Anti-cancerous efficacy and pharmacokinetics of 6-mercaptopurine loaded chitosan nanoparticles

被引：32

作者：

Kumar, G. Prem ^{[1
,2
]}

Sanganal, Jagadeesh S. ^{[2
]}

Phani, A. R. ^{[3
]}

Manohara, C. ^{[2
]}

Tripathi, Syamantak M. ^{[4
]}

Raghavendra, H. L. ^{[5
]}

Janardhana, P. B. ^{[6
]}

Amaresha, S. ^{[2
]}

Swamy, K. B. ^{[2
]}

Prasad, R. G. S. V. ^{[7
]}

机构：

[1] Bioneeds India Private Ltd, Dept Toxicol, Bangalore, Karnataka, India

[2] Vet Coll, Dept Vet Pharmacol & Toxicol, Bangalore, Karnataka, India

[3] Nano Res Adv Mat & Technol, Bangalore, Karnataka, India

[4] Coll Vet Sci & Anim Husb, Durg, Chhattisgarh, India

[5] Wollega Univ, Coll Med & Hlth Sci, Sch Med, Nekemte, Ethiopia

[6] Stellixir Biotech Private Ltd, Bangalore, Karnataka, India

[7] Asian Metropolitan Univ, Fac Pharmaceut Sci, Selangor, Kualalumpur, Malaysia

来源：

PHARMACOLOGICAL RESEARCH | 2015年 / 100卷

关键词：

Chitosan nanoparticles; Cytotoxic; Apoptosis; ROS and bioavailability; ACUTE LYMPHOBLASTIC-LEUKEMIA; CELL-CYCLE; IN-VIVO; DRUG; MERCAPTOPURINE; DERIVATIVES; PROGRESSION; ABROGATION; HYDROGELS; DESIGN;

D O I：

10.1016/j.phrs.2015.07.025

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

6-Mercaptopurine is a cytotoxic and immunosuppressant drug. The use of this drug is limited due to its poor bioavailability and short plasma half-life. In order to nullify these drawbacks, 6-mercaptopurine-chitosan nanoparticles (6-MP-CNPs) were prepared and evaluated to study the influence of preparation conditions on the physicochemical properties by using DLS, SEM, XRD and FTIR. The in vitro drug release profile at pH 4.8 and 7.4 revealed sustained release patterns for a period of 2 days. The nanoformulations showed enhanced in vitro anti-cancer activities (MU assay, apoptosis assay, cell cycle arrest and ROS indices) on HT-1080 and MCF-7 cells. In vivo pharmacokinetics profiles of 6-MP-CNPs showed improved bioavailability. Thus, the results of the present study revealed that, the prepared 6-MP-CNPs have a significant role in increasing anti-cancer efficacy, bioavailability and in vivo pharmacokinetics profiles. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：47 / 57

页数：11

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