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由聚甘油树枝状大分子制备的亲水性水凝胶:增强紫杉醇的溶解和释放

Hydrotropic Hydrogels Prepared from Polyglycerol Dendrimers: Enhanced Solubilization and Release of Paclitaxel.

作者信息

Ooya Tooru, Lee Jaehwi

机构信息

Department of Chemical Science and Engineering, Graduate School of Engineering, Kobe University, 1-1 Rokkodai-cho, Nada-ku, Kobe 657-8501, Japan.

Center for Advanced Medical Engineering Research & Development (CAMED), Kobe University, 1-5-1 Minatojima-Minamimachi, Kobe 657-0047, Japan.

出版信息

Gels. 2022 Sep 26;8(10):614. doi: 10.3390/gels8100614.

DOI:10.3390/gels8100614
PMID:36286115
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9602152/
Abstract

Polyglycerol dendrimers (PGD) exhibit unique properties such as drug delivery, drug solubilization, bioimaging, and diagnostics. In this study, PGD hydrogels were prepared and evaluated as devices for controlled drug release with good solubilization properties. The PGD hydrogels were prepared by crosslinking using ethylene glycol diglycidylether (EGDGE). The concentrations of EGDGE and PGDs were varied. The hydrogels were swellable in ethanol for loading paclitaxel (PTX). The amount of PTX in the hydrogels increased with the swelling ratio, which is proportional to EGDGE/OH ratio, meaning that heterogeneous crosslinking of PGD made high dense region of PGD molecules in the matrix. The hydrogels remained transparent after loading PTX and standing in water for one day, indicating that PTX was dispersed in the hydrogels without any crystallization in water. The results of FTIR imaging of the PTX-loaded PGD hydrogels revealed good dispersion of PTX in the hydrogel matrix. Sixty percent of the loaded PTX was released in a sink condition within 90 min, suggesting that the solubilized PTX would be useful for controlled release without any precipitation. Polyglycerol dendrimer hydrogels are expected to be applicable for rapid release of poorly water-soluble drugs, e.g., for oral administration.

摘要

聚甘油树枝状大分子(PGD)具有独特的性能,如药物递送、药物增溶、生物成像和诊断。在本研究中,制备了PGD水凝胶并将其评估为具有良好增溶性能的控释药物装置。PGD水凝胶通过使用乙二醇二缩水甘油醚(EGDGE)交联制备。EGDGE和PGD的浓度有所变化。水凝胶在乙醇中可溶胀以负载紫杉醇(PTX)。水凝胶中PTX的量随溶胀率增加,溶胀率与EGDGE/OH比成正比,这意味着PGD的非均相交联在基质中形成了高密度的PGD分子区域。负载PTX并在水中放置一天后,水凝胶仍保持透明,表明PTX分散在水凝胶中,在水中没有任何结晶。负载PTX的PGD水凝胶的FTIR成像结果显示PTX在水凝胶基质中分散良好。60%负载的PTX在漏槽条件下90分钟内释放,这表明增溶后的PTX可用于控释而不会有任何沉淀。聚甘油树枝状大分子水凝胶有望适用于难溶性药物的快速释放,例如口服给药。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/28be2fcc906b/gels-08-00614-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/a212a72de139/gels-08-00614-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/5d741b2cb4c7/gels-08-00614-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/802369b4757d/gels-08-00614-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/4b7a1c6e778c/gels-08-00614-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/79c8ac2de8de/gels-08-00614-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/327685c3853a/gels-08-00614-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/28be2fcc906b/gels-08-00614-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/a212a72de139/gels-08-00614-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/5d741b2cb4c7/gels-08-00614-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/802369b4757d/gels-08-00614-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/4b7a1c6e778c/gels-08-00614-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/79c8ac2de8de/gels-08-00614-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/327685c3853a/gels-08-00614-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bb1e/9602152/28be2fcc906b/gels-08-00614-g007.jpg

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