Abstract:
:Microemulsions show excellent potential as drug delivery systems, but the surfactants used to prepare them can cause side effects. Researchers have explored various strategies to expand microemulsion area and thereby reduce the surfactant content necessary, but how these strategies affect drug oral bioavailability has not been investigated in detail. Microemulsions were prepared using 16% or 24% mixed surfactant Tween 80-Cremophor EL-PEG400 (1:1:2) and either 6% caprylic/capric triglyceride oil (GTCC) or 6% or 15% mixed oil (Maisine™ 35-1 with GTCC). Some microemulsions contained just enough surfactant based on ternary phase diagrams, while others had excess surfactant. All empty and ibuprofen-loaded microemulsions were clear or translucent with a slight blue color, and they remained stable after dilution and centrifugation. In experiments with rats, oral bioavailability (AUC0⟶t) of ibuprofen in the microemulsions was similar for the different formulations (6779.0-7413.3 min μg/mL) and significantly higher than that of an ibuprofen suspension (4830.9 min μg/mL). The different formulations behaved similarly in a cellular uptake assay with Caco-2 cells. These results suggest that excess surfactant does not increase oral bioavailability or cellular uptake of ibuprofen. Therefore, to minimize side effects, using just enough surfactant to ensure microemulsion stability and drug solubility may be an appropriate strategy.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
You X,Xing Q,Tuo J,Song W,Zeng Y,Hu Hdoi
10.1016/j.ijpharm.2014.05.031subject
Has Abstractpub_date
2014-08-25 00:00:00pages
276-84issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(14)00371-8journal_volume
471pub_type
杂志文章abstract::Three innovative components (an annular gap spray system, a booster bottom and an outlet filter) have been developed by Innojet Technologies to improve fluid bed technology and to reduce the common interference factors (clogging of nozzles and outlet filters, spray loss, spray drying and fluidized bed heterogeneity). ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.07.051
更新日期:2005-03-03 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::Transdermal drug delivery via iontophoresis is reviewed with special focus on the delivery of lidocaine for local anesthesia and fentanyl for patient controlled acute therapy such as postoperative pain. The role of the microprocessor controller in achieving dosimetry, alternating/reverse polarity, pre-programmed, and ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2006.03.053
更新日期:2006-07-06 00:00:00
abstract::The present study evaluates the effect of several pharmaceutical plasticizers on the thermo-physical and physicochemical properties of partially hydrolyzed poly(vinyl alcohol) (PVA) used in fusion-based pharmaceutical formulation processes. Specifically, the effect of mannitol (MAN), sorbitol (SOR), sucrose (SUC), anh...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119121
更新日期:2020-03-30 00:00:00
abstract::Core-shell type of nanoparticles (NPs) with manipulated degradation rate and balanced hydrophilic/hydrophobic properties were designed and characterized. The NPs based on the copolymers of n-butyl cyanoacrylate (BCA) and 2-octyl cyanoacrylate (OCA) were prepared by anion emulsion polymerization in 0.01N HCl solution w...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.06.008
更新日期:2006-11-15 00:00:00
abstract::This study was conducted to evaluate the feasibility of developing inhalable dry powders of liposomal encapsulated ciprofloxacin nanocrystals (LECN) for controlled drug release. Dry powders of LECN were produced by freeze-thaw followed by spray drying. The formulations contained sucrose as a lyoprotectant in different...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.05.068
更新日期:2019-07-20 00:00:00
abstract::The sublingual administration of nifedipine (NIF) is currently used in clinical practice. The sublingual administration of NIF solid dispersions (SD), by using a suitable dispenser, appears an interesting approach in the treatment of moderate and severe hypertensive emergencies. With this aim nine SD made of NIF and a...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(02)00173-4
更新日期:2002-08-21 00:00:00
abstract::Rifampicin is a first-line, highly effective drug currently used orally as a part of a lengthy multi-drug regimen against tuberculosis (TB). Despite the potential of inhaled therapy as an effective approach for TB treatment, an inhalable formulation of rifampicin has not yet been developed for clinical use. In order t...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119602
更新日期:2020-09-25 00:00:00
abstract::A novel agglomeration process of pulverized pharmaceutical powders into subsieve-sized agglomerates (microagglomeration) was designed for manufacturing highly drug-incorporated core particles for subsequent microencapsulation by film-coating. The microagglomeration of pulverized phenacetin powder, whose mass median di...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00006-x
更新日期:1999-04-15 00:00:00
abstract::The purpose of the study is to screen the interactions of fourth generation fluoroquinolone-gatifloxacin with efflux pumps, i.e., P-gp, MRP2 and BCRP. Mechanism of gatifloxacin interaction with efflux transporters may explain its acquired resistance. Such clarification may lead to the development of strategies to over...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.05.027
更新日期:2010-08-16 00:00:00
abstract::A gastroretentive drug delivery system of DA-6034, a new synthetic flavonoid derivative, for the treatment of gastritis was developed by using effervescent floating matrix system (EFMS). The therapeutic limitations of DA-6034 caused by its low solubility in acidic conditions were overcome by using the EFMS, which was ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.12.042
更新日期:2008-05-22 00:00:00
abstract::Raman spectroscopy may be implemented through a microscope to provide fine scale axial and lateral chemical maps. The molecular structure of many drugs makes Raman spectroscopy particularly well suited to the investigation of pharmaceutical systems. Chemometric methods currently used to assess bulk Raman spectroscopic...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2010.12.030
更新日期:2011-09-30 00:00:00
abstract::Drug-loaded solid lipid nanoparticles (SLN) suitable for parenteral administration were freeze-dried. The lipid matrix Imwitor 900 (concentration, 2.5%) was stabilized with Lipoid E 80 and sodium glycocholate. The influence of different parameters of lyophilization like the protective effect of cryoprotectants, freezi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00424-x
更新日期:2000-03-10 00:00:00
abstract::This study aims to improve understanding of the powder fluidisation and aerosolisation processes unique to a split capsule dry powder inhaler. It uses a combination of dynamic real-time methods and a suite of powder material physicochemical characterisation methods. The study focused on examining the effect of differe...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.08.038
更新日期:2014-12-30 00:00:00
abstract::The knowledge of the solubility of PEG 1500 as well as the swelling and melting point variation in supercritical CO(2) in a relatively high-pressure range is a necessary prerequisite to set-up pharmaceutical processes dealing with the polymer in the molten state. Experiments carried out in a pressurized view cell indi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.12.048
更新日期:2008-05-22 00:00:00
abstract::Lipid-based liquid crystalline nanoparticles (LCNPs) have attracted growing interest as a new drug nanocarrier system for improving bioavailability for both hydrophilic and hydrophobic drugs. In this study, self-assembled LCNPs based on soy phosphatidyl choline and glycerol dioleate, which was known possessing low tox...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.12.058
更新日期:2012-03-15 00:00:00
abstract::The efficiency of drug depends not only on its potency but also on its ability to reach the target sites in preference to non-target sites. In this regard, protein assembled nanocarrier is the most promising strategy for intracellular anti-cancer drug delivery. The key motive of this study is to fabricate biocompatibl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119192
更新日期:2020-04-30 00:00:00
abstract::The breath-actuated mechanism (BAM) is a mechanical unit included in NEXThaler® with the role of delaying the emission of the drug until the inhalation flow rate of the patient is sufficiently high to detach the drug particles from their carriers. The main objective of this work was to analyse the effect of the presen...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.09.057
更新日期:2017-11-25 00:00:00
abstract::Emulsion technology has been utilized extensively in the pharmaceutical industry. This article presents a comprehensive review of the literature on an important subcategory of emulsions, microemulsions. Microemulsions are optically transparent, thermodynamically stable colloidal systems, 10-100nm diameter, that form s...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2017.05.005
更新日期:2017-06-30 00:00:00
abstract::This study was undertaken to prepare films by solvent evaporation method comprising well-known polymers in order to investigate their potential for buccal suitability. Mucoadhesive films were manufactured using different polymers such as ethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose as well as...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.08.032
更新日期:2018-10-25 00:00:00
abstract::The effect of carrier surface properties on drug particle detachment from carrier crystals during inhalation with a special test inhaler with basic air classifier has been studied for mixtures containing 0.4% budesonide. Carrier crystals were retained in the classifier during inhalation and subsequently examined for t...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(03)00264-3
更新日期:2003-07-24 00:00:00
abstract::Chemically modified tetracyclines (CMTs) have been reported to strongly inhibit proliferation and metastasis of various cancers, but their efficacy is restricted by poor water solubility. In the present study, a hydrophilic 4-dedimethylamino sancycline (CMT-3) loaded nanostructured lipid carrier (CMT-3/NLC) was produc...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.04.021
更新日期:2013-06-25 00:00:00
abstract::This study explored the transition of lamellar-type liquid crystal (LLC) to biocompatible oil-in-water nanoemulsions able to modify benznidazole (BNZ) release and target the drug to cells infected with the T. cruzi parasite. Three cosolvents (2methylpyrrolidone [NMP], polyethylene glycol [POL], and propylene glycol [P...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.11.041
更新日期:2019-01-30 00:00:00
abstract::The objective of this study was to determine the effect of iontophoresis on the delivery of terbinafine hydrochloride (4%, w/w) into and across hairless rat skin. In vitro skin uptake and permeation studies were performed using Franz diffusion cells. Anodal iontophoresis was applied for 1h at current densities of 0.2,...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.12.029
更新日期:2010-03-30 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:PURPOSE:In this paper we have evaluated the gene expression programming (GEP) methodology for modeling the effect of different variables (continuous and nominal) and their interactions on the properties of direct compression formulations. METHODS:The effect of four variables was studied; variety of diluents, type and ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.04.078
更新日期:2012-09-15 00:00:00
abstract::We developed a polyethylene glycol (PEG)-based biodegradable hydrogel through disulfide crosslinking of polyethylene oxide sulfide (PEOS). The crosslinking rate was highly dependent on temperature, and incubation at about 40-50 degrees C was required for efficient crosslinking. The crosslinked PEOS hydrogel showed glu...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.03.010
更新日期:2009-06-05 00:00:00
abstract::TXA497 is representative of a new class of guanidinomethyl biaryl compounds that exhibit potent bactericidal behavior against methicillin-resistant Staphylococcus aureus (MRSA). In this study, we compared the anti-staphylococcal, skin deposition, and skin permeation properties of TXA497 and the topical anti-MRSA antib...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.09.033
更新日期:2014-12-10 00:00:00
abstract::Genetic immunization through skin is highly desirable as skin has plenty of antigen presenting cells (APCs) and is easily accessible. The purpose of this study was to investigate the effects of electroporation pulse amplitude, pulse length and number of pulses on cutaneous plasmid DNA vaccine delivery and immune respo...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.12.014
更新日期:2005-04-27 00:00:00
abstract::3-D ordered macroporous carbon with different polymer coatings were developed as new oral vaccine immunological systems. Poly dimethyl diallyl ammonium (PDDA), polyethyleneimine (PEI) and chitosan (CTS), three different polymers with electropositive or adsorption-promoting properties, were chosen as the coating materi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.04.045
更新日期:2015-06-20 00:00:00