Development of Eudragit RS 100 Microparticles Loaded with Ropinirole: Optimization and In Vitro Evaluation Studies

被引:23
作者
Kashif, Prince Muhammad [1 ]
Madni, Asadullah [1 ]
Ashfaq, Muhammad [1 ]
Rehman, Mubashar [1 ]
Mahmood, Muhammad Ahmad [1 ]
Khan, Muhammad Imran [1 ]
Tahir, Nayab [1 ]
机构
[1] Islamia Univ Bahawalpur, Fac Pharm & Alternat Med, Dept Pharm, Bahawalpur 63100, Punjab, Pakistan
来源
AAPS PHARMSCITECH | 2017年 / 18卷 / 05期
关键词
Box-Behnken design; emulsion solvent evaporation; Eudragit RS 100; microparticles; ropinirole; SOLVENT EVAPORATION METHOD; PARKINSONS-DISEASE; DRUG-RELEASE; FORMULATION OPTIMIZATION; PLGA MICROPARTICLES; FACTORIAL DESIGN; MICROSPHERES; MICROENCAPSULATION; DELIVERY; ETHYLCELLULOSE;
D O I
10.1208/s12249-016-0653-5
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The current study aimed to develop novel pH independent microparticles loaded with ropinirole (ROP) for sustained drug release. Eudragit RS 100 was used as release retardant and microparticles were fabricated by oil-in-oil emulsion solvent evaporation method. A three-factor three-level Box-Behnken design using Design-Expert software was employed to optimize formulation variables. Ropinirole loaded microparticles were evaluated with respect to morphology, particle size, encapsulation efficiency, and in vitro release profile. Optical microscopy and SEM micrographs indicated spherical shape with smooth surface and well-defined boundary. The particle size was in the range of 98.86 to 236.29 mu m, being significantly increased with increasing polymer concentration. Higher polymer load also increased the thickness of internal polymer network, which led to reduced drug loss and higher entrapment efficiency (89%). The cumulative in vitro release was found to be in the range of 54.96 to 99.36% during the release studies (12 h) following zero order release kinetics and non-Fickian diffusion pattern. The developed microparticles have the potential to sustain the release of ropinirole, which may lead to a reduction in its adverse effects and improved management of Parkinson's disease.
引用
收藏
页码:1810 / 1822
页数:13
相关论文
共 55 条
[11]   Preparation and characterization of poly(lactic-co-glycolic acid) microspheres loaded with a labile antiparkinson prodrug [J].
D'Aurizio, E. ;
van Nostrum, C. F. ;
van Steenbergen, M. J. ;
Sozio, P. ;
Siepmann, F. ;
Siepmann, J. ;
Hennink, W. E. ;
Di Stefano, A. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2011, 409 (1-2) :289-296
[12]   Development of albendazole sulfoxide-loaded Eudragit microparticles: A potential strategy to improve the drug bioavailability [J].
de Souza, Marina Claro ;
Marchetti, Juliana Maldonado .
ADVANCED POWDER TECHNOLOGY, 2012, 23 (06) :801-807
[13]  
Dehghan S, 2010, AFR J PHARM PHARMACO, V4, P346
[14]   Aceclofenac microspheres: Quality by design approach [J].
Deshmukh, Rameshwar K. ;
Naik, Jitendra B. .
MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS, 2014, 36 :320-328
[15]  
Devrim Burcu, 2006, Acta Pol Pharm, V63, P521
[16]  
Dubey R, 2009, DEFENCE SCI J, V59, P82
[17]  
El-Bagory I.M., 2007, SAUDI PHARM J, V15, P213
[18]   Development and evaluation of sustained-release clonidine-loaded PLGA microparticles [J].
Gaignaux, Amelie ;
Reeff, Jonathan ;
Siepmann, Florence ;
Siepmann, Juergen ;
De Vriese, Carine ;
Goole, Jonathan ;
Amighi, Karim .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2012, 437 (1-2) :20-28
[19]   Enhanced bioavailability of lacidipine via microemulsion based transdermal gels: Formulation optimization, ex vivo and in vivo characterization [J].
Gannu, Ramesh ;
Palem, Chinna Reddy ;
Yamsani, Vamshi Vishnu ;
Yamsani, Shravan Kumar ;
Yamsani, Madhusudan Rao .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2010, 388 (1-2) :231-241
[20]   Drug development in Parkinson's disease: From emerging molecules to innovative drug delivery systems [J].
Garbayo, E. ;
Ansorena, E. ;
Blanco-Prieto, M. J. .
MATURITAS, 2013, 76 (03) :272-278