Chitosan nanoparticles for prolonged delivery of timolol maleate

被引:56
作者
Agnihotri, Sunil A. [1 ]
Aminabhavi, Tejraj M. [1 ]
机构
[1] Karnatak Univ, Ctr Excellence Polymer Sci, Drug Delivery Div, Dharwad 580003, Karnataka, India
关键词
chitosan; nanoparticles; timolol maleate; controlled release; desolvation; factorial design;
D O I
10.1080/03639040701384942
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Timolol maleate-loaded chitosan (CS) nanoparticles were prepared by desolvation method. Experimental variables such as molecular weight of CS and amount of crosslinking agent were varied to study their effect on drug entrapment efficiency, size and release rates of nanoparticles. Chemical stability of timolol maleate (TM) and crosslinking of CS were confirmed by Fourier transform infrared spectroscopy. Differential scanning calorimetric studies were performed on drug-loaded nanoparticles to investigate crystalline nature of the drug after entrapment. Results indicated amorphous dispersion of drug in the polymer matrix. Scanning electron microscopy revealed irregularly shaped particles. Mean particle size of nanoparticles ranged between 118 and 203 nm, while zeta potential ranged between +17 and +22 mV. Entrapment efficiency of nanoparticles ranged between 47.6 and 63.0%. In-vitro release studies were performed in phosphate buffer saline of pH 7.4. A slow release of TM up to 24 h was observed. A 3 2 full factorial design was employed and secondorder regression models were used to study the response (% drug release at 4 h). Release data as analyzed by an empirical relationship suggested that drug release deviated from the Fickian trend.
引用
收藏
页码:1254 / 1262
页数:9
相关论文
共 33 条
[1]   Improved pharmacodynamics of timolol maleate from a mucoadhesive niosomal ophthalmic drug delivery system [J].
Aggarwal, D ;
Kaur, IP .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2005, 290 (1-2) :155-159
[2]   Controlled release of clozapine through chitosan microparticles prepared by a novel method [J].
Agnihotri, SA ;
Aminabhavi, TM .
JOURNAL OF CONTROLLED RELEASE, 2004, 96 (02) :245-259
[3]   Recent advances on chitosan-based micro- and nanoparticles in drug delivery [J].
Agnihotri, SA ;
Mallikarjuna, NN ;
Aminabhavi, TM .
JOURNAL OF CONTROLLED RELEASE, 2004, 100 (01) :5-28
[4]   Rheological properties and drug release characteristics of pH-responsive hydrogels [J].
Aminabhavi, TM ;
Agnihotri, SA ;
Naidu, BVK .
JOURNAL OF APPLIED POLYMER SCIENCE, 2004, 94 (05) :2057-2064
[5]   EFFECT OF CHITOSAN ON THE PERMEABILITY OF MONOLAYERS OF INTESTINAL EPITHELIAL-CELLS (CACO-2) [J].
ARTURSSON, P ;
LINDMARK, T ;
DAVIS, SS ;
ILLUM, L .
PHARMACEUTICAL RESEARCH, 1994, 11 (09) :1358-1361
[6]   Evaluation of cationic polymer-coated nanocapsules as ocular drug carriers [J].
Calvo, P ;
VilaJato, JL ;
Alonso, MJ .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1997, 153 (01) :41-50
[7]   The effect of a PEG versus a chitosan coating on the interaction of drug colloidal carriers with the ocular mucosa [J].
De Campos, AM ;
Sánchez, A ;
Gref, R ;
Calvo, P ;
Alonso, MJ .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2003, 20 (01) :73-81
[8]   Chitosan nanoparticles:: a new vehicle for the improvement of the delivery of drugs to the ocular surface.: Application to cyclosporin A [J].
De Campos, AM ;
Sánchez, A ;
Alonso, MJ .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 224 (1-2) :159-168
[9]   Effect of chitosan on in vitro release and ocular delivery of ofloxacin from erodible inserts based on poly(ethylene oxide) [J].
Di Colo, G ;
Zambito, Y ;
Burgalassi, S ;
Serafini, A ;
Saettone, MF .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 248 (1-2) :115-122
[10]   In vitro and in vivo evaluation of Pluronic F127-based ocular delivery system for timolol maleate [J].
El-Kamel, AH .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 241 (01) :47-55