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经皮给药透过微针辅助电渗以递送磷酸地塞米松 - 炎症性疾病的潜在治疗选择。

Transcutaneous Delivery of Dexamethasone Sodium Phosphate Via Microneedle-Assisted Iontophoretic Enhancement - A Potential Therapeutic Option for Inflammatory Disorders.

机构信息

Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan.

Institute of Pharmaceutical Sciences, University of Veterinary and Animal Sciences, Lahore, Pakistan.

出版信息

Pharm Res. 2024 Jun;41(6):1183-1199. doi: 10.1007/s11095-024-03719-w. Epub 2024 Jun 7.


DOI:10.1007/s11095-024-03719-w
PMID:38849712
Abstract

AIM: This study aimed to fabricate dexamethasone sodium phosphate loaded microneedle arrays (MNA) and investigate their efficiency in combination with iontophoresis for the treatment of hind paw oedema in rats. METHODS: Drug loaded polyvinyl alcohol, polyvinyl pyrrolidone and D-sorbitol-based MNA11 were fabricated by vacuum micromolding. Physicochemical, morphological, thermal, in-silico, in-vitro insertion ability (on parafilm) and drug release studies were performed. Ex-vivo permeation, in-vivo insertion and anti-inflammatory studies were performed in combination with iontophoresis. RESULTS: MNA11 displayed sharp-tipped projections and acceptable physicochemical features. Differential scanning calorimetry results indicated that drug loaded MNA11 were amorphous solids. Drug interacted with PVP and PVA predominately via hydrogen bonding. Parafilm displayed conspicuously engraved complementary structure of MNA11. Within 60 min, 91.50 ± 3.1% drug released from MNA11. A significantly higher i.e., 95.06 ± 2.5% permeation of drug was observed rapidly (within 60 min) from MNA11-iontophoresis combination than MNA11 i.e., 84.07 ± 3.5% within 240 min. Rat skin treated using MNA11 and MNA11-iontophoresis showed disruptions / microchannels in the epidermis without any damage to underlying anatomical structures. MNA11-iontophoresis combination led to significant reduction (83.02 ± 3.9%) in paw oedema as compared to MNA11 alone (72.55 ± 4.1%). CONCLUSION: MNA11-iontophoresis combination can act as a promising candidate to deliver drugs transcutaneously for treating inflammatory diseases.

摘要

目的:本研究旨在制备磷酸地塞米松钠负载的微针阵列(MNA),并研究其与离子导入联合用于治疗大鼠后爪水肿的效果。

方法:通过真空微成型制备载药聚乙烯醇、聚乙烯吡咯烷酮和 D-山梨醇的 MNA11。进行了理化性质、形态、热学、计算机模拟、体外插入能力(在聚四氟乙烯薄膜上)和药物释放研究。进行了体外渗透、体内插入和抗炎研究,并与离子导入联合进行。

结果:MNA11 显示出尖锐的突起和可接受的理化特性。差示扫描量热法结果表明,载药 MNA11 为无定形固体。药物主要通过氢键与 PVP 和 PVA 相互作用。聚四氟乙烯薄膜显示出与 MNA11 明显互补的压痕结构。在 60 分钟内,91.50±3.1%的药物从 MNA11 中释放。从 MNA11-离子导入联合中观察到药物的渗透性显著增加,即 95.06±2.5%,而从 MNA11 中在 240 分钟内仅观察到 84.07±3.5%的药物渗透。使用 MNA11 和 MNA11-离子导入处理的大鼠皮肤在表皮中显示出破坏/微通道,而不会对下面的解剖结构造成任何损伤。与单独使用 MNA11 相比,MNA11-离子导入联合可显著减少(83.02±3.9%)后爪水肿。

结论:MNA11-离子导入联合可以作为一种有前途的候选药物,用于经皮输送药物治疗炎症性疾病。

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本文引用的文献

[1]
Drug permeation enhancement, efficacy, and safety assessment of azelaic acid loaded SNEDDS hydrogel to overcome the treatment barriers of atopic dermatitis.

Environ Res. 2023-11-1

[2]
Improved Transdermal Delivery of Rabies Vaccine using Iontophoresis Coupled Microneedle Approach.

Pharm Res. 2023-8

[3]
Engineering of clarithromycin loaded stimulus responsive dissolving microneedle patches for the treatment of biofilms.

Int J Pharm. 2023-6-10

[4]
Design, optimization and evaluation of dexamethasone-loaded microneedles for inflammatory disorders.

Int J Pharm. 2023-3-25

[5]
Engineering of tetanus toxoid-loaded polymeric microneedle patches.

Drug Deliv Transl Res. 2023-3

[6]
Microneedle and iontophoresis mediated delivery of methotrexate into and across healthy and psoriatic skin.

Int J Pharm. 2022-4-25

[7]
Microneedle Mediated Iontophoretic Delivery of Tofacitinib Citrate.

Pharm Res. 2023-3

[8]
Evaluation of sustained-release in-situ injectable gels, containing naproxen sodium, using in vitro, in silico and in vivo analysis.

Int J Pharm. 2022-3-25

[9]
Trilayer microneedle array assisted transdermal and intradermal delivery of dexamethasone.

Int J Pharm. 2022-1-25

[10]
Burden of skin disease and associated socioeconomic status in Asia: A cross-sectional analysis from the Global Burden of Disease Study 1990-2017.

JAAD Int. 2020-12-10

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