Microparticles based on chitosan/carboxymethylcellulose polyelectrolyte complexes for colon delivery of vancomycin

被引:82
作者
Cerchiara, T. [1 ]
Abruzzo, A. [1 ]
Parolin, C. [1 ]
Vitali, B. [1 ]
Bigucci, F. [1 ]
Gallucci, M. C. [2 ]
Nicoletta, F. P. [3 ]
Luppi, B. [1 ]
机构
[1] Univ Bologna, Dept Pharm & Biotechnol, Via San Donato 19-2, I-40127 Bologna, Italy
[2] Univ Calabria, Dept Chem & Chem Technol, Via P Bucci, I-87036 Arcavacata Di Rende, CS, Italy
[3] Univ Calabria, Dept Pharm Hlth & Nutr Sci, Edificio Polifunz, I-87036 Arcavacata Di Rende, CS, Italy
关键词
Polyelectrolyte complexes; Chitosan; Carboxymethylcellulose; Vancomycin; Colon-specific delivery; DRUG-DELIVERY; IN-VITRO; CONTROLLED-RELEASE; CHITOSAN; FORMULATION; SYSTEM; NANOPARTICLES; MICROSPHERES; GUIDELINES; MANAGEMENT;
D O I
10.1016/j.carbpol.2016.02.020
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
The aim of this work was to prepare polyelectrolyte complexes based on chitosan (CH) and carboxymethylcellulose (CMC) for colon delivery of vancomycin (VM). Various batches of polyelectrolyte complexes, using three different CH/CMC weight ratios (3:1, 1:1 and 1:3), were prepared and collected as microparticles by spray-drying process. Microparticles were characterized in terms of yield, encapsulation efficiency, drug loading, morphology and mucoadhesion properties. Microparticles water-uptake and VM release as well as its protection against gastric pepsin degradation were also investigated. Finally, the antibacterial activity against Staphylococcus aureus, a Gram-positive model strain, was evaluated. The best formulation CH/CMC 1:3 was selected based on the encapsulation efficiency, water-uptake and drug release rate. Moreover, microparticles were able to prevent VM degradation and showed a good antibacterial activity against S. aureus. Finally, to improve the release of VM in the colon the selected formulation was coated with lauric acid. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码:124 / 130
页数:7
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