Abstract:
:Freeze-drying is the preferred method to manufacture proteins in their solid state thus the understanding of the relationship between cycle parameters and cake properties remains of great interest. The present study aims to investigate the influence of the freezing conditions in the material properties at different layers throughout the dried structure, in the presence and absence of a protein. Placebo and protein formulations were dried applying different cooling rates: slow, fast and fast cooling with annealing. Non-uniform visual cake appearance, different pore sizes and endothermic events for release of structural water were observed throughout the cake at different freezing rates indicating heterogeneous properties of the dried material likely due to heating gradients during freezing. However, annealing increased the crystallinity and eliminated material inhomogeneities across the cake. The crystalline phase was mainly comprised of δ and hemihydrate mannitol (MHH) distributed at different ratios and influenced by the presence of the protein. The undesired formation of MHH is associated to currently used freezing temperatures or amorphous to crystalline material ratios. Thus, the correlation between the freezing step parameters and resulting material structure is a step forward to provide a better understanding of the freeze-dried cake formation and product quality improvement.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Badal Tejedor M,Fransson J,Millqvist-Fureby Adoi
10.1016/j.ijpharm.2020.119891subject
Has Abstractpub_date
2020-11-30 00:00:00pages
119891eissn
0378-5173issn
1873-3476pii
S0378-5173(20)30876-0journal_volume
590pub_type
杂志文章abstract::Hybrid liposomes can be prepared by simply ultrasonicating a mixture of vesicular and micellar molecules in aqueous solution. A clear solution of hybrid liposomes composed of 90 mol% dimyristoylphosphatidylcholine (DMPC) and 10 mol% polyoxyethylene(23)dodecyl ether (C12(EO)23) having a hydrodynamic diameter of 100-120...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.11.034
更新日期:2005-03-23 00:00:00
abstract::The aim of this study was to evaluate the transdermal permeation enhancement of N-trimethyl chitosan (TMC) with different degrees of quaternization (DQ). TMCs with DQ of 40 and 60% (TMC40 and TMC60) were synthesized and characterized by (1)H NMR. Testosterone (TS) used as an effective drug, four different gels were pr...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.12.050
更新日期:2008-05-22 00:00:00
abstract::Aggregation may compromise the stability as well as the biological activity of protein drugs. Detection of protein aggregates is needed in the process of protein characterization and during optimization of pharmaceutical formulations. This paper describes a technique, which consists of analysing protein aggregates by ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.08.024
更新日期:2007-02-01 00:00:00
abstract::A new class of surfactants with glycerate headgroups, that form viscous lyotropic liquid crystalline phases in excess water, have been investigated for their potential to provide sustained release matrices for depot drug delivery. Oleyl glycerate and phytanyl glycerate were used as representative surfactants of this n...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.11.033
更新日期:2006-02-17 00:00:00
abstract::A series of branched cationic beta-cyclodextrin polymers (CPbetaCDs) with designed chemical structures were synthesized from beta-cyclodextrin (beta-CD), epichlorohydrin (EP) and choline chloride (CC). Indomethacin (IDM), an anionic drug, was chosen as a model drug to evaluate the drug loading capacities of CPbetaCDs....
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.11.024
更新日期:2010-02-15 00:00:00
abstract::Anticancer drug doxorubicin (DOX) was physically loaded into the micelles prepared from poly(2-ethyl-2-oxazoline)-b-poly(L-lactide) diblock copolymers (PEOz-PLLA). PEOz-PLLA consists of hydrophilic segment PEOz and hydrophobic segment PLLA showed pH-sensitivity in the aqueous solution. The DOX-loaded micelle exhibited...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.03.002
更新日期:2006-07-06 00:00:00
abstract::The main complication of aortocoronary reconstruction with vein grafts is restenosis in the course of time. The aim was to assess the effect of a periadventitial polyester mesh releasing sirolimus on intimal hyperplasia of autologous grafts. We implanted v. jugularis ext. into a. carotis communis in rabbits. The vein ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.02.023
更新日期:2012-05-10 00:00:00
abstract::The optimized formulation of N-4472, N-[2-(3,5-di-tert-butyl-4-hydroxyphenethyl)-4,6-difluorophenyl]-N'-[4-(N-benzylpiperidyl)] urea, which was a poorly water-soluble drug, was developed by utilizing the complexation between N-4472 and L-ascorbic acid (VC). It was found that the formulation with Gelucire((R)) 44/14, H...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(02)00346-0
更新日期:2002-10-10 00:00:00
abstract::Electro-gene-therapy is a promising technique for cancer treatment. However, knowledge about mechanism of gene transfer with electric field in tumor is limited. Whereas in vitro electrotransfection is efficient, gene expression in tumoral cells in vivo is weak. To determine reasons for this difference and unravel gene...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.04.054
更新日期:2012-02-14 00:00:00
abstract::The purpose of this work is to study the effect of pH, buffer species, and temperature on the physicochemical stability of a humanized monoclonal antibody LA298. The study was carried out in solution state of the antibody in the presence of different buffer species at different pH values and storage temperature. No si...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.10.024
更新日期:2006-02-03 00:00:00
abstract::Modification of recombinant proteins with polyethylene-glycol (PEG) can improve their pharmacokinetic properties, although their bioactivity may be reduced after PEGylation due to structural changes. In this study, simultaneous optimization of PEGylation efficiency and preserved bioactivity of recombinant human growth...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.12.034
更新日期:2019-02-25 00:00:00
abstract::Targeting of drug delivery systems (DDSs) to specific intracellular organelles (i.e., subcellular targeting) has been investigated in numerous publications, but targeting efficiency of these systems is seldom reported. We searched scientific publications in the subcellular DDS targeting field and analyzed targeting ef...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2015.10.053
更新日期:2015-12-30 00:00:00
abstract::pH-responsive polymer shell chitosan/poly (methacrylic acid) (CS-PMAA) was coated on mesoporous silica nanoparticles (MSN) through the facile in situ polymerization method. The resultant composite microspheres showed a flexible control over shell thickness, surface charges and hydrodynamic size by adjusting the feedin...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.10.013
更新日期:2011-12-15 00:00:00
abstract::Lipid-Polycation-DNA complexes (LPD) is a promising non-viral system for nucleic acids delivery. Usually, LPD are prepared just before their use. In the present work, we have examined whether dehydration of a new type of LPD (named LPD100) might be a storage option. LPD100 comprises PEGylated histidylated polylysine/p...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.04.009
更新日期:2012-02-14 00:00:00
abstract::We report the preparation and evaluation of flurbiprofen loaded-poly-epsilon-caprolactone nanospheres obtained by solvent displacement method. Characterization by thermal methods, infrared spectroscopy and X-ray diffraction analysis can reveal the dispersion state of the drug inside the nanospheres. Such information p...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(98)00381-0
更新日期:1999-03-01 00:00:00
abstract::As with many other anti-cancer agents, docetaxel is a substrate for ATP-binding cassette transporters such as P-glycoprotein and its metabolism is mainly catalysed by CYP3A. In order to improve the oral bioavailability of docetaxel, a component of turmeric, curcumin, which can down-regulate the intestinal P-glycoprote...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.08.015
更新日期:2010-10-31 00:00:00
abstract::The application of cell-penetrating peptides (CPPs) for delivering various cargo molecules with biological functions into cells has gained much attention in recent years. However, the internalization mechanisms and delivery properties of CPP-cargo remains controversial. In this study, low- and high-molecular-weight ca...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.08.001
更新日期:2011-10-31 00:00:00
abstract::A certain number of filters have notable anti-inflammatory properties with percentage inhibition of PMA-induced edema in mice at over 70%. The question arose as to whether this effect was likely to continue after UV irradiation. It can be noted that 7 filters retain an equivalent anti-inflammatory effect before and af...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.04.067
更新日期:2013-08-16 00:00:00
abstract::The saturation solubilities of nicotine and scopolamine bases as well as acidic paracetamol were measured in two different model stratum corneum lipid matrices. Light microscopy visualized the presence of drug above its solubility either as droplets or crystalline particles. Neither wide-angle X-ray diffraction nor DS...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.06.057
更新日期:2014-10-01 00:00:00
abstract::Electrospun composite zein/eudragit nanofibers were developed with an aim to deliver two different classes of drugs simultaneously that would restrict/compensate the adverse effects of non-steroidal anti-inflammatory drugs (NSAIDs). Co-administration of proton pump inhibitors is beneficial for patients consuming NSAID...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.07.075
更新日期:2012-11-15 00:00:00
abstract::In the present work, we attempted to design a transdermal system for delivering selegiline using a hydrogel-based drug reservoir and a rate-controlling membrane (Solupor polyethylene membranes). The appearances of these preparations were evaluated by scanning electron microscopy (SEM), and the in vitro skin permeation...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.06.025
更新日期:2009-10-01 00:00:00
abstract::Cutaneous delivery of combinations of antioxidants offers the possibility of enhanced protection against UV-radiation. In this study, we investigated the potential of sugar-based microemulsions containing monoglycerides to promote simultaneous cutaneous delivery of lycopene and ascorbic acid, and increase tissue antio...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.06.016
更新日期:2012-09-15 00:00:00
abstract::The characterization of a pharmaceutical microemulsion system with glycerol monolaurate as oil, ethanol as cosurfactant, Tween 40 as surfactant, sodium diacetate and water, and the antimicrobial activities against Escherichia coli, Staphylococcus aureus, Bacillus subtilis, Candida albicans, Aspergillus niger and Penic...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.05.022
更新日期:2010-08-16 00:00:00
abstract:BACKGROUND:Perfluorocarbon-nanoemulsions (PFC-NE) made of PFC and phospholipids (PL) by homogenization are optimal for in vivo-19F labelling of monocytes and subsequently of inflamed tissues in magnetic resonance imaging (MRI). Necessary requirements for in vivo use of PFC-NE are sterility, suitable droplet sizes and t...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.118753
更新日期:2019-12-15 00:00:00
abstract::The melting point of lidocaine was significantly lowered when mixed with thymol and/or aqueous ethanol. Mixtures of lidocaine and thymol at ratios within the range of 30:70-70:30 (w:w) became homogeneous oils at 25 degrees C. In a pH 9.2 carbonate buffer containing 25% ethanol, lidocaine (5%, w:w) also liquefied at 25...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(01)00689-5
更新日期:2001-07-03 00:00:00
abstract::The purpose of the present work is to develop nanoparticles of a new antitubulin agent of the family of tripentones by means of a phase inversion process. Dynamic light scattering, transmission electron microscopy and zeta-potential measurements were used to characterize tripentone loaded nanoparticles. From interfaci...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.04.007
更新日期:2006-08-31 00:00:00
abstract::Aptamers, nucleic acid ligands that are specific against their corresponding targets are increasingly employed in a variety of applications including diagnostics and therapeutics. The specificity of the aptamers against their targets is also used as the basis for the formulation of the aptamer-based drug delivery syst...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2019.118483
更新日期:2019-08-15 00:00:00
abstract::The absorption mechanisms of drugs play an important role on development and various application of drugs. However, the present methods of absorption mechanisms are not perfect enough. Hence, exploring a novel method to accurately predict the absorption mechanisms is necessary. In this study, we developed an Ussing mo...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119170
更新日期:2020-04-15 00:00:00
abstract::The purpose of the present study was to investigate the effect of secondary structure of three model polypeptides on their apparent permeability (P(app)) across a synthetic, microporous membrane. Poly-L-lysine (PL), poly-L-glutamate (PGlu), and poly-L-lysine-L-phenylalanine (1:1) (PLP) were selected because a solution...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(02)00320-4
更新日期:2002-09-05 00:00:00
abstract::Anti-neuroexcitation peptide (ANEP) is a promising candidate for the treatment of neuroexcitation-associated diseases. N-Trimethyl chitosan (TMC) with different degrees of quaternization was synthesized, characterized and evaluated as a brain-targeting delivery vehicle for ANEP. ANEP-loaded TMC nanoparticles were prep...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.11.002
更新日期:2010-02-15 00:00:00