优化和体内评估萃取的卡兰金脂质体外用制剂在带状小鼠模型中治疗银屑病的效果。

IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Journal of microencapsulation Pub Date : 2024-08-01 Epub Date: 2024-05-23 DOI:10.1080/02652048.2024.2354249
Aditya Shiven, Afroze Alam, Hitesh Kumar Dewangan, Kamal Shah, Perwez Alam, Deepak N Kapoor
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引用次数: 0

摘要

目的:本研究的重点是开发卡兰金(从印度芒果种子油中分离出来)脂质体乳液的抗牛皮癣活性,以增强皮肤的渗透性和保留性:方法:采用液-液萃取法分离卡兰金,并通过高效液相色谱分析和分配系数对其进行表征。此外,还采用薄膜水合技术将分离出的卡兰金装入脂质体,并通过 Box-Behnken 设计进行优化。对选定的优化批次进行了表征,包括平均直径、PDI、ZETA电位、包埋效率、形态(TEM)、傅立叶变换红外光谱和体内外皮肤保留率。此外,还将负载 Karanjin 的脂质体配制成乳液,并对其流变性、铺展性、质地、体外皮肤渗透和保留、稳定性以及在小鼠尾部模型中的抗银屑病活性进行了表征:结果:从种子油中提取的卡兰金产量为 0.1% w/v,具有亲脂性。优化后的脂质体制剂平均直径为 195 ± 1.8 nm,PDI 为 0.271 ± 0.02,zeta 电位为 -27.0 ± 2.1 mV,EE 为 61.97 ± 2.5%。TEM 图像显示,脂质体呈球形,由单层磷脂双分子层包围,药物与辅料之间没有交错。此外,用 0.1% w/v carbopol 制备的乳液粘度为 615 mPa.sec,具有良好的触变性、铺展性和质地。经体内外渗透和保留研究证实,与纯卡朗金乳液相比,卡朗金负载脂质体乳液的药物渗透率提高了 22.44%。体内研究显示,卡朗金脂质体乳液的药物活性比 5%重量比的传统卡朗金乳液高出 16.09%:结论:卡兰金脂质体乳液是一种有效的抗银屑病药物,与传统的卡兰金乳液相比,其皮肤渗透性和滞留性更好。
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Optimisation and in-vivo evaluation of extracted Karanjin loaded liposomal topical formulation for treatment of psoriasis in tape-stripped mouse model.

Aim: The present work is focus on development of anti-psoriasis activity of Karanjin (isolated from Pongamia pinnata seed oil) loaded liposome based lotion for enhancement of skin permeation and retention.

Method: Karanjin was isolated using liquid-liquid extraction method and characterised by HPLC analysis and partition coefficient. Further, isolated Karanjin was loaded into liposomes using thin-film hydration technique and optimised by Box-Behnken design. Selected optimised batch was characterised their mean diameter, PDI, zeta potential, and entrapment efficiency, morphology (by TEM), FTIR and ex-vivo skin retention. Additionally, Karanjin loaded liposomes were formulated into lotion and characterise their rheological, spreadability, texture, ex-vivo skin permeation & retention, stability and anti-psoriatic activity in mouse tail model.

Result: The yield of Karanjin from seed oil was 0.1% w/v and have lipophilic nature. The optimised liposomal formulation showed 195 ± 1.8 nm mean diameter, 0.271 ± 0.02 PDI, -27.0 ± 2.1 mV zeta potential and 61.97 ± 2.5% EE. TEM image revel the spherical shap of liposome surrounded by single phospholipid bilayer and no interection between drug and excipients. Further, lotion was prepared by 0.1% w/v carbopol and found to 615 mPa.sec viscosity, good thixotropic behaviour, spreadability and texture. There was 22.44% increase in drug permeation for Karanjin loaded liposomal lotion compared to pure Karanjin lotion, confirm by ex-vivo permeation and retention. While, in-vivo study revel the liposomal lotion of Karanjin was found to have 16.09% higher drug activity then 5% w/w conventional Karanjin lotion.

Conclusion: Karanjin loaded liposomal lotion have an effective anti-psoriatic agent and showed better skin permeation and retention than the conventional Karanjin lotion.

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来源期刊
Journal of microencapsulation
Journal of microencapsulation 工程技术-工程:化工
CiteScore
6.30
自引率
2.60%
发文量
39
审稿时长
3 months
期刊介绍: The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.
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