Delivery of Ursolic Acid by Polyhydroxybutyrate Nanoparticles for Cancer Therapy: in silico and in vitro Studies

被引：8

作者：

Ram Kumar Pandian, Sureshbabu ^{[1
]}

Kunjiappan, Selvaraj ^{[1
]}

Pavadai, Parasuraman ^{[2
]}

Sundarapandian, Velmurugan ^{[1
]}

Chandramohan, Vivek ^{[3
]}

Sundar, Krishnan ^{[1
]}

机构：

[1] Kalasalingam Acad Res & Educ, Dept Biotechnol, Krishnankoil, Tamil Nadu, India

[2] MS Ramaiah Univ Appl Sci, Dept Pharmaceut Chem, Fac Pharm, Bengaluru, Karnataka, India

[3] Siddaganga Inst Technol, Dept Biotechnol, Tumakuru, Karnataka, India

来源：

DRUG RESEARCH | 2022年 / 72卷 / 02期

关键词：

PHB nanoparticles; plant metabolite; ursolic acid; drug delivery; EGFR; OLEANOLIC ACID; RELEASE; THYMOQUINONE; OPTIMIZATION; GROWTH; WASTE; SIZE;

D O I：

10.1055/a-1640-0009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Ursolic acid (UA), a pentacyclic triterpenoid and a phytochemical, is a potent inhibitory agent against proliferation of various tumors. Polyhydroxybutyrate nanoparticles (PHB NPs) are preferred in therapeutics due to their drug-stabilizing property and enhanced biological activity. In this study, PHB NPs were utilized to deliver and enhance the bioavailability of UA against cancer cells (HeLa). Further, molecular docking and dynamic studies were conducted to calculate the binding affinity and stability of UA at the active site of target protein (epidermal growth factor receptor-EGFR). The PHB NPs revealed the average size as 150-200 nm in TEM, which were used in subsequent experiments. The cytoplasmic uptake of nanoparticles was confirmed by florescent microscopy. The encapsulation potential of PHB NPs with UA was assessed by UV-visible spectrophotometer as 54 %. Besides, the drug release behavior, cytotoxicity and the regulation of apoptosis were investigated in vitro. The cytotoxicity results revealed that the maximum efficiency of drug delivery was at 96th hour.

引用

页码：72 / 81

页数：10

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