Abstract:
:Achieving drug delivery at the ocular level encounters many challenges and obstacles. In situ gelling delivery systems are now widely used for topical ocular administration and recognized as a promising strategy to improve the treatment of a wide range of ocular diseases. The present work describes the formulation and evaluation of a mucoadhesive and ion-activated in situ gelling delivery system based on gellan gum and hydroxyethylcellulose for the delivery of phenylephrine and tropicamide. First, physico-chemical characteristics were assessed to ensure suitable properties regarding ocular administration. Then, rheological properties such as viscosity and gelation capacity were determined. Gelation capacity of the formulations and the effect of hydroxyethylcellulose on viscosity were demonstrated. A new rheological method was developed to assess the gel resistance under simulated eye blinking. Afterward, mucoadhesion was evaluated using tensile strength test and rheological synergism method in both rotational and oscillatory mode allowing mucoadhesive properties of hydroxyethylcellulose to be point out. Finally, residence time on the ocular surface was investigated in vivo, using cyanine 5.5 dye as a fluorescent marker entrapped in the in situ gelling delivery systems. Residence performance was studied by non-invasive optical imaging on vigilant rabbits, allowing eye blinking and nasolacrimal drainage to occur physiologically. Fluorescence intensity profiles pointed out a prolonged residence time on the ocular surface region for the developed formulations compared to conventional eye drops, suggesting in vitro / in vivo correlations between rheological properties and in vivo residence performances.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Destruel PL,Zeng N,Seguin J,Douat S,Rosa F,Brignole-Baudouin F,Dufaÿ S,Dufaÿ-Wojcicki A,Maury M,Mignet N,Boudy Vdoi
10.1016/j.ijpharm.2019.118734subject
Has Abstractpub_date
2020-01-25 00:00:00pages
118734eissn
0378-5173issn
1873-3476pii
S0378-5173(19)30779-3journal_volume
574pub_type
杂志文章abstract::The influence of positively-charged and sterically stabilized liposomes and/or methyl-beta-cyclodextrin on rheological properties of Carbopol 974P NF hydrogels was investigated. All formulations have displayed a shear-thinning behavior of Carbopol gels, and the rate stress as a function of the shear rate was fitted us...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(02)00683-x
更新日期:2003-03-18 00:00:00
abstract::The goal of this work was to study the characteristics of a new phospholipid nanovesicular carrier for nasal administration of drugs. Multilamellar vesicles were visualized by electron microscopy, and their mean distribution size of 200 nm was evaluated by DLS. Measured pH and viscosity values were found adequate for ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119243
更新日期:2020-04-30 00:00:00
abstract::Mini-tablets are an age appropriate dosage form for oral administration to pediatric and geriatric patients, either as individual mini-tablets or as composite dosage units. Smaller size mini-tablets than the commonly used 2 mm or larger size would offer more tailored micro-dose delivery of investigational drugs. This ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.118905
更新日期:2020-01-25 00:00:00
abstract::The aim of this study was to evaluate the potential application of microemulsions as a transdermal drug delivery for naproxen (Np). The pseudo-ternary phase diagrams were developed for microemulsions composed of isopropyl myristate, Span 80, Labrafil M, Labrasol, and Cremophor EL, ethanol and isopropyl alcohol and 0.5...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.06.026
更新日期:2011-09-15 00:00:00
abstract::Plasma stability plays an important role in drug discovery and development. Unstable compounds tend to have rapid clearance and short half-life, resulting in poor in vivo performance. This paper examines the variables that affect the plasma stability assay results, including substrate concentration, %DMSO, plasma conc...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.03.022
更新日期:2005-06-13 00:00:00
abstract::Poorly soluble drug molecules often have low bioavailability issues and absorption problems in the clinical setting. As the number of poorly soluble drugs increases from discovery, developing technologies to enhance their solubility, while also controlling their release is one of the many challenges facing the pharmac...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2018.01.037
更新日期:2018-03-25 00:00:00
abstract::Dendrimers attract much attention as potential drug and gene carriers for intracellular delivery. From this point of view, it is crucial to extend our knowledge about their interactions with membranes. The influence of polyamidoamine (PAMAM) dendrimers on the thermotropic behavior of DPPC multilamellar vesicles and DM...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.08.015
更新日期:2005-11-23 00:00:00
abstract::The objective of this study was to enhance the oral bioavailability of itraconazole (ITZ) with dried drug nanosuspensions. The feasibility of using poloxamer 407 or HPMC (50 cp) as stabilizers for preparing ITZ nanosuspensions by facile acid-base neutralization was investigated. Dried ITZ nanosuspensions were prepared...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.04.034
更新日期:2011-07-15 00:00:00
abstract::This study proposed a new inorganic host for drug encapsulation. Porous clay heterostructure (PCH), synthesized using modified montmorillonite with hexadecyltrimethylammonium bromide, was used as host material and 5-fluorouracil (5-FU) as guest drug. Drug encapsulation within PCH in different conditions (soaking time,...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.05.053
更新日期:2015-08-01 00:00:00
abstract::Using monomethoxy poly(ethylene glycol) (mPEG)-trypsin conjugates we recently showed that both PEG molecular weight (1100-5000 g/mol) and linker chemistry affect the rate of protein autolysis and thermal stability. These important factors are often overlooked but they can guide the early choice of optimal polymer/chem...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.02.008
更新日期:2009-05-21 00:00:00
abstract::Topical iodine forms are used for infected and necrotic pressure ulcers. Despite antimicrobial advantages several potential disadvantages were observed with controversial results. To clarify the controversy, the reactivity of povidone-iodine (PI) sugar ointment and cadexomer-iodine (CI) ointment toward biological comp...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.01.007
更新日期:2009-05-08 00:00:00
abstract::Isoniazid (INH) is a first-line therapy for bone tuberculosis (TB), but its clinic benefits are limited by severe side-effects after long-time administration. While nano-drug delivery systems present as promising strategies for INH delivery, the therapeutic efficacies are usually suboptimal due to ineffective drug acc...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.12.083
更新日期:2019-03-10 00:00:00
abstract::In the pharmaceutical industry, in vitro dissolution testing ofsolid oral dosage forms is a very important tool for drug development and quality control. However, ion-pairing interaction between the ionic drugand surfactants in dissolution medium often occurs, resulting in inconsistent and incomplete drug release. The...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.10.063
更新日期:2018-01-15 00:00:00
abstract::Solid lipid nanoparticles have been reported as possible carrier for skin drug delivery. Solid lipid nanoparticles are produced from biocompatible and biodegradable lipids. Solid lipid nanoparticles made of semi-synthetic triglycerides stabilized with a mixture of polysorbate and sorbitan oleate were loaded with 5% of...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.06.014
更新日期:2011-09-15 00:00:00
abstract::The aim of this study was using Eudragit-cysteine conjugate to coat on chitosan microspheres (CMs) for developing an oral protein drug delivery system, having mucoadhesive and pH-sensitive property. Bovine serum albumin (BSA) as a protein model drug was loaded in thiolated Eudragit-coated CMs (TECMs) to study the rele...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2008.04.003
更新日期:2008-07-09 00:00:00
abstract:PURPOSE:Currently, in vivo or in vitro(99m)Tc-radiolabelled red blood cells are the standard blood pool imaging agents. Due to risks associated with handling of blood and the problems with the current (99m)Tc shortage, we were interested in a long-circulating biocompatible synthetic macromolecule that would be simple t...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.10.036
更新日期:2012-01-17 00:00:00
abstract::Recently, significant research efforts have been devoted to the finding of efficient approaches in order to reduce the side effects of traditional cancer therapy and diagnosis. In this context, magnetic nanoparticles have attracted much attention because of their unique physical properties, magnetic susceptibility, bi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2015.07.059
更新日期:2015-09-30 00:00:00
abstract::Heart failure still represents the leading cause of death worldwide. Novel strategies using stem cells and growth factors have been investigated for effective cardiac tissue regeneration and heart function recovery. However, some major challenges limit their translation to the clinic. Recently, biomaterials have emerg...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2016.10.061
更新日期:2017-05-25 00:00:00
abstract::The purpose of this study was to evaluate a single-step, organic solvent-free supercritical fluid process for the preparation of olanzapine-methyl-β-cyclodextrin complexes with an express goal to enhance the dissolution properties of olanzapine. The complexes were prepared by supercritical carbon dioxide processing, c...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.08.062
更新日期:2015-10-15 00:00:00
abstract::The effect of 35 newly synthesized O-ethylmenthol (MET) derivatives on percutaneous absorption of ketoprofen was investigated in rats. In order to understand the relationship between the structure of compounds and promoting activity (structure-activity relationship), an artificial neural network (ANN) was employed. In...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00608-6
更新日期:2001-01-16 00:00:00
abstract::This paper describes design and evaluation of parenteral lecithin-based nanoemulsions intended for brain delivery of risperidone, a poorly water-soluble psychopharmacological drug. The nanoemulsions were prepared through cold/hot high pressure homogenization and characterized regarding droplet size, polydispersity, su...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.07.007
更新日期:2015-09-30 00:00:00
abstract::In recent years, core-shell nanofibrous drug delivery systems have received increasing attention due to their ability to incorporate two or more active pharmaceutical ingredients (APIs) individually into the desired layer (either core or sheath) and thereby finely tune the release profiles of even incompatible drugs i...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119706
更新日期:2020-09-25 00:00:00
abstract::The influence of crystallographic structural anisotropy on the breakage behaviour of Aspirin under impact loading is highlighted. Under both quasi-static testing conditions, using nano-indentation, and dynamic impact tests, Aspirin demonstrates clear anisotropy in its slip and fracture behaviour. During nano-indentati...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.03.039
更新日期:2011-06-15 00:00:00
abstract::Achieving stable, efficient and non-toxic pulmonary gene delivery is most challenging requirement for successful gene therapy to lung. Composite nanoparticles (NPs) of the poly(lactic-co-glycolic acid) (PLGA) and cationic polymer polyethyleneimine (PEI) is an efficient alternative to viral and liposomal vectors for th...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.03.094
更新日期:2017-05-30 00:00:00
abstract::Honokiol (HK) shows potential application in cancer treatment, but its poor water solubility restricts clinical application greatly. In this paper, monomethoxy poly(ethylene glycol)-poly(lactic acid) (MPEG-PLA) was synthesized by ring-opening polymerization and processed into nanoparticle for honokiol delivery. Chemic...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.11.014
更新日期:2010-02-15 00:00:00
abstract::The aim of this study was to investigate the potential of solid dispersion to improve the dissolution rate and bioavailability of osthole (Ost), a coumarin derivative with various pharmacological activities but with poor aqueous solubility. In present studies, the Ost solid dispersions were prepared with various polym...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.02.040
更新日期:2014-04-25 00:00:00
abstract::This article has been withdrawn at the request of the authors. The Publisher apologizes for any inconvenience this may cause. The full Elsevier Policy on Article Withdrawal can be found at http://www.elsevier.com/locate/withdrawalpolicy. ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.11.046
更新日期:2012-12-20 00:00:00
abstract::Quantitative analysis using proton NMR (1H qNMR) has been employed in various areas such as pharmaceutical analysis (e.g., dissolution study), vaccines, natural products analysis, metabolites, and macrolide antibiotics in agriculture industry. However, it is not routinely used in the quantification of saccharides in d...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.03.030
更新日期:2019-06-10 00:00:00
abstract::Recently, many people have developed rheumatoid arthritis (RA), and prednisolone (PD) is often used for treatment; however, long use and a large dose of PD can cause toxic side effects. In this study, in order to enhance the therapeutic effects and to suppress the toxic side effects, the conjugate (GC-SP) was prepared...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.03.004
更新日期:2011-05-30 00:00:00
abstract::Protein aggregates have been discussed for a long time as a potential risk factor for immunogenicity in patients. Meanwhile, many research groups have investigated the immunogenicity of differently produced aggregates using in vitro or in vivo models. Despite all knowledge gained in these studies still little is known...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2019.01.015
更新日期:2019-03-25 00:00:00