Abstract:
:Formulation effects on the entrapment of beclometasone dipropionate (BDP) in liposomes generated by hydration of proliposomes were studied, using the high-density dispersion medium deuterium oxide in comparison to deionized water (DW). Proliposomes incorporating BDP (2 mol% of the lipid phase consisting of soya phosphatidylcholine (SPC) and cholesterol; 1:1) were manufactured, using lactose monohydrate (LMH), sorbitol or D-mannitol as carbohydrate carriers (1:5 w/w lipid to carrier). Following hydration of proliposomes, separation of BDP-entrapped liposomes from the unentrapped (free) BDP at an optimized centrifugation duration of 90 min and a centrifugation force of 15,500g were identified. The dispersion medium was found to have a major influence on separation of BDP-entrapped liposomes from the unentrapped drug. Entrapment efficiency values were higher than 95% as estimated when DW was used. By contrast, the entrapment efficiency was 19.69 ± 5.88, 28.78 ± 4.69 and 34.84 ± 3.62% upon using D2O as a dispersion medium (for LMH-, sorbitol- and D-mannitol-based proliposomes, respectively). The similarity in size of liposomes and BDP crystals was found to be responsible for co-sedimentation of liposomes and free BDP crystals upon centrifugation in DW, giving rise to the falsely high entrapment values estimated. This was remedied by the use of D2O as confirmed by light microscopy, nuclear magnetic resonance (1HNMR), X-ray diffraction (XRD) and entrapment studies. This study showed that carrier type has a significant influence on the entrapment of BDP in liposomes generated from proliposomes, and using D2O is essential for accurate determination of steroid entrapment in the vesicles.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Khan I,Yousaf S,Subramanian S,Alhnan MA,Ahmed W,Elhissi Adoi
10.1208/s12249-017-0793-2subject
Has Abstractpub_date
2018-01-01 00:00:00pages
262-274issue
1issn
1530-9932pii
10.1208/s12249-017-0793-2journal_volume
19pub_type
杂志文章abstract::Lipid-based drug carriers are likely to have influence on bioavailability through enhanced solubilization of the drug in the gastrointestinal tract. The study was designed to investigate the lipid formulation digestibility in the simulated gastro intestinal media. Fenofibrate was formulated in representative Type II, ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-012-9787-2
更新日期:2012-06-01 00:00:00
abstract::The purpose of the present study was to design mucoadhesive gliadin nanoparticles (GNP) containing amoxicillin and to evaluate their effectiveness in eradicating Helicobacter pylori. GNP-bearing amoxicillin (AGNP) was prepared by desolvation method. The effect of process variables such as gliadin concentration and ini...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt050232
更新日期:2004-04-07 00:00:00
abstract::Hypertension remains a significant risk factor for several cardiovascular disorders including coronary artery disease and heart failure. Despite the large armamentarium of drugs available for the management of high blood pressure, low oral availability is an ongoing challenge. Researchers are constantly developing alt...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-019-1583-9
更新日期:2020-01-06 00:00:00
abstract::The specific aim of the present study was to investigate the biodegradation and biocompatibility characteristics of rosin, a natural film-forming polymer. Both in vitro as well as in vivo methods were used for assessment of the same. The in vitro degradation of rosin films was followed in pH 7.4 phosphate buffered sal...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt040455
更新日期:2003-10-22 00:00:00
abstract::Bilayer nicotine mucoadhesive patches were prepared and evaluated to determine the feasibility of the formulation as a nicotine replacement product to aid in smoking cessation. Nicotine patches were prepared using xanthan gum or carbopol 934 as a mucoadhesive polymers and ethyl cellulose as a backing layer. The patche...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-010-9534-5
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abstract::Hypertension shows circadian blood pressure rhythms (day-night pattern) that urge the delivery of antihypertensive drugs at the right time in the desired levels. Thus, a bilayered core-in-cup buccoadhesive tablet was formulated that immediately releases olmesartan, to give a burst effect, and controls azelnidipine rel...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1575-9
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abstract::As of March 10, 2020, more than 100,000 novel coronavirus pneumonia cases have been confirmed globally. With the continuous spread of the new coronavirus pneumonia epidemic in even the world, prevention and treatment of the disease have become urgent tasks. The drugs currently being developed are not adequate to deal ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-020-01679-z
更新日期:2020-05-13 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1220-z
更新日期:2018-12-18 00:00:00
abstract::The aim of this study was to evaluate and compare the in vitro and in vivo transdermal potential of w/o microemulsion (M) and gel (G) bases for diclofenac sodium (DS). The effect of dimethyl sulfoxide (DMSO) as a penetration enhancer was also examined when it was added to the M formulation. To study the in vitro poten...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt070488
更新日期:2006-10-20 00:00:00
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journal_title:AAPS PharmSciTech
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更新日期:2013-06-01 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1008-1
更新日期:2018-07-01 00:00:00
abstract::The closed-die compaction behaviour of D-mannitol granules has been simulated by the discrete element method (DEM) to investigate the granule rearrangement and fracture behaviour during compaction which affects the compactibility of the tablet. The D-mannitol granules produced in a fluidized bed were modelled as agglo...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0719-z
更新日期:2017-08-01 00:00:00
abstract::The effects of solvent [acetonitrile, methanol, and acetonitrile/water mixture (20:80, v/v)], buffer concentration (phosphate buffer, pH 7.5), ionic strength and commonly employed adjuvants on the photodegradation of betamethasone-17 valerate in cream and gel formulations have been studied on exposure to UV light (300...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-012-9902-4
更新日期:2013-03-01 00:00:00
abstract::Onychomycosis is a chronic disorder that is difficult to manage and hard to eradicate with perilous trends to relapse. Due to increased prevalence of HIV, use of immunosuppressant drugs and lifestyle-related factors, population affected with fungal infection of nail (Onychomycosis) happens to increase extensively in l...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-019-1591-9
更新日期:2020-01-14 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-015-0404-z
更新日期:2016-06-01 00:00:00
abstract::Gliclazide (GLI), a poorly water-soluble antidiabetic, was transformed into a glassy state by melt quench technique in order to improve its physicochemical properties. Chemical stability of GLI during formation of glass was assessed by monitoring thin-layer chromatography, and an existence of amorphous form was confir...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-012-9760-0
更新日期:2012-06-01 00:00:00
abstract::This paper is a continuation of the research published by the Stability Shelf Life Working Group as chartered under the Product Quality Research Institute. The Working Group was formed in 2006 and disbanded in late 2019. Following the philosophy presented by the Working Group on how to characterize the stability shelf...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01800-2
更新日期:2020-10-20 00:00:00
abstract::Nanoparticles, of the poorly water-soluble drug, itraconazole (ITZ), were produced by the Advanced Evaporative Precipitation into Aqueous Solution process (Advanced EPAS). This process combines emulsion templating and EPAS processing to provide improved control over the size distribution of precipitated particles. Spe...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-012-9817-0
更新日期:2012-09-01 00:00:00
abstract::Children frequently receive medicines that are designed for adults. The dose of commercially available products is adapted, mostly based on the child's bodyweight, thereby neglecting differences in pharmacokinetic and pharmacodynamics parameters. If commercial products are unsuitable for administration to children or ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-016-0515-1
更新日期:2017-02-01 00:00:00
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journal_title:AAPS PharmSciTech
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更新日期:2010-03-01 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0858-2
更新日期:2018-02-01 00:00:00
abstract::A new, simple, inexpensive, and rapid 96-well plate UV spectrophotometric method was developed and validated for the quantification of compound 48/80 (C48/80) associated with particles. C48/80 was quantified at 570 nm after reaction with acetaldehyde and sodium nitroprusside in an alkaline solution (pH 9.6). The metho...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-9950-4
更新日期:2013-06-01 00:00:00
abstract::An innovative and simple methodology has been developed and used for the evaluation of mucoadhesive properties of several polymers by means of sound speed measurements using high-resolution acoustic spectroscopy. In systems made of polymers in water, variations in hydration shell of polymeric chains determine changes ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-010-9490-0
更新日期:2010-09-01 00:00:00
abstract::This investigation aimed to develop nimesulide (NMS)-loaded poly(lactic-co-glycolic acid) (PLGA)-based nanoparticulate formulations as a biodegradable polymeric drug carrier to treat rheumatoid arthritis. Polymeric nanoparticles (NPs) were prepared with two different nonionic surfactants, vitamin E d-α-tocopheryl poly...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-0048-9
更新日期:2014-02-01 00:00:00
abstract::This study focused on the chemical stability of the cephalosporin (6R, 7R)-7-(1-pentafluorophenoxyacetamido)-3-[2-(5-methyl-1,3,4-thiodiazolyl)thiomethyl]-Delta(3)-cephem-4-carboxylic acid, sodium salt (cephem 1) formulation after electron beam (e-beam) irradiation. The cephem 1 concentrations of samples irradiated at...
journal_title:AAPS PharmSciTech
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更新日期:2001-11-19 00:00:00
abstract::The aim of this work is to improve the understanding of the physicochemical mechanisms involved in the functionality of cross-linked carboxymethyl sodium starch (CCSS) as a tablet super disintegrant (SD). The behavior and properties of this SD (medium uptake, disintegration times, particle size, and rheology) was inve...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-014-0121-z
更新日期:2015-04-01 00:00:00
abstract::Ambient air humidity and temperature are known to influence the mechanical strength of tablets. The objective of this work is to understand the influence of processing parameters and environmental conditions (humidity and temperature) on the strength of bilayer tablets. As part of this study, bilayer tablets were comp...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-012-9846-8
更新日期:2012-12-01 00:00:00
abstract::Emulsions are widely used as topical formulations in the pharmaceutical and cosmetic industries. They are thermodynamically unstable and require emulsifiers for stabilization. Studies have indicated that emulsifiers could affect topical delivery of actives, and this study was therefore designed to investigate the effe...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
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更新日期:2014-06-01 00:00:00
abstract::To investigate the possibility of liquid proliposomes being carriers for oral delivery, nimodipine liquid proliposomes-based soft capsules (NPSC) were prepared. Nimodipine proliposomes were characterized by transmission electron microscopy (TEM), conversion rate from proliposomes to liposomes, entrapment efficiency, p...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-9924-6
更新日期:2013-03-01 00:00:00
abstract::The purpose of this study was to demonstrate acoustic resonance spectrometry (ARS) as an alternative process analytical technology to near infrared (NIR) spectroscopy for the quantification of active pharmaceutical ingredient (API) in semi-solids such as creams, gels, ointments, and lotions. The ARS used for this rese...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
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更新日期:2006-07-14 00:00:00