Abstract:
PURPOSE:Exenatide, a potent insulinotropic agent, can be used for the treatment of non-insulin-dependent diabetes mellitus. However, the need for frequent injections seriously limits its therapeutic utility. The aim of present report was to develop an orally available exenatide formulation using goblet cell-targeting nanoparticles (NPs). METHOD:The exenatide-loaded nanoparticles were prepared with modified chitosan which was conjugated with a goblet cell-target peptide, CSKSSDYQC (CSK) peptide. RESULTS:The CSK-chitosan nanoparticles shown reduced chitosan toxicity and enhanced the permeation of drugs across the Caco-2/HT-29 co-cultured cell monolayer, which simulated the intestinal epithelium. Following the oral administration of near-infrared fluorescent probe Cy-7-loaded NPs to mice, the distribution of the drugs was investigated with a near-infrared in vivo image system (FX Pro, Bruker, USA). The results showed that Cy-7 fluorescence disseminated from the oesophagus, then to stomach and small intestine and then was absorbed into hepatic, finally into the bladder; over time, Cy-7 was metabolized and excreted. The bioavailability of the modified nanoparticles was found to be 1.7-fold higher compared with the unmodified ones, and the hypoglycemic effect was also better. CONCLUSION:CSK peptide-modified chitosan nanoparticles could be a potential therapeutics for Type II diabetes patients.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Li X,Wang C,Liang R,Sun F,Shi Y,Wang A,Liu W,Sun K,Li Ydoi
10.1007/s11095-014-1513-1subject
Has Abstractpub_date
2015-03-01 00:00:00pages
1017-27issue
3eissn
0724-8741issn
1573-904Xjournal_volume
32pub_type
杂志文章abstract:PURPOSE:The objective of this study was to determine the pharmacokinetics and safety for NX1838 following injection into the vitreous humor of rhesus monkeys. METHODS:Plasma and vitreous humor pharmacokinetics were determined following a single bilateral 0.25, 0.50, 1.0, 1.5, or 2.0 mg/eye dose. In addition, the pharm...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007657109012
更新日期:2000-12-01 00:00:00
abstract:PURPOSE:To develop a new technique, spray freeze drying, for preparing protein aerosol powders. Also, to compare the spray freeze-dried powders with spray-dried powders in terms of physical properties and aerosol performance. METHODS:Protein powders were characterized using particle size analysis, thermogravimetric an...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018828425184
更新日期:1999-02-01 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::Diltiazem (DTZ) is a calcium channel blocker widely used in the treatment of angina and hypertension. DTZ undergoes extensive metabolism yielding several metabolites, some of which are active like N-desmethyldiltiazem (MA), desacetyldiltiazem (M1) and N-desmethyl,desacetyldiltiazem (M2). Due to the nature of its biotr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016226601988
更新日期:1995-04-01 00:00:00
abstract:PURPOSE:Using monolayers of human pancreatic adenocarcinoma cells (Panc-1) that express multidrug resistance-associated protein (MRP), the present work investigates the effects of Pluronic block copolymers on the functional activity of MRP. METHODS:The studies examined the accumulation and efflux of the MRP selective ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018873702411
更新日期:1999-03-01 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:To prepare a thermoreversible gel system able to work as a medium for crystallization at around 20°C, allowing easy retrieval of crystals by simply decreasing the gel temperature. Lactose was selected has model substance for crystallization. METHODS:Water solutions with different% of poloxamer 407, α-Lactose m...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0606-3
更新日期:2012-03-01 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:The aim of this work was to develop a quantitative, flow cytometric method for tracking the endolysosomal escape of a fluorescently labelled saporin toxin. METHODS:Flow cytometric measurements of fluorescent pulse width and height were used to track the endocytic uptake into Daudi cells of a fluorescently labe...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2725-1
更新日期:2019-12-23 00:00:00
abstract::The new generation of nanotechnology-based drug formulations is challenging the accepted ways of cancer treatment. Multi-functional nanomaterial constructs have the capability to be delivered directly to the tumor site and eradicate cancer cells selectively, while sparing healthy cells. Tailoring of the nano-construct...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0214-7
更新日期:2011-02-01 00:00:00
abstract:PURPOSE:To identify materials and processes which effect supersaturation of the GI milieu for low solubility drugs in order to increase oral bioavailability. METHODS:A variety of small and polymeric molecules were screened for their ability to inhibit drug precipitation in supersaturated solutions. The best polymeric ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9852-z
更新日期:2009-06-01 00:00:00
abstract:PURPOSE:The long-term stability and nasal absorption characteristics of a basic nasal formulation of azetirelin, a thyrotropin-releasing hormone analog and its absorption enhancement by incorporation of acylcarnitines in the formulation were investigated. METHODS:The long-term stability of basic nasal azetirelin formu...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011952804479
更新日期:1998-01-01 00:00:00
abstract:PURPOSE:The aim of this study was to identify the dominant factors affecting the stability of nanoemulsions, using artificial neural networks (ANNs). METHODS:A nanoemulsion preparation of budesonide containing polysorbate 80, ethanol, medium chain triglycerides and saline solution was designed, and the particle size o...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-0004-2
更新日期:2010-01-01 00:00:00
abstract::Animal models are used commonly in various stages of drug discovery and development to aid in the prospective assessment of drug-drug interaction (DDI) potential and the understanding of the underlying mechanism for DDI of a drug candidate. In vivo assessments in an appropriate animal model can be very valuable, when ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-010-0157-z
更新日期:2010-09-01 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
abstract:PURPOSE:Orthorhombic crystals of paracetamol exhibit good technological properties during compression. The purpose of this study was to investigate the compression behavior of this substance and to compare it to that of monoclinic paracetamol. From the crystal structure, it could be hypothesized that sliding planes are...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011954800246
更新日期:1998-07-01 00:00:00
abstract::The effect of γ-cyclodextrin and its four derivatives on the solubility of progesterone in phosphate buffer pH 7.4 was investigated. γ-Cyclodextrin forms a complex precipitating from solution at low cyclodextrin concentrations. No precipitation of complexes was observed with the γ-cyclodextrin derivatives. This change...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016301919928
更新日期:1985-11-01 00:00:00
abstract::The partitioning of a series of nine nitroimidazole drugs in liposomes (log Km) of various compositions has been determined and compared to their partitioning in the n-octanol/saline system (log K) at 30 degrees C. The log Km ranged from 1.5 to 0.5 and was three- to fourfold greater than the log K; further, the linear...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015931431817
更新日期:1989-05-01 00:00:00
abstract:PURPOSE:Pluronics are known as inhibitors of multidrug resistance thus making tumor cells sensitive to therapeutic doses of drugs. The purpose of our study consists in revealing molecular targets of the hydrophobic poly(propylene oxide) block of pluronics in living cells and the dependence of the polymers chemosensitiz...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2484-4
更新日期:2018-09-06 00:00:00
abstract:PURPOSE:To demonstrate that polyanhydride copolymer chemistry affects the uptake and intracellular compartmentalization of nanospheres by THP-1 human monocytic cells. METHODS:Polyanhydride nanospheres were prepared by an anti-solvent nanoprecipitation technique. Morphology and particle diameter were confirmed via scan...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9760-7
更新日期:2009-03-01 00:00:00
abstract:PURPOSE:It was the purpose of this study to develop a new oral drug delivery system for low molecular weight heparin (LMWH) providing an improved bioavailability and a prolonged therapeutic effect. METHODS:The permeation enhancing polycarbophil-cysteine conjugate (PCP-Cys) used in this study displayed 111.4 +/- 6.4 mi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023803706746
更新日期:2003-06-01 00:00:00
abstract::5'-Ester derivatives of 5-iodo-2'-deoxyuridine (IDU) with varying degrees of lipophilicity were examined to evaluate the effectiveness of lipophilic ester prodrugs for enhanced and sustained delivery of IDU to the brain parenchyma. Approximately 1.0% (1.0 +/- 0.19; n = 4) of the total radioactivity was found in the br...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015803922401
更新日期:1992-09-01 00:00:00
abstract:PURPOSE:Propofol is a widely used anesthetic agent with highly desirable fast "on" and "off" effects. It is currently formulated as lipid emulsions, which are known to support microbial growth. In this study, a novel, lipid-free nanodispersion formulation of propofol was characterized. METHODS:The formulation was eval...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-1872-0
更新日期:2005-03-01 00:00:00
abstract:PURPOSE:To characterize the uptake mechanism of zidovudine (AZT), a nucleoside reverse transcriptase inhibitor, in syncytiotrophoblast cells using the TR-TBT 18d-1 cell line previously established by our group. MATERIALS AND METHODS:The effects of several transporter inhibitors on the initial and steady-state apical u...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9564-9
更新日期:2008-07-01 00:00:00
abstract::The area function method for assessing zero-order (ko) drug absorption rates was compared to four other methods under conditions where variation occurs in the plasma concentration data and in the elimination rate constant (kel or k10) for one- or two-compartment models. For deviant kel values of a one-compartment mode...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015843811150
更新日期:1990-01-01 00:00:00
abstract:PURPOSE:S-(4-Nitrobenzyl)-6-thioinosine (NBMPR) is routinely used at concentrations of 0.10 μM and 0.10 mM to specifically inhibit transport of nucleosides mediated by equilibrative nucleoside transporters 1 (ENT1) and 2 (ENT2), respectively. We recently showed that NBMPR (0.10 mM) might also inhibit placental active e...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-2782-5
更新日期:2020-02-21 00:00:00
abstract:PURPOSE:1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which l...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016243706415
更新日期:1995-10-01 00:00:00
abstract:PURPOSE:Vancomycin (VCM) concentration is often out of therapeutic range (10-20 μg/ml) in patients receiving continuous renal replacement therapy (CRRT). The purposes of this study were to develop a practical VCM population pharmacokinetic (PPK) model and to evaluate the potential of Bayesian prediction-based therapeut...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02820-0
更新日期:2020-05-28 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:Paclitaxel is a first-line drug for the therapy of lung cancer, however, drug resistance is a serious limiting factor, related to overexpression of anti-apoptotic proteins like survivin. To overcome this phenomenon, developing novel ultrasound responsive nanobubbles - nanosized drug delivery system- for the del...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02885-x
更新日期:2020-08-05 00:00:00