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微阵列贴片辅助经皮递增高剂量布洛芬钠,使用热敏性海藻酸钠/聚(乙烯己内酰胺)原位凝胶储库。

Micro array patch assisted transdermal delivery of high dose, ibuprofen sodium using thermoresponsive sodium alginate/poly (vinylcaprolactam) in situ gels depot.

机构信息

Centre for Eye and Vision Research, 17W Science Park, Hong Kong.

College of Pharmacy, University of Sargodha Punjab, Pakistan.

出版信息

Int J Biol Macromol. 2023 Dec 1;252:126464. doi: 10.1016/j.ijbiomac.2023.126464. Epub 2023 Aug 23.

Abstract

Current study reports the combined technique of microneedle array patches and thermoresponsive gels. Microneedles array patch mediated insitu skin depots were evaluated for sustain drug delivery using sodium alginate/Poly (vinylcaprolactam) thermoresponsive gels. Their phase transition property from sol-gel state was monitored with AR2000 rheometer. Ibuprofen sodium was loaded in optimized formulations. The non-soluble cross-linked microneedle array patches (MAPs) were prepared from variable biocompatible polymers using silicone micromoulds. The fabricated MAPs were evaluated for mechanical stability, inskin dissolution, insertion forces and moisture contents. The penetration depth of MAPs in neonatal rabbit skin was tracked by optical coherence tomography. The optimized MAPs (GP10000) were used as microporation source in skin owing to their stable nature. Pores formation in skin samples after MAPs treatment was confirmed by optical coherence tomography, dye binding and skin integrity analysis. The invitro permeation of Ibuprofen sodium from formulations was studied using Franz cells across intact skin and MAPs applied skin. It was concluded from the results that Ibuprofen sodium permeation was observed for longer time through MAPs treated skin as compared to intact skin. Confocal study confirmed the diffusion of drug loaded formulations in deeper tissues with higher intensity.

摘要

本研究报告了微针阵列贴剂和温敏凝胶的联合技术。使用海藻酸钠/聚(乙烯己内酯)温敏凝胶评估了微针阵列贴剂介导的原位皮肤储库以实现持续药物递送。使用 AR2000 流变仪监测其从溶胶-凝胶状态向凝胶-溶胶状态的相转变特性。将布洛芬钠载入优化的配方中。使用硅酮微模具,从各种生物相容性聚合物制备不可溶性交联微针阵列贴片(MAPs)。评估了制备的 MAPs 的机械稳定性、在皮肤中的溶解、插入力和水分含量。通过光学相干断层扫描跟踪 MAPs 在新生兔皮中的穿透深度。由于其稳定的性质,优化的 MAPs(GP10000)被用作皮肤的微孔源。通过光学相干断层扫描、染料结合和皮肤完整性分析确认 MAPs 处理后皮肤中的孔形成。使用 Franz 细胞在完整皮肤和应用 MAPs 的皮肤上研究了布洛芬钠从制剂中的体外渗透。结果表明,与完整皮肤相比,通过 MAPs 处理的皮肤观察到布洛芬钠更长时间的渗透。共聚焦研究证实,负载药物的制剂在更深的组织中以更高的强度扩散。

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