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质量源于设计(Qbd)辅助开发用于局部给药的芦荟提取物磷脂体凝胶。

Quality by design (Qbd) assisted development of phytosomal gel of aloe vera extract for topical delivery.

作者信息

Jain Pooja, Taleuzzaman Mohamad, Kala Chandra, Kumar Gupta Dipak, Ali Asad, Aslam Mohammed

机构信息

Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.

Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Maulana Azad University, Jodhpur, India.

出版信息

J Liposome Res. 2021 Dec;31(4):381-388. doi: 10.1080/08982104.2020.1849279. Epub 2020 Nov 19.

DOI:10.1080/08982104.2020.1849279
PMID:33183121
Abstract

The aim of the current study was to develop the phytosomal gel of aloe vera extract for improved topical delivery. Aloe vera extract loaded phytosomal system was developed by fixing the amount of aloe vera extract and ethanol and by varying the concentration of lecithin (0.15-0.25% w/v) and speed of rotation (80-120 rpm). Different formulation batches were prepared as per the Design expert software. A 2 Factorial design was applied to optimize the formulation on the basis of vesicular size and entrapment efficiency. Developed formulations were evaluated for vesicular size, entrapment efficiency, PDI, zeta potential and release. Further stability studies were also performed. For the optimized formulation (F09), vesicular size, entrapment efficiency and PDI were found as 123.1 ± 1.44 nm, 95.67 ± 0.27% and 0.98 ± 0.06. Zeta potential of -11.9 mV and drug release of 56.91 ± 4.1% obtained in 24 h. Drug release kinetics from the phytosomes follows Higuchi model. TEM micrograph confirms the uniform structure of phytosomes. Phytosomal gel of optimized phytosomal formulation (F09) was developed with 1% Carbopol 934 and physically characterized on the basis of pH, viscosity, homogeneity and drug content. permeation study showed the better permeation and flux profile of phytosomal gel with the conventional aloe vera extract gel. Also, studies on phytosomal formulation and gel showed stability up-to 3 months. Thus overall, it can be concluded that the phytosomal gel is a good carrier for topical delivery of herbal extract such as aloe vera.

摘要

本研究的目的是开发芦荟提取物的磷脂体凝胶,以改善局部给药效果。通过固定芦荟提取物和乙醇的量,并改变卵磷脂浓度(0.15 - 0.25% w/v)和旋转速度(80 - 120 rpm),开发了负载芦荟提取物的磷脂体系统。根据Design expert软件制备了不同的制剂批次。应用二因素设计,基于囊泡大小和包封率优化制剂。对所开发的制剂进行了囊泡大小、包封率、多分散指数(PDI)、zeta电位和释放度的评估。还进行了进一步的稳定性研究。对于优化后的制剂(F09),囊泡大小、包封率和PDI分别为123.1±1.44 nm、95.67±0.27%和0.98±0.06。24小时内获得的zeta电位为 - 11.9 mV,药物释放率为56.91±4.1%。药物从磷脂体中的释放动力学符合Higuchi模型。透射电子显微镜(TEM)显微照片证实了磷脂体的均匀结构。用1%卡波姆934制备了优化后的磷脂体制剂(F09)的磷脂体凝胶,并根据pH值、粘度、均匀性和药物含量进行了物理表征。渗透研究表明,与传统芦荟提取物凝胶相比,磷脂体凝胶具有更好的渗透和通量曲线。此外,对磷脂体制剂和凝胶的研究表明其稳定性可达3个月。因此,总体而言,可以得出结论,磷脂体凝胶是芦荟等草药提取物局部给药的良好载体。

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