皮内注射热致伸缩性聚合地塞米松原药(ProGel-Dex)可改善咪喹莫特(IMQ)诱导的类银屑病小鼠模型的皮炎。

IF 4.5 2区 医学 Q2 MEDICINE, RESEARCH & EXPERIMENTAL
Haochen Jiang, Xin Fu, Gang Zhao, Xiaoqing Du, Corey Georgesen, Geoffrey M Thiele, Steven R Goldring, Dong Wang
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引用次数: 0

摘要

银屑病是一种慢性免疫介导的炎症性皮肤病,发病率占美国总人口的 3%。虽然已有多种新的系统疗法用于治疗银屑病皮肤病,但外用和内服糖皮质激素(GCs)仍然是有效的银屑病疗法。然而,这些药物在临床上的应用却受到明显不良反应的影响,包括皮肤萎缩和色素沉着以及血糖水平升高和高血压。为了缓解这些局限性,我们开发了一种基于 N-(2-羟丙基)甲基丙烯酰胺(HPMA)共聚物的热致伸缩性地塞米松(Dex)原药(ProGel-Dex),并在咪喹莫特(IMQ)诱导的类银屑病(PL)小鼠模型中评估了其疗效和安全性。在研究开始时,按0.5、1.0和2.0毫克/千克/天的Dex当量三个剂量水平皮内注射一次ProGel-Dex。PL小鼠还接受了每日局部生理盐水或Dex治疗,作为对照组。用 ProGel-Dex 治疗 PL 小鼠,剂量为 0.5 毫克/千克/天,结果鳞屑和红斑显著减少。大体病理学评分、皮肤组织学评分和血清细胞因子水平也有所改善。有趣的是,在使用 ProGel-Dex 的小鼠中,Dex 当量为 1.0 和 2.0 毫克/公斤/天时,只观察到皮肤红斑有所改善。使用 0.5 和 1.0 毫克/千克/天 Dex 当量的 ProGel-Dex 治疗的小鼠没有观察到与 GC 相关的副作用,如血清丙氨酸氨基转移酶(ALT)和淀粉酶水平升高以及体重下降。总之,这些结果表明,与外用Dex治疗相比,ProGel-Dex在治疗银屑病皮损方面具有更高的疗效和安全性,支持其在皮损型银屑病临床治疗方面的转化潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Intradermal Injection of a Thermoresponsive Polymeric Dexamethasone Prodrug (ProGel-Dex) Ameliorate Dermatitis in an Imiquimod (IMQ)-Induced Psoriasis-like Mouse Model.

Intradermal Injection of a Thermoresponsive Polymeric Dexamethasone Prodrug (ProGel-Dex) Ameliorate Dermatitis in an Imiquimod (IMQ)-Induced Psoriasis-like Mouse Model.

Psoriasis is a chronic immune-mediated inflammatory skin disease, affecting ∼ 3% of the US population. Although multiple new systemic therapies have been introduced for the treatment of psoriatic skin disease, topical and intralesional glucocorticoids (GCs) continue to be used as effective psoriasis therapies. Their clinical utility, however, has been hampered by significant adverse effects, including skin atrophy and pigmentation as well as elevated blood glucose levels and hypertension. To mitigate these limitations, we have developed a N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer-based thermoresponsive dexamethasone (Dex) prodrug (ProGel-Dex) and assessed its therapeutic efficacy and safety in an imiquimod (IMQ)-induced psoriasis-like (PL) mouse model. ProGel-Dex was intradermally administered once at three dosing levels: 0.5, 1.0, and 2.0 mg/kg/day Dex equivalent at the beginning of the study. PL mice were also treated with daily topical saline or Dex, which were used as control groups. Treatment of PL mice with ProGel-Dex dosed at 0.5 mg/kg/day resulted in a significant reduction in scaling and erythema. Improvement in gross pathology scores, skin histological scores, and serum cytokine levels was also observed. Interestingly, for mice treated with ProGel-Dex at 1.0 and 2.0 mg/kg/day Dex equivalent, only improvement in skin erythema was observed. GC-associated side effects, such as elevation of serum alanine aminotransferase (ALT) and amylase levels and body weight loss, were not observed in mice treated with ProGel-Dex at 0.5 and 1.0 mg/kg/day Dex equivalent. Collectively, these results demonstrate the efficacy and improved safety of ProGel-Dex in treating psoriatic skin lesions when compared to topical Dex treatment, supporting its translational potential for clinical management of lesional skin psoriasis.

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来源期刊
Molecular Pharmaceutics
Molecular Pharmaceutics 医学-药学
CiteScore
8.00
自引率
6.10%
发文量
391
审稿时长
2 months
期刊介绍: Molecular Pharmaceutics publishes the results of original research that contributes significantly to the molecular mechanistic understanding of drug delivery and drug delivery systems. The journal encourages contributions describing research at the interface of drug discovery and drug development. Scientific areas within the scope of the journal include physical and pharmaceutical chemistry, biochemistry and biophysics, molecular and cellular biology, and polymer and materials science as they relate to drug and drug delivery system efficacy. Mechanistic Drug Delivery and Drug Targeting research on modulating activity and efficacy of a drug or drug product is within the scope of Molecular Pharmaceutics. Theoretical and experimental peer-reviewed research articles, communications, reviews, and perspectives are welcomed.
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