Abstract:
:While the heightened tumor accumulation of systemically administered nanomedicines relative to conventional chemotherapeutic agents has been well established, corresponding improvements in therapeutic efficacy have often been incommensurate. This observation may be attributed to the limited exposure of cancer cells to therapy due to the heterogeneous intratumoral distribution and poor interstitial penetration of nanoparticle-based drug delivery systems. In the present work, the spatio-temporal distribution of block copolymer micelles (BCMs) of different sizes was evaluated in multicellular tumor spheroids (MCTS) and tumor xenografts originating from human cervical (HeLa) and colon (HT29) cancer cells using image-based, computational techniques. Micelle penetration was found to depend on nanoparticle size, time as well as tumor and spheroid cell line. Moreover, spheroids demonstrated the capacity to predict relative trends in nanoparticle interstitial transport in tumor xenografts. Overall, techniques are presented for the assessment of nanoparticle distribution in spheroids and xenografts and used to evaluate the influence of micelle size and cell-line specific tissue properties on micelle interstitial penetration.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Mikhail AS,Eetezadi S,Ekdawi SN,Stewart J,Allen Cdoi
10.1016/j.ijpharm.2014.01.010subject
Has Abstractpub_date
2014-04-10 00:00:00pages
168-77issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(14)00020-9journal_volume
464pub_type
杂志文章abstract::Active pharmaceutical ingredients (APIs) are predominantly organic solid powders. Due to their bulk properties many APIs require processing to improve pharmaceutical formulation and manufacturing in the preparation for various drug dosage forms. Improved powder flow and protection of the APIs are often anticipated cha...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.04.031
更新日期:2017-06-15 00:00:00
abstract::The purpose of this study was to develop a novel featured and flexible methotrexate (MTX) formulation, in which MTX was physically entrapped and chemically conjugated in the same drug delivery system. A series of poloxamer-MTX (p-MTX) conjugates was synthesized, wherein MTX was grafted to poloxamer through an ester bo...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.04.014
更新日期:2015-06-20 00:00:00
abstract::CHF5633 (Chiesi Farmaceutici, Italy) is a synthetic pulmonary surfactant currently under clinical development for the treatment of Respiratory Distress Syndrome in premature infants. The product is composed of phospholipids in liposomal organization, together with two peptide analogues of human surfactant proteins B a...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.10.045
更新日期:2018-12-20 00:00:00
abstract::The objective of this study was to investigate the presence of amino acid transporters on the corneal epithelium and to enhance corneal drug absorption through prodrug modification targeted to the amino acid transporters. SIRC was used as a model cell line representing the corneal epithelium. Uptake studies were carri...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(02)00405-2
更新日期:2002-10-24 00:00:00
abstract::Liposomal formulations were made using Solvent-assisted active loading technology (SALT). Two formulations composed of HSPC:DPPG:Chol:DSPE-mPEG2000 (PG-LipCUR) and HSPC:Chol:DSPE-mPEG2000 (LipCUR) demonstrated good colloidal properties and the CUR-encapsulation of 82% and 89% for PG-LipCUR and LipCUR, respectively. Th...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119211
更新日期:2020-04-30 00:00:00
abstract::Naltrexone hydrochloride (NTX) is a promising treatment for corneal disorders linked to diabetes mellitus (diabetic keratopathy). However, NTX has a major stability problem due to autoxidation, which is likely to hinder its formulation as eye drops for treatment of diabetic keratopathy. In this study, in-house develop...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.05.011
更新日期:2012-08-20 00:00:00
abstract::This study aims to investigate the effect of carrier characteristics and dosator capsule filling operation on the in vitro deposition of mixtures containing salbutamol sulphate (SS) and lactose and mannitol as model carrier materials. The carrier surfaces of lactose and mannitol were modified via wet decantation. The ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.06.044
更新日期:2015-08-01 00:00:00
abstract::The primary aim of the study was to investigate the effects of pulsed liquid feed on granule size. The secondary aim was to increase knowledge of this technique in granule size targeting. Pulsed liquid feed refers to the pump changing between on- and off-positions in sequences, called duty cycles. One duty cycle consi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.04.041
更新日期:2009-07-30 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::Previous data from our research group showed that chitosan-coated poly(isobutylcyanoacrylate) nanoparticles (NPs) (denoted PIBCA/Chito20) exhibited intrinsic anti-Trichomonas vaginalis activity, while PIBCA/pluronic® F68 without chitosan (PIBCA/F68) were inactive. However, the mechanism of anti-T. vaginalis activity o...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.07.006
更新日期:2018-09-05 00:00:00
abstract::The objective was to quantify drug loss due to cold flow (CF) in marketed estradiol transdermal drug delivery systems (TDDS), and study its influence on the in vitro flux and drug transfer across contacting skin. TDDS samples (products-A and B) were induced with CF at 25 and 32°C/60% RH by applying 1-kg force for 72h....
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.10.013
更新日期:2014-12-30 00:00:00
abstract::To evaluate the intestinal permeability of poorly water-soluble compounds, it is of importance to completely dissolve them in a medium and to avoid precipitation during experiments. This study was undertaken to find an agent possessing a high-solubilizing capacity and exhibiting minimal modulating impact on membrane i...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.05.003
更新日期:2004-08-06 00:00:00
abstract::9-(2-phosphonyomethoxypropyl)adenine (PMPA) and AMD3100 are highly potent and selective antiretroviral agents. Since PMPA is negatively charged and AMD3100 positively charged at physiological pH, their transepithelial transport and their potential for oral drug delivery is very low. In this study, ion pair formation w...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00150-7
更新日期:1999-09-20 00:00:00
abstract::A procedure is developed that allows particles inhaled with realistic breath patterns to be sized by cascade impaction at a constant flow rate. This procedure is then used to examine the difference between particle sizes obtained with constant flow rate (step profile) versus actual-subject breath patterns for two dry ...
journal_title:International journal of pharmaceutics
pub_type: 临床试验,杂志文章
doi:10.1016/s0378-5173(00)00569-x
更新日期:2000-12-04 00:00:00
abstract::Micellization offers several advantages for the delivery of water insoluble drugs including a nanoparticulate 'core-shell' delivery system for drug targeting. Recently, hydrophobically modified polysaccharides (HMPs) are gaining recognition as micelle forming polymers to encapsulate hydrophobic drugs. In this manuscri...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.01.005
更新日期:2016-03-16 00:00:00
abstract::The breast cancer resistance protein (BCRP) is an efflux transporter expressed at the apical surface of human brain endothelial cells of the blood-brain barrier (BBB). It was proposed as one of the transporters responsible for the development of drug resistance to several central nervous system (CNS) drugs, including ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.120161
更新日期:2021-01-25 00:00:00
abstract::Distribution of PLGA-microparticles in porcine skin, after its topical application, was studied in vitro using microparticles containing rhodamine as a fluorescent probe. PLGA-microparticles loaded with rhodamine were prepared using a solvent evaporation technique. Skin distribution of fluorescent microparticles was p...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(01)00811-0
更新日期:2001-09-11 00:00:00
abstract::Various strategies to deliver antimalarials using nanocarriers have been evaluated. However, taking into account the peculiarities of malaria parasites, the focus is placed mainly polymer-based chitosan nanocarriers. Our purpose of the study is to develop chitosan-tripolyphosphate (CS-TPP) nanoparticles (NPs) conjugat...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.05.064
更新日期:2012-09-15 00:00:00
abstract::In this study, the preparation of N-pamitoyl chitosan (ChP) anchored oleic acid (OA) liposome was demonstrated. Two different types of water-soluble ChPs with different degrees of acylation (DA) were selected for this study. The presence of ChPs on the surface of OA liposome was confirmed with their micrographs and ph...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.11.013
更新日期:2013-01-30 00:00:00
abstract::The pharmacokinetics of miconazole were studied after intravenous administration to six sheep (4 mg/kg) of three aqueous solutions: a marketed micellar solution containing polyoxyl-35 castor oil (Daktarin IV(R)) was compared with two solutions both containing 50 mM lactic acid and a cyclodextrin derivative (100 mM HP-...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(98)00403-7
更新日期:1999-03-25 00:00:00
abstract::The purpose of this research was to investigate drug dose, solubility, permeability, and their interplay, as key factors in oral formulation development for lipophilic drugs. A PEG400-based formulation was studied for five doses of the lipophilic drug carbamazepine, accounting for biorelevant dissolution of the dose i...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119307
更新日期:2020-05-30 00:00:00
abstract::This study demonstrates the use of optical coherence tomography (OCT) to simultaneously characterize the roughness of the tablet core and coating of pharmaceutical tablets. OCT is a high resolution non-destructive and contactless imaging methodology to characterize structural properties of solid dosage forms. Besides ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.12.023
更新日期:2018-01-30 00:00:00
abstract::This study focused on the design, biometric simulation and optimization of an intracranial nano-enabled scaffold device (NESD) for the site-specific delivery of dopamine (DA) as a strategy to minimize the peripheral side-effects of conventional forms of Parkinson's disease therapy. The NESD was modulated through biome...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.08.021
更新日期:2009-12-01 00:00:00
abstract::Poly[lactic-co-glycolide] (PLGA) nanoparticles, chitosan-dextran sulphate microparticles, and DOTAP-liposomes were prepared as vaccine adjuvants and drug carriers for a small hydrophilic model peptide, and their different physico-chemical properties (size, PDI, zeta-potential, pH-value and peptide loading) were invest...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.09.011
更新日期:2011-12-12 00:00:00
abstract::The key parameter of the oral film production process is the wet film thickness since it regulates the active pharmaceutical ingredient (API) content of the finished product. There is no general recommendation on how to adjust the gap height of the coating knife during the film manufacturing process to obtain the targ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.09.028
更新日期:2018-11-15 00:00:00
abstract::Maedi Visna virus (MVV) is an ovine lentivirus with high prevalence all over the world. Since conventional vaccines had failed in protecting animals against the infection, the development of a DNA vaccine can be an alternative. The candidate vaccine was constructed by cloning the sequence encoding MVV p25 protein and ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.05.005
更新日期:2009-07-30 00:00:00
abstract::In general, absorption enhancing effects of various absorption enhancers were greater in the large intestine than those in the small intestinal regions. Therefore, the effectiveness of absorption enhancers is expected to be remarkably observed, if these enhancers can be delivered to the large intestine with some poorl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.12.017
更新日期:2005-04-11 00:00:00
abstract::In this study, a temperature and ROS-responsive drug delivery system ROSP@MSN based on mesoporous silica nanoparticles has been designed and synthesized by taking advantage of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl acrylate modified polymers (ROSP) as "nano-valve", which can respond selectively to cance...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.11.025
更新日期:2018-01-30 00:00:00
abstract::The study of controlled release and drug release devices has been dominated by considerations of the bulk or average properties of material or devices. Yet the outermost surface atoms play a central role in their performance. The objective of this article has been to characterize the surface of hydrophilic matrix tabl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.11.054
更新日期:2015-01-15 00:00:00
abstract::The aim of this study was to introduce a fast and reliable differential scanning calorimetry (DSC)-based method to determine the monomolecular loading capacity of drugs with good glass-forming ability in mesoporous silica (MS). The proposed method is based on a solvent-free melting/fusion of drug into the MS during a ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.04.035
更新日期:2018-06-10 00:00:00