Abstract：
OBJECTIVE: This study aimed to fabricate dexamethasone sodium phosphate loaded microneedle arrays (MNA) and investigate their efficiency in combination with iontophoresis for the treatment of hind paw oedema in rats.
METHODS: Drug loaded polyvinyl alcohol, polyvinyl pyrrolidone and D-sorbitol-based MNA11 were fabricated by vacuum micromolding. Physicochemical, morphological, thermal, in-silico, in-vitro insertion ability (on parafilm) and drug release studies were performed. Ex-vivo permeation, in-vivo insertion and anti-inflammatory studies were performed in combination with iontophoresis.
RESULTS: MNA11 displayed sharp-tipped projections and acceptable physicochemical features. Differential scanning calorimetry results indicated that drug loaded MNA11 were amorphous solids. Drug interacted with PVP and PVA predominately via hydrogen bonding. Parafilm displayed conspicuously engraved complementary structure of MNA11. Within 60 min, 91.50 ± 3.1% drug released from MNA11. A significantly higher i.e., 95.06 ± 2.5% permeation of drug was observed rapidly (within 60 min) from MNA11-iontophoresis combination than MNA11 i.e., 84.07 ± 3.5% within 240 min. Rat skin treated using MNA11 and MNA11-iontophoresis showed disruptions / microchannels in the epidermis without any damage to underlying anatomical structures. MNA11-iontophoresis combination led to significant reduction (83.02 ± 3.9%) in paw oedema as compared to MNA11 alone (72.55 ± 4.1%).
CONCLUSIONS: MNA11-iontophoresis combination can act as a promising candidate to deliver drugs transcutaneously for treating inflammatory diseases.
METHODS: Drug loaded polyvinyl alcohol, polyvinyl pyrrolidone and D-sorbitol-based MNA11 were fabricated by vacuum micromolding. Physicochemical, morphological, thermal, in-silico, in-vitro insertion ability (on parafilm) and drug release studies were performed. Ex-vivo permeation, in-vivo insertion and anti-inflammatory studies were performed in combination with iontophoresis.
RESULTS: MNA11 displayed sharp-tipped projections and acceptable physicochemical features. Differential scanning calorimetry results indicated that drug loaded MNA11 were amorphous solids. Drug interacted with PVP and PVA predominately via hydrogen bonding. Parafilm displayed conspicuously engraved complementary structure of MNA11. Within 60 min, 91.50 ± 3.1% drug released from MNA11. A significantly higher i.e., 95.06 ± 2.5% permeation of drug was observed rapidly (within 60 min) from MNA11-iontophoresis combination than MNA11 i.e., 84.07 ± 3.5% within 240 min. Rat skin treated using MNA11 and MNA11-iontophoresis showed disruptions / microchannels in the epidermis without any damage to underlying anatomical structures. MNA11-iontophoresis combination led to significant reduction (83.02 ± 3.9%) in paw oedema as compared to MNA11 alone (72.55 ± 4.1%).
CONCLUSIONS: MNA11-iontophoresis combination can act as a promising candidate to deliver drugs transcutaneously for treating inflammatory diseases.
摘要：
目的：本研究旨在制备负载地塞米松磷酸钠的微针阵列（MNA），并研究其与离子电渗疗法联合治疗大鼠后爪水肿的效率。
方法：载药聚乙烯醇，聚乙烯吡咯烷酮和D-山梨醇基MNA11通过真空微成型制备。物理化学,形态学,热,在硅，进行了体外插入能力（在parafilm上）和药物释放研究。离体渗透,体内插入和抗炎研究与离子电渗疗法联合进行.
结果：MNA11显示出尖锐的突起和可接受的物理化学特征。差示扫描量热法结果表明,载药MNA11为无定形固体。药物主要通过氢键与PVP和PVA相互作用。Parafilm显示出明显雕刻的MNA11互补结构。60分钟内,从MNA11释放91.50±3.1%的药物。A明显更高，即，从MNA11-离子电渗疗法组合比MNA11快速观察到95.06±2.5%的药物渗透(在60分钟内)，即240分钟内84.07±3.5%。使用MNA11和MNA11-离子电渗疗法处理的大鼠皮肤显示表皮中的破坏/微通道,而对潜在的解剖结构没有任何损害。与单独的MNA11(72.55±4.1%)相比,MNA11-离子电渗疗法组合导致爪水肿的显著减少(83.02±3.9%)。
结论：MNA11-离子电渗疗法组合可以作为一种有希望的候选药物经皮给药治疗炎症性疾病。
方法：载药聚乙烯醇，聚乙烯吡咯烷酮和D-山梨醇基MNA11通过真空微成型制备。物理化学,形态学,热,在硅，进行了体外插入能力（在parafilm上）和药物释放研究。离体渗透,体内插入和抗炎研究与离子电渗疗法联合进行.
结果：MNA11显示出尖锐的突起和可接受的物理化学特征。差示扫描量热法结果表明,载药MNA11为无定形固体。药物主要通过氢键与PVP和PVA相互作用。Parafilm显示出明显雕刻的MNA11互补结构。60分钟内,从MNA11释放91.50±3.1%的药物。A明显更高，即，从MNA11-离子电渗疗法组合比MNA11快速观察到95.06±2.5%的药物渗透(在60分钟内)，即240分钟内84.07±3.5%。使用MNA11和MNA11-离子电渗疗法处理的大鼠皮肤显示表皮中的破坏/微通道,而对潜在的解剖结构没有任何损害。与单独的MNA11(72.55±4.1%)相比,MNA11-离子电渗疗法组合导致爪水肿的显著减少(83.02±3.9%)。
结论：MNA11-离子电渗疗法组合可以作为一种有希望的候选药物经皮给药治疗炎症性疾病。
