首页|基质组成对抗肿瘤药物白藜芦醇可溶性微针成型及其穿透性的影响

基质组成对抗肿瘤药物白藜芦醇可溶性微针成型及其穿透性的影响

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目的 评估微针基质组成对白藜芦醇可溶性微针(Res-DMNs)成型性及穿透性能的影响,以提高抗肿瘤药物白藜芦醇的经皮递送效率.方法 采用多步减压扩散法制备Res-DMNs,以成膜性、平整度、气泡数和含针率为考察指标,对聚乙烯醇(PVA)不同聚合度的单一基质材料(PVA-0488、PVA-0588、PVA-1788)以及PVA与聚乙烯吡咯烷酮(PVP-K30)混合体系进行成型性评价,以确定最佳混合比例,并对制得的可溶性微针的形貌、溶解性能、机械性能、体外穿刺性能和离体皮肤穿刺效率进行全面评价.结果 采用PVA-0588与PVP-K30混合基质(2∶1,体积比)制备的Res-DMNs,其含针率可达90%以上,针长约为720 μm,针尖距离约800 μm;在刺入皮肤后10 min内,微针几乎完全溶解;通过固定皮肤组织测量,Res-DMNs的刺入深度平均为(535.23±87.24)μm,且刺入率达到92.4%.结论 可溶性微针的成型性和穿透性能是其临床应用成功的关键,本研究确定了适宜的基质材料组成,为保证Res-DMNs治疗效果提供了基础.
The impact of matrix composition on the needle formation and penetration of soluble microneedles containing anti-tumor drug resveratrol
Objective To evaluate how the composition of the microneedle matrix influences the formability and penetration performance of resveratrol-soluble microneedles,so as to improve the transdermal delivery efficiency of resveratrol,an anti-tumor drug.Methods Resveratrol-soluble microneedles(Res-DMNs)were prepared by utilizing a multi-step reduced pressure diffusion method.The formability of single-matrix materials with varying degrees of polyvinyl alcohol(PVA)polymerization(PVA-0488,PVA-0588,PVA-1788)and a mixed PVA and polyvinylpyrrolidone(PVP-K30)system were assessed with the film-forming ability,smoothness,bubble count,and needle density as indexes to establish the optimal mixing ratio.The morphology,dissolution performance,mechanical properties,in vitro puncture performance,and ex vivo skin puncture efficiency of the microneedles were then thoroughly evaluated.Results The microneedles fabricated with a PVA-0588 and PVP-K30 mixed matrix demonstrated a needle density exceeding 90%.The microneedle patch featured needle length of approximately 720 μm and tip spacing of about 800 μm.After insertion into the skin,the microneedles were almost completely dissolved within 10 minutes.By measuring fixed skin tissue,the mean puncture depth of the microneedles was(535.23±87.24)μm,accompanied by a puncture rate of 92.4%.Conclusion The formability and penetration performance of resveratrol-soluble microneedles are paramount for their clinical application.The findings have identified an optimal matrix composition,laying a robust foundation for the therapeutic efficacy of these microneedles.These attributes are essential for the clinical application of microneedles,with the suitable matrix material composition being crucial for their therapeutic effectiveness.

resveratrolanticancer agentsdissolving microneedlestransdermal drug deliverypenetrativity

方泽慧、黄仨、廖丽琪、伍国羽、潘育方

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东莞市滨海湾中心医院,广东 东莞 523000

广东药科大学药学院,广东 广州 510006

广东药科大学新药研发中心,广东 广州 510006

白藜芦醇 可溶性微针 抗肿瘤药物 经皮递送 穿透性

2024

广东药科大学学报
广东药学院

广东药科大学学报

CSTPCD
影响因子:0.698
ISSN:1006-8783
年,卷(期):2024.40(4)