Diclofenac enables prolonged delivery of naltrexone through microneedle-treated skin.
Diclofenac enables prolonged delivery of naltrexone through microneedle-treated skin.
复制标题
DOI：
10.1007/s11095-011-0372-2
复制
发表时间：
2011-05
影响因子：
3.7
通讯作者：
Stinchcomb AL
中科院分区：
文献类型：
--
作者：
Banks SL;Paudel KS;Brogden NK;Loftin CD;Stinchcomb AL
本研究的目的是确定非特异性考克斯抑制是否可以延长无毛豚鼠在微针治疗后的毛孔寿命。无毛豚鼠用微针阵列处理±每天应用Solaraze®凝胶（3%双氯芬酸钠（非特异性考克斯抑制剂）和2.5%透明质酸）;经表皮水分损失用于评价毛孔寿命。为了检查纳洛酮的渗透性，用微针±每日Solaraze®凝胶处理另外的豚鼠，随后施用16%经皮纳洛酮贴剂;进行血浆纳洛酮水平的药代动力学分析。采用组织学分析来可视化微针和Solaraze®处理后的形态学变化。用微针+ Solaraze®治疗的动物显示延长的孔寿命（通过经表皮水分损失测量确定）长达7天。在用微针+ Solaraze®治疗的动物中，也观察到纳洛酮渗透增强的时间延长。未观察到微针处理或考克斯抑制导致的形态学变化。非特异性考克斯抑制是延长无毛豚鼠微针治疗后孔寿命的有效方法。这可能具有延长透皮贴剂贴敷时间的临床意义，从而增加患者对治疗的依从性。
The purpose of this study was to determine if non-specific COX inhibition could extend pore lifetime in hairless guinea pigs following microneedle treatment. Hairless guinea pigs were treated with microneedle arrays ± daily application of Solaraze® gel (3% diclofenac sodium (non-specific COX inhibitor) and 2.5% hyaluronic acid); transepidermal water loss was utilized to evaluate pore lifetime. To examine the permeation of naltrexone, additional guinea pigs were treated with microneedles ± daily Solaraze® gel followed by application of a 16% transdermal naltrexone patch; pharmacokinetic analysis of plasma naltrexone levels was performed. Histological analysis was employed to visualize morphological changes following microneedle and Solaraze® treatment. Animals treated with microneedles + Solaraze® displayed extended pore lifetime (determined by transepidermal water loss measurements) for up to 7 days. Enhanced naltrexone permeation was also observed for an extended amount of time in animals treated with microneedles + Solaraze®. No morphological changes resulting from microneedle treatment or COX inhibition were noted. Non-specific COX inhibition is an effective means of extending pore lifetime following microneedle treatment in hairless guinea pigs. This may have clinical implications for extending transdermal patch wear time and therefore increasing patient compliance with therapy.