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含β-环糊精的多糖冷冻凝胶用于大麻二酚的递送

Polysaccharide Cryogels Containing β-Cyclodextrin for the Delivery of Cannabidiol.

作者信息

Momekova Denitsa, Danov Yavor, Momekov Georgi, Ivanov Ervin, Petrov Petar

机构信息

Faculty of Pharmacy, Medical University of Sofia, 1000 Sofia, Bulgaria.

Institute of Polymers, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.

出版信息

Pharmaceutics. 2021 Oct 23;13(11):1774. doi: 10.3390/pharmaceutics13111774.

DOI:10.3390/pharmaceutics13111774
PMID:34834189
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8618209/
Abstract

Cannabidiol (CBD) has attracted increasing interest due to its therapeutic potential for treating numerous diseases. However, CBD is very lipophilic and has very unfavorable pharmacokinetics and low bioavailability. Efforts are focused on developing drug delivery systems for enhanced solubilization and therapeutic activity of CBD. Here, we report the preparation of original super-macroporous cryogels from 2-hydroxyethyl cellulose (HEC) and β-cyclodextrin (β-CD) designed for the topical delivery of CBD. The cryogels were synthesized by photochemical crosslinking in a frozen aqueous system, purified, and then loaded with CBD. The effect of HEC/β-CD mass ratio (100:0; 50:50; 40:60 and 20:80) in the reaction mixture on the reaction efficiency, physico-mechanical properties of cryogels, drug release profile, and antineoplastic potential were evaluated in detail. The cryogels showed a bi-phasic release behavior: initial burst release in the first 3 hours followed by slower drug release which can be beneficial in the treatment of cutaneous neoplastic diseases.

摘要

大麻二酚（CBD）因其在治疗多种疾病方面的治疗潜力而受到越来越多的关注。然而，CBD具有很强的亲脂性，其药代动力学特性不佳，生物利用度较低。目前的研究重点是开发药物递送系统，以提高CBD的溶解度和治疗活性。在此，我们报告了由2-羟乙基纤维素（HEC）和β-环糊精（β-CD）制备的新型超大孔冷冻凝胶，该冷冻凝胶专为CBD的局部递送而设计。冷冻凝胶通过在冷冻水体系中进行光化学交联合成，经过纯化后再负载CBD。详细评估了反应混合物中HEC/β-CD质量比（100:0；50:50；40:60和20:80）对反应效率、冷冻凝胶的物理机械性能、药物释放曲线和抗肿瘤潜力的影响。冷冻凝胶呈现出双相释放行为：在最初3小时内出现初始突释，随后药物释放较慢，这可能对皮肤肿瘤疾病的治疗有益。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/85778d45bbeb/pharmaceutics-13-01774-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/bacaec32e080/pharmaceutics-13-01774-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/ed177125f6a2/pharmaceutics-13-01774-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/7d78a697a0ea/pharmaceutics-13-01774-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/29bd4e76974e/pharmaceutics-13-01774-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/050ef6f71293/pharmaceutics-13-01774-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/e6b88a4dd7a0/pharmaceutics-13-01774-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/5dc5c333e89d/pharmaceutics-13-01774-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/85778d45bbeb/pharmaceutics-13-01774-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/bacaec32e080/pharmaceutics-13-01774-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/ed177125f6a2/pharmaceutics-13-01774-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/7d78a697a0ea/pharmaceutics-13-01774-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/29bd4e76974e/pharmaceutics-13-01774-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/050ef6f71293/pharmaceutics-13-01774-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/e6b88a4dd7a0/pharmaceutics-13-01774-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/5dc5c333e89d/pharmaceutics-13-01774-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b9b/8618209/85778d45bbeb/pharmaceutics-13-01774-g008.jpg

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