Formulation and In Vitro Evaluation of Gelatin Nanospheres for the Oral Delivery of Selegiline

被引:0
作者
Al-Dhubiab, Bandar E. [1 ]
机构
[1] King Faisal Univ, Coll Clin Pharm, Dept Pharmaceut Sci, Al Hasa, Saudi Arabia
关键词
Selegiline; nanospheres; gelatin; in vitro; release kinetics; L-DEPRENYL SELEGILINE; CONTROLLED-RELEASE; PARKINSONS-DISEASE; TRANSDERMAL SYSTEM; NANOPARTICLES; OPTIMIZATION; PHARMACOKINETICS; HYDROCHLORIDE; MICROSPHERES; LUNGS;
D O I
10.2174/157341313805117866
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
A controlled drug delivery system which provides stable plasma concentration could be the most appropriate dosage form for the successful delivery of selegiline. The objective of this study was to develop nanospheres of selegiline using gelatin and evaluate in vitro for the feasibility of oral delivery. Nanospheres of selegiline were prepared by spray drying method and evaluated for compatibility, particle size, surface morphology and in vitro drug release. Compatibility studies indicate no interaction between selegiline and gelatin. Moderate production recovery (89.52 +/- 3.71%) and high drug content (98.41 +/- 1.22%) were observed for the prepared formulation. Scanning electron microscopy images indicate that the prepared nanospheres possess round external smooth surface with a continuous wall, although they were shriveled. In vitro drug release profile suggests two phase drug release, an initial burst release followed by a slow release over an extended period of time (similar to 10 h). The release kinetics indicates higher regression coefficient values (R-2 = 0.9641) with Korsmeyer-Peppas fit, suggesting that the release of the drug primarily governed by Fick's law of diffusion. The in vitro data provided above indicate that the newly developed gelatin nanospheres have the desired characteristics for the controlled delivery of selegiline by oral route, which necessitate further in vivo studies.
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页码:21 / 25
页数:5
相关论文
共 33 条
[1]  
Azarmi S, 2006, J PHARM PHARM SCI, V9, P124
[2]   Absorption and presystemic metabolism of selegiline hydrochloride at different regions in the gastrointestinal tract in healthy males [J].
Barrett, JS ;
Szego, P ;
Rohatagi, S ;
Morales, RJ ;
DeWitt, KE ;
Rajewski, G ;
Ireland, J .
PHARMACEUTICAL RESEARCH, 1996, 13 (10) :1535-1540
[3]   Studies on biodegradation and release of gentamicin sulphate from interpenetrating network hydrogels based on poly(acrylic acid) and gelatin: in vitro and in vivo [J].
Changez, M ;
Koul, V ;
Krishna, B ;
Dinda, AK ;
Choudhary, V .
BIOMATERIALS, 2004, 25 (01) :139-146
[4]  
CHRISP P, 1991, Drugs and Aging, V1, P228, DOI 10.2165/00002512-199101030-00006
[5]   A new low-dose formulation of selegiline: clinical efficacy, patient preference and selectivity for MAO-B inhibition [J].
Clarke, A ;
Johnson, ES ;
Mallard, N ;
Corn, TH ;
Johnston, A ;
Boyce, M ;
Warrington, S ;
MacMahon, DG .
JOURNAL OF NEURAL TRANSMISSION, 2003, 110 (11) :1257-1271
[6]   Anesthetics Promoting in vitro AβPP Metabolism and Amyloid-β Toxicity [J].
Eckel, Barbara ;
Blobner, Manfred ;
Rammes, Gerhard .
JOURNAL OF ALZHEIMERS DISEASE, 2010, 22 :S21-S26
[7]   CONTROLLED-RELEASE OF 1-BETA-D-ARABINOFURANOSYLCYTOSINE (ARA-C) FROM HYDROPHILIC GELATIN MICROSPHERES - IN-VITRO STUDIES [J].
ESPOSITO, E ;
PASTESINI, C ;
CORTESI, R ;
GAMBARI, R ;
MENEGATTI, E ;
NASTRUZZI, C .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1995, 117 (02) :151-158
[8]   Selegiline transdermal system for the treatment of major depressive disorder: An 8-week, double-blind, placebo-controlled, flexible-dose titration trial [J].
Feiger, Alan D. ;
Rickels, Karl ;
Rynn, Moira A. ;
Zimbroff, Dan L. ;
Robinson, Donald S. .
JOURNAL OF CLINICAL PSYCHIATRY, 2006, 67 (09) :1354-1361
[9]  
Filip V, 1999, J PSYCHIATR NEUROSCI, V24, P234
[10]  
Frampton JE, 2007, DRUGS, V67, P257, DOI 10.2165/00003495-200767020-00006