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基于载药适配体偶联脂质体的制剂作为基底细胞癌局部治疗的可行策略——体外试验

Formulations Based on Drug Loaded Aptamer-Conjugated Liposomes as a Viable Strategy for the Topical Treatment of Basal Cell Carcinoma-In Vitro Tests.

作者信息

Cadinoiu Anca N, Rata Delia M, Atanase Leonard I, Mihai Cosmin T, Bacaita Simona E, Popa Marcel

机构信息

Faculty of Medical Dentistry, "Apollonia" University of Iasi, 700511 Iasi, Romania.

Department of Experimental and Applied Biology, NIRDBS-Institute of Biological Research Iasi, 700107 Iasi, Romania.

出版信息

Pharmaceutics. 2021 Jun 11;13(6):866. doi: 10.3390/pharmaceutics13060866.

DOI:10.3390/pharmaceutics13060866
PMID:34208362
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8231244/
Abstract

Topical liposomal drug formulations containing AS1411-aptamer conjugated liposomes were designed to deliver in a sustained way the 5-fluorouracil to the tumor site but also to increase the compliance of patients with basal cell carcinoma. The 5-fluorouracil penetrability efficiency through the Strat-M membrane and the skin irritation potential of the obtained topical liposomal formulations were evaluated in vitro and the Korsmeyer Peppas equation was considered as the most appropriate to model the drug release. Additionally, the efficiency of cytostatic activity for targeted antitumor therapy and the hemolytic capacity were performed in vitro. The obtained results showed that the optimal liposomal formulation is a crosslinked gel based on sodium alginate and hyaluronic acid containing AS1411-aptamer conjugated liposomes loaded with 5-fluorouracil, which appeared to have favorable biosafety effects and may be used as a new therapeutic approach for the topical treatment of basal cell carcinoma.

摘要

含有AS1411适配体缀合脂质体的局部脂质体药物制剂旨在以持续的方式将5-氟尿嘧啶递送至肿瘤部位，同时提高基底细胞癌患者的依从性。在体外评估了5-氟尿嘧啶透过Strat-M膜的渗透效率以及所获得的局部脂质体制剂的皮肤刺激潜力，并且认为Korsmeyer Peppas方程是模拟药物释放最合适的方程。此外，还进行了靶向抗肿瘤治疗的细胞抑制活性效率和溶血能力的体外研究。所得结果表明，最佳脂质体制剂是基于海藻酸钠和透明质酸的交联凝胶，其含有负载5-氟尿嘧啶的AS1411适配体缀合脂质体，该制剂似乎具有良好的生物安全效应，可用作基底细胞癌局部治疗的新方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/b128d01612f8/pharmaceutics-13-00866-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/5dd94bdb86f0/pharmaceutics-13-00866-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/bdb74d7e89af/pharmaceutics-13-00866-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/9aa313dc1f28/pharmaceutics-13-00866-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/7addcbe0439c/pharmaceutics-13-00866-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/a762aab7076b/pharmaceutics-13-00866-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/a9dc272e1cb3/pharmaceutics-13-00866-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/b128d01612f8/pharmaceutics-13-00866-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/5dd94bdb86f0/pharmaceutics-13-00866-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/bdb74d7e89af/pharmaceutics-13-00866-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/9aa313dc1f28/pharmaceutics-13-00866-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/7addcbe0439c/pharmaceutics-13-00866-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/a762aab7076b/pharmaceutics-13-00866-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/a9dc272e1cb3/pharmaceutics-13-00866-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/8231244/b128d01612f8/pharmaceutics-13-00866-g007.jpg

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