Abstract:
PURPOSE:The in vitro inhibitory effect of Docetaxel (DTX) and Everolimus (EVR) alone and together in poly(ethylene glycol)-block-poly(D,L-lactic acid) (PEG-b-PLA) nanocarriers on angiogenic processes and acute toxicity in mice was evaluated. METHODS:PEG-b-PLA DTX and/or EVR nanocarriers were characterized for size, drug loading, stability, and drug release. Cell proliferation, tubule formation, and migration studies were performed in Human Umbilical Vein Endothelial Cells (HUVEC) and Maximum Tolerated Doses (MTD) studies were in mice. RESULTS:DTX and EVR loading was 1.93 and 2.00 mg/mL respectively with similar solubilities for dual-drug micelles. All micelles were below 30 nm with diffusion controlled drug release. The IC50 for DTX, EVR micelles were, 6.80 ± 0.67, 18.57 ± 2.86 and 0.65 ± 0.11 nM respectively with a synergistic inhibitory effect for dual-drug nanocarriers. Significant inhibition of tube formation occurred upon treatment with dual-drug nanocarriers as compared to individual micelles. EVR presence in dual-drug nanocarriers was able to significantly increase the inhibition of the migration of HUVEC by DTX. The MTDs for EVR, DTX and dual-drug micelles were 50, 30 and 20 mg/kg for each respectively. CONCLUSIONS:DTX-EVR dual-drug nanocarriers have antiangiogenic effects in vitro mediated through cellular angiogenic process and possess clinically relevant MTD.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Mishra GP,Doddapaneni BS,Nguyen D,Alani AWdoi
10.1007/s11095-013-1188-zsubject
Has Abstractpub_date
2014-03-01 00:00:00pages
660-9issue
3eissn
0724-8741issn
1573-904Xjournal_volume
31pub_type
杂志文章abstract:PURPOSE:The aim was to design and thoroughly characterize monodisperse Fe3O4@SiO2-Ag nanoparticles with strong antibacterial properties, which makes them a candidate for targeting bacterial infections. METHODS:The monodisperse Fe3O4 nanoparticles were prepared by oleic acid-stabilized thermal decomposition of Fe(III) ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2680-x
更新日期:2019-08-14 00:00:00
abstract:PURPOSE:This study uses high drug content solid dispersions for dose window extension beyond current demonstrations using fused deposition modelling (FDM) to; i) accommodate pharmaceutically relevant doses of drugs of varying potencies at acceptable dosage form sizes and ii) enable enhanced dose flexibility via modular...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2720-6
更新日期:2019-12-17 00:00:00
abstract:PURPOSE:This study was carried out to examine the blood-brain barrier (BBB) transport of human basic fibroblast growth factor (bFGF) and investigate its mechanism. METHODS:The BBB transport of 125I-bFGF was measured by several in vivo methods including intravenous administration, in situ internal carotid artery perfus...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007570509232
更新日期:2000-01-01 00:00:00
abstract::Molecular dynamics simulations and the generation of ad hoc chemical libraries are playing an increasingly important and recognized role in structure-based virtual screening. These approaches are important for treating target flexibility and improving the drug discovery pipeline. In this article I will comment on thes...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1012-9
更新日期:2013-05-01 00:00:00
abstract:PURPOSE:Development of a human mitochondrial gene delivery vector is a critical step in the ability to treat diseases arising from mutations in mitochondrial DNA. Although we have previously cloned the mouse mitochondrial genome in its entirety and developed it as a mitochondrial gene therapy vector, the human mitochon...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0527-1
更新日期:2011-11-01 00:00:00
abstract::Since many chiral pharmaceutical excipients, such as cellulose polymers and cyclodextrins, are used as stationary phases for the separation of enantiomers by high performance liquid chromatography (HPLC), it is hypothesized that one enantiomer of a chiral drug will be released faster than the other from a pharmaceutic...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018937123058
更新日期:1993-11-01 00:00:00
abstract:PURPOSE:The aim of this study was to examine if sparging with CO2(g) could be used to establish stable biorelevant bicarbonate buffers, in aqueous medium, for use in dissolution characterization of low-solubility ionizable drugs. METHODS:Preparation of the bicarbonate-containing dissolution medium was monitored by use...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1026147620304
更新日期:2003-10-01 00:00:00
abstract:PURPOSE:Study on curcumin dissolved in natural deep eutectic solvents (NADES) was aimed at exploiting their beneficial properties as drug carriers. METHODS:The concentration of dissolved curcumin in NADES was measured. Simulated gastrointestinal fluids were used to determine the concentration of curcumin and quantum c...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2643-2
更新日期:2019-06-03 00:00:00
abstract:PURPOSE:To examine and determine the sites and the kinetics of IgG1 mAb modifications from both in vitro (rat plasma and PBS) and in vivo (rat model) time-course studies. METHODS:A comprehensive set of protein characterization methods, including RPLC/MS, LC-MS/MS, iCIEF, capSEC, and CE-SDS were performed in this repor...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0860-z
更新日期:2013-01-01 00:00:00
abstract:PURPOSE:To study the influence of crystallizing and non-crystallizing cosolutes on the crystallization behavior of trehalose in frozen solutions and to monitor the phase behavior of trehalose dihydrate and mannitol hemihydrate during drying. METHODS:Trehalose (a lyoprotectant) and mannitol (a bulking agent) are widely...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0221-8
更新日期:2010-11-01 00:00:00
abstract::New generation vaccines, particularly those based on recombinant proteins and DNA, are likely to be less reactogenic than traditional vaccines but are also less immunogenic. Therefore, there is an urgent need for the development of new and improved vaccine adjuvants. Adjuvants can be broadly separated into two classes...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1016104910582
更新日期:2002-06-01 00:00:00
abstract::Colonic absorption of recombinant human insulin-like growth factor I (rhIGF-I) was measured in vitro using both rat and minipig colon. The permeability coefficients were 8.03 +/- 1.03 and 4.75 +/- 0.43 x 10(-8) cm sec-1 in the rat and minipig, respectively. The steady-state flux in rat colon was linearly related to th...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018999106684
更新日期:1994-02-01 00:00:00
abstract:PURPOSE:To assess the effects of co-delivering osteoinductive DNA and/or small interfering RNA in directing the osteogenic differentiation of human adipose-derived stem cells (hADSCs) using a combinatorial, non-viral gene delivery approach. METHODS:hADSCs were transfected using combinations of the following genes: BMP...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0406-9
更新日期:2011-06-01 00:00:00
abstract:PURPOSE:Generalizations based upon behavior of small molecules have established that a crystalline solid is generally much more stable toward chemical degradation than is the amorphous solid. This study examines the validity of this generalization for proteins using biosynthetic human insulin as the model protein. MET...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012164520429
更新日期:1997-10-01 00:00:00
abstract:PURPOSE:To develop a semi-physiological-based model describing simultaneously the time course of immature and mature B-lymphocytes after topotecan (TPT) administration to tumor-bearing rats. METHODS:Twenty-four tumor-bearing BDIX male rats received a single 6 mg/kg intra-peritoneal dose of TPT or saline. Mature and im...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-0025-x
更新日期:2010-03-01 00:00:00
abstract::Nonstereospecific studies have indicated that the pharmacokinetics of propranolol (PR) are altered in inflammatory conditions such as arthritis. However, as the kinetics and dynamics of PR are stereoselective, we examined the effect of adjuvant arthritis (AA) on the disposition of the individual enantiomers. A novel n...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018907431893
更新日期:1993-02-01 00:00:00
abstract:PURPOSE:The organic cation transporters (OCTs) and multidrug and toxin extrusions (MATEs) together are regarded as an organic cation transport system critical to the disposition and response of many organic cationic drugs. Patient response to the analgesic morphine, a characterized substrate for human OCT1, is highly v...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2526-y
更新日期:2018-10-25 00:00:00
abstract::A liposomal formulation of methylprednisolone (L-MPL) was developed to improve localization of this immunosuppressant in lymphatic tissues. Liposomes containing MPL were formulated from a mixture of phosphatydylcholine and phosphatydylglycerol (molar ratio, 9:1) and sized by extrusion through a 0.1-micron membrane. Ma...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018954704886
更新日期:1993-10-01 00:00:00
abstract:PURPOSE:To better understand the nature of drug-excipient interactions we have studied the phase behavior of amorphous binary and ternary mixtures of citric acid, indomethacin and PVP, as model systems. METHODS:We have prepared amorphous mixtures by co-melting or coprecipitation from solvents, and have measured glass ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011983606606
更新日期:1998-08-01 00:00:00
abstract::The plasma concentration-time profiles and pharmacokinetics were characterized for nicotine and its major metabolite, cotinine, after multiple daily application of a nicotine user-activated transdermal therapeutic system (UATTS) to nine healthy smokers. The volunteers abstained from smoking 24 hr prior to and during t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015810019076
更新日期:1991-03-01 00:00:00
abstract:PURPOSE:To investigate the effect of polyelectrolytes on the formation and physicochemical properties of chitosan nanoparticles (CS-NPs) used for the delivery of an anticancer drug, doxorubicin (DOX). METHOD:Three DOX-loaded CS-NPs were formulated with tripolyphosphate (CS-TP/DOX NPs), dextran sulfate (CS-DS/DOX NPs),...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1251-9
更新日期:2014-05-01 00:00:00
abstract:PURPOSE:To investigate whether conjunctival epithelial cells express transport processes for opioid peptides. METHODS:We monitored the uptake of [(3)H]deltorphin II and [(3)H]DADLE, two hydrolysis-resistant synthetic opioid peptides, in the rabbit conjunctival epithelial cell line CJVE and elucidated the characteristi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9709-x
更新日期:2009-05-01 00:00:00
abstract:PURPOSE:To compare the systemic delivery of deslorelin following intratracheal administration of different deslorelin formulations. The formulations included dry powders of deslorelin, large-porous deslorelin-poly(lactide-co-glycolide) (PLGA) particles, and small conventional deslorelin-PLGA particles. Also, solution f...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000032997.96823.88
更新日期:2004-07-01 00:00:00
abstract:PURPOSE:We describe the AERX aerosol delivery system, a new, bolus inhalation device that is actuated at preprogrammed values of inspiratory flow rate and inhaled volume. We report on its in vitro characterization using a particular set of conditions used in pharmacokinetic and scintigraphic studies. METHODS:Multiple ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012058323754
更新日期:1997-03-01 00:00:00
abstract:PURPOSE:The investigation was aimed at developing micellar nanocarriers for nose-to-brain delivery of zolmitriptan with the objective to investigate the pathway involved in the drug transport. METHODS:The micellar nanocarrier was successfully formulated and characterized for particle size and shape by multi-angle dyna...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-0041-x
更新日期:2010-04-01 00:00:00
abstract:PURPOSE:The passage of molecules across cell membranes is a crucial step in many physiological processes. We therefore seek physical models of this process, in order to predict permeation for new molecules, and to better understand the important interactions which determine the rate of permeation. METHODS:Several sets...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007543708522
更新日期:2000-08-01 00:00:00
abstract:PURPOSE:Gastrointestinal deposition of nanoparticles was examined after oral administration to mice suffering from an experimental gastric ulcer model. Local drug delivery could reduce side effects and would be a distinct improvement compared to existing therapeutic approaches, e.g. in the local therapy of Helicobacter...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9834-1
更新日期:2009-05-01 00:00:00
abstract:PURPOSE:To study the pulmonary absorption and tolerability of various formulations of the decapeptide cetrorelix acetate in rats by a new aerosol delivery system (ASTA-ADS) for intratracheal application. METHODS:Using the ASTA-ADS, cetrorelix liquid formulations (aqueous solutions for ultrasonic nebulization) were fir...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011028227155
更新日期:2001-06-01 00:00:00
abstract::(+)-Propranolol was infused at two rates into the pyloric vein (a portal vein tributary) of 15 male Sprague Dawley rats until apparent steady-state conditions were established (i.e., 8 hr at each rate). One group (n = 7) received the high dose (40 micrograms/min/kg) first, and in the other group (n = 8) the low dose (...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018921306200
更新日期:1994-03-01 00:00:00
abstract::The transepithelial transport of arginine vasopressin (AVP) across cultured rat alveolar epithelial cell monolayers was studied. At 0.1 nM donor [125I]AVP, the radiolabel flux measured in the apical-to-basolateral (AB) direction was about 10 times greater than that in the reverse (BA) direction. HPLC analyses of the b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018918022865
更新日期:1994-11-01 00:00:00