Abstract：
PURPOSE:The objective of the present work was to prepare safe and effective Ciclosporin A Lipid nanocapsule (CsA-LNC) eye-drops for the treatment of DED. METHODS:The phase-inversion method was used to prepared different sizes CsA-LNC. CsA biodistribution in ocular after topical administration in rabbits was analyzed by a validated UPLC-MS/MS method. The efficacy of CsA-LNCs (25 nm, 50 nm, 85 nm) was evaluated using the tear breakup time, fluorescein staining, tear production, inflammatory cytokines and histopathology tests. The safety of CsA-LNCs was study by the score of ocular irritation and histological examination study. RESULTS:CsA-LNCs(20-100 nm) were successfully prepared, An in vivo PK study showed significant improvement of the bioavailability (4.20-fold (25 nm), 2.15-fold (50 nm) and 2.33-fold (85 nm)) in bulbar conjunctiva, and great permeability was observed in the cornea for CsA-LNCs compared with CsA emulsion. An in vivo PD study showed that CsA-LNCs have great efficacy for DED, and the effect was improved over CsA emulsion. CsA-LNCs were safe and not cause significant irritation to the eyes surface of rabbits. CONCLUSION:This work has demonstrated CsA-LNCs, in particular small sizes CsA-LNC, are safe and effective with promising potential to treat DED. Grapical abstract.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Zhang A,Sun R,Ran M,Deng Y,Ge Y,Zhu Y,Tao X,Shang L,Gou J,He H,Yin T,Wang Y,Zhang Y,Tang Xdoi
10.1007/s11095-020-02872-2subject
Has Abstractpub_date
2020-07-14 00:00:00pages
146issue
7eissn
0724-8741issn
1573-904Xpii
10.1007/s11095-020-02872-2journal_volume
37pub_type
杂志文章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:The purpose of this study was to stabilize the vinca alkaloids, vincristine sulfate (VCR) and vinblastine sulfate (VBL), in poly(lactide-co-glycolide) (PLGA) microspheres and to release the drugs in a sustained manner for more than a month. METHODS:An oil-in-oil emulsion-solvent extraction method was used to e...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007522013835
更新日期：2000-06-01 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:Locoregional recurrence is the most common complication after adenocarcinoma resection in the colon, despite adjuvant chemotherapy. Therapy efficacy could be improved if designed to target malignant cells by incorporating specific recognition factors in the drugs or the drug vehicles. The aim of this study was ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9330-4
更新日期：2008-02-01 00:00:00
abstract：PURPOSE:To investigate the mechanisms involved in transport of sulfasalazine in Caco-2 cells. METHODS:Permeability coefficients of sulfasalazine and its analogs across Caco-2 cell monolayers were measured as a function of direction of transport, energy and concentration dependence, and in the presence of inhibitors of...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1026450326712
更新日期：2000-10-01 00:00:00
abstract：PURPOSE:Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that facilitate the lymphatic transport of the TG prodrug (1,3-dipalmitoyl-2-mycophenoloyl glycerol, 2-MPA-TG) were exam...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1579-9
更新日期：2015-05-01 00:00:00
abstract：PURPOSE:Nonlinear conjugation metabolic rate of valproic acid (VPA) has been speculated previously from plasma elimination and liver concentration of VPA in guinea pigs. The purposes of the present study were to assess our speculation by direct measurement of VPA glucuronidation rate in vitro. METHODS:VPA at various c...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016028707130
更新日期：1996-08-01 00:00:00
abstract：PURPOSE:The objective of this study was to develop and characterize long-circulating, biodegradable, and biocompatible nanoparticulate formulation as an intracellular delivery vehicle. METHODS:Poly(ethylene glycol) (PEG)-modified gelatin was synthesized by reacting Type-B gelatin with PEG-epoxide. The nanoparticles, p...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016486910719
更新日期：2002-07-01 00:00:00
abstract：PURPOSE:Levofloxacin, a quinolone antibacterial drug, is a zwitterion at physiological pH. We examined the effect of cationic and anionic drugs on renal excretion of levofloxacin by means of in vivo clearance to characterize the mechanisms of renal excretion of this drug. METHODS:In vivo clearance was studied in male ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012111902798
更新日期：1997-04-01 00:00:00
abstract：PURPOSE:The aim of the study is to investigate the effect of polymer blending on entrapment and release of ganciclovir (GCV) from poly(D,L-lactide-co-glycolide) (PLGA) microspheres using a set of empirical equations. METHODS:Two grades of PLGA, PLGA 7525 [D,L-lactide:glycolide(75:25), MW 90,000-126,000 Da] and Resomer...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-005-9042-6
更新日期：2006-01-01 00:00:00
abstract：PURPOSE:To develop a new bionic system from an existing drug dissolution/absorption simulating system (DDASS) to simultaneously predict the release and absorption of enteric-coated formulations. METHODS:In accordance with the pH-dependent characteristics of enteric-coated formulations, the modified DDASS was designed ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0905-3
更新日期：2013-02-01 00:00:00
abstract：PURPOSE:In the present study we investigated the root-cause of an interference signal (100-200 nm) of sugar-containing solutions in dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA) and its consequences for the analysis of particles in biopharmaceutical drug products. METHODS:Different sugars as ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1634-1
更新日期：2015-07-01 00:00:00
abstract：PURPOSE:Orally absorbable anticancer medications have great advantages for conventional cancer therapies to patients. Here we evaluated the potent anticancer effect of orally absorbable LHD, a chemical conjugate of low-molecular-weight heparin and deoxycholic acid, on tumor graft growth models. METHODS:We characterize...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9989-9
更新日期：2009-12-01 00:00:00
abstract：:Assessment of bioavailability/bioequivalence generally relies on the comparison of rate and extent of drug absorption between products. Rate of absorption is commonly expressed by peak concentration (C(max)) and time to peak concentration (T(max)), although these parameters are indirect measures of absorption rate. Re...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-011-0421-x
更新日期：2011-08-01 00:00:00
abstract：PURPOSE:Previously, a respirable powder (RP) formulation of pirfenidone (PFD) was developed for reducing phototoxic risk; however, PFD-RP demonstrated unacceptable in vitro inhalation performance. The present study aimed to develop a new RP system of PFD with favorable inhalation properties by spray-drying method. MET...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1887-3
更新日期：2016-06-01 00:00:00
abstract：PURPOSE:The aim of this study was to examine if sparging with CO2(g) could be used to establish stable biorelevant bicarbonate buffers, in aqueous medium, for use in dissolution characterization of low-solubility ionizable drugs. METHODS:Preparation of the bicarbonate-containing dissolution medium was monitored by use...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1026147620304
更新日期：2003-10-01 00:00:00
abstract：PURPOSE:To investigate the potential of a novel lipid carrier, comprising beads of alpha-cyclodextrin and soybean oil, for topical drug delivery. Adapalene was chosen as a model drug to explore the ability of the beads to encapsulate and release a highly lipophilic compound. MATERIALS AND METHODS:Adapalene-loaded bead...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9395-0
更新日期：2008-02-01 00:00:00
abstract：PURPOSE:To compare the adjuvanticity of polymeric particles (new-generation adjuvant) and alum (the traditional and FDA-approved adjuvant) for H5N1 influenza split vaccine, and to investigate respective action mode. METHODS:Vaccine formulations were prepared by incubating lyophilized poly(lactic acid) (PLA) microparti...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1224-z
更新日期：2014-04-01 00:00:00
abstract：PURPOSE:The purpose of the study was to examine the suitability of using laser diffraction to measure the fine particle fraction (FPF) of drugs emitted from carrier-free dry powder aerosol formulations. MATERIALS AND METHODS:Particle size distribution of terbutaline sulphate from Bricanyl Turbohaler, which contained l...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9056-8
更新日期：2006-09-01 00:00:00
abstract：PURPOSE:The fate of inhaled salmon calcitonin (sCT) at the respiratory epithelial barrier was studied with particular emphasis on enzymatic degradation by trypsin, chymotrypsin, and neutrophil elastase. METHODS:Degradation of sCT was assessed by HPLC in cell homogenate, supernatant and intact monolayers of human respi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0553-z
更新日期：2012-01-01 00:00:00
abstract：PURPOSE:To investigate the effects of small aliphatic pendent groups conjugated through an acid-sensitive linker to the core of brushed block copolymer micelles on particle properties. METHODS:The brushed block copolymers were synthesized by conjugating five types of 2-alkanone (2-butanone, 2-hexanone, 2-octanone, 2-d...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1060-1
更新日期：2013-08-01 00:00:00
abstract：PURPOSE:To investigate the moisture-induced aggregation (i.e., a loss of solubility in water) of DNA in a solid state and to develop rational strategies for its prevention. METHODS:Lyophilized calf thymus DNA was exposed to relative humidity (RH) levels from 11% to 96% at 55 degrees C. Following a 24-h incubation unde...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9138-7
更新日期：2007-01-01 00:00:00
abstract：PURPOSE:The growing amount of heterogeneous bioactivity data requires effective strategies to assess the promiscuity/selectivity of small-molecules and aid drug discovery. In the current study, we aim to evaluate the potential of assay profiles (APs, i.e., unique combinations of assay-related features describing how ac...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2523-1
更新日期：2018-10-18 00:00:00
abstract：PURPOSE:This work describes a method for functionalisation of nanoparticle surfaces with hydrophilic "nano-shields" and the application of advanced surface characterisation to determine PEG amount and accumulation at the outmost 10 nm surface that is the predominant factor in determining protein and cellular interactio...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1018-3
更新日期：2013-07-01 00:00:00
abstract：PURPOSE:Indocyanine green (ICG), an FDA-approved near infrared (NIR) dye, has potential application as a contrast agent for tumor detection. Because ICG binds strongly to plasma proteins and exhibits aqueous, photo, and thermal instability, its current applications are largely limited to monitoring blood flow. To addre...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0190-y
更新日期：2010-09-01 00:00:00
abstract：PURPOSE:To characterize the distribution of water among various components in a powder blend using solid-state NMR spectroscopy. METHODS:Water sorption behavior of theophylline anhydrate and excipients was determined by dynamic vapor sorption (DVS) and Karl Fischer Titration (KFT) after storing them in humidity chambe...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1972-7
更新日期：2016-10-01 00:00:00
abstract：PURPOSE:We reported that suramin produced chemosensitization at nontoxic doses. This benefit was lost at the approximately 10-fold higher, maximally tolerated doses (MTD). The aim of the current study was to identify in patients the chemosensitizing suramin dose that delivers 10-50 microM plasma concentrations over 48 ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-0165-1
更新日期：2006-06-01 00:00:00
abstract：PURPOSE:To characterize temporal exposure and elimination of 5 gold/dendrimer composite nanodevices (CNDs) (5 nm positive, negative, and neutral, 11 nm negative, 22 nm positive) in mice using a physiologically based mathematical model. METHODS:400 ug of CNDs is injected intravenously to mice bearing melanoma cell line...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0784-7
更新日期：2012-09-01 00:00:00
abstract：PURPOSE:To study the influence of solid form on the behavior of the salt siramesine hydrochloride in aqueous environments. METHODS:The solubilities and dissolution rates of siramesine hydrochloride anhydrate and monohydrate were determined at pH 3.4 and 6.4, and precipitates were examined by X-ray powder diffraction. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9783-0
更新日期：2009-04-01 00:00:00
abstract：PURPOSE:The purpose of the present study was to investigate changes of blood-brain barrier (BBB) and brain parenchymal protein expression due to type II diabetes mellitus (T2DM) induced by a high-fat diet (HFD) by using SWATH-based quantitative proteomics. METHODS:Mice were fed a HFD for 2 or 10 weeks, and then SWATH-...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2674-8
更新日期：2019-07-31 00:00:00
