Abstract：
PURPOSE:The lack of effective delivery vehicles impedes in vivo applications of siRNA. The trimethyl chitosan-cysteine (TC) nanoparticles (NPs) were developed for in vivo delivery of tumor necrosis factor α (TNF-α) siRNA via oral gavage and intraperitoneal injection. METHODS:The nanoparticles formulated from TC conjugate of 100, 200, and 500 kDa were prepared through ionic gelation with sodium tripolyphosphate, termed as TC100 NPs, TC200 NPs, and TC500 NPs, respectively. They were evaluated in terms of stability, siRNA protection, cellular uptake and TNF-α knockdown in peritoneal exudates macrophage cells (PECs), and in vivo TNF-α silencing in acute hepatic injury mice. RESULTS:TC100 NPs exhibited poor stability in simulated physiological environment compared to TC200 NPs and TC500 NPs. Compared to TC500 NPs, TC200 NPs could significantly enhance in vitro and in vivo cellular uptake by PECs and facilitate cytoplasmic siRNA release, resulting in high in vitro and in vivo TNF-α knockdown. Superior TNF-α suppressing level was obtained with TC200 NPs via oral gavage rather than intraperitoneal injection. CONCLUSIONS:The efficacies of in vivo TNF-α silencing were related to the molecular weight of TC conjugate and the administration route, which would assist in the rational design of siRNA vehicles.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
He C,Yin L,Tang C,Yin Cdoi
10.1007/s11095-013-1086-4subject
Has Abstractpub_date
2013-10-01 00:00:00pages
2596-606issue
10eissn
0724-8741issn
1573-904Xjournal_volume
30pub_type
杂志文章abstract：:Previous work from this laboratory showed site-dependent variations in the apparent permeability of insulin as measured using the everted rat gut sac technique, with the greatest permeability in the distal jejunum and the lowest in the duodenum (5). To quantify better the rate and extent of insulin absorption from the...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015894125611
更新日期：1992-08-01 00:00:00
abstract：PURPOSE:This work investigated the effect of relative humidity (RH) on bipolar electrostatic charge profiles of dry powder inhaler aerosols using the Bipolar Charge Analyzer (BOLAR). METHODS:Two commercial products, Pulmicort® (400 μg, budesonide) and Bricanyl® (500 μg, terbutaline sulfate) Turbuhaler®, were used as m...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2178-3
更新日期：2017-08-01 00:00:00
abstract：:The mechanical properties of dry and wet polymeric films prepared from various aqueous polymeric dispersions were evaluated by a puncture test. They were studied with respect to type of polymer dispersion [cellulosic: Aquacoat and Surelease; acrylic: Eudragit NE, L, RS, and RL 30 D], plasticizer type (water-soluble or...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018942127524
更新日期：1994-06-01 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
doi：10.1023/a:1016237216352
更新日期：1995-12-01 00:00:00
abstract：PURPOSE:To provide a systematic biophysical approach towards a better understanding of impact of conjugation chemistry on higher order structure and physical stability of an antibody drug conjugate (ADC). METHODS:ADC was prepared using thiol-maleimide chemistry. Physical stabilities of ADC and its parent IgG1 mAb were...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1274-2
更新日期：2014-07-01 00:00:00
abstract：:The interaction between several marker solutes and a polyolefin laminate polymer was studied in several solutions. Solutions studied included mixtures of sodium chloride and dextrose (at concentrations more less typical of i.v. administration solutions) and several actual i.v. products [lactated Ringer's injection, Di...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015866420836
更新日期：1991-06-01 00:00:00
abstract：PURPOSE:This work describes the synthesis of block co-polymeric micelles, methoxy-poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA) to encapsulate Curcumin (CUR), thereby improving the dispersibility and chemical stability of curcumin, prolonging its cellular uptake and enhancing its bioavailability. METHODS:CUR-mPEG...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1830-z
更新日期：2016-04-01 00:00:00
abstract：PURPOSE:The cause of antibody positive pure red cell aplasia associated with the subcutaneous administration of EPREX to patients with chronic kidney failure has been determined to be due to the leaching of weakly adjuvant compounds from the uncoated rubber stoppers that were formerly used in prefilled syringes. Other ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-5356-7
更新日期：2005-07-01 00:00:00
abstract：PURPOSE:Under different charging conditions, particles can be either attracted or repulsed by each other, causing powder agglomeration or segregation. Such behavior can be detrimental in many processes aimed at achieving particulate mixture homogeneity. Consequently, the effects of electrostatic charges on mixing kinet...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9934-0
更新日期：2006-05-01 00:00:00
abstract：PURPOSE:To study the structure and function of the intestinal H+/ peptide transporter PET1, we compared its amino acid sequence with those of related transporters belonging to the oligopeptide transporter family PTR, and with more distant transporter families. METHODS:We have developed a new approach to the sequence a...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012070726480
更新日期：1997-04-01 00:00:00
abstract：PURPOSE:A novel bioequivalence limit is proposed taking into account the therapeutic window. METHODS:The therapeutic range is introduced as the ratios maximum tolerated dose/therapeutic dose (MTD/D) and the therapeutic dose/lowest effective dose. The performance of the new acceptance range was compared with the method...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9680-6
更新日期：2008-11-01 00:00:00
abstract：PURPOSE:Novel itraconazole (ITZ)-based dry powders for inhalation (DPI) were optimized for aerodynamic and dissolution properties and contained excipients that are acceptable for inhalation. METHODS:The DPI were produced by spray drying solutions. The drug content, crystallinity state, and morphological evaluation of ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0779-4
更新日期：2012-10-01 00:00:00
abstract：:Nucleic acids are increasingly being considered for therapeutic uses, either to interfere with the function of specific nucleic acids or to bind specific proteins. Three types of nucleic acid drugs are discussed in this review: aptamers, compounds which bind specific proteins; triplex forming (antigene) compounds; whi...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1023/a:1016281324761
更新日期：1995-04-01 00:00:00
abstract：PURPOSE:The prognosis for glioma patients is poor, and development of new treatments is critical. Previously, we engineered polymer-based vaccines that control GM-CSF, CpG-oligonucleotide, and tumor-lysate presentation to regulate immune cell trafficking and activation, which promoted potent immune responses against pe...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0361-x
更新日期：2011-05-01 00:00:00
abstract：:The pharmacokinetics of trilostane and one of its metabolites ketotrilostane are described and characterized in the rat following the separate intravenous administration of trilostane and ketotrilostane. It was noted during these studies that the parent compound and its metabolite undergo metabolic interconversion-tri...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015828027060
更新日期：1992-04-01 00:00:00
abstract：PURPOSE:Microphysiological systems (MPS), also known as "organs-on-chips" or "tissue chips," leverage recent advances in cell biology, tissue engineering, and microfabrication to create in vitro models of human organs and tissues. These systems offer promising solutions for modeling human physiology and disease in vitr...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-019-2742-0
更新日期：2019-12-17 00:00:00
abstract：PURPOSE:Knowledge about the uptake mechanism and subsequent intracellular routing of non-viral gene delivery systems is important for the development of more efficient carriers. In this study we compared two established cationic polymers pDMAEMA and PEI with regard to their transfection efficiency and mechanism of cell...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9287-3
更新日期：2007-08-01 00:00:00
abstract：PURPOSE:The aim was to evaluate fluorescent molecular rotors (DCVJ and CCVJ), which are mainly sensitive to viscosity, for the characterization of polysorbate-containing IgG formulations and compare them to the polarity-sensitive dyes ANS, Bis-ANS and Nile Red. METHODS:IgG formulations with polysorbate 20 or 80 were s...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-0020-2
更新日期：2010-02-01 00:00:00
abstract：:The aim of this investigation was to assess whether immunosuppression induced by total-body irradiation (TBI) affects the pharmacodynamics of centrally acting drugs. Female Sabra rats were exposed to a single dose of gamma irradiation (5.3 Gy). Four days later, when both the cellular and the humoral immune responses w...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018928329824
更新日期：1994-05-01 00:00:00
abstract：PURPOSE:Scutellarin, a flavonoid derived from the plant Erigeron breviscapus, is currently widely used to treat cerebrovascular diseases, liver-related diseases, and hyperlipidemia in china and other East Asian countries. This study was to investigate the effect of scutellarin on the uptake of rosuvastatin in HEK293T c...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02950-5
更新日期：2020-10-29 00:00:00
abstract：PURPOSE:Design of intravaginal rings (IVRs) for delivery of antiretrovirals is often guided by in vitro release under sink conditions, based on the assumption that in vivo release will follow a similar release profile. METHODS:We conducted a dose-ranging study in the female reproductive tract of pigtail macaques using...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2224-1
更新日期：2017-10-01 00:00:00
abstract：:Penetration of various compounds through shed snake skin was measured in vitro to examine the effect of lipophilicity and molecular size of a compound on permeability through this model membrane. The permeabilities were found to be controlled by the lipophilicity and the molecular size of the permeant. The smaller and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015902308676
更新日期：1990-12-01 00:00:00
abstract：PURPOSE:The stability of lipid emulsions (LE) containing various cosurfactants (oleic acid, cholesterol, Tween 80, or HCO-60) was evaluated using the maximum total interaction energy, Vtmax and the energy barrier for coalescence, W. METHODS:The Vtmax and W were calculated from the zeta potential and the rate of increa...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016205203264
更新日期：1995-09-01 00:00:00
abstract：:The intrasubject and intersubject variabilities for CGS 16617, an angiotensin converting enzyme inhibitor, were evaluated in an open-label, repeat single-dose bioavailability trial. Eight healthy male volunteers each received a 20-mg oral dose of CGS 16617 as an aqueous solution on four separate occasions. Components ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015954609527
更新日期：1989-04-01 00:00:00
abstract：PURPOSE:This study aimed to develop a sustained-release formulation of exenatide (EXT) for the long-term therapeutic efficacy in the treatment of type II diabetes. METHODS:In this study, we present an injectable phospholipid gel by mixing biocompatible phospholipid S100, medium chain triglyceride (MCT) with 85% (w/w) ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1873-9
更新日期：2016-06-01 00:00:00
abstract：PURPOSE:Characterization of virosomes, in late stage preclinical development as vaccines for Respiratory Syncytial Virus (RSV), with a membrane-incorporated synthetic monophosphoryl lipid A, 3D-PHAD® adjuvant. METHODS:Virosomes were initially formed by contacting a lipid film containing 3D-PHAD® with viral membranes s...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2453-y
更新日期：2018-07-03 00:00:00
abstract：:Pediatric brain tumors are most common cancers in childhood and among the leading causes of death in children. Chemotherapy has been used as adjuvant (i.e. after) or neoadjuvant (i.e. before) therapy to surgery and radiotherapy for the management of pediatric brain tumors for more than four decades and gained more att...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-013-1196-z
更新日期：2014-03-01 00:00:00
abstract：:Using brine shrimp lethality to direct fractionation, extracts of the bark of Annona bullata Rich. (Annonaceae) have yielded 16 alpha-hydroxy-(-)-kauranoic acid as a bioactive plant constituent. This previously known diterpene showed significant (ED50 8.25 x 10(-2) micrograms/ml) and selective cytotoxicity against A-5...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015819422479
更新日期：1990-04-01 00:00:00
abstract：PURPOSE:This study aimed to assess impact of different vehicles for laser-assisted skin drug delivery. We also tried to uncover the mechanisms by which different vehicles affect laser-aided skin permeation. METHODS:Full-surface ablative (conventional) and fractional lasers were used to irradiate nude mouse skin. Imiqu...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1167-4
更新日期：2014-02-01 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
