Abstract：
:The effect of different formulation factors (lipid type, cholesterol, charge, internal buffer capacity, drug-to-lipid incubation ratio) on the encapsulation efficiency and size of primaquine liposomes (SUV's) in response to a pH gradient was investigated by a fractional factorial screen ing design. Three of the factors (charge, internal buffer capacity, drug -to-lipid incubation ratio) were further studied in a Box--Behnken optimisation design. The lipid type was the most important parameter followed by the drug-to-lipid incubation ratio, buffer capacity, cholesterol and charge. Several of the interactions wer e important. In the optimisation design a robust region with high encapsulation efficiency (>95%) was obtained for DSPC: 33.33 mol% cholesterol-liposomes at high internal citrate concentration (200 mM) by maintaining the drug-to-lipid incubation ratio below 0.15:1 (mol:mol) and varying the charge incorporation between 2 and 10%. In order to achieve long-term stability and sterility, the liposomes were lyophilised followed by gamma irradiation. The pH gradient was maintained during this treatment with little chemical degradation of the substances. The final preparation consisted of three separate vials with lyophilised liposomes, solid state primaquine and hydration medium.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Stensrud G,Sande SA,Kristensen S,Smistad Gdoi
10.1016/s0378-5173(00)00338-0keywords:
subject
Has Abstractpub_date
2000-04-05 00:00:00pages
213-28issue
2eissn
0378-5173issn
1873-3476pii
S0378517300003380journal_volume
198pub_type
杂志文章abstract：:An innovative bioadhesive patch intended primarily as a vulval drug delivery system and, specifically, as a means to deliver photosensitisers, or their prodrugs, for photodynamic purposes is described. The patch was formulated with a copolymer of methyl vinyl ether and maleic anhydride (PMVE/MA) as a bioadhesive matri...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.11.035
更新日期：2005-04-11 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：:With the current transformation of the pharmaceutical industry towards continuous manufacturing, there is an inherent need to embrace this concept already during the early stages of drug formulation. Therefore, this research paper investigated the feasibility of using miniaturized forced feeders on a high-speed rotary...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.09.006
更新日期：2018-10-25 00:00:00
abstract：:Several classes of antifungal have been employed in candidiasis treatment, but patients with advanced immunodeficiency can present unsatisfactory results after therapy. In these cases, high doses of drugs or the use of multiple agents are sometimes used, and hence increasing the risk of serious side effects. Consideri...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.08.002
更新日期：2008-02-12 00:00:00
abstract：:In this study, we demonstrate the feasibility of using the thermal adhesion granulation (TAG) method to improve granular properties for preparing highly compressible excipients as direct tabletting aids. The TAG method subjects a mixture containing excipients, such as microcrystalline cellulose (MCC), lactose, starch,...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.02.002
更新日期：2008-06-05 00:00:00
abstract：:A gastroretentive drug delivery system of DA-6034, a new synthetic flavonoid derivative, for the treatment of gastritis was developed by using effervescent floating matrix system (EFMS). The therapeutic limitations of DA-6034 caused by its low solubility in acidic conditions were overcome by using the EFMS, which was ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.12.042
更新日期：2008-05-22 00:00:00
abstract：:Ciprofloxacin (CPX) physicochemical properties, mainly hydrophobicity and microspeciation, appear to be related with the ability of this drug to adsorb and diffuse through lipid environments. We have combined the information from fluorescence anisotropy, quenching and epifluorescence of phospholipid monolayers, to exp...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00633-6
更新日期：2003-02-18 00:00:00
abstract：:The self-organizing complexes with hyaluronic acid (HA) and polydopamine (PDA), an adhesion mediator via hydrogen bonding, were investigated for use as protein drug carriers. The complexes were prepared with HA of different molecular weights (20 kDa and 200 kDa) and various molar ratios of dopamine and lysozyme, a mod...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.03.007
更新日期：2018-05-05 00:00:00
abstract：:This work presents a simple and fast method for the simultaneous determination of amiloride and furosemide by digital derivative spectrophotometry. HCl 1 x 10(-2) mol/l dissolved in ethanol was used as solvent and to extract drugs from formulations. Subsequently the samples were evaluated directly by first digital der...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00482-9
更新日期：2002-12-05 00:00:00
abstract：:Herein, a series of new amino acid-functionalized hollow mesoporous silica nanospheres (HMSNs) by post-grafting methods were prepared. These new materials were characterized by different techniques and were studied as matrices for the antineoplastic drug (cisplatin) transport and delivery. The results demonstrate that...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118709
更新日期：2019-12-15 00:00:00
abstract：:Twenty diclofenac sodium buccoadhesive discs containing Cp974p, polycarbophil, PEO, SCMC-medium viscosity (SCMC-MV), SCMC-ultrahigh viscosity (SCMC-UHV) or their combinations were prepared. These buccoadhesive discs were evaluated for release pattern, swelling capacity, surface pH, mucoadhesion performance, and in vit...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.07.033
更新日期：2004-11-22 00:00:00
abstract：:Different types of ibuprofen- and lidocaine-loaded, poly(lactic-co-glycolic acid) (PLGA)-based microparticles and thin, free films of various dimensions were prepared and physico-chemically characterized in vitro. The obtained experimental results were analyzed using mathematical theories based on Fick's second law of...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.10.030
更新日期：2008-04-16 00:00:00
abstract：:Despite that in solution we cannot detect the interaction between Ni(2+) and mitoxantrone (MIT), Ni(2+) could mediate effective and stable MIT loading into large unilamellar vesicles (LUVs). The presence of nigericin had almost no influences on MIT encapsulation. However, in the presence of NH(3), the drug loading kin...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.09.045
更新日期：2009-02-23 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
doi：10.1016/s0378-5173(99)00184-2
更新日期：1999-09-20 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：:The cyclooxygenase-2 (COX-2)/prostaglandin E2 (PGE2) pathway plays an important role in tumor development and formation of metastases. It was earlier reported that cyclodextrin derivatives have a high affinity to form complexes with PGE2. Based on these results radiolabeled cyclodextrins - as new radiopharmaceuticals ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118954
更新日期：2020-02-25 00:00:00
abstract：:Diabetic ulcers are prone to bacterial contamination and can severely affect patient's quality of life. This study is first report to explore copper-grafted graphene oxide-crosslinked zein scaffolds (Cu-GZS) for promoting cutaneous excision wounds healing as a promising therapeutic modality in diabetic male-rats. Cu-G...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119919
更新日期：2020-11-30 00:00:00
abstract：:This review aims to give to the reader some new light on cyclodextrin (CD)-based theranostic agents in order to complete our recently published review dedicated to CD-particles conjugates in drug delivery systems (Zafar et al., 2014). CDs are biocompatible sugar-based macrocycles used in a wide range of biomedical app...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2014.06.004
更新日期：2014-09-10 00:00:00
abstract：:Naltrexone hydrochloride (NTX) is a promising treatment for corneal disorders linked to diabetes mellitus (diabetic keratopathy). However, NTX has a major stability problem due to autoxidation, which is likely to hinder its formulation as eye drops for treatment of diabetic keratopathy. In this study, in-house develop...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.05.011
更新日期：2012-08-20 00:00:00
abstract：:Fluorinated graphene has recently gained much attention for cancer drug delivery, owing to its peculiar properties including high electronegativity difference, magnetic resonance imaging contrast agent, and the photothermal effect. However, the hydrophobic nature of fluorinated graphene greatly hinders its application...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118791
更新日期：2019-12-15 00:00:00
abstract：:Low-frequency Raman (LFR) spectroscopy probes vibrational modes related to long-range order (i.e., crystallinity) that can provide unique information on the solid-state/structural characteristics among other properties. Furthermore, the recent advancements in instrumentation (most notably, narrow wavelength band filte...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.120034
更新日期：2021-01-05 00:00:00
abstract：:In the present paper the interaction between lambda carrageenan, a natural sulphated polysaccharide, and diltiazem HCl, a Ca channel blocking agent, was studied. Dialysis equilibria were performed to quantify the binding capacity of lambda carrageenan for diltiazem. The relevance of the interaction to hydrophilic matr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00389-6
更新日期：2000-05-10 00:00:00
abstract：:Plasma stability plays an important role in drug discovery and development. Unstable compounds tend to have rapid clearance and short half-life, resulting in poor in vivo performance. This paper examines the variables that affect the plasma stability assay results, including substrate concentration, %DMSO, plasma conc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.03.022
更新日期：2005-06-13 00:00:00
abstract：:The majority of innovative drug candidates are poorly water soluble and exhibit basic properties. This makes them highly dependent on the in vivo encountered acid-neutral pH sequence to achieve a sufficient dissolution and thus absorption. In this study, we evaluated the pH-independent generation of intraluminally ind...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.01.049
更新日期：2008-06-05 00:00:00
abstract：:Drug development is a long process which requires careful evaluation of the drug substance (active pharmaceutical ingredient, API), drug product (tablet, capsule etc.) and the bioperformance (both pre-clinical and clinical) before testing the efficacy of the final dosage form. The earliest assessment of a new drug sub...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.08.055
更新日期：2018-10-25 00:00:00
abstract：:Curcumin shows effective anti-inflammatory activities but is seldom used in clinic because of its poor solubility in water and vulnerablity to sunshine ultraviolet effect. Novel lipid vesicles have been developed as carriers for skin delivery. In this paper, lipid vesicles-propylene glycol liposomes (PGL), Ethosomes a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.06.052
更新日期：2013-09-15 00:00:00
abstract：:DNA fragments such as oligodeoxynucleotides (ODNs) are under investigation for a possible utilization in nuclear medicine. Until now, experiments on 99mTc-labeled ODNs in vitro or in vivo have required the application of time-consuming procedures to obtain and control the purity of the radiolabeled compound. A lyophil...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00293-8
更新日期：1999-11-15 00:00:00
abstract：:Dermally applied poorly soluble actives whether in cosmetics or pharmaceuticals show insufficient skin penetration. Especially actives being insoluble in both phases of dermal vehicles, i.e. water and oil have no or less real effect. An approach to overcome this obstacle is the use of amorphous actives instead of the ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2018.11.018
更新日期：2019-01-30 00:00:00
abstract：:The hypothesis for the investigation was that the overall mechanism of action of skin penetration enhancers is best explained by the Solubility-Physicochemical-Thermodynamic (SPT) theory. To our knowledge, this is the first report of the application of SPT theory in transdermal/topical/enhancer research. The SPT theor...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118920
更新日期：2020-02-15 00:00:00
abstract：:The dehydration of nedocromil magnesium (NM) pentahydrate proceeds in two steps, corresponding to the loss of four water molecules in the first step and one water molecule in the second step. The effects of temperature, particle size, sample weight, water vapor pressure and dehydration-rehydration cycle on both the ki...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00700-6
更新日期：2001-03-14 00:00:00
