Abstract:
PURPOSE:The aim of this work is to design new chitosan conjugates able to self-organize in aqueous solution in the form of micrometer-size platelets. When mixed with amphotericin B deoxycholate (AmB-DOC), micro-platelets act as a drug booster allowing further improvement in AmB-DOC anti-Candida albicans activity. METHODS:Micro-platelets were obtained by mixing oleoyl chitosan and α-cyclodextrin in water. The formulation is specifically-engineered for mucosal application by dispersing chitosan micro-platelets into thermosensitive pluronic® F127 20 wt% hydrogel. RESULTS:The formulation completely cured C. albicans vaginal infection in mice and had a superior activity in comparison with AmB-DOC without addition of chitosan micro-platelets. In vitro studies showed that the platelets significantly enhance AmB-DOC antifungal activity since the IC50 and the MIC90 decrease 4.5 and 4.8-times. Calculation of fractional inhibitory concentration index (FICI = 0.198) showed that chitosan micro-platelets act in a synergistic way with AmB-DOC against C. albicans. No synergy is found between spherical nanoparticles composed poly(isobutylcyanoacrylate)/chitosan and AmB-DOC. CONCLUSION:These results demonstrate for the first time the ability of flattened chitosan micro-platelets to have synergistic activity with AmB-DOC against C. albicans candidiasis and highlight the importance of rheological and mucoadhesive behaviors of hydrogels in the efficacy of the treatment.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Grisin T,Bories C,Bombardi M,Loiseau PM,Rouffiac V,Solgadi A,Mallet JM,Ponchel G,Bouchemal Kdoi
10.1007/s11095-017-2117-3subject
Has Abstractpub_date
2017-05-01 00:00:00pages
1067-1082issue
5eissn
0724-8741issn
1573-904Xpii
10.1007/s11095-017-2117-3journal_volume
34pub_type
杂志文章abstract:BACKGROUND:With the recent approval of the first small interfering RNA (siRNA) therapeutic formulated as nanoparticles, there is increased incentive for establishing the factors of importance for the design of stable solid dosage forms of such complex nanomedicines. METHODS:The aims of this study were: (i) to identify...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2663-y
更新日期:2019-08-02 00:00:00
abstract:PURPOSE:To create poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs), where a drug-encapsulating NP core is covered with polyethylene glycol (PEG) in a normal condition but exposes a cell-interactive TAT-modified surface in an environment rich in matrix metalloproteinases (MMPs). METHODS:PLGA NPs were modified w...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1039-y
更新日期:2013-08-01 00:00:00
abstract:PURPOSE:Near-infrared reflectance spectroscopy (NIRS) was used to evaluate and quantify the effect of compression force on the NIR spectra of tablets. METHODS:Flat, white tablets with no orientation (scoring, etc.) were manufactured on a Stokes Rotary Tablet Press. NIRS was used to predict tablet hardness on the follo...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012071904673
更新日期:1997-01-01 00:00:00
abstract:PURPOSE:Excipients are added to lyophilized protein drug formulations to protect the protein during processing and storage, but the mechanisms are poorly understood. Here, hydrogen/deuterium (H/D) exchange with mass spectrometry was used to assess protein conformation and excipient interactions in lyophilized solids. ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9365-6
更新日期:2008-02-01 00:00:00
abstract:PURPOSE:Changes in drug absorption and first-pass metabolism have been reported throughout the pediatric age range. Our aim is to characterize both intestinal and hepatic CYP3A-mediated metabolism of midazolam in children in order to predict first-pass and systemic metabolism of CYP3A substrates. METHODS:Pharmacokinet...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2458-6
更新日期:2018-07-30 00:00:00
abstract:PURPOSE:To examine the iontophoretic delivery of ALA as a function of pH and to determine the principal mechanisms responsible for its electrotransport. METHODS:Anodal iontophoretic transport of ALA was measured as a function of its concentration and pH of the donor solution. Experiments were performed in vitro using ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011050829531
更新日期:2001-03-01 00:00:00
abstract:PURPOSE:To characterize the pharmacokinetic/pharmacodynamic (PK/PD) properties of a new polyethylene glycol (PEG) conjugate formulation of interferon (IFN)-beta la following subcutaneous (SC) administration in monkeys. METHODS:Single SC injections of 0.3, 1, and 3 million international units (MIU)/kg of PEG-IFN-beta 1...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-9009-z
更新日期:2005-01-01 00:00:00
abstract:PURPOSE:To identify materials and processes which effect supersaturation of the GI milieu for low solubility drugs in order to increase oral bioavailability. METHODS:A variety of small and polymeric molecules were screened for their ability to inhibit drug precipitation in supersaturated solutions. The best polymeric ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9852-z
更新日期:2009-06-01 00:00:00
abstract:PURPOSE:This study focuses on the formulation optimization, in vitro and in vivo performance of differently sized nano-crystalline liquid suspensions and spray-dried powders of a poorly soluble BCS class II compound i.e. Danazol. METHODS:A DoE approach was utilized to optimize stabilizer concentration and formulate da...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1567-0
更新日期:2015-05-01 00:00:00
abstract::Four lipophilic, low molecular weight drugs solubilized in phosphatidylcholine-bile salt mixed micelles were injected s.c. into the hind legs of sheep and their cumulative recoveries in lymph draining from the site of application were determined. Surprisingly, the cumulative recoveries (percentage of dose) varied betw...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015807913934
更新日期:1991-10-01 00:00:00
abstract::Animal models are used commonly in various stages of drug discovery and development to aid in the prospective assessment of drug-drug interaction (DDI) potential and the understanding of the underlying mechanism for DDI of a drug candidate. In vivo assessments in an appropriate animal model can be very valuable, when ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-010-0157-z
更新日期:2010-09-01 00:00:00
abstract::The limitations of traditional gas adsorption models for describing water vapor sorption by amorphous pharmaceutical solids are described and an alternative approach based on polymer solution theories is proposed. The approach is tested by comparing a priori predicted isotherms with literature data for the poly(vinylp...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018901325842
更新日期:1993-09-01 00:00:00
abstract:PURPOSE:β-Hydroxy-β-methylbutyrate (HMB), a nutritional supplement, elicits anabolic activity in muscle. Here we investigated the mechanism of HMB uptake in muscle cells. METHODS:Murine muscle cells (C2C12) and human mammary epithelial cells (MCF7) were used for uptake. As HMB is a monocarboxylate, focus was on monoca...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2626-3
更新日期:2019-04-17 00:00:00
abstract:PURPOSE:Characterization of virosomes, in late stage preclinical development as vaccines for Respiratory Syncytial Virus (RSV), with a membrane-incorporated synthetic monophosphoryl lipid A, 3D-PHAD® adjuvant. METHODS:Virosomes were initially formed by contacting a lipid film containing 3D-PHAD® with viral membranes s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2453-y
更新日期:2018-07-03 00:00:00
abstract:PURPOSE:To group microcrystalline celluloses (MCCs) using a combination of artificial neural network (ANN) and data clustering. METHODS:Radial basis function (RBF) network was used to model the torque measurements of the various MCCs. Output from the RBF network was used to group the MCCs using a data clustering techn...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-7690-6
更新日期:2004-12-01 00:00:00
abstract:PURPOSE:This study aimed to investigate the impact of the size of X-ray iodinated contrast agent in nano-emulsions, on their toxicity and fate in vivo. METHODS:A new compound, triiodobenzoate cholecalciferol, was synthetized, formulated as nano-emulsions, and followed after i.v. administration in mice by X-ray imaging...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1813-0
更新日期:2016-03-01 00:00:00
abstract:PURPOSE:We prepared injectable microspheres for controlled release of TAK-029, a water-soluble GPIIb/IIIa antagonist and discussed the characteristics of controlled release from microspheres. METHODS:Copoly(dl-lactic/glycolic)acid (PLGA) microspheres were used for controlled release of TAK-029 [4-(4-amidinobenzoylglyc...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012190304074
更新日期:1997-09-01 00:00:00
abstract::Equations for the steady-state volumes of distribution (Vss) and the mean residence times in the body (MRT) are derived for a drug and its metabolite subject to reversible metabolism and separately infused intravenously at a constant rate to steady state of both compounds. The Vss and MRT parameters are functions of t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015874329265
更新日期:1990-06-01 00:00:00
abstract::Five aliphatic 5'-esters of 5-iodo-2'deoxyuridine (IDU) were synthesized via an acid chloride alcoholysis reaction. The solubility in pH 7.4 phosphate buffer, lipophilicity as determined by partition experiments in octanol/pH 7.4 buffer, and cytotoxicity of these potential prodrugs were evaluated. The esters showed a ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015968113838
更新日期:1988-11-01 00:00:00
abstract:PURPOSE:The purpose of the present study was to use the human colorectal carcinoma cell line. Caco-2, as a human intestinal epithelial model for studying the effects of cyclodextrins as absorption enhancers. METHODS:Cyclodextrins of varying sizes and physicochemical characters were investigated. The effects of the cyc...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016225707807
更新日期:1995-09-01 00:00:00
abstract::Knowledge Management (KM) is a key enabler for achieving quality in a lifecycle approach for production of biopharmaceuticals. Due to the important role that it plays towards successful implementation of Quality by Design (QbD), an analysis of KM solutions is needed. This work provides a comprehensive review of the in...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-016-2043-9
更新日期:2017-02-01 00:00:00
abstract:PURPOSE:To investigate if gamma-Hydroxybutyrate (GHB) tolerance is mediated by alterations in GHB systemic pharmacokinetics, transport (blood brain barrier (BBB) and neuronal) or membrane fluidity. MATERIALS AND METHODS:GHB tolerance in rats was attained by repeated GHB administration (5.31 mmol/kg, s.c., QD for 5 day...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9066-6
更新日期:2006-09-01 00:00:00
abstract:PURPOSE:Using monolayers of human pancreatic adenocarcinoma cells (Panc-1) that express multidrug resistance-associated protein (MRP), the present work investigates the effects of Pluronic block copolymers on the functional activity of MRP. METHODS:The studies examined the accumulation and efflux of the MRP selective ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018873702411
更新日期:1999-03-01 00:00:00
abstract::A series of multilamellar liposome dispersions was prepared from lipids of soy phosphatidylcholine or hydrogenated soy phosphatidylcholine containing from 0 to 30 mol% of either cholesterol, stearylamine, or dipalmitoyl phosphatidylglycerol. The liposome dispersions were aerosolized with a Collison nebulizer for 80 mi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015924124180
更新日期:1990-11-01 00:00:00
abstract:PURPOSE:To measure the charge to mass (Q/M) ratios of the impactor stage masses (ISM) from commercial Flixotide™ 250 μg Evohaler, containing fluticasone propionate (FP), Serevent™ 25 μg Evohaler, containing salmeterol xinafoate (SX), and a combination Seretide™ 250/25 μg (FP/SX) Evohaler metered dose inhalers (MDIs). M...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2544-9
更新日期:2018-11-26 00:00:00
abstract:PURPOSES:To evaluate the effects of component contents in different colistin methanesulfonate (CMS) formulas on their clinical pharmacokinetics of the prodrug CMS and the formed colistin. METHODS:Two CMS formulas (CTTQ and Parkedale) were investigated in a single dose, randomized, open-label, crossover study conducted...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-021-02991-4
更新日期:2021-01-26 00:00:00
abstract:PURPOSE:Induction of cell-mediated immune (CMI) responses is crucial for vaccine-mediated protection against difficult vaccine targets, e.g., Chlamydia trachomatis (Ct). Adjuvants are included in subunit vaccines to potentiate immune responses, but many marketed adjuvants stimulate predominantly humoral immune response...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2180-9
更新日期:2017-08-01 00:00:00
abstract:PURPOSE:Indocyanine green (ICG), an FDA-approved near infrared (NIR) dye, has potential application as a contrast agent for tumor detection. Because ICG binds strongly to plasma proteins and exhibits aqueous, photo, and thermal instability, its current applications are largely limited to monitoring blood flow. To addre...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0190-y
更新日期:2010-09-01 00:00:00
abstract:PURPOSE:SN-38, a potent chemotherapeutic drug, has not been used clinically because of its severe side effects and poor solubility. In this work, we aimed to evaluate the effect of dose and multiple injections of SN-38-loaded polymeric depots on antitumor efficacy and toxicity in vivo. METHODS:Preparation and characte...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2011-4
更新日期:2016-12-01 00:00:00
abstract:PURPOSE:To examine and determine the sites and the kinetics of IgG1 mAb modifications from both in vitro (rat plasma and PBS) and in vivo (rat model) time-course studies. METHODS:A comprehensive set of protein characterization methods, including RPLC/MS, LC-MS/MS, iCIEF, capSEC, and CE-SDS were performed in this repor...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0860-z
更新日期:2013-01-01 00:00:00