid nanoparticles (SLNs) for use in skin diffusion studies, thus resulting in six formulations (ethanol niosome, water niosome, 50% ethanol niosome, ethanol SLN, water SLN, and 50% ethanol SLN). The diffusion of two marker compounds (withaferin A and withanolide A) from the formulations into the skin was then determined. API: Active pharmaceutical ingredient, ANOVA: Analysis of variance, ED: Epidermis-dermis, HPLC: High-performance liquid chromatography, HLB: Hydrophilic-lipophilic balance, NMR: Nuclear magnetic resonance spectroscopy, PDI: Polydispersity index, SLN: Solid lipid nanoparticle, SD: Standard deviation, SCE: Stratum corneum-epidermis, TEM: Transmission electron microscopy.

摘要

背景

是一种原产于印度的药用植物,已知具有抗癌特性。它已被研究其抗黑色素瘤特性,由于黑色素瘤出现在皮肤上,因此谨慎探索其在局部制剂中的应用。为了增强局部药物递送并实现控释,研究了使用非离子表面活性剂囊泡和固体脂质纳米粒(SLN)作为递送载体。

目的

本研究的目的是确定包裹在非离子表面活性剂囊泡和固体脂质纳米粒中的粗提物的稳定性和局部递送情况。

材料与方法

使用24小时索氏提取法制备水、乙醇和50%乙醇粗提物,将每种粗提物分别包裹在非离子表面活性剂囊泡和固体脂质纳米粒中。用包裹后的提取物进行Franz细胞扩散研究,以确定植物分子、阿魏酸A和睡茄内酯A的释放和皮肤渗透情况。

结果

非离子表面活性剂囊泡和固体脂质纳米粒制剂的平均粒径范围为165.9±9.4至304.6±52.4nm,其中50%乙醇提取物制剂的粒径最大。小粒径似乎与阿魏酸A的低包封率(EE)相关,但与睡茄内酯A的高EE相关。从每种制剂中释放的阿魏酸A和睡茄内酯A含量之间存在显著差异(P<0.05),但只有固体脂质纳米粒制剂能够将阿魏酸A递送至皮肤的角质层-表皮层和表皮-真皮层。

结论

固体脂质纳米粒和非离子表面活性剂囊泡能够包裹粗提物并释放标记化合物阿魏酸A和睡茄内酯A,以递送至皮肤的特定层。

总结

使用乙醇、水和50%乙醇作为溶剂制备粗提物。然后将这三种提取物分别掺入非离子表面活性剂囊泡和固体脂质纳米粒中用于皮肤扩散研究,从而得到六种制剂(乙醇非离子表面活性剂囊泡、水非离子表面活性剂囊泡、50%乙醇非离子表面活性剂囊泡、乙醇固体脂质纳米粒、水固体脂质纳米粒和50%乙醇固体脂质纳米粒)。然后测定两种标记化合物(阿魏酸A和睡茄内酯A)从制剂向皮肤中的扩散情况。 API:活性药物成分,ANOVA:方差分析,ED:表皮-真皮,HPLC:高效液相色谱,HLB:亲水亲油平衡,NMR:核磁共振光谱,PDI:多分散指数,SLN:固体脂质纳米粒,SD:标准差,SCE:角质层-表皮,TEM:透射电子显微镜

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e604/5669113/6163022b5cbf/PM-13-663-g003.jpg

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