Abstract：
PURPOSE:To develop novel biomineral-binding liposomes (BBL) for the prevention of orthopedic implant associated osteomyelitis. METHODS:A biomineral-binding lipid, alendronate-tri(ethyleneglycol)-cholesterol conjugate (ALN-TEG-Chol), was synthesized through Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition (a versatile click reaction). Mixing with other excipients, the new lipid was used to develop BBL. Thermodynamic behavior was studied by differential scanning calorimetry (DSC). In vitro biomineral-binding potential and kinetics were evaluated on hydroxyapatite (HA, a widely used material for orthopedic implant devices) particles. Oxacillin was encapsulated into BBL and used for in vitro evaluation in preventing Staphylococcus aureus biofilm formation. RESULTS:DSC analysis showed that ALN-TEG-Chol could inhibit the phase transition of liposomes by reducing its cooperativity, yielding liposomes with thermodynamic stability similar to liposomes containing regular cholesterol. BBL showed fast and strong binding ability to HA. Oxacillin-loading BBL demonstrated significantly better preventive efficacy against bacteria colonization when challenged with S. aureus isolate, implying its potential in preventing orthopedic implant associated osteomyelitis. CONCLUSIONS:In this proof of concept study, novel BBL has been successfully developed and validated for reducing the frequency of implantable device-related infections.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Liu XM,Zhang Y,Chen F,Khutsishvili I,Fehringer EV,Marky LA,Bayles KW,Wang Ddoi
10.1007/s11095-012-0812-7subject
Has Abstractpub_date
2012-11-01 00:00:00pages
3169-79issue
11eissn
0724-8741issn
1573-904Xjournal_volume
29pub_type
杂志文章abstract：:A simple viscometric method was used to quantify mucin-polymer bioadhesive bond strength. Viscosities of 15% (w/v) porcine gastric mucin dispersions in 0.1 N HCl (pH 1) or 0.1 N acetate buffer (pH 5.5) were measured with a Brookfield viscometer in the absence (eta m) or presence (eta t) of selected neutral, anionic, a...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015812615635
更新日期：1990-05-01 00:00:00
abstract：PURPOSE:To test the hypothesis of surface displacement as the underlying mechanism for IgG stabilization by polysorbates and HPβCD against surface-induced aggregation. METHODS:Adsorption/desorption-kinetics of IgG-polysorbate 80/-HPβCD were monitored. Maximum bubble pressure method was used for processes within second...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0854-x
更新日期：2013-01-01 00:00:00
abstract：PURPOSE:The purpose of this study was to assess the effect of several chemical permeation enhancers on the buccal permeability of nicotine and to image the spatial distribution of nicotine in buccal mucosa with and without buccal permeation enhancers. METHODS:The impact of sodium taurodeoxycholate (STDC), sodium dodec...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2332-y
更新日期：2018-02-21 00:00:00
abstract：PURPOSE:Chemically modified heparin-DOCA was prepared and found to have markedly lower anticoagulant activity than heparin. In the present study, we elucidated the antiangiogenic and antitumoral activities of heparin-DOCA derivative. METHODS:To evaluate the antiangiogenic and antitumoral effects of heparin-DOCA, capil...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9139-6
更新日期：2007-01-01 00:00:00
abstract：PURPOSE:Labrasol and Gelucire 44/14 are defined admixtures of acylglycerols and PEG esters which are substrates for digestive lipases. METHODS:We investigated their in vitro gastrointestinal lipolysis to understand which compounds are, after digestion, responsible for keeping poorly water-soluble drugs in solution. Th...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9906-2
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2117-3
更新日期：2017-05-01 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
abstract：PURPOSE:Comparison of the dissociation kinetics of rapid-acting insulins lispro, aspart, glulisine and human insulin under physiologically relevant conditions. METHODS:Dissociation kinetics after dilution were monitored directly in terms of the average molecular mass using combined static and dynamic light scattering....
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2233-0
更新日期：2017-11-01 00:00:00
abstract：:High molecular weight drugs in general, and peptides in particular, are usually delivered by parenteral route because they are poorly absorbed or degraded in the gastrointestinal tract. To optimize therapy, it is desirable to search for nonparenteral routes of administration and to deliver the drug in a controlled-rel...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018948924992
更新日期：1993-06-01 00:00:00
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journal_title：Pharmaceutical research
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doi：10.1007/s11095-012-0875-5
更新日期：2013-02-01 00:00:00
abstract：PURPOSE:To analyze the mechanics of some pharmaceutical agglomerates during uniaxial confined compression by using compression parameters derived from the Heckel, Kawakita and Adams equations, and to study the influence of these compression parameters on the tablet-forming ability of agglomerates. METHODS:Force and di...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007575120817
更新日期：2000-08-01 00:00:00
abstract：PURPOSE:The effect of the molecular weight of dextran on the molecular mobility and protein stability of freeze-dried serum gamma-globulin (BGG) formulations was studied. The stabilizing effect of higher molecular weight dextran is discussed in relation to the molecular mobility of the formulations. METHODS:The molecu...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012194220970
更新日期：1997-06-01 00:00:00
abstract：PURPOSE:To develop a semi-distributed liver model for the evaluation of saturable sinusoidal uptake and binding kinetics of the Oatp1a4 substrate digoxin. METHODS:In the perfused rat liver, two successive digoxin doses of 42 and 125 microg were administered, and the outflow concentration was determined by LC/MS/MS. [1...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0204-9
更新日期：2010-09-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012111902798
更新日期：1997-04-01 00:00:00
abstract：:A number of substituted phthalimide, 1, 8-naphthalimide, succinimide and glutarimide derivatives demonstrated significant hypolipidemic activity at 20 mg/kg/ day, I.P. after 16 days dosing. The N-(n-pentyl) succinimide proved to be the most potent analogue of the new compounds, lowering serum triglyceride levels 51 % ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016346018962
更新日期：1984-11-01 00:00:00
abstract：PURPOSE:Nanocrystalline drug-polymer dispersions are of significant interest in pharmaceutical delivery. The purpose of this work is to demonstrate the applicability of methods based on two-dimensional (2D) and multinuclear solid-state NMR (SSNMR) to a novel nanocrystalline pharmaceutical dispersion of ebselen with pol...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0713-9
更新日期：2012-07-01 00:00:00
abstract：PURPOSE:Understanding the critical factors governing the crystallization tendency of organic compounds is vital when assessing the feasibility of an amorphous formulation to improve oral bioavailability. The objective of this study was to investigate potential links between viscosity and crystallization tendency for or...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0540-4
更新日期：2012-01-01 00:00:00
abstract：PURPOSE:The purpose of this research was to evaluate the effect of ultrasound on mass transport across fetal membrane for direct fetal drug delivery and sensing of the amniotic fluid in a noninvasive manner. METHODS:Post-delivery human fetal membranes (chorioamnion) were used for in vitro experiments, in which the eff...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1470-8
更新日期：2015-02-01 00:00:00
abstract：PURPOSE:This study was conducted to investigate the cause of incomplete protein release from photopolymerized poly(ethylene glycol) (PEG) hydrogels and verify the protein-protection mechanism provided by iminodiacetic acid (IDA). METHODS:The in vitro release of bovine serum albumin (BSA) from PEG hydrogels prepared un...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2006-03-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9568-2
更新日期：2006-03-01 00:00:00
abstract：PURPOSE:Our previous studies indicated that drug leaked from discoidal reconstituted high density lipoprotein (d-rHDL) during the remodeling behaviors induced by lecithin cholesterol acyl transferase (LCAT) abundant in circulation, thus decreasing the drug amount delivered into the target. In this study, arachidonic ac...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1273-3
更新日期：2014-07-01 00:00:00
abstract：:The simultaneous diffusion and metabolism of the D- and L-isomers of the aminopeptidase substrate, leucine-p-nitroanilide (LPNA), were examined in vitro in the hamster cheek pouch. L-LPNA was completely hydrolyzed during diffusion across the cheek pouch, whereas D-LPNA crossed the cheek pouch intact. The metabolic bar...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015949614437
更新日期：1989-11-01 00:00:00
abstract：PURPOSE:Several phenomena in tablets indicate that an inhomogeneous pore distribution is formed during the compaction process. Examples are lamination and the capping of corners. In order to gain an understanding of the relation between structure and compact properties, analyzing the structure in a location dependent m...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-5280-x
更新日期：2005-08-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1019814713428
更新日期：2002-08-01 00:00:00
abstract：:Short-lived gamma emitting radioisotopes can be incorporated into polylactide/glycolide polymeric microspheres with various specific activities for possible use in understanding the in-vivo deposition, distribution and clearance of microparticulate drug carrier systems. The incorporated radiolabel is stable with negli...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1995-12-01 00:00:00
abstract：:Moisture sorption characteristics and the effect of moisture content on the compression properties of two dextrose-based directly compressible diluents, namely, Emdex (diluent A) and Sweetrex (diluent B) were studied. Both diluents sorbed moisture rapidly at relative humidities greater than 60%. For both the diluents,...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015889414533
更新日期：1991-03-01 00:00:00
abstract：PURPOSE:Tumor vascular normalization by antiangiogenic agents may increase tumor perfusion but reestablish vascular barrier properties in CNS tumors. Vascular priming via nanoparticulate carriers represents a mechanistically distinct alternative. This study investigated mechanisms by which sterically-stabilized liposom...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2012-12-01 00:00:00
abstract：PURPOSE:Nine common excipients were examined to determine their ability to cause disproportionation of the HCl salt of a a weakly basic compound. The goal was to determine which excipients were problematic and correlate the results to known properties such as surface pH, slurry pH, or molecular structure. Such a correl...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2013-06-01 00:00:00
abstract：PURPOSE:Hydrogen/deuterium (H/D) exchange over a range of temperatures suggests a protein structural/mobility transition in the solid state below the system glass transition temperature (Tg). The purpose of this study was to determine whether solid-state protein stability correlates with the difference between storage ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02897-7
更新日期：2020-08-13 00:00:00
abstract：PURPOSE:Proteasome inhibition induces endoplasmic reticulum (ER) stress and compensatory autophagy to relieve ER stress. Disturbance of intracellular calcium homeostasis can lead to ER stress and alter the autophagy process. It has been suggested that inhibition of the proteasome disrupts intracellular calcium homeosta...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1139-8
更新日期：2013-09-01 00:00:00
