Engineering Eutectogel Microneedle Patch as Effective Transdermal Delivery System of Hydrophobic Drugs

IF 3.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Danilo M. dos Santos, Hasika Suresh, Samantha J. Kruzshak, Jihyun Kim, Peggy Cebe, James D. Baleja, Emmanuel S. Tzanakakis, Sameer Sonkusale
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Abstract

Conventional drug delivery methods often face challenges in terms of patient adherence and drug administration. Microneedles (MNs) patches have emerged as a promising alternative, offering a minimally invasive transdermal route for medications. However, their drug-loading capacity remains limited, particularly for hydrophobic active pharmaceutical ingredients (APIs). Herein, microneedles are designed based on eutectic solvent gels (eutectogels) as transdermal carriers for hydrophobic APIs. A natural deep eutectic solvent (NADES) is combined to enhance the solubility of the hydrophobic APIs within the GelMA/PEGDA matrix for mechanical strength and sustained release from the resulting eutectogels microneedles (EU-MNs). Using docetaxel, 5-fluorouracil, and curcumin as hydrophobic APIs models, the superior drug-loading capacity of the EU-MNs is demonstrated. In vitro experiments revealed that the EU-MNs provided a sustained release of distinct hydrophobic APIs over 4 days. Additionally, by properly adjusting the concentration and type of APIs, these microneedle patches do not exhibit cytotoxic effects on fibroblasts cell line (NIH/3T3), underscoring their potential for safe and effective transdermal drug delivery. These findings highlight the potential of EU-MNs as versatile, eco-friendly transdermal vehicles for large amounts of hydrophobic APIs, leading to more effective treatments for these drugs.

Abstract Image

工程共tectol微针贴剂作为疏水药物的有效透皮给药系统
传统的给药方法在患者依从性和给药方面经常面临挑战。微针(MNs)贴片作为一种有前途的替代方案,提供了一种微创的透皮药物治疗途径。然而,它们的载药能力仍然有限,特别是疏水性活性药物成分(api)。本文设计了基于共熔溶剂凝胶(eutectogel)作为疏水原料药透皮载体的微针。一种天然的深共晶溶剂(NADES)结合在一起,提高了疏水原料药在GelMA/PEGDA基质中的溶解度,提高了机械强度,并从所得的共凝胶微针(EU-MNs)中持续释放。以多西紫杉醇、5-氟尿嘧啶和姜黄素为疏水性原料药模型,证明了eu - mn具有优越的载药能力。体外实验表明,EU-MNs可在4天内持续释放不同的疏水原料药。此外,通过适当调整原料药的浓度和类型,这些微针贴片不会对成纤维细胞细胞系产生细胞毒性作用(NIH/3T3),强调了它们安全有效的经皮给药潜力。这些发现强调了EU-MNs作为大量疏水原料药的多功能、环保透皮载体的潜力,从而为这些药物带来更有效的治疗。
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来源期刊
Advanced Therapeutics
Advanced Therapeutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.10
自引率
2.20%
发文量
130
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