Abstract：
PURPOSE:We have evaluated a new process, involving solution-enhanced dispersion by supercritical fluids (SEDS), for the production of polymeric microparticles. METHODS:The biodegradable polymers, Poly (DL-lactide-co-glycolide): copolymer composition 50:50 (DL-PLG), Poly (L-lactide) (L-PLA), Poly (DL-lactide) (DL-PLA) and Polycaprolactone (PCL), were used for preparation of microparticles using SEDS. Solutions of the polymers in organic solvents were dispersed and sprayed with supercritical CO2. Extraction of the organic solvents resulted in the formation of solid microparticles. The amounts of highly toxic solvents such as dichloromethane (MC) were reduced in the process. RESULTS:Microparticles were obtained from all polymers. The mean particle size and shape varied with the polymer used. The morphology of the particles was strongly affected by the choice of polymer solvent. Discrete spherical microparticles of DL-PLG were produced with a mean volumetric diameter of 130 microm. The microparticles of the L-PLA were almost spherical, and their size increased from 0.5 to 5 microm as the density of supercritical CO2 decreased. PCL formed microparticles with diameters of 30-210 microm and showed a strong tendency to form films at high pressure. CONCLUSIONS:The SEDS process appears a promising method for production of microparticles from biodegradable polymers without the use of toxic solvents.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Ghaderi R,Artursson P,Carlfors Jdoi
10.1023/a:1018868423309subject
Has Abstractpub_date
1999-05-01 00:00:00pages
676-81issue
5eissn
0724-8741issn
1573-904Xjournal_volume
16pub_type
杂志文章abstract：PURPOSE:To compare the physical stability of amorphous molecular level solid dispersions of nifedipine and felodipine, in the presence of poly(vinylpyrrolidone) (PVP) and small amounts of moisture. METHODS:Thin amorphous films of nifedipine and felodipine and amorphous molecular level solid dispersions with PVP were s...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9420-3
更新日期：2008-03-01 00:00:00
abstract：PURPOSE:It was the aim of this study to synthesize and characterize a novel chitosan-glutathione (GSH) conjugate providing improved mucoadhesive and permeation-enhancing properties. METHODS:Mediated by carbodiimide and N-hydroxysuccinimide, glutathione was covalently attached to chitosan via the formation of an amide ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-6248-6
更新日期：2005-09-01 00:00:00
abstract：:Nanoparticles, including lipopolyamines leading to lipoplexes, liposomes, and polyplexes are targeted drug carrier systems in the current search for a successful delivery system for polynucleic acids. This review is focused on the impact of gene and siRNA delivery for studies of efficacy, pharmacodynamics, and pharmac...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-008-9646-8
更新日期：2009-01-01 00:00:00
abstract：PURPOSE:Hydroxylation of the antidepressant and smoking deterrent drug bupropion is a clinically important bioactivation and elimination pathway. Bupropion hydroxylation is catalyzed selectively by cytochrome P4502B6 (CYP2B6). CYP2B6-catalyzed bupropion hydroxylation has been used as an in vitro and in vivo phenotypic ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9535-1
更新日期：2008-06-01 00:00:00
abstract：PURPOSE:4-Phenylbutyrate (4-PBA) is expected to be a potential therapeutic for several neurodegenerative diseases. These activities require 4-PBA transport into the brain across the blood-brain barrier (BBB). The objective of the present study was to characterize the brain transport mechanism of 4-PBA through the BBB. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1912-6
更新日期：2016-07-01 00:00:00
abstract：:Monte Carlo simulation technique used to evaluate the effect of the arrangement of concentrations on the efficiency of estimation of population pharmacokinetic parameters in the preclinical setting is described. Although the simulations were restricted to the one compartment model with intravenous bolus input, they pr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016267811074
更新日期：1995-05-01 00:00:00
abstract：PURPOSE:Information on genetic variants that affect the pharmacokinetics and pharmacodynamics (PK/PD) of drugs in different populations from Mexico is still an ongoing endeavor. Here, we investigate allele frequencies on pharmacogenetic targets in Mexican Mestizos and Natives from three different States and its associa...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1990-5
更新日期：2016-11-01 00:00:00
abstract：PURPOSE:To investigate the effect of tyrphostin 8 (T-8), a GTPase inhibitor, on transferrin receptor (TfR)-mediated transcytosis of insulin-transferrin (In-Tf) conjugate in cultured enterocyte-like Caco-2 cells and on gastrointestinal (GI) absorption of In-Tf in streptozotocin (STZ)-induced diabetic rats. METHODS:Caco...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011032502097
更新日期：2001-02-01 00:00:00
abstract：PURPOSE:We present a smart intradermal interface suitable for skin-attached drug delivery devices. Our solution enables injections or infusions that are less invasive compared to subcutaneous injections and are leakage-free at the location of penetration. METHODS:The intradermal interface is based on a 31-gauge cannul...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0319-z
更新日期：2011-03-01 00:00:00
abstract：:Gene delivery vectors based on adeno-associated virus (AAV) are highly promising due to several desirable features of this parent virus, including a lack of pathogenicity, efficient infection of dividing and non-dividing cells, and sustained maintenance of the viral genome. However, several problems should be addresse...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-007-9431-0
更新日期：2008-03-01 00:00:00
abstract：PURPOSE:The aim was to investigate anticancer drug-loaded poly(carbonate-ester) nanospheres as potential drug delivery systems for cancer therapy. METHODS:Functional poly(carbonate-ester) copolymers (HPCP-SD) were synthesized by the incorporation of sulfadiazine as the tumor-targeting groups to hydroxyl groups of poly...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0275-7
更新日期：2010-12-01 00:00:00
abstract：PURPOSE:The pharmacokinetics of corticosteroids in pregnancy were analyzed to assess maternal/fetal disposition and factors controlling fetal exposure. Area/Moment equations and compartmental models for estimating pharmacokinetic parameters from single dose data during pregnancy were developed. METHODS:Betamethasone i...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-004-7681-7
更新日期：2004-12-01 00:00:00
abstract：PURPOSE:Gastroduodenal and intestinal permeability were compared after single doses of sustained release and regular release flurbiprofen in the rat to assess possible site-specific formulation-dependent toxicity. METHODS:Pharmacokinetics was assessed and gastrointestinal permeability was evaluated using sucrose and 5...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012134503107
更新日期：1997-11-01 00:00:00
abstract：:The transport of thyrotropin releasing hormone (TRH) in rabbit buccal mucosa in vitro has been investigated with respect to (a) rate and type of metabolism of TRH on mucosal and serosal sides of buccal mucosa, (b) mechanism of TRH transport including charge effect on its permeability, and (c) pathway and rate-limiting...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015883217858
更新日期：1992-09-01 00:00:00
abstract：PURPOSE:To identify the molecules responsible for amyloid beta-peptide (1-40) (Abeta(1-40)) uptake by the liver, which play a major role in the systemic clearance of Abeta(1-40). METHODS:The liver uptake index method was used to examine the mechanisms of Abeta(1-40) uptake by the liver in vivo. RESULTS:[125I]Abeta(1-...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-0208-7
更新日期：2006-07-01 00:00:00
abstract：:An open, randomized, six-way crossover study was conducted in 12 healthy males to assess pharmacokinetics and bioinversion of ibuprofen enantiomers. The mean plasma terminal half-life (t1/2) of R(-)ibuprofen was 1.74 hr when intravenously infused as a racemic mixture and was 1.84 hr when intravenously infused alone. T...
journal_title：Pharmaceutical research
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1023/a:1018969506143
更新日期：1994-06-01 00:00:00
abstract：PURPOSE:To show that atomic force microscopy (AFM) can be used to directly study the electrostatic charging and dissipation of single pharmaceutical particles. MATERIALS AND METHODS:Particles of lactose attached to AFM cantilevers were charged on a glass surface at a relative humidity (RH) of 0.1%. By recording force-...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9230-z
更新日期：2007-06-01 00:00:00
abstract：PURPOSE:To assess the effects of selective lipid extraction and tape stripping on transepidermal water loss (TEWL) at three body regions in the pig. METHODS:Lipids were extracted from the abdominal, inguinal. and back regions using three different solvent extraction procedures or cellophane tape stripping (15x) on Yor...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1010944529387
更新日期：2001-07-01 00:00:00
abstract：PURPOSE:A major challenge facing nanoparticle-based delivery of chemotherapy agents is the natural and unavoidable accumulation of these particles in healthy tissue resulting in local toxicity and dose-limiting side effects. To address this issue, we have designed and characterized a new prodrug nanoparticle with contr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2205-4
更新日期：2017-10-01 00:00:00
abstract：:One of the barriers to transdermal delivery of peptides is the metabolic activity of the epidermis. To define this metabolic activity, aminopeptidase activity and Leu-enkephalin metabolism were measured in the epidermis obtained from neonatal mouse skin and in cultured mouse keratinocytes. Aminopeptidase activity was ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015882323677
更新日期：1991-01-01 00:00:00
abstract：PURPOSE:Recently identified organic solute transporter (Ost) alpha and beta are located on the basolateral membrane of enterocytes and may be responsible for the intestinal absorption of many substrates including bile acids. In the present study, the mechanism governing the transcriptional regulation of their expressio...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9163-6
更新日期：2007-02-01 00:00:00
abstract：PURPOSE:The combination of morphine and gabapentin seems promising for the treatment of postoperative and neuropathic pain. Despite the well characterised pharmacodynamic interaction, little is known about possible pharmacokinetic interactions. The aim of this study was to evaluate whether co-administration of the two ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1988-z
更新日期：2016-11-01 00:00:00
abstract：PURPOSE:The objective of the current study was to investigate whether blood-brain barrier (BBB) permeability studies in vitro could be accelerated by running several compounds together in the same experiment. METHODS:To address this question, we compared the transport of six compounds run separately with the results o...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000026424.78528.11
更新日期：2004-05-01 00:00:00
abstract：PURPOSE:To devise experimental and computational models to predict aqueous drug solubility. METHODS:A simple and reliable modification of the shake flask method to a small-scale format was devised, and the intrinsic solubilities of 17 structurally diverse drugs were determined. The experimental solubility data were us...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1014224900524
更新日期：2002-02-01 00:00:00
abstract：PURPOSE:The purpose of the current study is to evaluate the solubility advantage offered by celecoxib (CEL) amorphous systems and to characterize and correlate the physical and thermodynamic properties of CEL and its amorphous molecular dispersions containing poly(vinylpyrrolidone) (PVP). METHODS:The measurement of cr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000045226.42859.b8
更新日期：2004-10-01 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：PURPOSE:The gadopentetic acid (Gd-DTPA)-loaded chitosan nanoparticles (Gd-nanoCPs) were prepared for gadolinium neutron-capture therapy (Gd-NCT) and characterized and evaluated as a device for intratumoral (i.t.) injection. METHODS:Gd-nanoCPs were prepared by a novel emulsion-droplet coalescence technique. The effects...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018995124527
更新日期：1999-12-01 00:00:00
abstract：PURPOSES:To evaluate the effects of component contents in different colistin methanesulfonate (CMS) formulas on their clinical pharmacokinetics of the prodrug CMS and the formed colistin. METHODS:Two CMS formulas (CTTQ and Parkedale) were investigated in a single dose, randomized, open-label, crossover study conducted...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-021-02991-4
更新日期：2021-01-26 00:00:00
abstract：:A method of immobilizing urokinase on albumin microspheres has been developed. Laser scattering, which was used to follow particle size from the initial emulsification stage to the final aqueous resuspension of the microsphere stage, showed that particle coalescence and crosslinking were critical parameters in manufac...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015855622459
更新日期：1992-06-01 00:00:00
abstract：PURPOSE:Cationic host defence peptides constitute a promising class of therapeutic drug leads with a wide range of therapeutic applications, including anticancer therapy, immunomodulation, and antimicrobial activity. Although potent and efficacious, systemic toxicity and low chemical stability have hampered their comme...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1658-6
更新日期：2015-08-01 00:00:00
