Loading hydrophilic drug in solid lipid media as nanoparticles: Statistical modeling of entrapment efficiency and particle size

被引:123
作者
Ghadiri, Maryam [1 ]
Fatemi, Shohreh [1 ]
Vatanara, Alireza [2 ]
Doroud, Delaram [2 ]
Najafabadi, Abdolhossein Rouholamini [2 ]
Darabi, Majid [2 ]
Rahimi, Amir Abbas [3 ]
机构
[1] Univ Tehran, Coll Engn, Sch Chem Engn, Tehran, Iran
[2] Univ Tehran Med Sci, Sch Pharm, Dept Pharmaceut, Tehran, Iran
[3] Pasteur Inst Iran, Nanobiotechnol Dept, Tehran, Iran
关键词
Paromomycin; Solid lipid nanoparticles; Entrapment efficiency; Statistical modeling; PAROMOMYCIN; OPTIMIZATION;
D O I
10.1016/j.ijpharm.2011.12.037
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Solid lipid nanoparticle (SLN) is a very well tolerated carrier systems for dermal application due to the employment physiological and/or biodegradable lipids. The effects of five factors, two categorical and three quantitative factors, were studied on the mean diameter and entrapment efficiency of the produced SLNs using response surface method (RSM), D-optimal design. Two methods of microemulsion and solvent diffusion and two types of lipid, cetyl palmitate and stearic acid, were examined comparatively. The quantitative variables were studied in three levels; amount of original Paromomycin (60.90 and 120 mg), fraction of surfactant (0.5, 0.75 and 1 w/v %) and drug to lipid ratio (2,4 and 6). Mean particle size and entrapment efficiency of the loaded Paromomycin were modeled statistically and the optimal condition was determined to approach to the maximum entrapment efficiency. The drug release profile of the optimal formulated material was examined in aqueous media and 64% of the Paromomycin loaded in SLNs was gradually released during 24 h, which reveals efficient prolonged release of the drug. (C) 2011 Elsevier B.V. All rights reserved.
引用
收藏
页码:128 / 137
页数:10
相关论文
共 29 条
[1]   Optimization and physicochemical characterization of a triamcinolone acetonide-loaded NLC for ocular antiangiogenic applications [J].
Araujo, J. ;
Gonzalez-Mira, E. ;
Egea, M. A. ;
Garcia, M. L. ;
Souto, E. B. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2010, 393 (1-2) :167-175
[2]  
Arcamone M., 1977, US patent, Patent No. [4,021,601, 4021601]
[3]   Comparison of the effectiveness of two topical paromomycin treatments versus meglumine antimoniate for New World cutaneous leishmaniasis [J].
Armijos, RX ;
Weigel, MM ;
Calvopiña, M ;
Mancheno, M ;
Rodriguez, R .
ACTA TROPICA, 2004, 91 (02) :153-160
[4]  
Asilian A, 2003, B WORLD HEALTH ORGAN, V81, P353
[5]   SNEDDS containing bioenhancers for improvement of dissolution and oral absorption of lacidipine. I: Development and optimization [J].
Basalious, Emad B. ;
Shawky, Nevine ;
Badr-Eldin, Shaimaa M. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2010, 391 (1-2) :203-211
[6]  
Box G., 1976, Statistics for Experiments
[7]  
DERRINGER G, 1980, J QUAL TECHNOL, V12, P214, DOI 10.1080/00224065.1980.11980968
[8]   In vitro skin permeation and retention of paromomycin from liposomes for topical treatment of the cutaneous leishmaniasis [J].
Ferreira, LS ;
Ramaldes, GA ;
Nunan, EA ;
Ferreira, LAM .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2004, 30 (03) :289-296
[9]   Non-stealth and stealth solid lipid nanoparticles (SLN) carrying doxorubicin:: Pharmacokinetics and tissue distribution after i.v. administration to rats [J].
Fundarò, A ;
Cavalli, R ;
Bargoni, A ;
Vighetto, D ;
Zara, GP ;
Gasco, MR .
PHARMACOLOGICAL RESEARCH, 2000, 42 (04) :337-343
[10]   Effect of surfactant surface coverage on formation of solid lipid nanoparticles (SLN) [J].
Helgason, T. ;
Awad, T. S. ;
Kristbergsson, K. ;
McClements, D. J. ;
Weiss, J. .
JOURNAL OF COLLOID AND INTERFACE SCIENCE, 2009, 334 (01) :75-81