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通过热熔法制备的用于辣椒素缓释的无溶剂聚己内酯溶解微针

Solvent-Free Polycaprolactone Dissolving Microneedles Generated via the Thermal Melting Method for the Sustained Release of Capsaicin.

作者信息

Eum Jaehong, Kim Youseong, Um Daniel Junmin, Shin Jiwoo, Yang Huisuk, Jung Hyungil

机构信息

Department of Biotechnology, Yonsei University, Seoul 03722, Korea.

JUVIC Inc., Seoul 08389, Korea.

出版信息

Micromachines (Basel). 2021 Feb 8;12(2):167. doi: 10.3390/mi12020167.

Abstract

(1) Background: Dissolving microneedles (DMNs), a transdermal drug delivery system, have been developed to treat various diseases in a minimally invasive, painless manner. However, the currently available DMNs are based on burst release systems due to their hydrophilic backbone polymer. Although hydrophobic biodegradable polymers have been employed on DMNs for sustained release, dissolution in an organic solvent is required for fabrication of such DMNs. (2) Method: To overcome the aforementioned limitation, novel separable polycaprolactone (PCL) DMNs (SPCL-DMNs) were developed to implant a PCL-encapsulated drug into the skin. PCL is highly hydrophobic, degrades over a long time, and has a low melting point. Under thermal melting, PCL encapsulated capsaicin and could be fabricated into a DMN without the risk of toxicity from an organic solvent. (3) Results: Optimized SPCL-DMNs, containing PCL (height 498.3 ± 5.8 µm) encapsulating 86.66 ± 1.13 µg capsaicin with a 10% (/) polyvinyl alcohol and 20% (/) polyvinylpyrrolidone mixture as a base polymer, were generated. Assessment of the drug release profile revealed that this system could sustainably release capsaicin for 15 days from PCL being implanted in porcine skin. (4) Conclusion: The implantable SPCL-DMN developed here has the potential for future development of toxicity-free, sustained release DMNs.

摘要

(1) 背景:溶蚀性微针(DMNs)作为一种经皮给药系统,已被开发用于以微创、无痛的方式治疗各种疾病。然而,由于其亲水性主链聚合物,目前可用的DMNs基于速释系统。尽管疏水性可生物降解聚合物已被用于DMNs以实现持续释放,但制造此类DMNs需要在有机溶剂中溶解。(2) 方法:为克服上述局限性,开发了新型可分离聚己内酯(PCL)微针(SPCL-DMNs),用于将PCL包裹的药物植入皮肤。PCL高度疏水,降解时间长,熔点低。在热熔条件下,PCL包裹辣椒素,可制成微针,而无有机溶剂毒性风险。(3) 结果:生成了优化的SPCL-DMNs,其包含PCL(高度498.3±5.8 µm)包裹86.66±1.13 µg辣椒素,并以10%(/)聚乙烯醇和20%(/)聚乙烯吡咯烷酮混合物作为基础聚合物。对药物释放曲线的评估表明,该系统可从植入猪皮肤的PCL中持续释放辣椒素15天。(4) 结论:此处开发的可植入SPCL-DMN具有未来开发无毒、持续释放DMNs的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2cd8/7914501/6cee8b32bbc6/micromachines-12-00167-g001.jpg

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