Abstract:
:The number of mixed micellar (MM) drug products being introduced into the commercial pharmaceutical market is very limited although there is need for alternative dosage forms for poorly soluble active drug substances. While known systems are composed of phosphatidylcholine and bile salts, it was the aim of this study to investigate if alternative surfactants are able to form isotropically clear solutions over a broad range of concentrations and at higher ratios of phosphatidylcholine (PC). It was a particular challenge of this work to find a MM system with a unimodal particle size distribution since it is known that surfactants often form vesicles with phospholipids instead of MM. The theoretical approach behind this work was the transfer of the packing parameter concept, which describes the molecular association of one amphiphilic species, to the organisation behaviour of two different amphiphilic species (water-insoluble phospholipid+surfactant leading to MM). Therefore the influence of the surfactant molecular geometry on the ability to form MM with phospholipids was investigated. A homologous series of two different surfactant classes, namely polyglycerol esters and sucrose esters, with a large hydrophilic head region leading to a smaller packing parameter were analysed regarding their ability to form clear MM solutions with PC. For comparison, surfactants with no strictly defined partition between a polar head and a non-polar tail (e.g. Poloxamer 188) were tested. Decaglycerol laurate and especially sucrose laurate (SL) were superior compared to all other tested surfactants with respect to their ability to form clear solutions with hydrogenated PC (hPC) at a higher ratio and over a broad range of concentrations while unsaturated PC showed an inferior performance to form MM. The favourite MM system composed of SL with 0.5 weight fractions of hPC formed about 20 nm sized MM in a concentration range of 1.0-80 mg/mL and showing a unimodal particle size distribution with a PDI value <0.1. The results of the study have shown that the transferred packing parameter concept is applicable to the tested surfactants to describe their ability forming mixed micelles with PC.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Rupp C,Steckel H,Müller BWdoi
10.1016/j.ijpharm.2009.12.018subject
Has Abstractpub_date
2010-03-15 00:00:00pages
120-8issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(09)00875-8journal_volume
387pub_type
杂志文章abstract::The purpose of this study was to determine quantitatively the amorphous fraction in crystalline-amorphous powder mixtures of trehalose, in order to assess the ability of the (13)C NMR technique for quantitative amorphous characterization. The NMR method is described in detail and its accuracy is compared to that of th...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.05.012
更新日期:2004-08-06 00:00:00
abstract::Niosomes are vesicles formed by self-assembly of non-ionic surfactants. In this investigation, the effects of processing variables, particularly temperature and sonication, on the physical characteristics and phase transitional behaviour of two niosomal systems based on a hexadecyl diglycerol ether (C(16)G(2)) have be...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00362-8
更新日期:2000-05-15 00:00:00
abstract::Sustained release of active interferon-α (IFN-α) has been achieved from core-shell nanoparticles (NPs) prepared by aqueous precipitation of IFN-α-enriched human serum albumin (HSA-IFN-α) and layer-by-layer (L-b-L) by coating of the IFN-α NPs with poly(sodium-4-styrene) sulphonate (PSS) and chitosan (Chit). The concent...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.118825
更新日期:2020-01-05 00:00:00
abstract::This study was aimed at developing a liposome delivery system for a new and potential antitumor lipophilic prodrug of 5-fluorouracil (5-Fu)-N(3)-O-toluyl-fluorouracil (TFu), intended to improve the bioavailability and therapeutic efficacy of 5-Fu by oral and intravenous administration. TFu-loaded liposomes were prepar...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.11.017
更新日期:2008-04-02 00:00:00
abstract::A new system for prediction of drug absorption that takes into account drug dissolution and pH change in the gastro-intestinal tract was developed. In this new system, a drug (solid form) is added into a drug-dissolving vessel (pH 1.0) and the dissolved drug is transferred to a pH adjustment vessel (pH 6.0). Then the ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(01)00663-9
更新日期:2001-06-19 00:00:00
abstract::This work describes the development of heparinized polymeric micelle as a novel injectable carrier for the dual drug delivery that can simultaneously release basic fibroblast growth factor (bFGF) and indomethacin (IMC), which can promote the regeneration of damaged tissue and prevent the inflammatory response after im...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2007.06.025
更新日期:2008-01-04 00:00:00
abstract::Controlled release of hydrophilic drugs from carriers is still faced with problems due to the poor compatibility of such substances with slowly degradable polymers leading to challenges regarding fabrication as well as undesired burst release of the encapsulated drugs. In this context, coaxial electrospinning being ca...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.12.026
更新日期:2019-02-10 00:00:00
abstract::Pharmacopoeias prescribe tests to determine the levels of arsenic in raw materials and glass containers. In this study, glass ampoules for injectables containing individually the main components of intravenous nutrition formulations were submitted to the hydrolytic resistance test by heating at 121 degrees C for 30 mi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.02.008
更新日期:2006-06-06 00:00:00
abstract::The objective of this study was to evaluate mucoadhesive properties and gastrointestinal transit of microspheres made of oppositely charged dextran derivatives and cellulose acetate butyrate (CAB). The microspheres were prepared by emulsion solvent evaporation method. A reference microsphere was made of lactose instea...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(03)00159-5
更新日期:2003-06-04 00:00:00
abstract::Mirena® is long-acting (5 years) contraceptive intrauterine device. It is composed of a hollow cylindrical drug reservoir (containing Levonorgestrel and polydimethylsiloxane), which is covered with a release rate controlling silicone membrane. This structure presents a manufacturing challenge and to date, there have b...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.09.004
更新日期:2018-10-25 00:00:00
abstract::In situ amorphization is a concept that allows to amorphize a given drug in its final dosage form right before administration. Hence, this approach can potentially be used to circumvent recrystallization issues that other amorphous formulation approaches are facing during storage. In this study, the feasibility of mic...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.01.035
更新日期:2017-03-15 00:00:00
abstract::Despite their great potential, the nano-sized extracellular vesicles are yet to become effective delivery systems for poorly water-soluble drugs. Here, we present a novel platform of exosomes as a drug delivery system by engineering of a poorly water-soluble drug into a poloxamer-based molecular nanostructured dispers...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.06.028
更新日期:2019-07-20 00:00:00
abstract::The present investigation aims at formulating lipid based drug delivery system of β-Artemether and Lumefantrine and comparative pharmacological evaluation with innovator formulation. Commercial modified oil and indigenous natural fatty acids comprised the oily phase in developing lipidic formulation of β-Artemether an...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.07.033
更新日期:2013-10-15 00:00:00
abstract::The aim of this study was to design a controlled release vehicle for insulin to preserve its stability and biological activity during fabrication and release. A modified, double emulsion, solvent evaporation, technique using homogenisation force optimised entrapment efficiency of insulin into biodegradable nanoparticl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.12.063
更新日期:2016-02-29 00:00:00
abstract::A mechanistic particle scale model is proposed for bilayer tablet compaction. Making bilayer tablets involves the application of first layer compaction pressure on the first layer powder and a second layer compaction pressure on entire powder bed. The bonding formed between the first layer and the second layer particl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.07.032
更新日期:2017-08-30 00:00:00
abstract::The aim of this study was to investigate the in vitro dissolution characteristics of pH-responsive polymers in a variety of simulated fluids. Prednisolone tablets were fabricated and coated with the following polymer systems: Eudragit S (organic solution), Eudragit S (aqueous dispersion), Eudragit FS (aqueous dispersi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2005.10.038
更新日期:2006-02-03 00:00:00
abstract::Although RNA interference (RNAi) technology shows great potential in cancer treatment, the tumor target delivery and sufficient cytosolic transport of RNAi agents are still the main obstacles for its clinical applications. Herein, we report a functional supramolecular self-assembled nanoparticle vector for RNAi agent ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.118898
更新日期:2020-02-15 00:00:00
abstract::The efficiency of drug depends not only on its potency but also on its ability to reach the target sites in preference to non-target sites. In this regard, protein assembled nanocarrier is the most promising strategy for intracellular anti-cancer drug delivery. The key motive of this study is to fabricate biocompatibl...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119192
更新日期:2020-04-30 00:00:00
abstract::Preparation conditions of nanoparticles greatly influence their physicochemical characteristics. A factorial design was used to evaluate the influence of these conditions on the particle diameter, zeta potential, polydispersity, percentage recovery, and molecular weight of poly(isobutylcyanoacrylate) nanoparticles. Th...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00311-7
更新日期:1999-12-20 00:00:00
abstract::Designed for gene therapy of chronic diseases, HBP-DEAPA 60 is a non-toxic biodegradable amine modified hyperbranched polyester. This candidate was chosen from a series of hyperbranched polymers for further characterization as it showed the best transfection efficiency and fastest degradation rate. HBP-DEAPA 60/DNA co...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.06.065
更新日期:2012-10-15 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::Glycerosomes were formulated using 1,2-dimyristoyl-sn-glycero-3-phosphatidycholine (DMPC), diclofenac sodium salt and 10, 20 or 30% glycerol in the water phase, while corresponding liposomes were prepared with the same amount of DMPC and diclofenac, without glycerol. The aim of the present work was to evaluate the eff...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.09.026
更新日期:2017-10-30 00:00:00
abstract::A drug's solubility in a polymeric excipient is an important parameter that dictates the process window of hot-melt extrusion (HME) and product stability during storage. However, it is rather challenging to experimentally determine the solubility and there is very few published work in this field. In this study, the s...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.10.026
更新日期:2011-01-17 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::Influenza vaccines administered intramuscularly exhibit poor mucosal immune responses in the respiratory tract which is the prime site of the infection. Intranasal vaccination is a potential route for vaccine delivery which has been demonstrated effective in inducing protective immune responses in both systemic and mu...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119348
更新日期:2020-05-30 00:00:00
abstract::The current study aimed to develop an effective transdermal nanovesicular carrier of diflunisal that provides enhanced delivery through the skin. Two types of nanovesicles, ethosomes and transfersomes, were investigated and compared to conventional liposomes. Ethosomes with variable ethanol contents (10, 30 and 50%) a...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.04.001
更新日期:2019-05-30 00:00:00
abstract::Primary objective of this investigation was to delineate the differential impact of efflux transporters P-glycoprotein (P-gp/Abcb1) and breast cancer resistance protein (Bcrp1/Abcg2) on brain disposition and plasma pharmacokinetics of pazopanib. In addition, this research investigated whether inhibition of these efflu...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.05.038
更新日期:2012-10-15 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::Although the taste-masking of bitter drug using ion exchange resin has been recognized, in vitro testing using an electronic tongue (e-Tongue) and in vivo bitterness test by human panel test was not fully understood. In case of orally disintegrating tablet (ODT) containing bitter medicine, in vitro and in vivo disinte...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.07.072
更新日期:2013-10-15 00:00:00
abstract::This work describes the pharmacokinetics of a novel carbamazepine nanoemulsion. The plasma concentration profiles were determined in beagle dogs after i.v. bolus administration of a 5 mg/kg carbamazepine nanoemulsion and compared to the corresponding carbamazepine/hydroxypropyl-beta-cyclodextrin complex solution. Both...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.05.055
更新日期:2009-08-13 00:00:00