Abstract：
:Meso-tetraphenyl porphine (mTPP) is a highly lipophilic, fluorescent porphyrin derivate and it is used as photosensitizer on the treatment of malign neoplasms. The aim of this study was to prepare mTPP loaded pluronic F127 and polyethylene glycol-distearoyl phosphatidylethanolamine (PEG(2000)-DSPE) micelles to evaluate polymeric micelles potential for the transport of drugs through intestinal mucosa. Transport and bioadhesion behaviors of polymeric micelles was investigated using Caco-2 cell monolayer and everted rat intestine models. In order to show that Caco-2 cells can be used as a transport model cytotoxicity of formulations was tested. Cell viability was more than 80%, showing that Caco-2 cells will keep their viability during the transport studies demonstrating that prepared formulations can be securely used as oral drug carrier systems. Plain micelles were labeled with a fluorescent agent rhodamine-phosphatidylethanolamine (Rh-PE) and their transport through Caco-2 cells was investigated beside mTPP loaded micelles. At the end of 4h transport study through Caco-2 cells, cumulative transport (%) of fluorescent agents were around 14% and 1% in Rh-PE labeled and mTPP loaded micelles This difference was attributed to the different placement of mTPP and Rh-PE in the micellar core. Drug transport was not estimated in everted rat intestine model but the bioadhesion was 79% and 70% for mTPP loaded pluronic F127 and PEG(2000)-DSPE micelles. These good bioadhesion rates are promising for oral drug delivery.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Sezgin Z,Yuksel N,Baykara Tdoi
10.1016/j.ijpharm.2006.09.030subject
Has Abstractpub_date
2007-03-06 00:00:00pages
161-7issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(06)00782-4journal_volume
332pub_type
杂志文章abstract：:In the present paper the interaction between lambda carrageenan, a natural sulphated polysaccharide, and diltiazem HCl, a Ca channel blocking agent, was studied. Dialysis equilibria were performed to quantify the binding capacity of lambda carrageenan for diltiazem. The relevance of the interaction to hydrophilic matr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00389-6
更新日期：2000-05-10 00:00:00
abstract：:The work was aimed at developing an in vitro method able to provide rapid and reliable evaluation of drug absorption through buccal mucosa. Absorption simulator apparatus endowed with an artificial membrane was purposely developed by experimental design. The apparent permeation coefficient (Papp) through excised porci...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.06.032
更新日期：2018-08-25 00:00:00
abstract：:The role of water activity (a(w)), relative humidity (RH) and temperature on the hydration state of theophylline has been investigated. Slurry bridging experiments at controlled water activities, using powder X-ray diffraction (PXRD) and thermogravimetric analysis (TGA) to characterise the solid phase, established tha...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00277-6
更新日期：2002-10-24 00:00:00
abstract：:Although the extraordinary solubility advantage afforded by cyclodextrins has led to their widespread use as pharmaceutical solubilizers, several reports have emerged that cyclodextrins may also reduce the apparent permeability of the drug. With the purpose to investigate this solubility-permeability interplay, we hav...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.03.017
更新日期：2012-07-01 00:00:00
abstract：:Solid dosage forms are the pharmaceutical drug delivery systems of choice for oral drug delivery. These solid dosage forms are often coated to modify the physico-chemical properties of the active pharmaceutical ingredients (APIs), in particular to alter release kinetics. Since the product performance of coated dosage ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2013.03.053
更新日期：2013-12-05 00:00:00
abstract：:The aim of this work was to evaluate the suitability of stereolithography (SLA) to fabricate drug-loaded tablets with modified-release characteristics. The SLA printer creates solid objects by using a laser beam to photopolymerise monomers. In this work polyethylene glycol diacrylate (PEGDA) was used as a monomer and ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.03.016
更新日期：2016-04-30 00:00:00
abstract：:The forces experienced by the particles inside a twin screw granulator (TSG) are one of the most difficult parameters to measure quantitatively. However, it is possible to perform accurately this measurement through the use of dye containing calibrated microencapsulated sensors (CAMES) whose rupture is directly depend...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.12.052
更新日期：2019-03-10 00:00:00
abstract：:Biomaterials for applications in the urinary tract are challenged with both biofilm formation and encrustation, two highly interconnected processes. While great effort has been achieved developing promising materials there is only a limited choice of sophisticated in vitro models that are available to analyse the perf...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.04.023
更新日期：2018-07-30 00:00:00
abstract：:A wet-primed ready-to-use extracorporeal membrane oxygenation (ECMO) circuit is used in some centres for rapid deployment of ECMO during cardiopulmonary resuscitation. Yet, the potential release of plasticizer di(2-ethylhexyl)phthalate (DEHP) from the polyvinyl chloride tubing in the circuit during storage is a concer...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.01.030
更新日期：2005-04-27 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：:A centrifuge method has been applied to the assessment of water retention in pharmaceutical powders. Five drug models and microcrystalline cellulose (MCC) were each mixed with different amounts of water and centrifuged at different speeds. The amount of water retained by the wet mass was evaluated by drying the powder...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00201-x
更新日期：1999-10-15 00:00:00
abstract：:Exposure of a drug to irradiation can influence the stability of the formulation, leading to changes in the physicochemical properties of the product. The influence of excipients of frequently used stabilizers is often difficult to predict and, therefore, stability testing of the final preparation is important. The se...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/s0378-5173(01)00746-3
更新日期：2001-08-28 00:00:00
abstract：:Extruded 3D printing is emerging as an attractive fabrication technology in the field of personalized oral medicines. The objective of this study was to develop a tunable extruded 3D printing platform based on thermo-sensitive gelatin pastes to meet the needs of achieving different drug release characteristics with fl...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119360
更新日期：2020-06-15 00:00:00
abstract：:A simple and readily manoeuverable method for preparing immuno-magnetic liposomes that indigenously contain binding sites for attaching other molecules like antibodies on their exterior surface is described. In this method magnetic unilamellar vesicles are prepared from a mixture of phosphatidylcholine, cholesterol, s...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00667-0
更新日期：2001-03-14 00:00:00
abstract：:The role of the newly discovered cysteine protease, cathepsin K, in osteoporosis and rheumatoid arthritis is reviewed. The current development of cathepsin K inhibitors and their targeted delivery using synthetic polymer carriers are discussed. Future challenges and possible strategies to improve these delivery system...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2003.03.003
更新日期：2004-06-11 00:00:00
abstract：:Aerosolization behavior of carrier-free l-leucine coated salbutamol sulphate inhalable powders has been studied. L-Leucine coatings were formed by physical vapour deposition (PVD) on the surface of the spherical particles in the gas phase. While depositing L-leucine formed pointy crystalline asperities whose size and ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.08.017
更新日期：2009-01-05 00:00:00
abstract：:Hydrotalcite (HT), also known as a layered double hydroxide (LDH) compound, has been widely used in past years in the formulation of drugs due to its specific properties including good biocompatibility, null toxicity, high chemical stability and pH-dependent solubility which aid in drug controlled release. In this wor...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.04.048
更新日期：2016-06-15 00:00:00
abstract：:The aim of this study was to investigate the ability of L-leucine (LL) in preventing moisture-induced deterioration in the in vitro aerosolization performance of spray-dried (SD) salbutamol sulfate (SS). Increasing mass fraction of LL (5-80%) were co-spray dried with SS, and the physicochemical properties of the powde...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.07.033
更新日期：2017-09-15 00:00:00
abstract：:d-β-hydroxybutyrate and melatonin (BHB/MLT) infusion improves survival in hemorrhagic shock models. The original BHB/MLT formulation contains dimethyl sulfoxide (DMSO) to increase melatonin solubility. We formulated BHB/MLT solutions wherein DMSO was replaced either with 10% polyvinylpyrrolidone (BHB/MLT/PVP) or with ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.06.046
更新日期：2018-09-05 00:00:00
abstract：:Microemulsions show significant promise for enhancing the oral bioavailability of biopharmaceutics classification system (BCS) class II drugs, but how about class III drugs remains unclear. Here we employed metformin hydrochloride (MET) as the model drug and prepared drug-loaded water-in-oil (W/O) microemulsions selec...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.07.011
更新日期：2014-10-01 00:00:00
abstract：:Coronary artery disease is the first cause of death across the world. Targeted delivery of therapeutics through controlled release of micro- and nano-particles remains a very capable approach to develop new strategies in treating restenosis and atherosclerotic plaques. In this research, to produce the arterial geometr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.12.088
更新日期：2019-03-25 00:00:00
abstract：:The objective of this study was to gain insights into the structural integrity of PLGA during an ammonolysis-based microencapsulation process. PLGA (lactide:glycolide ratio=75:25; M(w)=25,925 g/mol) was dissolved in ethyl acetate or isopropyl formate (3-6 ml), which was emulsified in an aqueous phase. Ammonia, being a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.07.022
更新日期：2011-10-31 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：:The aim of this study was to investigate the impact of the addition of magnesium aluminum silicate (MAS), a natural clay, on the properties of polymeric films based on quaternary polymethacrylates (QPMs). Two commercially available aqueous QPM dispersions were studied: Eudragit(®) RS 30D and Eudragit(®) RL 30D (the dr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.10.016
更新日期：2013-12-15 00:00:00
abstract：:Poloxamer-407 (P-407) is a nonionic surfactant that induces atheroma formation in the aortas of C57BL/6 mice with long-term (14 weeks) administration. The objectives of the present study were to determine the mechanism(s) responsible for the induction of hypercholesterolemia as well as to determine whether this animal...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00834-1
更新日期：2001-10-23 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：:In this study, we evaluated the palatability of orally disintegrating tablets (ODTs) containing core granules with different particle sizes, coating, and types of materials using visual analog scales (VAS). Tableting the core granules into ODTs reduced rough mouth feel and improved overall palatability compared to the...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.ijpharm.2015.02.023
更新日期：2015-04-30 00:00:00
abstract：:Ciclopirox olamine (CPO) metal complexes have been prepared and characterized using elemental analysis, infra red (IR), melting point and differential scanning calorimetry (DSC). Spectroscopic titration using molar ratio method indicated the occurrence of 1:1 complexes for CPO with almost all the examined metals. Phys...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.11.009
更新日期：2005-01-31 00:00:00
abstract：:This paper reports on measurements of the release characteristics of the model drug salbutamol base from a liquid crystalline vehicle across a non-rate limiting synthetic membrane. The measured passive release rates were compared with analogous behaviour: (i) when a penetration enhancer such as oleic acid was incorpor...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00108-x
更新日期：2003-05-12 00:00:00
abstract：:Sodium salts are often used in drug formulation but their partial solubility parameters are not available. Sodium alters the physical properties of the drug and the knowledge of these parameters would help to predict adhesion properties that cannot be estimated using the solubility parameters of the parent acid. This ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00374-9
更新日期：2000-01-20 00:00:00
