Abstract：
:This is the first report on the efficacy of a new controlled release system developed for rasagiline mesylate (RM) in a rotenone-induced rat model of Parkinson's disease (PD). PLGA microspheres in vitro released RM at a constant rate of 62.3 μg/day for two weeks. Intraperitoneal injection of rotenone (2 mg/kg/day) to Wistar rats produced typical PD symptoms. Catalepsy, akinesia and swim tests outcomes in animals receiving RM either in solution or within microspheres showed a reversal in descent latency when compared to rotenone-treated animals, being this reversal specially pronounced in animals receiving RM microspheres (dose equivalent to 1 mg/kg/day RM injected i.p. every 15 days). Nissl-staining of brain sections showed selective degeneration of the substantia nigra (SNc) dopaminergic neurons in rotenone-treated animals which was markedly reverted by RM microspheres. PET/CT with (18)F-DG resulted in mean increases of accumulation of radiotracer in striatum and SNc of around 40% in animals treated with RM microspheres which also had significant beneficial effects on Bcl-2, Bax, TNF-α mRNA and SOD2 levels as detected by real-time RT-PCR. Our results confirm the robust effect achieved by the new controlled release system developed for RM which exhibited better in vivo efficacy than RM given in solution.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Fernández M,Negro S,Slowing K,Fernández-Carballido A,Barcia Edoi
10.1016/j.ijpharm.2011.07.029subject
Has Abstractpub_date
2011-10-31 00:00:00pages
271-80issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(11)00660-0journal_volume
419pub_type
杂志文章abstract：:The blood-brain barrier (BBB) has a pivotal role in maintaining brain homeostasis. It robustly protects the brain parenchyma against the invasion of irrelevant substances, which may interrupt its critical function. From a pharmaceutical point of view, such a barrier may cause central nervous system (CNS) disorders ref...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2020.119582
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abstract：:To enhance the medicinal activity of bee venom (BV) acupuncture, bee venom was loaded into biodegradable poly(D,L-lactide-co-glycolide) nanoparticles (BV-PLGA-NPs) by a water-in-oil-in-water-emulsion/solvent-evaporation technique. Rat formalin tests were performed after subcutaneous injection of BV-PLGA-NPs to the Zus...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.06.034
更新日期：2009-10-01 00:00:00
abstract：:The effects of inlet air humidity, granulation liquid feed rate and granulation liquid feed pulsing on the particle-size distribution of final granules were studied in a laboratory scale fluid-bed granulator using a central composite study design. The factors examined were modelled using three different particle-size ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.01.060
更新日期：2008-06-05 00:00:00
abstract：:Multiple sclerosis (MS) is the most common demyelinating disease. Despite the historical use of interferon-beta (IFN-β) for the treatment of patients with MS, concerns exist regarding the side effects of IFN-β. In this study, we designed a series of novel IFN-β fusion proteins containing galectin-9 (gal-9), which exer...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.12.010
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abstract：:The aim of the current study was to improve the knowledge of drug-glycol-phospholipid-interactions and their effects in lamellar vesicle suitability as drug delivery systems. Liposomes were prepared using hydrogenated soy phosphatidylcholine (P90H, 60 mg/ml) and diclofenac sodium salt at two concentrations (5-10 mg/ml...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.08.034
更新日期：2013-11-01 00:00:00
abstract：:The aim of this study was to apply near-infrared (NIR) spectroscopy to the simultaneous in-line monitoring of two active pharmaceutical ingredients (APIs) in a pharmaceutical batch blending process. The formulation under study consisted of a high load API (A1), one polymer, a second API (A2) and one lubricant. Additio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2013-07-15 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2016-07-11 00:00:00
abstract：:Amphotericin B (AmB) has a broad antifungal and leishmanicidal activity with low incidence of clinical resistance. Its parenteral administration has high risk of nephrotoxicity that limits its use. In order to treat cutaneous infections, AmB topical administration is a safer therapy because of the low systemic absorpt...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.07.004
更新日期：2014-10-01 00:00:00
abstract：:In this paper, we describe the haemolytic effect of parent para-sulphonato-calix-[n]-arenes and their derivatives bearing one pendant group at the lower rim of calix-arene towards human erythrocytes. A maximum of 30% of haemolysis has been observed for para-sulphonato-calix-[8]-arene for a concentration of 200 mM repr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2003.12.008
更新日期：2004-04-01 00:00:00
abstract：:The aim of the present work was to study the influence of surface hydrophilicity of biodegradable polymeric nanoparticles on cellular uptake by Caco-2 cells. Poly(D,L-lactide-co-glycolide acid) particles loaded with a fluorescent dye, 3,3'-dioctadecyloxacarbo-cyanine perchlorate (DiO), were prepared by the emulsion-ev...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.10.008
更新日期：2010-05-05 00:00:00
abstract：:Topical aciclovir cream (ACV, Zovirax Cream) containing 40% propylene glycol (PG), the optimum found for skin penetration, is clinically effective in the treatment of recurrent herpes labialis. One hundred and thirty-nine ACV generic creams were analysed and 80% of these contained less than 20% PG. From this, we hypot...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.07.020
更新日期：2005-11-04 00:00:00
abstract：:Biodegradable and biocompatible microspheres represent a promising alternative to conventional adjuvants for anti-tumour vaccination. Focusing on glioma, we developed two poly(D,L-lactide-co-glycolide) (PLGA)-based particulate systems presenting tumour antigens associated with plasma membranes or with cell lysates. Gl...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.10.046
更新日期：2006-02-17 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.03.049
更新日期：2012-07-15 00:00:00
abstract：:Dosage forms with fixed dose combinations of drugs is a frequent and advantageous mode of administration, but their production involves a number of technological problems. Numerous interactions in a homogeneous vehicle may be avoided through the use of layered tablets. The mechanical properties of these dosage forms d...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.10.061
更新日期：2015-12-30 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.12.026
更新日期：2019-02-10 00:00:00
abstract：:Development of novel anticancer formulations is a priority challenge in biomedicine. However, in vitro models based on monolayer cultures (2D) which are currently used for cytotoxicity tests leave much to be desired. More and more attention is focusing on 3D in vitro systems which can better mimic solid tumors. The ai...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.04.005
更新日期：2016-06-15 00:00:00
abstract：:Epidermal growth factor receptor (EGFR) is an important anti-cancer therapy target that is applicable to many cancer types. We had previously reported the screening and discovery of a novel peptide ligand against EGFR named GE11. It was shown to bind to EGFR competitively with EGF and mediate gene delivery to cancer c...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.07.012
更新日期：2008-11-03 00:00:00
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更新日期：2013-08-16 00:00:00
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更新日期：2015-03-15 00:00:00
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更新日期：2010-10-15 00:00:00
abstract：:Intake of probiotics is associated with many health benefits, which has generated an interest in formulating viable probiotic supplements. The present study had two aims. The first aim was to achieve gastrointestinal protection and delayed release of viable probiotics by pelletizing and coating freeze-dried probiotic ...
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更新日期：2019-06-30 00:00:00
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journal_title：International journal of pharmaceutics
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更新日期：2000-09-15 00:00:00
abstract：:The partial or Hansen solubility parameters (HSP) are important properties of the various substances and very useful tools for the selection of their solvents or the prediction of their behaviour in numerous applications. Their design and evaluation relies on the basic rule of "similarity matching" for solubility. The...
journal_title：International journal of pharmaceutics
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更新日期：2012-04-15 00:00:00
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journal_title：International journal of pharmaceutics
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更新日期：2004-07-08 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2002-12-05 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2015-02-01 00:00:00
abstract：:The kinetics of fenoprofen release from poly[alpha,beta-(N-2-hydroxyethyl-DL-aspartamide)]-fenoprofen conjugate (PHEA-Fen) in aqueous buffer solutions (pH 10 and 1.1), simulated gastric (SGF) and intestinal fluids (SIF) was studied. In borate buffer pH 10, the following rate constants were obtained: k=0.2659 (t=60 deg...
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pub_type： 杂志文章
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更新日期：2002-07-25 00:00:00
