Abstract：
PURPOSE:The lack of water-solubility hampers the use of many potent pharmaceuticals. Polymeric micelles are self-assembled nanocarriers with versatile properties that can be engineered to solubilize, target, and release hydrophobic drugs in a controlled-release fashion. Unfortunately, their large-scale use is limited by the incorporation methods available, especially when sterile dosage forms are sought. METHODS:In this manuscript, we describe a straightforward, economical, and innovative drug-loading procedure that consists in dissolving both the drug and an amphiphilic diblock copolymer in a water/tert-butanol mixture that is subsequently freeze-dried. RESULTS:We demonstrate that monodisperse 20-60 nm-sized drug-loaded polymeric micelles are produced directly and spontaneously upon rehydration of the freeze-dried cake. To establish the proof-of-principle, two hydrophobic taxane derivatives were solubilized in the micelles, and their partition coefficient was determined. CONCLUSIONS:This approach is efficient yet astonishingly simple and may be of great interest for scientists working in nanotechnology and pharmaceutical sciences.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Fournier E,Dufresne MH,Smith DC,Ranger M,Leroux JCdoi
10.1023/b:pham.0000029284.40637.69subject
Has Abstractpub_date
2004-06-01 00:00:00pages
962-8issue
6eissn
0724-8741issn
1573-904Xjournal_volume
21pub_type
杂志文章abstract：PURPOSE:To characterize the electrochemical behavior of the photodegradation product of nifedipine, i.e., 2,6-dimethyl-4-(2-nitrosophenyl)-3,5-pyridine-carboxylic acid dimethyl ester (NPD) in different electrolytic media. We also evaluated the interaction between free radicals generated from NPD and xeno/endobiotics. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015112216360
更新日期：2002-04-01 00:00:00
abstract：PURPOSE:The heparin-paclitaxel conjugates using amino acid as linker (HD2), with low anticoagulant activity, the similar anticancer activity as paclitaxel, offer great potential for further investigation. METHODS:Two types of heparin-paclitaxel conjugates (HD) have been developed, in which O-acetylated heparin as carr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9762-5
更新日期：2009-04-01 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：:A new enteric-coated formulation of sodium ursodeoxycholate was prepared and administered to man. The barrier film disintegrates and releases the drug only at pH > or = 5.5. The sodium salt of glycoursodeoxycholate was also prepared and encapsulated like ursodeoxycholate. Serum levels of ursodeoxycholate and glycourso...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018907825281
更新日期：1994-05-01 00:00:00
abstract：PURPOSE:This study aims to develop liposomal formulations containing synergistic antibiotics of colistin and ciprofloxacin for the treatment of infections caused by multidrug-resistant Pseudomonas aeruginosa. METHODS:Colistin (Col) and ciprofloxacin (Cip) were co-encapsulated in anionic liposomes by ammonium sulfate g...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2464-8
更新日期：2018-08-09 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：PURPOSE:An asymmetric membrane (AM) tablet was developed for a soluble model compound to study the in vitro drug release mechanisms in challenge conditions, including osmotic gradients, concentration gradients, and under potential coating failure modes. Porous, semipermable membrane integrity may be compromised by a hi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9142-y
更新日期：2007-02-01 00:00:00
abstract：:Excessive production of reactive oxygen species by alveolar macrophages (AMs) in response to inhaled toxic substances is a major cause of oxidative lung injury. Therapeutic approaches designed to protect the lungs from oxidative injury by administering native antioxidant enzymes such as catalase and superoxide dismuta...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018976529766
更新日期：1994-08-01 00:00:00
abstract：PURPOSE:This study focuses on the formulation optimization, in vitro and in vivo performance of differently sized nano-crystalline liquid suspensions and spray-dried powders of a poorly soluble BCS class II compound i.e. Danazol. METHODS:A DoE approach was utilized to optimize stabilizer concentration and formulate da...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1567-0
更新日期：2015-05-01 00:00:00
abstract：:Prinomide tromethamine, a nonsteroidal antiinflammatory drug, was orally administered at doses of 250, 500, and 1000 mg every 12 hr for 28 days to healthy male volunteers. The pharmacokinetic behavior of prinomide and its primary plasma metabolite displayed nonlinear characteristics, while those of free prinomide and ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018916811904
更新日期：1993-01-01 00:00:00
abstract：PURPOSE:[corrected] The purpose of this study was to design novel gastroretentive dosage forms (GRDFs) based on unfolding multilayer polymeric films, to investigate the mechanism of their gastroretentivity in dogs, and to assess the effect of compounding a narrow absorption window drug in a GRDF on the drug's absorptio...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1020412817716
更新日期：2002-10-01 00:00:00
abstract：PURPOSE:Ruthenium complex is a potentially theranostic agent for cancer imaging and therapy, however its application is limited due to poor water-solubility and lack of tumor selectivity. To overcome the above drawbacks, pH-sensitive nanocapsule as a novel targeting carrier was designed to deliver ruthenium complex for...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2021-2
更新日期：2016-12-01 00:00:00
abstract：PURPOSE:To test the hypothesis that coating particles with a highly bonding polymer is effective in improving tabletability of poorly compressible drugs. METHODS:Micronized acetaminophen (d (90) < 10 μm, Form I) was coated with 1%-10% (wt%) hydroxypropyl cellulose (HPC) by spray-drying. Phase nature of acetaminophen p...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0518-2
更新日期：2011-12-01 00:00:00
abstract：:Photodegradation of solutions of metronidazole in the presence and absence of sodium urate was studied. Photodegradation appeared to follow zero-order kinetics and was found to be dependent on the pH, buffer species, sodium urate concentration, and light source. Complex formation between metronidazole and sodium urate...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015851719579
更新日期：1989-01-01 00:00:00
abstract：PURPOSE:This study was conducted to demonstrate the use of differential scanning calorimetry (DSC) in detecting and measuring beta-relaxation processes in amorphous pharmaceutical systems. METHODS:DSC was employed to study amorphous samples of poly(vinylpyrrolidone) (PVP), indomethacin (IM), and ursodeoxycholic acid (...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-9044-4
更新日期：2006-02-01 00:00:00
abstract：PURPOSE:Drug transfer into milk is a general concern during lactation. Because data are limited in human subjects, particularly for new drugs, experimental animal models of lactational drug transfer are critical. This study analyzed drug transfer into milk in a mouse model, as well as the contribution of similar and di...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1085-5
更新日期：2013-09-01 00:00:00
abstract：PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011913723928
更新日期：1998-07-01 00:00:00
abstract：:Inkjet printing is an attractive material deposition and patterning technology that has received significant attention in the recent years. It has been exploited for novel applications including high throughput screening, pharmaceutical formulations, medical devices and implants. Moreover, inkjet printing has been imp...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-016-1931-3
更新日期：2016-08-01 00:00:00
abstract：PURPOSE:Radial basis function artificial neural networks and theoretical descriptors were used to develop a quantitative structure-pharmacokinetic relationship for structurally diverse drug compounds. METHODS:Human bioavailability values were taken from the literature and descriptors were generated from the drug struc...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000012154.09631.26
更新日期：2004-01-01 00:00:00
abstract：PURPOSE:A plasmid-based gene expression system was complexed with protective, interactive, and non-condensing (PINC) polymer system and administered with Medi-Jector, a needle-free injection device (NFID), to achieve high and sustained levels of antigen-specific antibodies in blood circulation. METHODS:Human growth ho...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018834305079
更新日期：1999-06-01 00:00:00
abstract：PURPOSE:Formulate phospho-sulindac (P-S, OXT-328) in a Pluronic hydrogel to be used as a topical anti-inflammatory agent and study its efficacy, safety and pharmacokinetics in an arthritis model. METHODS:LEW/crlBR rats with Freund's adjuvant-induced arthritis were treated with P-S formulated in Pluronic hydrogel (PSH)...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0953-8
更新日期：2013-06-01 00:00:00
abstract：:Various diesters of 9-[(1,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) were screened in order to identify a derivative with improved oral absorption. The solubilities and dissolution rates decreased with increasing chain length and branching of the ester group. However, the dipropionate ester showed an anomalously fas...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016462801968
更新日期：1987-04-01 00:00:00
abstract：PURPOSE:The present study evaluates immobilized artificial membrane (IAM) chromatography for predicting drug permeability across the blood-brain barrier (BBB) and outlines the potential and limitations of IAMs as a predictive tool by comparison with conventional methods based on octanol/water partitioning and octadecyl...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011904311149
更新日期：1998-08-01 00:00:00
abstract：PURPOSE:A rapid immune response is required to prevent death from Anthrax, caused by Bacillus anthracis. METHOD:We formulated a vaccine carrier comprised of acetalated dextran microparticles encapsulating recombinant protective antigen (rPA) and resiquimod (a toll-like receptor 7/8 agonist). RESULTS:We were able to p...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-0975-x
更新日期：2013-05-01 00:00:00
abstract：:The binding of 1-anilino-8-naphthalenesulfonate (ANS) to bovine serum albumin (BSA), human serum albumin (HSA), and human plasma has been studied by potentiometric titration utilizing a laboratory constructed ion selective electrode (ISE) of ANS. Three classes of ANS binding sites were found on BSA, HSA, and plasma at...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015855613083
更新日期：1991-07-01 00:00:00
abstract：PURPOSE:The study was performed for clarifying the mechanism of interaction between indoxyl sulfate (IS), a typical uremic toxin bound to site II, and site I-ligands when bound to human serum albumin (HSA). The effect of the N to B transition on the interactions was also examined. METHODS:Quantitative investigation of...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011014629551
更新日期：2001-04-01 00:00:00
abstract：:The influence of varying protein and fat content in milk of New Zealand White rabbits on the milk-to-plasma drug concentration (M/P) ratio of diazepam was studied. At various time points after littering, a bolus dose (1.5 mg/kg) followed by a 26-hr infusion (1.8 mg/h) of diazepam was administered to freely moving rabb...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015809418284
更新日期：1992-10-01 00:00:00
abstract：PURPOSE:To determine the correlation among progesterone dose, rate of import of progesterone-occupied progesterone receptor (PR) complexes into the nucleus of cells, and transcriptional activity of progesterone-PR complexes. METHODS:Live cell imaging and time-lapse microscopy of green fluorescent protein-tagged PR wer...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1026127015761
更新日期：2003-10-01 00:00:00
abstract：PURPOSE:To investigate the effect of benzofusion on NO donor properties and related biological activities of the furoxan system. The biological properties considered were the ability to increase the cytosolic levels of cGMP in C6 cells and vasodilation. METHODS:NO donor properties were investigated either in the prese...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018974409622
更新日期：1999-06-01 00:00:00
abstract：PURPOSE:To investigate, for the first time, the performance of a dry powder inhaler (DPI, Aerolizer(®)) in the case of a model drug (i.e. albuterol sulphate) formulated with spray dried mannitol carrier particles with homogeneous shape and solid-state form but different sizes. METHODS:Spray dried mannitol (SDM) partic...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1132-2
更新日期：2014-01-01 00:00:00
