Abstract：
:To evaluate relationships between the extent of protein-excipient interactions, structural relaxation of an amorphous matrix, and the physico-chemical stability of a protein, human growth hormone (hGH) was lyophilized with sucrose and trehalose in a 1:2 weight ratio. The protein-excipient interactions were analyzed immediately after lyophilization with isoperibol solution calorimetry (ISC), water sorption analysis (WSA), differential scanning calorimetry (DSC) and Fourier Transform Infrared Spectroscopy (FTIR). The physical and chemical stability of hGH during storage at 50 degrees C was monitored by reverse phase (RP)-HPLC, SEC-HPLC and UV absorption spectroscopy. The hGH formulation containing sucrose demonstrated greater protein-excipient interactions and faster initial relaxation times compared to the trehalose formulation. Although both formulations had similar chemical stability (rate of deamidation), physical stabilities (e.g. degree of aggregation) were different. The hGH/sucrose formulation manifested a higher rate and lower extent of insoluble aggregate formation. The decreased amount of aggregation in the sucrose formulation could be correlated with a greater extent of protein-excipient interactions and the presence of a more homogeneous mixture. In contrast, the higher rate of aggregation in the sucrose formulation could be directly correlated with the higher molecular mobility of the matrix.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Salnikova MS,Middaugh CR,Rytting JHdoi
10.1016/j.ijpharm.2008.02.022subject
Has Abstractpub_date
2008-06-24 00:00:00pages
108-13issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(08)00150-6journal_volume
358pub_type
杂志文章abstract：:N-(2-Hydroxypropyl) methacrylamide (HPMA) copolymer has been extensively studied as drug carrier for tumor therapy. Due to the Enhanced Permeability and Retention (EPR) effect, HPMA copolymer drug conjugates are able to be passively accumulated in the tumor site. Currently, efficient uptake of this polymeric system by...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.12.018
更新日期：2018-01-30 00:00:00
abstract：:In a previous study, it was shown that the incorporation of poorly soluble drugs (BCS class II) in sugar glasses could largely increase the drug's dissolution rate [van Drooge, D.J., Hinrichs, W.L.J., Frijlink, H.W., 2004 b. Anomalous dissolution behaviour of tablets prepared from sugar glass-based solid dispersions. ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.07.023
更新日期：2008-02-12 00:00:00
abstract：:The stratum corneum possesses a very heterogenous structure. As such a diffusing molecule can access a number of different pathways. It is probable that the excellent barrier properties of the stratum corneum result from a tortuous diffusional pathway around the dead cells. However, there are considerable problems in ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00161-1
更新日期：1999-10-15 00:00:00
abstract：:The role of water activity (a(w)), relative humidity (RH) and temperature on the hydration state of theophylline has been investigated. Slurry bridging experiments at controlled water activities, using powder X-ray diffraction (PXRD) and thermogravimetric analysis (TGA) to characterise the solid phase, established tha...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00277-6
更新日期：2002-10-24 00:00:00
abstract：:The aim of this study was to investigate possible interactions between a polymeric emulsifier and a non-ionic surfactant, with a view of achieving better understanding of emulsion stabilisation mechanisms. The polymeric emulsifier used was acrylates/C10-30 alkyl acrylate crosspolymer (Pemulen TR-2(R)), while Polyoxyet...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00097-6
更新日期：1999-07-20 00:00:00
abstract：:The objective of this study was to prepare Herceptin (HCT)-functionalized paclitaxel nanocrystals and evaluated their cell-specific interactions, cellular accumulation, and growth inhibition in HER2-positve breast cancer cells as a tumor-targeted delivery module. Paclitaxel (PTX) was fabricated in the form of nanocrys...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.09.067
更新日期：2016-11-20 00:00:00
abstract：:The role of the newly discovered cysteine protease, cathepsin K, in osteoporosis and rheumatoid arthritis is reviewed. The current development of cathepsin K inhibitors and their targeted delivery using synthetic polymer carriers are discussed. Future challenges and possible strategies to improve these delivery system...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2003.03.003
更新日期：2004-06-11 00:00:00
abstract：:A bioadhesive drug delivery system, wheat germ agglutinin (WGA)-grafted lipid nanoparticles, was developed for the oral delivery of bufalin (a hydrophobic active component extracted from the traditional Chinese medicine Chan'su). The lipid nanoparticles associated with poly(vinyl alcohol) (PVA) were prepared by high-p...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.06.030
更新日期：2010-09-15 00:00:00
abstract：:Previously, chemical enhancer-induced permeation enhancement on human stratum corneum (SC) lipoidal pathway at enhancer thermodynamic activities approaching unity in the absence of cosolvents (defined as Emax) was determined and hypothesized to be related to the enhancer solubilities in the SC lipid domain. The object...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.09.014
更新日期：2010-01-04 00:00:00
abstract：:The objective of this study was to develop mucoadhesive polymeric excipients for vaginal drug delivery systems. Hyaluronic acid was thiolated and subsequently preactivated with 6-mercaptonicotinamide (HA-CYS-MNA) to enhance stability and mucoadhesive properties on vaginal mucosa. After determination of the thiol group...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.11.048
更新日期：2015-01-15 00:00:00
abstract：:Lipid-based formulations can be effective drug delivery systems for poorly water-soluble chemical entities, provided they are designed with careful selection of the excipients, based on their role in the delivery system and in relation to drug properties. The primary factor leading to increased bioavailability is the ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.09.009
更新日期：2015-11-10 00:00:00
abstract：:Extruded 3D printing is emerging as an attractive fabrication technology in the field of personalized oral medicines. The objective of this study was to develop a tunable extruded 3D printing platform based on thermo-sensitive gelatin pastes to meet the needs of achieving different drug release characteristics with fl...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119360
更新日期：2020-06-15 00:00:00
abstract：:Alzheimer's disease (AD) is a common and severe brain disease with a high mortality among the elders, but no highly efficient medications are currently available. For example, timosaponin BII, an efficient anti-AD agent, has low oral bioavailability. Here, timosaponin BII was formulated in a temperature/ion-sensitive ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119115
更新日期：2020-03-30 00:00:00
abstract：:The potential of two derivatives of vitamin E, i.e. α-tocopheryl phosphate (TP) and di-α-tocopheryl phosphate (T2P), for the protection and delivery of therapeutics is being investigated in our laboratory and some promising results have been obtained so far. Novel nanocarrier systems containing TP, T2P and different l...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.06.037
更新日期：2017-08-07 00:00:00
abstract：:To ensure success in the development and manufacturing of nanomedicines requires forces of an interdisciplinary team that combines medicine, engineering, chemistry, biology, material and pharmaceutical areas. Numerous researches in nanotechnology applied to human health are available in the literature. Althought, the ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2020.119214
更新日期：2020-04-30 00:00:00
abstract：:This work aims to prepare sustained release buccal mucoadhesive tablets of buspirone hydrochloride (BH) to improve its systemic bioavailability. The tablets were prepared according to 5×3 factorial design where polymer type was set at five levels (carbopol, hydroxypropyl methylcellulose, sodium alginate, sodium carbox...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.ijpharm.2014.01.003
更新日期：2014-03-10 00:00:00
abstract：:Various processing variables that can influence granulation characteristics of a lactose-based formulation were evaluated using a Plackett-Burman experimental design. These parameters were impeller speed, granulating solution addition rate, total amount of water added in the granulation step, wet massing time, moistur...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00445-7
更新日期：2000-03-30 00:00:00
abstract：:During the pharmaceutical development of pregabalin extended-release tablets, an unknown degradant at a relative retention time (RRT) of 11.7 was observed and its nominal amount exceeded the ICH identification threshold in an accelerated stability study. The aim of this study is to identify the structure and investiga...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118910
更新日期：2020-02-15 00:00:00
abstract：:Nanoparticles (NPs) have shown a certain potential to overcome the drawbacks of oral peptide delivery in the gastrointestinal tract such as low peptide stability and permeability. The preparation of insulin loaded NPs was carried out with Eudragit RL or RS dissolved in different non-toxic polyethylene glycol (PEG) der...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.01.017
更新日期：2013-02-25 00:00:00
abstract：:Remote controlled capsule (RCC) has been extensively used in the field of site-specific drug delivery. It is a potent tool to study the regional drug absorption of the gastrointestinal (GI) tract that provides pharmaceutical scientists with significant pharmacokinetics data for oral drug formulation development. In pr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.08.026
更新日期：2009-12-01 00:00:00
abstract：:D-borneolum is commonly used as a permeation enhancer in Traditional Chinese Medicine (TCM) formulas for transdermal application. Additionally, two other sources of borneolums were recorded in the 2015 edition of the Chinese Pharmacopoeia (ChP), including L-borneolum and borneolum syntheticum. To guide the selection a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119225
更新日期：2020-04-30 00:00:00
abstract：:The mechanical properties of casted Eudragit E-100 films were tested for the combined effect of two cohesion promoters (succinic or citric acid) and triacetin as a plasticizer. The prepared films were elastic, self-adhesive, transparent and pale yellow in colour. Films containing either of the tested cohesion promoter...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.03.026
更新日期：2009-07-06 00:00:00
abstract：:In this study, solid lipid nanoparticles (SLN) loaded with MBO-asGCS oligonucleotide were prepared, characterized and evaluated for cytotoxicity against NCI/ADR-RES human ovary cancer cells. Two types of cetyltrimethyl ammonium bromide (CTAB) stabilized SLN, with or without ceramide VI, were prepared by mixed homogeni...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.08.044
更新日期：2010-11-15 00:00:00
abstract：:The effects of vehicles and penetration enhancers on the in vitro permeation of tenoxicam from saturated solutions through dorsal hairless mouse skin were investigated. Various types of vehicles, including ester-, alcohol-, and ether-types and their mixtures, were used as vehicles, and then a series of fatty acids and...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00009-1
更新日期：2002-04-02 00:00:00
abstract：PURPOSE:This study aimed to investigate the penetration of topical and oral ofloxacin into aqueous humor and vitreous humor in post-traumatic endophthalmitis model in rabbits. METHODS:A standardized intraocular infection after penetrating injury was made in the right eyes of 16 rabbits. Intraocular infection was induc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00482-8
更新日期：2000-08-25 00:00:00
abstract：:The breast cancer resistance protein (BCRP) is an efflux transporter expressed at the apical surface of human brain endothelial cells of the blood-brain barrier (BBB). It was proposed as one of the transporters responsible for the development of drug resistance to several central nervous system (CNS) drugs, including ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.120161
更新日期：2021-01-25 00:00:00
abstract：:The study was aimed at evaluating whether the ocular hypotensive effect of melatonin (MEL) was enhanced by its encapsulation in cationic solid lipid nanoparticles (cSLN), as well as at determining the tolerability of these formulations on the ocular surface. MEL was loaded in cSLN that had already been shown to be sui...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.11.032
更新日期：2015-01-15 00:00:00
abstract：:The improvements in healthcare systems and the advent of the precision medicine initiative have created the need to develop more innovative manufacturing methods for the delivery and production of individualized dosing and personalized treatments. In accordance with the changes observed in healthcare systems towards m...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.04.003
更新日期：2017-05-30 00:00:00
abstract：:From the viewpoint of effective utilization of natural resources and development of new pharmaceutical materials, acid-treated yeast cell wall (AYC) was prepared via a novel approach involving acidification of brewers' yeast cell wall. AYC aqueous dispersion containing 5% (w/v) AYC and 0.5% (w/v) glycerol was prepared...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00008-x
更新日期：2002-04-26 00:00:00
abstract：:In this report, we describe the design of an aerosol exposure chamber to reproducibly produce uniformly distributed clouds of droplet nuclei. The device can deliver desired number of bacilli (20-2000) in lungs of mice. All safety measures to handle infectious bacteria have been incorporated in the design and it is con...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(03)00023-1
更新日期：2003-04-14 00:00:00
