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 by spray drying. The effect of matrix former on the dissolution rate of dried ITZ nanosuspensions was investigated. Results from dissolution test revealed that spray-dried ITZ nanosuspensions (ITZ:HPMC:mannitol 1:0.5:2, w/w) preserved the high dissolution rate from nanosuspensions. After oral administration in rats, the AUC(0-36) from dried ITZ nanosuspensions was 1.5-fold and 1.8-fold higher than the AUC(0-36) from sporanox pellets (commercial product) in the fed and fasted states, respectively (p<0.05). More importantly, the AUC(0-36) from dried ITZ nanosuspensions showed no difference between fed/fasted states, because this formulation could enhance the adsorption of ITZ in target site (small intestine) regardless of food intake. In addition, dried ITZ nanosuspensions showed a lower inter-individual variability in terms of bioavailability. Positive results demonstrate that dried drug nanosuspensions formulation prepared by acid-base neutralization combined with spray drying may be a promising method for enhancing the oral bioavailability of poorly soluble drugs with pH-dependent solubility.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Mou D,Chen H,Wan J,Xu H,Yang Xdoi
10.1016/j.ijpharm.2011.04.034subject
Has Abstractpub_date
2011-07-15 00:00:00pages
237-44issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(11)00361-9journal_volume
413pub_type
杂志文章abstract::Autophagy is a lysosomal degradation pathway that acts as a cytoprotective mechanism causing treatment resistance in various cancer cells. Recent studies showed that hydroxychloroquine can inhibit the latter step of autophagy and therefore enhance the anti-glioma efficiency of ZD6474, a tyrosine kinase inhibitor. Howe...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.09.007
更新日期:2018-01-30 00:00:00
abstract::The present study puts forward a miniaturized high-throughput platform to understand influence of excipient selection and processing on the stability of a given drug compound. Four model drugs (sodium naproxen, theophylline, amlodipine besylate and nitrofurantoin) and ten different excipients were selected. Binary phy...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.08.025
更新日期:2013-08-30 00:00:00
abstract::The current investigation was carried out to identify appropriate parameters for measuring the in vitro release of tobramycin (TOB) ophthalmic ointments and to evaluate the feasibility of in vitro release testing methods to assess the product performance. Drug release was assessed using USP dissolution apparatus IV an...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119938
更新日期:2020-11-30 00:00:00
abstract::The kinetics of degradation of the new anti-tumor drug, 4-dedimethylamino sancycline (col-3) in aqueous solution at 25oC were investigated by high-pressure liquid chromatography (HPLC) over the pH-range of 2-10. The influences of pH, buffer concentration, light, temperature, and some additives on the degradation rate ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(98)00417-7
更新日期:1999-04-20 00:00:00
abstract::Developments in the field of molecular oncology have revealed that resistance to chemotherapeutics is acqured through several mechanisms including overexpression of common oncogenic proteins. Signal Transducer and Activator of Transcription 3 (STAT3) is one of these oncogenes that is overexpressed in many cancer types...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.04.034
更新日期:2017-06-15 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::The present investigation describes a procedure for the synthesis of a glycidyl methacrylated derivative from galactomannan, GA-MA, and the respective hydrogel formation. The galactomannan (GA), raw material, was purified and dissolved in DMSO. After dissolution, 4-dimethyl-amino-pyridine (DMAP) and glycidyl methacryl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2003.08.001
更新日期:2003-11-28 00:00:00
abstract::Albumin microparticles have found many applications in diagnosis and treatment in recent years and more than 100 diagnostic agents and drugs have been incorporated into albumin microparticles. In the present study, bovine serum albumin (BSA) based microparticles bearing captopril were prepared by an emulsification-hea...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.10.025
更新日期:2006-01-03 00:00:00
abstract::The purpose of the present study was to design and evaluate a novel wax matrix system containing various ratios of aminoalkyl methacrylate copolymer E (AMCE) and ethylcellulose (EC) as functional polymers in order to achieve the optimal acetaminophen (APAP) release rate for taste masking. A two factor, three level (3(...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.05.007
更新日期:2010-08-16 00:00:00
abstract::This work presents a study based on the preparation and characterization of drug-collagen hybrid materials. Materials used for obtaining drug-collagen hybrids were collagen type I (Coll) as matrix and fludarabine (F) and epirubicin (E) as hydrophilic active substances. After incorporation of drugs into Coll in differe...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.11.054
更新日期:2016-08-30 00:00:00
abstract::This work was aimed at assessing the preparation and characteristics of "dextran-magnetic layered double hydroxide-fluorouracil" liposomes (DMFL). DMFL was prepared by the optimized reverse evaporation method, which concerned the entrapment efficiency and slow-released effect. The factors affecting the entrapment effi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.04.010
更新日期:2013-06-25 00:00:00
abstract::The aim of this study was to prepare different types of paclitaxel-loaded, PLGA-based microparticles and lipidic implants, which can directly be injected into the brain tissue. Releasing the drug in a time-controlled manner over several weeks, these systems are intended to optimize the treatment of brain tumors. The l...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.07.028
更新日期:2006-05-18 00:00:00
abstract::Microneedle systems have gained attention as having many advantages over transdermal patches and hypodermic needles. The procedure provides adequate skin permeation rates without pain or severe infection. To obtain information for designing a microneedle system, macroneedles were used instead of microneedles to invest...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.02.046
更新日期:2006-06-19 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::In this work calcium stearate (CaSt) multi-particulates loaded with codeine phosphate (COP) were developed in an attempt to provide extended release (ER) combined with alcohol dose dumping (ADD) resistance. The pellets were prepared via wet/extrusion spheronization and ER characteristics were obtained after fluid bed ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.05.049
更新日期:2016-07-25 00:00:00
abstract::Lipid nanoparticles (LNs) are widely investigated for oral drug delivery, and for achieving significant advantages in colloidal stability, biocompatibility and scaled-up possibility. However, researchers face challenge of developing methods to improve the ability of LNs in overcoming multiple barriers (i.e., mucus and...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.02.015
更新日期:2017-03-30 00:00:00
abstract::The aim of present study was to develop folate appended PEGylated solid lipid nanoparticles(SLNs) of paclitaxel(FPS) and artemether(FAS). The SLNs were prepared by employing high pressure homogenization technique. The results of MTT assays revealed better cytotoxicity of FPS when given in combination with FAS on human...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119386
更新日期:2020-06-15 00:00:00
abstract::The aim of the present study was to investigate the relationship between formulation/process variables versus the critical quality attributes (CQAs) of cyclosporine ophthalmic ointments and to explore the feasibility of using an in vitro approach to assess product sameness. A definitive screening design (DSD) was used...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.04.042
更新日期:2018-06-10 00:00:00
abstract::An aerosol system is described for the generation and delivery of measured doses of monodisperse therapeutic drug particles to the human lungs. The system comprises a spinning top aerosol generator (STAG), aerosol chamber and inhalation control unit. Monodisperse aerosols allow drug particle size effects to be studied...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(03)00032-2
更新日期:2003-03-26 00:00:00
abstract::Ibuprofen (IBU) was chosen as a model drug to investigate the drug delivery rate. Mesoporous MCM-41 has been charged with ibuprofen (MCM-41_IBU). Calcium alginate was applied to encapsulate free drug and the mesoporous material. The system with double barrier demonstrated a slower release of IBU than free ibuprofen-lo...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.06.037
更新日期:2014-09-10 00:00:00
abstract::Cell-based and acute and subchronic in vivo toxicity profiles of a dendrimer based on melamine reveal that this class of molecules warrants additional study as vehicles for drug delivery. In cell culture, a substantial decrease in viability was observed at 0.1 mg/mL. For the acute studies, mice were administered 2.5, ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2004.04.023
更新日期:2004-08-20 00:00:00
abstract::Ball Milling technique has been used to prepare for the first time Vitis Vinifera extract-silica nanocomposites (VV-SiO2 NCs), which combine the pharmacological effects of the extract with the effectiveness of silica as drug delivery system and active component in the treatment of wound healing. Different contents (1....
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.08.057
更新日期:2018-11-15 00:00:00
abstract::A new targeted intravenous conjugate of nystatin with pentaerythritol poly(ethylene glycol)ether has been prepared and characterised (NY(4)-sPEG, M=25 160). The conjugate contains a beta-d-glucopyranoside molecular switch sensitive to beta-glucosidases (E.C.3.2.1.21), which are specifically present in the enzyme outfi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.10.034
更新日期:2010-02-15 00:00:00
abstract::Drug delivery using suitable polymeric devices has gathered momentum in the recent years due to their remarkable properties. The versatility of polymeric materials makes them reliable candidates for site targeted drug release. Among them biodegradable sutures has received considerable attention because they offer grea...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2017.03.041
更新日期:2017-05-30 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::Alkylcarbonates of gamma-cyclodextrins were produced and their inclusion complexes with four poorly water-soluble drugs of different structures and solubilities were prepared. The alkylcarbonates and the alkylcarbonate drug complexes were characterized by DSC and XRPD; the physical mixtures were used as control. Solub...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.03.001
更新日期:2007-07-18 00:00:00
abstract::The potential of two derivatives of vitamin E, i.e. α-tocopheryl phosphate (TP) and di-α-tocopheryl phosphate (T2P), for the protection and delivery of therapeutics is being investigated in our laboratory and some promising results have been obtained so far. Novel nanocarrier systems containing TP, T2P and different l...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.06.037
更新日期:2017-08-07 00:00:00
abstract::The objective of this work was to develop a fast and significant method for the determination of the intraparticulate pore size distribution of microspheres. Poly(lactide-co-glycolide) (PLGA) microspheres prepared with a solvent extraction/evaporation process were studied. From the envelope and the skeletal volume of ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.09.014
更新日期:2010-12-15 00:00:00
abstract::The aim of the current study was to improve the knowledge of drug-glycol-phospholipid-interactions and their effects in lamellar vesicle suitability as drug delivery systems. Liposomes were prepared using hydrogenated soy phosphatidylcholine (P90H, 60 mg/ml) and diclofenac sodium salt at two concentrations (5-10 mg/ml...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.08.034
更新日期:2013-11-01 00:00:00
abstract::Dissolution profiles of diltiazem hydrochloride (DIL) contained in core tablets from press-coated (PC) tablets with hydroxypropylmethylcellulose acetate succinate (HPMCAS) and plasticizers-adsorbent in the outer shell were investigated. Although, on the addition of triethyl citrate (TEC), triacetin (TA), and acetyltri...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(01)00578-6
更新日期:2001-04-17 00:00:00