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用于银屑病治疗的甲氨蝶呤和黄芩苷纳米脂质载体的研发与评价

Development and Evaluation of Methotrexate and Baicalin-Loaded Nanolipid Carriers for Psoriasis Treatment.

作者信息

Sohail Sundus, Arshad Saloma, Khalid Sidra, Dar Muhammad Junaid, Iqbal Kashif, Sohail Hassan

机构信息

University of Lahore (Islamabad Campus) Faculty of Pharmacy, Department of Pharmacy, Islamabad, Pakistan.

Drug Regulatory Authority of Pakistan, Islamabad, Pakistan.

出版信息

Turk J Pharm Sci. 2024 Sep 2;21(4):327-339. doi: 10.4274/tjps.galenos.2023.71242.

DOI:10.4274/tjps.galenos.2023.71242
PMID:39224396
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11589095/
Abstract

OBJECTIVES

Psoriasis is a chronic inflammatory, T-lymphocyte immune-mediated skin disease. In this study, skin-permeating nanolipid carriers (NLCs) of Methotrexate (MTX) and Baicalin (BL) were formulated. This further gave formulation of nano-lipid encapsulated carriers for dual-drug delivery of the hydrophilic and hydrophobic drugs through the liposomal gel.

MATERIALS AND METHODS

Optimization of the formulation of NLCs was performed and characterized by determining their particle size, drug permeation, skin irritation, drug loading capacity, stability, drug release behavior, and cellular viability. skin permeation and in vivo psoriatic efficiency were also evaluated and compared.

RESULTS

Results revealed that the amount of MTX permeating the skin was 2.4 to 4.4 fold greater for dual-drug s than for single NLCs. The optimized dual-drug loaded NLCs had an average particle size (150.20 ± 3.57 nm) and polydispersity index (0.301 ± 0.01) and high entrapment (86.32 ± 2.78% ). The MTX nanoparticles exhibit a positive Zeta potential of 38.6 mV. The psoriasis area and severity index scoring showed the lowest skin erythema, skin thickness and scaling. MTX-BL NLCs were inhibited the expression of inflammatory cytokines (tumor necrosis factor-alpha, and interleukin-17) .

CONCLUSION

It can be concluded that newer targeting strategies for NLCs for dual-drug delivery of nano-lipid carriers could be administered topically for the treatment of psoriasis.

摘要

目的

银屑病是一种慢性炎症性、T淋巴细胞免疫介导的皮肤病。在本研究中,制备了甲氨蝶呤(MTX)和黄芩苷(BL)的皮肤渗透纳米脂质载体(NLCs)。这进一步实现了纳米脂质包封载体的制剂,用于通过脂质体凝胶对亲水和疏水药物进行双药递送。

材料和方法

对NLCs制剂进行优化,并通过测定其粒径、药物渗透、皮肤刺激性、载药量、稳定性、药物释放行为和细胞活力进行表征。还评估并比较了皮肤渗透性和体内银屑病治疗效果。

结果

结果显示双药制剂的MTX透过皮肤的量比单一NLCs高2.4至4.4倍。优化后的双药负载NLCs平均粒径为(150.20±3.57nm),多分散指数为(0.301±0.01),包封率高(86.32±2.78%)。MTX纳米颗粒的Zeta电位为正38.6mV。银屑病面积和严重程度指数评分显示皮肤红斑、皮肤厚度和脱屑程度最低。MTX-BL NLCs抑制了炎症细胞因子(肿瘤坏死因子-α和白细胞介素-17)的表达。

结论

可以得出结论,纳米脂质载体双药递送的新型NLC靶向策略可局部给药用于治疗银屑病。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/824b/11589095/17b632868a59/TurkJPharmSci-21-327-figure-4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/824b/11589095/a1a0f415bc78/TurkJPharmSci-21-327-figure-1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/824b/11589095/8ba153db4d2e/TurkJPharmSci-21-327-figure-2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/824b/11589095/9d3d87c96d39/TurkJPharmSci-21-327-figure-3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/824b/11589095/17b632868a59/TurkJPharmSci-21-327-figure-4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/824b/11589095/a1a0f415bc78/TurkJPharmSci-21-327-figure-1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/824b/11589095/8ba153db4d2e/TurkJPharmSci-21-327-figure-2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/824b/11589095/9d3d87c96d39/TurkJPharmSci-21-327-figure-3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/824b/11589095/17b632868a59/TurkJPharmSci-21-327-figure-4.jpg

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