Controlled release studies of antimalarial 1, 3, 5-trisubstituted-2-pyrazolines from biocompatible chitosan-heparin Layer-by-Layer (LbL) self assembled thin films

被引:16
作者
Bhalerao, Uma M. [1 ]
Valiveti, Aditya Kapil [1 ]
Acharya, Jyotiranjan [1 ]
Halve, Anand K. [2 ]
Kaushik, Mahabir Parshad [1 ]
机构
[1] Def Res & Dev Estab, Proc Technol Dev Div, Gwalior 474002, Madhya Pradesh, India
[2] Jiwaji Univ, Sch Studies Chem, Gwalior 474011, Madhya Pradesh, India
关键词
Polyelectrolytes; Biocompatible; Antimalarials; Quartz crystal microbalance; Controlled release; IONIC-STRENGTH; DELIVERY; DRUG; ACID; FORMULATIONS; MULTILAYERS; DERIVATIVES; ARTEMETHER; EFFICACY; PH;
D O I
10.1016/j.colsurfb.2014.11.016
中图分类号
Q6 [生物物理学];
学科分类号
071011 ;
摘要
Herein we report the in-vitro controlled release properties of 1, 3, 5-trisubstituted-2-pyrazolines through Layer-by-Layer (LbL) self assembled thin films fabricated from chitosan and heparin sodium salt as biocompatible polyelectrolytes. This study was carried out as a preliminary step towards the applicability of LbL technique in prophylactic drug delivery of antimalarial drugs. The growth of LbL self assembly was monitored by UV-Visible spectrophotometry and Quartz Crystal Microbalance (QCM). The loading as well as in-vitro release studies (in phosphate buffer saline at pH 7.4) were carried out using UV-Visible spectroscopy. Three compounds having good antimalarial activity were tested and the release rate was found inversely proportional to the hydrophobicity of the drug. Pzln-4 has shown best release among all the three compounds (up to 780 min) followed by Pzln-5 and Pzln-8. The release trend was that of a fast release up to first 2 h followed by a steady release. Kinetic fitting of the data confirmed the process of drug release followed a pseudo second order kinetics (R-2 >= 0.99). A large value of rate constant (k) revealed a faster release. Pzln-4 has shown smallest value of k corresponding to slowest release among all the three compounds. (C) 2014 Elsevier B.V. All rights reserved.
引用
收藏
页码:151 / 159
页数:9
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