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双重作用脂质体制剂的物理化学特性:抗癌和抗菌作用

Physicochemical characterization of dual action liposomal formulations: anticancer and antimicrobial.

作者信息

Das Asmita, Konyak Pangwan M, Das Argha, Dey Subrata Kumar, Saha Chabita

机构信息

Department of Biotechnology, Maulana Abul Kalam Azad University of Technology, NH-12, Simhat, Haringhata, Nadia- 741249 and BF-142, Salt Lake, Kolkata, 700 064, India.

出版信息

Heliyon. 2019 Aug 27;5(8):e02372. doi: 10.1016/j.heliyon.2019.e02372. eCollection 2019 Aug.

Abstract

BACKGROUND

Cancer till date remains one of the world's most life threatening disease accompanied by risk of secondary infections. Therefore formulations carrying anticancer drugs which can also decrease the risk of secondary infection are inevitable. Chemotherapeutic drug doxorubicin along with flavonoids quercetin and epigallocatechin gallate (EGCG) is simultaneously loaded on liposomal formulation exploiting the amphiphilic property of the liposomes.

RESULTS

Atomic force microscope imaging reveal the size of liposomal formulation loaded with doxorubicin, quercetin and EGCG to be greater than void liposome confirming the presence of drugs. Liposomal stability is improved by PEGylation; adding to the drug release time . The charge of phosphatidylcholine is rendered positive by coating the formulation with histone. The average size of the formulation is 342 nm. The encapsulation efficiency of doxorubicin, quercetin and EGCG is found to be 65.8%, 96.8% and 98% respectively. The above formulation demonstrated both anticancer and antimicrobial activity.

CONCLUSION

The formulation will provide dual anticancer and antimicrobial therapy thereby evading secondary infection in cancer patients along with chemotherapy.

摘要

背景

迄今为止,癌症仍然是世界上最具生命威胁的疾病之一,并伴有继发感染的风险。因此,携带抗癌药物且能降低继发感染风险的制剂是必不可少的。利用脂质体的两亲性,将化疗药物阿霉素与类黄酮槲皮素和表没食子儿茶素没食子酸酯(EGCG)同时负载于脂质体制剂中。

结果

原子力显微镜成像显示,负载阿霉素、槲皮素和EGCG的脂质体制剂的尺寸大于空白脂质体,证实了药物的存在。聚乙二醇化提高了脂质体的稳定性,延长了药物释放时间。通过用组蛋白包被制剂,使磷脂酰胆碱带正电荷。制剂的平均尺寸为342纳米。阿霉素、槲皮素和EGCG的包封率分别为65.8%、96.8%和98%。上述制剂表现出抗癌和抗菌活性。

结论

该制剂将提供双重抗癌和抗菌治疗,从而在癌症患者化疗期间避免继发感染。

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