Abstract:
:Water-insoluble suspensions of itraconazole and budesonide were sterically stabilized using nonionic polymers (poloxamer 188 or polysorbate 80) and probed for polymer-anion interactions by measuring changes in particle zeta potential. Anions comprising a range of functionalities and aqueous solubilities were examined. Results showed that the more hydrophobic anions partitioned to the particle interface, and a simple model for predicting anion adsorption was developed from their calculated properties. Anions with a calculated Klopman water solubility less than 10 microM or a calculated log P>3.5 were adsorbed to the particle-polymer interface effectively increasing the overall particle charge. Anions of similar hydrophobicities with sulfonate or sulfate functionalities showed a much higher degree of particle charging compared with their carboxylate and phosphonate analogs at pH 9.5. In addition, the electrostatic charging of particles occurred at lower solution concentrations of sulfonate derivatives. These results suggest that the relative basicity of the oxoanion functionality may influence protonation or ion-pairing phenomena of the anions when adsorbed at the particle-polymer interface. Cetyltetramethylammonium bromide (CTAB) produced a positively charged particle consistent with the model developed for anion adsorption. Particle charging of sterically stabilized drug suspensions appeared largely independent of drug and polymer type. Anion hydrophobicity (solubility) and headgroup functionality dictated the observed charging behavior.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Owen H,Graham S,Werling JO,Carter PWdoi
10.1016/j.ijpharm.2008.10.004subject
Has Abstractpub_date
2009-02-23 00:00:00pages
154-9issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(08)00705-9journal_volume
368pub_type
杂志文章abstract::The aim of the current study is to explore the potential of PEG-30-dipolyhydroxystearate (Cithrol(®) DPHS) and Soluplus(®) as ingredients in novel semisolid self-nanoemulsifying drug delivery systems (SNEDDS). Semisolid SNEDDS consisting of Cithrol(®) DPHS, Capmul(®) MCM and Kolliphor(®) HS 15 were successfully prepar...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.10.063
更新日期:2014-12-30 00:00:00
abstract::Lipid-based liquid crystalline nanoparticles (LCNPs) have attracted growing interest as a new drug nanocarrier system for improving bioavailability for both hydrophilic and hydrophobic drugs. In this study, self-assembled LCNPs based on soy phosphatidyl choline and glycerol dioleate, which was known possessing low tox...
journal_title:International journal of pharmaceutics
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journal_title:International journal of pharmaceutics
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abstract::Size reduction of microcrystalline cellulose (MCC, Avicel PH-101) powder by ball milling was poorly effective, particularly in the presence of sodium lauryl sulphate (SLS), which tended to form a protective foam. Ultrasonic homogenisation of an aqueous suspension more readily produced ultra-fine MCC, even in the prese...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00652-9
更新日期:2001-02-01 00:00:00
abstract::This work focuses on the relevance of antibacterial nanofibers based on a polyelectrolyte complex formed between positively charged chitosan (CHT) and an anionic hydroxypropyl betacyclodextrin (CD)-citric acid polymer (PCD) complexing triclosan (TCL). The study of PCD/TCL inclusion complex and its release in dynamic c...
journal_title:International journal of pharmaceutics
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更新日期:2016-11-20 00:00:00
abstract::Combination strategy involving cyclodextrin (CD) complexation and liposomal system was investigated for Paclitaxel (PTX) to improve loading. Complexation was done using 2,6-di-O-methylbetacyclodextrin (DMβCD). Sterically stabilized double loaded PEGylated liposomes (DLPLs) containing PTX and PTX-DMβCD complex were pre...
journal_title:International journal of pharmaceutics
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doi:10.1016/j.ijpharm.2017.11.048
更新日期:2018-01-30 00:00:00
abstract::Andrographolide (AG) is a chemical entity from traditional Chinese herbs and its oral pills have been applied to the treatment of respiratory inflammation. Here we report pulmonary delivery of liposomal AG dry powder inhalers (LADPIs) for treatment of Staphylococcus aureus-induced pneumonia. AG liposomes were prepared...
journal_title:International journal of pharmaceutics
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更新日期:2017-08-07 00:00:00
abstract::The pharmacokinetics of NS-49, a newly developed phenethylamine class alpha(1A)-adrenoceptor agonist, was investigated in rats, rabbits, and dogs given intravenous and oral doses that have little effect on the renal blood flow rate (approximating the range of clinical doses). A three-compartment open model adequately ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
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更新日期:1999-09-20 00:00:00
abstract::Oral administration of proteins and peptides still is a challenging task to overcome due to low permeability through absorptive epithelia, degradation and metabolism that lead to poor bioavailability. Attempting to overcome such limitations, an antihypertensive peptide derived from whey protein, with KGYGGVSLPEW seque...
journal_title:International journal of pharmaceutics
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abstract::The aim of this study was to provide preliminary validation of a new sublingual mucosal cell line (HO-1-u-1) for use as in vitro sublingual drug delivery screening of compounds involving passive diffusion. HO-1-u-1 cells were seeded on cell culture inserts. The ultrastructure and integrity of cell layers, inter-passag...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.10.012
更新日期:2007-04-04 00:00:00
abstract::There are a range of products available which claim to accelerate the healing of burns; these include topical agents, interactive dressings and biomembranes. The aim of this study was to assess the effect of a gelatin-based membrane containing usnic acid/liposomes on the healing of burns in comparison to silver sulfad...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.09.040
更新日期:2016-11-20 00:00:00
abstract::Quantitative analysis using proton NMR (1H qNMR) has been employed in various areas such as pharmaceutical analysis (e.g., dissolution study), vaccines, natural products analysis, metabolites, and macrolide antibiotics in agriculture industry. However, it is not routinely used in the quantification of saccharides in d...
journal_title:International journal of pharmaceutics
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doi:10.1016/j.ijpharm.2019.03.030
更新日期:2019-06-10 00:00:00
abstract::Fucoidan, a sulphated polysaccharide, plays a vital role in reducing cellular oxidative damage by exerting potential antioxidant activity. However, because of the negative surface charges of oligofucoidan, it shows poor oral intestinal absorption. To overcome this drawback, the oligofucoidan polysaccharides self-assem...
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abstract::Novel biodegradable amphiphilic copolymers hy-PEI-g-PCL-b-PEG were prepared by grafting PCL-b-PEG chains onto hyper-branched poly(ethylene imine) as non-viral gene delivery vectors. Our investigations focused on the influence of graft densities of PCL-b-PEG chains on physico-chemical properties, DNA complexation and t...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.05.017
更新日期:2012-05-01 00:00:00
abstract::Nanoparticles delivery of oligonucleotides represents a potential approach for cancer treatment. However, most of the experiments were based on established cancer cell lines and may not reflect the original solid tumor in vivo. Both, tumor microenvironment and tumor cell biological properties in the tumor can influenc...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.07.009
更新日期:2011-10-31 00:00:00
abstract::Inadequate flowability of powders in industries during handling can cause many problems. For example, lack of flow from hoppers, poor tablet weight consistency, and low production rate in tableting. Many factors are known to commonly affect flow properties of powders, such as temperature, humidity and conditioning dur...
journal_title:International journal of pharmaceutics
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更新日期:2021-01-20 00:00:00
abstract::Active drug targeting and controlled release of hydrophilic macromolecular drugs represent crucial points in designing efficient polymeric drug delivery nanoplatforms. In the present work EGFR-targeted polylactide-co-glycolide (PLGA) nanoparticles were made by a blend of two different PLGA-based polymers. The first, G...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.08.011
更新日期:2016-09-25 00:00:00
abstract::Polymer microcapsules offer a possibility of storing increased amounts of drugs. Appropriate design and composition of the microcapsules allow tuning of the drug-release process. In this paper, we report on synthesis of hydrogel microcapsules sensitive to temperature and pH and degradable by glutathione and hydrogen p...
journal_title:International journal of pharmaceutics
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journal_title:International journal of pharmaceutics
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更新日期:2016-03-30 00:00:00
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journal_title:International journal of pharmaceutics
pub_type: 杂志文章
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更新日期:1999-06-25 00:00:00
abstract::Over the last 10 years, the development of intelligent biomaterials for medical and pharmaceutical applications has attracted growing interest by combining interdisciplinary efforts. Between them nanogels represent one of the most attractive carriers for innovative drug delivery systems. In the present investigation n...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.10.017
更新日期:2016-12-30 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
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更新日期:2001-07-03 00:00:00
abstract::An aerosol system is described for the generation and delivery of measured doses of monodisperse therapeutic drug particles to the human lungs. The system comprises a spinning top aerosol generator (STAG), aerosol chamber and inhalation control unit. Monodisperse aerosols allow drug particle size effects to be studied...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
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更新日期:2003-03-26 00:00:00
abstract::The aim of this study is to develop an aqueous parenteral solution of docetaxel using prodrugs. Docetaxel (DTX) is a highly lipophilic drug and practically insoluble in water. To overcome insolubility of docetaxel, three kinds of docetaxel prodrugs were synthesized using succinyl linker such as DTX-G, DTX-L or DTX-S a...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
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更新日期:2014-02-28 00:00:00
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journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.03.004
更新日期:2019-05-01 00:00:00
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journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.01.024
更新日期:2016-03-16 00:00:00
abstract:PURPOSE:Application of spray-dried chitinosans as excipients for use in drug delivery systems was explored. METHODS:Spray- and tray-dried chitinosans previously N-deacetylated and depolymerized were used. Directly compressed tablets (200mg) containing tetracycline, chitinosan, and magnesium stearate were prepared. The...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
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更新日期:2003-02-18 00:00:00
abstract::The current research work explores the potential applications of cationic self-nanoemulsifying oily formulations (CSNEOFs) for enhancing the oral bioavailability of olmesartan medoxomil. Initial preformulation studies, risk assessment and factor screening studies revealed selection of oleic acid, Tween 40 and Transcut...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.07.048
更新日期:2015-09-30 00:00:00