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Liposomal methotrexate hydrogel for treatment of localized psoriasis: preparation, characterization and laser targeting

机译:脂质体甲氨蝶呤水凝胶治疗局限性牛皮癣:制备,表征和激光靶向

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Background Because systemic treatment of psoriasis is associated with several adverse effects, methotrexate (MTX), either topically or as targeted delivery, has become a more-interesting alternative. Material and Method Methotrexate liposomes (LMTX) were prepared from DPPC, soy PC, egg yolk PC, and cholesterol. We studied the characterization, formulation of hydrogel (MTX 0.25%), and skin permeability, and compared LMTX gel with plain MTX gel and placebo for treating localized psoriasis in a double-blind study using albino mice. Gel formulations were applied daily, followed by irradiation with 80 joules from a 650-nm diode laser 3 times weekly for 12 weeks. Changes in disease signs and histopathological features were assessed. Results Drug release increased as laser energy increased following Higuchi's diffusion model and changed to zero order with energies > or = 80 J; significantly more MTX was released at all time intervals. Both LMTX and FMTX gels showed zero order kinetic release and antipsoriatic activity. During 8 months' follow-up, up to 60% of the patients treated with LMTX gel had no recurrence; this difference was statistically significant. No clinically significant changes were seen regarding blood or other laboratory variables. Conclusions Application of an 80-J diode laser to 0.25% LMTX hydrogel was beneficial for relieving psoriasis and did not exert systemic toxicity.
机译:背景技术由于牛皮癣的全身治疗与多种不良反应有关,因此甲氨蝶呤(MTX)局部给药或靶向给药已成为一种更有趣的选择。材料和方法甲氨蝶呤脂质体(LMTX)由DPPC,大豆PC,蛋黄PC和胆固醇制备。我们研究了水凝胶的特性,配方(MTX 0.25%)和皮肤渗透性,并在一项使用白化病小鼠的双盲研究中将LMTX凝胶与普通MTX凝胶和安慰剂进行了比较,以治疗局部牛皮癣。每天使用凝胶制剂,然后每周三次用650 nm二极管激光器的80焦耳照射3次,持续12周。评估疾病体征和组织病理学特征的变化。结果遵循Higuchi扩散模型,随着激光能量的增加,药物释放增加,并且当能量大于或等于80 J时,药物释放变为零级。在所有时间间隔,明显释放出更多的MTX。 LMTX和FMTX凝胶均显示零级动力学释放和抗银屑病活性。在8个月的随访中,接受LMTX凝胶治疗的患者中多达60%没有复发。这种差异具有统计学意义。在血液或其他实验室变量方面,未见临床显着变化。结论在0.25%LMTX水凝胶上使用80-J二极管激光器可缓解银屑病,且无全身毒性。

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