Abstract:
:Hesperetin, an aglycone of the flavanone hesperidin, is a potential candidate for the treatment of diabetic retinopathy and macular edema. The purpose of this investigation was to determine solubility, stability and in vitro permeability characteristics of hesperetin across excised rabbit corneas. Aqueous and pH dependent solubility was determined using standard shake flask method. Solution stability was evaluated as a function of pH (1.2-9) and temperature (25 and 40 degrees C). Permeability of hesperetin was determined across the isolated rabbit cornea utilizing a side-bi-side diffusion apparatus, in the apical to basolateral (A-B) and basolateral to apical (B-A) directions. Hesperetin displayed asymmetrical transcorneal transport with a 2.3-fold higher apparent permeability in the B-A direction compared to the A-B direction. The transport process was observed to be pH dependent. Surprisingly, however, the involvement of efflux transporters or proton-coupled carrier-systems was not evident in this asymmetric transcorneal diffusion process. The passive and pH dependent corneal transport of hesperetin could probably be attributable to corneal ultrastructure, physicochemical characteristics of hesperetin and the role of transport buffer components.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Srirangam R,Majumdar Sdoi
10.1016/j.ijpharm.2010.04.036subject
Has Abstractpub_date
2010-07-15 00:00:00pages
60-7issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(10)00308-Xjournal_volume
394pub_type
杂志文章abstract:AIM:Assessment of preactivated carboxymethyl cellulose as potential excipient for buccal drug delivery. METHODS:Firstly, carboxymethyl cellulose (CMC) and cysteine (SH) were covalently coupled via amide bond formation to obtain thiolated carboxymethyl cellulose (CMC-SH). Further, preactivated carboxymethyl cellulose (...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.01.012
更新日期:2016-03-16 00:00:00
abstract::Poor mechanical properties of crystalline drug particles require wet granulation technique for tablet production which is uneconomical, laborious, and tedious. The present investigation was aimed to improve flow and mechanical properties of racecadotril (RCD), a poorly water soluble antidiarrheal agent, by a crystallo...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.04.073
更新日期:2013-08-16 00:00:00
abstract::Drug interactions with diosmectite, a gastric-protective drug, were studied in vitro using an artificial stomach-duodenum model. The behavior of neutral and ionisable drugs with pKa values ranging between 2 and 8 was monitored to determine the physicochemical characteristics of the interactions. The main neutral (digo...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00073-3
更新日期:1999-05-10 00:00:00
abstract::Designing strategies for targeting antigens to dendritic cells is a major goal in vaccinology. Here, PLGA (poly lactic-co-glycolic acid) microspheres and with several surface modifications that affect to their uptake by human blood primary dendritic cells and monocytes have been evaluated. Higher uptake was found by a...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.10.037
更新日期:2015-12-30 00:00:00
abstract::3D-printing is a promising tool to pave the way to the widespread adaption of individualized medicine. Several printing techniques have been investigated and introduced to pharmaceutical research. Until now, only one 3D-printed medicine is approved on the US market. The medicine is manufactured via drop-on-powder depo...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.11.048
更新日期:2019-01-30 00:00:00
abstract::In order to improve the dissolution and absorption properties of loviride, a poorly soluble antiviral agent, sucrose co-freeze-dried nanopowders were prepared, characterized and evaluated. Tween 80/poloxamer 188-stabilized nanosuspensions were produced on a laboratory scale using media milling. The milling process was...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.02.005
更新日期:2007-06-29 00:00:00
abstract::An increasing elderly population is leading to a change in the global demographics. This presents a new challenge to society and the pharmaceutical industry. This demographic shift is providing an opportunity for the pharmaceutical industry to meet the specific needs of the changing patient population. One issue that ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2016.03.008
更新日期:2016-10-30 00:00:00
abstract::The study deals with the intercalation of procainamide hydrochloride (PA), an antiarrythmia drug in montmorillonite (MMT), as a new drug delivery device. Optimum intercalation of PA molecules within the interlayer space of MMT was achieved by means of different reaction conditions. Intercalation of PA in the MMT galle...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.01.002
更新日期:2010-03-30 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::Lansoprazole (LPZ) is a representative drug that shows a high inter-subject variation of bioavailability (BA). Solid preparation composed of surfactant, adsorbent and LPZ were prepared to improve the dissolution and absorption of LPZ, and the BA of LPZ was measured in rats and dogs. As surfactant, Tween 80, polyoxy 60...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.10.010
更新日期:2005-01-31 00:00:00
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 LR12 peptide has been reported to reduce the size of infarct and improve both cardiac function and survival in myocardial infarction in murine models, after daily repeated intraperitoneal injections. In order to protect peptide from degrading and to prolong its release, in situ implants based on biocompatible biod...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.02.046
更新日期:2017-04-15 00:00:00
abstract::A highly accurate nephelometric titration for the determination of promethazine hydrochloride and its preparations was presented. The titration operating conditions were studied and the solubility product constant of promethazine tetraphenylboron precipitation was determined. The result of the titration is comparable ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.05.043
更新日期:2005-09-30 00:00:00
abstract::In the fluid bed agglomeration processes liquid distribution influences the agglomerate growth. We developed a new nozzle that produces uniform droplets, which allows droplets to be easily controlled in size independently of liquid- and airflow of the nozzle. It was found that the spray rate and the mixing in the spra...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00329-4
更新日期:2000-01-05 00:00:00
abstract::To develop a novel sodium fusidate-loaded triple polymer hydrogel dressing (TPHD), numerious polyvinyl alcohol-based (PVA) hydrogel dressings were prepared with various hydrophilic polymers using the freeze-thaw method, and their hydrogel dressing properties were assessed. Among the hydrophilic polymers tested, sodium...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.12.007
更新日期:2016-01-30 00:00:00
abstract::In this study, topical minoxidil solutions supplemented with TPGS in cosolvent systems of various compositions consisting of water, alcohol, and polyethylene glycol 400 were designed to evaluate the efficacy of promoting hair growth after topical application and the safety in terms of the amount of minoxidil absorbed ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.09.005
更新日期:2005-12-08 00:00:00
abstract::DNA as a novel biomaterial can be used to fabricate different kinds of DNA nanostructures based on its principle of GC/AT complementary base pairing. Studies have shown that DNA nanostructure is a nice drug carrier to overcome big obstacles existing in cancer therapy such as systemic toxicity and unsatisfied drug effi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2017.09.032
更新日期:2017-11-25 00:00:00
abstract::Previously, chemical enhancer-induced permeation enhancement on human stratum corneum (SC) lipoidal pathway at enhancer thermodynamic activities approaching unity in the absence of cosolvents (defined as Emax) was determined and hypothesized to be related to the enhancer solubilities in the SC lipid domain. The object...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.09.014
更新日期:2010-01-04 00:00:00
abstract::The conventional medications are still facing a huge challenge for the treatment of rheumatoid arthritis (RA). Thus, looking for an effective therapy of RA has became an urgent issue nowadays. In this study, a novel thermosensitive liposome loaded with sinomenine hydrochloride (SIN-TSL) was developed by a pH gradient ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.119001
更新日期:2020-02-25 00:00:00
abstract::A genetically modified recombinant tumor necrosis factor (TNF)-alpha (rKRKTNF) was conjugated to the terminal carboxyl groups of liposome grafted polyethyleneglycol (PEG) chains. The long-circulating liposomes were composed of egg phosphatidylcholine, cholesterol (chol) and 7% carboxyl PEG-phosphatidylethanolamine. Th...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00092-7
更新日期:1999-07-05 00:00:00
abstract::The pharmacokinetics of acetaminophen have been well studied in different populations, especially in Caucasians. However, limited studies on acetaminophen pharmacokinetics have been conducted in the native Chinese and few such data have been reported in the English language literature. Previous published studies sugge...
journal_title:International journal of pharmaceutics
pub_type: 临床试验,杂志文章
doi:10.1016/s0378-5173(01)00712-8
更新日期:2001-07-17 00:00:00
abstract::We developed dual paclitaxel (PTX)/superparamagnetic iron oxide (SPIO)-loaded PLGA-based nanoparticles for a theranostic purpose. Nanoparticles presented a spherical morphology and a size of 240 nm. The PTX and iron loading were 1.84 ± 0.4 and 10.4 ± 1.93 mg/100 mg respectively. Relaxometry studies and phantom MRI dem...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.02.042
更新日期:2013-04-15 00:00:00
abstract::Niosomes are vesicles formed by self-assembly of non-ionic surfactants. In this investigation, the effects of processing variables, particularly temperature and sonication, on the physical characteristics and phase transitional behaviour of two niosomal systems based on a hexadecyl diglycerol ether (C(16)G(2)) have be...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00362-8
更新日期:2000-05-15 00:00:00
abstract::N-Acetyl-l-cysteine (NAC) commonly used as an antidote in acetaminophen poisoning has shown promise in the treatment of neurological disorders such as cerebral palsy (CP). However, NAC suffers from drawbacks such as poor oral bioavailability and suboptimal blood-brain-barrier (BBB) permeability limiting its clinical s...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.04.040
更新日期:2018-07-10 00:00:00
abstract::Pharmaceutical powders are typically insulators consisting of relatively small particles and thus they usually exhibit significant electrostatic charging behaviours. In the inhalation field, the measurement of electrostatic charge is an imperative stage during pharmaceutical formulation development. The electrostatic ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2016.01.076
更新日期:2016-04-30 00:00:00
abstract::A polymeric prodrug of cisplatin (CP) with simple chemical structure was synthesized based on pullulan and its therapeutic effects on human hepatocellular carcinoma (HCC) were studied in vitro and in vivo. Briefly, CP was linked to pullulan monosuccinate (SUPA) via coordination bond to form prodrug of CP-SUPA with the...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.02.027
更新日期:2015-04-10 00:00:00
abstract::Since the application of nanotechnology to drug delivery, both polymer-based and lipid-based nanocarriers have demonstrated clinical benefits, improving both drug efficacy and safety. However, to further address the challenges of the drug delivery field, hybrid lipid-polymer nanocomposites have been designed to merge ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119467
更新日期:2020-07-30 00:00:00
abstract::Local drug delivery into oral cavity offers many advantages over systemic administration in treatment of the oral infections. In this study, monolayer and bilayered mucoadhesive film and wafer formulations were developed as local drug delivery platforms using chitosan and hydroxypropyl methylcellulose (HPMC). Cefuroxi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.01.029
更新日期:2019-03-25 00:00:00
abstract::Acylation of proteins with a fatty acid chain has proven useful for prolonging the plasma half-lives of proteins. In formulation of acylated protein drugs, knowledge about the effect of acylation with fatty acids on the adsorption behaviour of proteins at interfaces will be valuable. The aim of this work was to study ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.01.040
更新日期:2013-01-02 00:00:00
abstract::The terahertz region of the electromagnetic spectrum spans the frequency range between the infrared and the microwave. Traditionally the exploitation of this spectral region has been difficult owing to the lack of suitable source and detector. Over the last ten years or so, terahertz technology has advanced considerab...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2011.01.012
更新日期:2011-09-30 00:00:00