Abstract:
PURPOSE:Solid lipid nanoparticles (SLNs) have been proposed as a colloidal carrier system that could enhance the oral bioavailability of curcumin. However, a burst release of the loaded drug, which occurs in acidic environments, has been a main obstacle to the oral delivery of curcumin by using SLNs as a carrier system. We hypothesized that a quarternized chitosan derivative could be used for acid-resistant coating to stabilize the SLNs and circumvent the burst release. METHODS:N-trimethyl chitosan (TMC) was synthesized and determined by (1)H-NMR and FT-IR. To investigate the details of chitosan and TMC surface modification on SLCNs composed of palmitic acid, cholesterol, TPGS and curcumin, a number of factors such as optimized SLNs composition, solid state characterization, stability, cell viability, in vitro release in GI conditions, curcumin oral bioavailability and brain distribution studies, were evaluated. RESULTS:The TMC-SLCNs exhibited prolonged stability in room and refrigerated conditions, controlled drug release in simulated intestinal fluid, significantly higher oral bioavailability, and brain distribution of curcumin than free curcumin, chitosan and non-coated SLCNs. CONCLUSIONS:These finding suggests that the TMC-SLCNs is a promising nanocarrier system for oral delivery and brain distribution of curcumin.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Ramalingam P,Ko YTdoi
10.1007/s11095-014-1469-1subject
Has Abstractpub_date
2015-02-01 00:00:00pages
389-402issue
2eissn
0724-8741issn
1573-904Xjournal_volume
32pub_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::Magnetic nanoparticles are useful as contrast agents for magnetic resonance imaging (MRI). Paramagnetic contrast agents have been used for a long time, but more recently superparamagnetic iron oxide nanoparticles (SPIOs) have been discovered to influence MRI contrast as well. In contrast to paramagnetic contrast agent...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-012-0711-y
更新日期:2012-05-01 00:00:00
abstract:PURPOSE:One of the major hurdles facing nanomedicines is the antibody production against nanoparticles that subsequently results in their opsonization and clearance by macrophages. The objective of this research was to examine and identify the sequence of a low-immunogenic peptide based on recombinant elastin-like poly...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1683-5
更新日期:2015-09-01 00:00:00
abstract:PURPOSE:To quantitatively compare in vitro dissolution data in biorelevant and compendial media, to investigate whether in vitro differences are reflected in the simulated plasma profile and to specify under which circumstances prediction of the plasma profile of orally administered lipophilic drugs can be achieved. M...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011071401306
更新日期:2001-03-01 00:00:00
abstract::A series of multilamellar liposome dispersions was prepared from lipids of soy phosphatidylcholine or hydrogenated soy phosphatidylcholine containing from 0 to 30 mol% of either cholesterol, stearylamine, or dipalmitoyl phosphatidylglycerol. The liposome dispersions were aerosolized with a Collison nebulizer for 80 mi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015924124180
更新日期:1990-11-01 00:00:00
abstract:PURPOSE:Nasal delivery is a favorable route for vaccination against most respiratory infections, as antigen deposited in the nasal turbinate and Waldeyer's ring areas induce mucosal and systemic immune responses. However, little is known about the nasal distribution of the vaccines, specifically for infants. METHODS:A...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02976-9
更新日期:2021-01-15 00:00:00
abstract::Although much effort has been devoted to opioid research since the identification of enkephalins, understanding of the physiological importance and mechanisms of action of endogenous opioids lags behind understanding of opiate alkaloids such as morphine. In recent years, several novel approaches have been refined with...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1015809702296
更新日期:1991-01-01 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:PURPOSE:Preparation of Nanographene oxide (NGO) - Gelatin hybrids for efficient treatment of Neuroblastoma. METHODS:Nanohybrids were prepared via non-covalent interactions. Spectroscopic tools have been used to discriminate the chemical states of NGO prior and after gelatin coating, with UV visible spectroscopy reveal...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1604-z
更新日期:2015-06-01 00:00:00
abstract:PURPOSE:To assess the role of intestinal CYP2D6 in oral first-pass drug clearance by comparing the enzyme content and catalytic activity of a prototype CYP2D6 substrate, metoprolol, between microsomes prepared from human intestinal mucosa and from human livers. METHODS:Microsomes were prepared from a panel of 31 human...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018989211864
更新日期:1999-08-01 00:00:00
abstract::Microbial metabolism studies of the antimalarial drug arteether (1) have shown that arteether is metabolized by a number of microorganisms. Large-scale fermentation with Aspergillus niger (ATCC 10549) and Nocardia corallina (ATCC 19070) have resulted in the isolation of four microbial metabolites which have been chara...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015845306124
更新日期:1990-02-01 00:00:00
abstract::Loracarbef is an oral 1-carba-1-dethiacephalosporin antibiotic structurally related to cefaclor. Like many beta-lactam antibiotics, loracarbef exists in several hydrated crystalline forms. The pH-solubility profile curve for loracarbef monohydrate is U-shaped, resembling those of other zwitterionic cephalosporins. Lor...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018949709797
更新日期:1992-02-01 00:00:00
abstract:PURPOSE:Penetration enhancers (PEs) enhancing efficacy depends on two processes: PEs release from patches and action on skin. Compared with their action on skin, PEs release process was poorly understood. Therefore, the purpose of this study was to make a mechanistic understanding of PEs release from acrylic pressure-s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02901-0
更新日期:2020-08-13 00:00:00
abstract:PURPOSE:We compared cationic, polyamine-coated microparticles (MPs) and anionic, protein-coated MPs with respect to their phagocytosis and phagosomal fate in dendritic cells (DCs) and macrophages (Mphi). METHODS:Polystyrene MPs were surface modified by covalent coupling with fluorescein isothiocyanate-labeled polyamin...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1022271020390
更新日期:2003-02-01 00:00:00
abstract:PURPOSE:To investigate influence of inflammation on metabolism and pharmacokinetics (PK) of midazolam (MDZ) and construct a semi-physiologically based pharmacokinetic (PBPK) model to predict PK in mice with inflammatory disease. METHODS:Glucose-6-phosphate isomerase (GPI)-mediated inflammation was used as a preclinica...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2447-9
更新日期:2018-06-21 00:00:00
abstract:PURPOSE:The purpose of this study was (a) to suggest a novel dermatopharmacokinetic (DPK) approach from which pharmacokinetic parameters relevant to the bioequivalence (BE) assessment of a topical formulation can be deduced while circumventing the need for numerous measurements and assumptions, and (b) to investigate w...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2724-2
更新日期:2020-01-02 00:00:00
abstract::To clarify the mechanism by which basic drugs accumulate in the lung, the binding selectivity of drugs to different subcellular structures of the perfused rat lung was examined. Imipramine, quinine, and metoclopramide were used as examples of basic drugs. The accumulation of basic drugs was highest in the mitochondria...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016481911538
更新日期:1987-02-01 00:00:00
abstract::Turbidimetric or light scattering assays can be used to determine the extent of aggregation in protein formulations. Using low molecular weight urokinase (LMW-UK) as a model protein, the effect of polymeric additives on heat-induced aggregation was evaluated. Previous work has shown that under 60 degrees C heat treatm...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018935420680
更新日期:1994-07-01 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::We studied the effects of two verapamil analogs, anipamil and ronipamil, in traumatic shock. Noble-Collip drum trauma produced a shock state characterized by an eight-fold increase in plasma cathepsin D activity, a 13-fold increase in the rate of plasma myocardial depressant factor (MDF) accumulation, and a survival t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016363316777
更新日期:1985-05-01 00:00:00
abstract::A new high-performance liquid chromatographic (HPLC) assay suitable for pharmacokinetic studies of enantiomers of fenoprofen (FEN) was developed. Following the addition of internal standard (IS; racemic ketoprofen), the plasma or urine constituents are extracted into a mixture of isooctane:isopropanol (95:5), back ext...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015867513045
更新日期:1988-01-01 00:00:00
abstract:PURPOSE:Magnetic resonance imaging (MRI) is widely used for diagnostic imaging in preclinical studies and in clinical settings. Considering the intrinsic low sensitivity and poor specificity of standard MRI contrast agents, the enhanced delivery of MRI tracers into tumors is an important challenge to be addressed. This...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1736-9
更新日期:2015-11-01 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:Iontophoresis was employed for enhancing the transdermal delivery of acyclovir through nude mouse skin in vitro, with the aim of understanding the mechanisms responsible for drug transport, in order to properly set the conditions of therapeutical application. METHODS:Experiments were done in horizontal diffusi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016284815501
更新日期:1995-11-01 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::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: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
更新日期:2009-08-01 00:00:00
abstract::An alternative procedure for the simultaneous determination of trimethoprim and sulfamethoxazole in an intravenous pharmaceutical formulation is presented. Infrared spectra of 14 calibration and 6 validation samples were collected using Fourier transform-infrared/attenuated total reflectance (FT-IR/ATR). Partial least...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015957632242
更新日期:1989-07-01 00:00:00
abstract::Molecular modeling has been used to study the complexation between alpha, beta, or gamma-cyclodextrin (CD) and a group of amine compounds having the diphenylmethyl functionality. The computer program SYBYL 5.3 and the Tripos force field (version 5.2) were used for all the calculations. Three-dimensional structures of ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015816215751
更新日期:1991-10-01 00:00:00
abstract:PURPOSE:To investigate plasmid DNA interactions with liposomes prepared from dimyristoylglyceroethylphosphocholine (EDMPC) and DOPE using high sensitivity differential scanning calorimetry (HSDSC). MATERIALS AND METHODS:Large unilamellar liposomes of EDMPC with DOPE (mol ratio 0-50%) were prepared. Plasmid DNA was add...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9325-1
更新日期:2007-10-01 00:00:00