Abstract:
:This work investigated the permeation of primaquine across full-thickness excised human skin from two acrylate transdermal adhesives. Primaquine base was formulated with National Starch 387-2516 and 387-2287 to provide aluminium foil-backed 1-cm diameter patches, each loaded with 10 mg drug. Other patches were prepared that included Migliol 840 as a potential penetration enhancer. The patches were applied to cadaver skin in Franz-type diffusion cells and the permeation of primaquine determined over a 24-h period. Relatively high fluxes were found, the highest being from those formulations lacking the Migliol 840: 5.68+/-0.30x10(-2) mg cm(-2) h(-1) from 387-2516; 4.94+/-0.20x10(-2) mg cm(-2) h(-1) from 387-2287. It was determined that a simple patch with a diameter of approximately 13 cm(2) could deliver a therapeutic in vivo dose, with possibilities for the treatment and prophylaxis of Plasmodium vivax, P. ovale and P. falciparum forms of malaria. The presence of Migliol 840 failed to produce the anticipated enhancing effect: flux rates that were approximately halved. These results could to a certain extent be rationalised in terms of thermodynamic activity.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Jeans CW,Heard CMdoi
10.1016/s0378-5173(99)00215-xkeywords:
subject
Has Abstractpub_date
1999-10-28 00:00:00pages
1-6issue
1eissn
0378-5173issn
1873-3476pii
S0378-5173(99)00215-Xjournal_volume
189pub_type
杂志文章abstract::Administration of drugs via the oral route is the most common and preferred route due to its ease of administration, cost-effectiveness and flexibility in design. However, if the drug being administered has limited aqueous solubility it can result in poor bioavailability. Furthermore, the low pH of the stomach as well...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.11.029
更新日期:2016-01-30 00:00:00
abstract::Cyclosporine A (CsA) is a well-known immunosuppressive agent used as rescue therapy in severe steroid-refractory ulcerative colitis (UC). However, toxicity issues associated with CsA when administered in its commercially available formulations have been reported in clinical practice. Since nanotechnology has been prop...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.03.012
更新日期:2016-04-30 00:00:00
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: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::Substitutive hormonal therapies have to be administered for long periods. Thus, the development of sustained-release forms, as microparticle suspensions, is interesting in order to improve patient compliance by reducing dosing frequencies and side effects. The aim of this work was to compare different formulations of ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2003.09.040
更新日期:2004-01-28 00:00:00
abstract::Azithromycin loaded microspheres with blends of poly-l-lactide and ploy-D,L-lactide-co-glycolide as matrices were prepared by the atmosphere-solvent evaporation (ASE) and reduced pressure-solvent evaporation (RSE) method. Both the X-ray diffraction spectra and DSC thermographs demonstrated that poly-L-lactide existed ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.04.081
更新日期:2012-08-20 00:00:00
abstract::The kinetics of degradation of the new anti-tumor drug, 4-dedimethylamino sancycline (col-3) in aqueous solution at 25oC were investigated by high-pressure liquid chromatography (HPLC) over the pH-range of 2-10. The influences of pH, buffer concentration, light, temperature, and some additives on the degradation rate ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(98)00417-7
更新日期:1999-04-20 00:00:00
abstract::This work aims to study the biophysical interactions of rifampicin (RIF) with three-dimensional macrophage membrane models, under environments with physiological and pathological relevance. The interaction of RIF with liposomes formed by 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) in different pH values (i.e., ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.03.005
更新日期:2014-05-15 00:00:00
abstract::The use of experimental design for the robustness testing of a flow-through dissolution method (Ph Eur/USP Apparatus 4) for atovaquone, one of the drug substances in a dual-active anti-malarial tablet formulation, Malarone tablets, is described. This procedure was developed to overcome the suppression of the atovaquon...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00509-3
更新日期:2000-09-25 00:00:00
abstract::The adsorption profiles of the antibiotic metronidazole (MNE) into the K10-montmorillonite (MMT-K10) clay and the subsequent release have been investigated as a function of pH and MNE/MMT-K10 ratio, in order to evaluate the potential of the MNE/MMT-K10 hybrids as controlled drug delivery system. The adsorption mechani...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.09.017
更新日期:2013-11-30 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
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2011.12.058
更新日期:2012-03-15 00:00:00
abstract::Following vascular bypass interventions, autologous saphenous vein grafts are prone to fail due to intimal hyperplasia development. An atorvastatin (ATV)-eluting tubular mesh coated with poly(d,l-lactide-co-glycolisde) acid (PLGA) was designed for perivascular application, in order to prevent the development of this p...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.12.026
更新日期:2018-02-15 00:00:00
abstract::Lipid emulsions can be used as a vehicle for the production of low-volume injectable preparations with minimally water-soluble active ingredients. First, we focus on the galenic and technological conditions established by ultrasound techniques. A 2(5) factorial design was used to optimize the carrier emulsion. The stu...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00664-5
更新日期:2001-03-23 00:00:00
abstract::The objective of this study was to evaluate the combination of pH-dependent and time-dependent polymers as a single coating for design of colon delivery system of indomethacin pellets. Eudragit S100 and Eudragit L100 were used as pH-dependent polymers and Eudragit RS was used as a time-dependent polymer. A statistical...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.05.011
更新日期:2006-08-31 00:00:00
abstract::The aim of this study is to compare microparticle uptake in animals of different ages, gender and species and at different time points. The 2mum latex/in vivo in situ model uses the observation of animal responses or post-mortem changes and also particle identification by fluorescence microscopy in nine sequential int...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.10.043
更新日期:2007-04-20 00:00:00
abstract::The inhalation of tobramycin is part of current cystic fibrosis (CF) therapy. Local therapy with inhaled antibiotics has demonstrated improvements in pulmonary function. Current inhalation therapy is limited by the available drug formulations in combination with the nebulization time. The aim of this study is to devel...
journal_title:International journal of pharmaceutics
pub_type: 评论,杂志文章
doi:10.1016/s0378-5173(99)00252-5
更新日期:1999-11-05 00:00:00
abstract::The ability to predict mechanical properties of compacted powder blends of Active Pharmaceutical Ingredients (API) and excipients solely from component properties can reduce the amount of 'trial-and-error' involved in formulation design. Machine Learning (ML) can reduce model development time and effort with the imper...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.120049
更新日期:2021-01-05 00:00:00
abstract::HN-1, a 12-amino acid peptide, has been reported to possess strong capabilities for targeting and penetrating head and neck squamous cell carcinoma. Here, we designed a simple but effective nanoparticle system for the delivery of doxorubicin (DOX) targeting oral squamous cell carcinoma (OSCC) through the mediation of ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.04.027
更新日期:2017-06-15 00:00:00
abstract::The concept of skin-specific drug delivery with a spatio-temporal control has just recently received concerns in dermatology. Inspired by the progress in smart materials and their perspective application in medicine science, development of stimuli responsive drug delivery systems with skin-specificity has become possi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2020.120081
更新日期:2021-01-05 00:00:00
abstract::The aim of this study was to investigate the equilibrium swelling properties in urea solutions of gamma-radiation induced polyelectrolyte copolymeric hydrogels consisting of acrylamide (AAm) and crotonic acid (CA). Poly(acrylamide-co-crotonic acid), poly(AAm-co-CA) hydrogels containing different amounts of CA were obt...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.05.026
更新日期:2005-09-14 00:00:00
abstract::The presence of large amounts of reactive oxygen species (ROS) leads to oxidative stress that can damage cell membranes, lead to DNA breakage and cause inactivation of free radical scavenger enzymes, eventually resulting in skin damage. Quercetin is a natural flavonoid that has been shown to have the highest anti-radi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.12.013
更新日期:2013-01-30 00:00:00
abstract::The objective of this study was to examine the use of transdermal iontophoresis for the delivery of ranitidine hydrochloride in children. Constant, direct current, anodal iontophoresis of ranitidine was performed in vitro across dermatomed pig skin. The effect of donor vehicle, current intensity, and drug concentratio...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.03.006
更新日期:2012-10-01 00:00:00
abstract::Superdisintegrants are a key excipient used in immediate release formulations to promote fast tablet disintegration, therefore understanding the impact of superdisintegrant variability on product performance is important. The current study examined the impact of superdisintegrant critical material attributes (viscosit...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119080
更新日期:2020-03-15 00:00:00
abstract::The objective of this study was the development of a niosomal formulation for improving skin permeation and penetration of 5-aminolevulinic acid (ALA) in the treatment of skin malignancies by photodynamic therapy (PDT). Different niosomal dispersions were prepared, using two different preparation methods. The effect o...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.08.036
更新日期:2015-10-15 00:00:00
abstract::To enhance the stability of the anticancer drug gemcitabine (2'-deoxy-2',2'-difluorocytidine), it was conjugated to poly-l-glutamic acid (PG-H) via a carbodiimide reaction. The synthesised poly-l-glutamic acid-gemcitabine (PG-G) was purified and characterised by using SDS-PAGE to estimate its molecular weight, HPLC to...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.03.010
更新日期:2010-05-31 00:00:00
abstract::Poly(ethylene oxide)-block-poly(epsilon-caprolactone) (PEO-b-PCL) and newly developed poly(ethylene oxide)-block-poly(alpha-benzyl carboxylate epsilon-caprolactone) (PEO-b-PBCL) micelles were evaluated for the solubilization and delivery of cucurbitacin I and B, poorly water soluble inhibitors of signal transducer and...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.06.032
更新日期:2008-01-22 00:00:00
abstract::The purpose of this study was to investigate the formation mechanism of colloidal nanoparticles after dispersion of probucol/polyvinylpyrrolidone (PVP)/sodium dodecyl sulphate (SDS) ternary ground mixture (GM) into water. Probucol, PVP and SDS were mixed at a weight ratio of 1:3:1 and ground for 30 min with a vibratio...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.10.052
更新日期:2008-03-20 00:00:00
abstract::Piroxicam crystallises into two polytypes, α1 and α2, with crystal structures that contain identical molecular layers but differ in the way that these layers are stacked. In spite of having close structural similarity, the polytypes have significantly different powder tabletting behaviour: α2 forms only weak tablets a...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.03.040
更新日期:2018-05-30 00:00:00
abstract::Photothermal therapy had great potential in being a new approach of tumour ablation due to their high selectivity and low side effect. However, the shallow penetration depth of near-infrared (NIR) irradiation resulted in the limited curative effect. Herein, a novel nanomedicine was developed based on the indocyanine g...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.05.056
更新日期:2019-07-20 00:00:00
abstract::Oral delivery is the most fascinating route for interminable drug remedy. However, the intestinal absorption of alendronate (ALN), a bisphosphonate drug after oral administration is very poor. Absorption enhancers, which help to achieve the efficiency-safety balance, are considered one of the most promising agents for...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2016.10.046
更新日期:2016-12-30 00:00:00