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 alternative drug delivery systems. This review focuses on the transcutaneous delivery of antihypertensive agents. The use of diverse technologies for the delivery of specific antihypertensive agents is emphasized. The advances made and the challenges encountered are highlighted. Several transdermal drug delivery strategies are employed for the transport of this group of therapeutic agents across the skin and the most widely used techniques include microneedles, iontophoresis, sonophoresis, and chemical penetration enhancers. Each of these methods has benefits and limitations, and there are ongoing attempts by scientists to address the shortcomings. For instance, skin irritation continues to be a major challenge with iontophoretic transport while the quantity of a medication that can be incorporated into dissolving microneedles is limited. With skin permeation enhancers, concerns relating to cytotoxicity and irritation are common. Even though the use of ultrasound is exciting, this mode of delivery is also accompanied by challenges such as the design of a battery system that is potent enough to drive a low-frequency sonophoretic cymbal array, while still being portable enough to function as a wearable device. Although most researchers report enhanced drug delivery with the aforementioned methods, it is important to deliver therapeutically useful doses of these medications.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Ita K,Ashong Sdoi
10.1208/s12249-019-1583-9subject
Has Abstractpub_date
2020-01-06 00:00:00pages
56issue
2issn
1530-9932pii
10.1208/s12249-019-1583-9journal_volume
21pub_type
杂志文章,评审abstract::High inter- and intra-individual variability in the pH of fluids in the human gastrointestinal (GI) tract has been described in the literature. The aim of this study was to assess the influence of physiological variability in fasted pH profiles of media along the GI tract on diclofenac sodium (DF-Na) dissolution from ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1140-y
更新日期:2018-10-01 00:00:00
abstract::The solvent used for preparing the binder solution in wet granulation can affect the granulation end point and also impact the thermal, rheological, and flow properties of the granules. The present study investigates the effect of solvents and percentage relative humidity (RH) on the granules of microcrystalline cellu...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-015-0424-8
更新日期:2016-08-01 00:00:00
abstract::The objective of the present study was to develop fast dissolving oral film of the antipsychotic drug, flupentixol dihydrochloride, to enhance its bioavailability, optimize its therapeutic effect when used to treat depression with anxiety, and increase the convenience and compliance by the mentally ill, developmentall...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,随机对照试验
doi:10.1208/s12249-014-0186-8
更新日期:2014-12-01 00:00:00
abstract::The purpose of this study was to develop formulations and systematically evaluate in vitro performances of buccoadhesive patches of propranolol hydrochloride using the hydrophobic polymer Eudragit L-100 as the base matrix. The hydrophilic polymers Carbopol 934 and polyvinyl pyrrolidone (PVP) K30 were incorporated into...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt0802045
更新日期:2007-06-22 00:00:00
abstract::The current study explains the development of sorbitan monostearate and sesame oil-based organogels for topical drug delivery. The organogels were prepared by dissolving sorbitan monostearate in sesame oil (70°C). Metronidazole was used as a model antimicrobial. The formulations were characterized using phase contrast...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-014-0223-7
更新日期:2015-04-01 00:00:00
abstract::Capsaicin has multiple pharmacological activities including antioxidant, anticancer, and anti-inflammatory activities. However, its clinical application is limited due to its poor aqueous solubility, gastric irritation, and low oral bioavailability. This research was aimed at preparing sustained-release matrix pellets...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-015-0352-7
更新日期:2016-04-01 00:00:00
abstract::The aim of this work was to assess the effect of formulation parameters of a mucoadhesive vaginal gel based on chitosan and lactic acid, and to highlight its release mechanisms. Two molecular weight chitosans were used to prepare gels with 2 lactic acid concentrations. Both chitosan molecular weight and lactic acid co...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt0704104
更新日期:2006-01-01 00:00:00
abstract::The objective of this paper is to assess the number of drug particles or droplets contained in metered dose inhaler (MDI) aerosols. Equations were developed to estimate this. The number of drug particles was estimated to be as high as about 300 million for QVAR solution MDIs and as low as 670,000 for Beclovent MDIs. T...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-007-9006-8
更新日期:2008-01-01 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
doi:10.1208/s12249-014-0081-3
更新日期:2014-06-01 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
pub_type: 杂志文章
doi:10.1208/pt020423
更新日期:2001-11-19 00:00:00
abstract::The purpose of this present study was to evaluate the antiangiogenic activity of sterically stabilized liposomes containing paclitaxel (SSL-PTX). The SSL-PTX was prepared by the thin-film method. The release of paclitaxel from SSL-PTX was analyzed using a dialysis method. The effect of SSL-PTX on endothelial cell prol...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-010-9430-z
更新日期:2010-06-01 00:00:00
abstract::This proof-of-concept study explores the feasibility of using a drug-loaded hydrophilic polymeric layer sandwiched between two hydrophobic layers for improving film drug load while achieving sustained release of poorly water-soluble drug. Such films having total thickness in range ~ 146-250 μm were prepared by slurry-...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1089-x
更新日期:2018-08-01 00:00:00
abstract::The paper introduces evaluation methodologies and associated statistical approaches for process validation lifecycle Stage 3A. The assessment tools proposed can be applied to newly developed and launched small molecule as well as bio-pharma products, where substantial process and product knowledge has been gathered. T...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-016-0641-9
更新日期:2017-07-01 00:00:00
abstract::In this study, we investigated the in vitro characteristics of mefenamic acid (MA) microparticles as well as their effects on DNA damage. MA-loaded chitosan and alginate beads were prepared by the ionotropic gelation process. Microsponges containing MA and Eudragit RS 100 were prepared by quasi-emulsion solvent diffus...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-008-9183-0
更新日期:2009-01-01 00:00:00
abstract::The aim of this work was the formulation and characterization of alginate (ALG)-doxycycline (DOX) hydrogel microparticles (MPs) embedded into Pluronic F127 thermogel for DOX intradermal sustained delivery. ALG-DOX MPs were formed by adding a solution of the drug into a 1.5% polymer solution while stirring. The MPs wer...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-009-9361-8
更新日期:2010-03-01 00:00:00
abstract::This work aimed to develop a fast-dissolving film made of low dextrose equivalent maltodextrins (MDX) containing nicotine hydrogen tartrate salt (NHT). Particular attention was given to the selection of the suitable taste-masking agent (TMA) and the characterisation of the ductility and flexibility under different mec...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-010-9525-6
更新日期:2010-12-01 00:00:00
abstract::The objective of this study was to produce microparticles of a new asthma-controlling drug by supercritical assisted atomization (SAA), proposed as an alternative to conventional jet-milling process. SAA is based on the solubilization of supercritical carbon dioxide in a liquid solution containing the drug; the ternar...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt060352
更新日期:2005-10-22 00:00:00
abstract::One-third of the population of the USA suffers from metabolic syndrome (MetS). Treatment of patients with MetS regularly includes drugs prescribed simultaneously to treat diabetes and cardiovascular diseases. Therefore, the development of novel multidrug formulations is recommended. However, the main problem with thes...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1359-2
更新日期:2019-03-18 00:00:00
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
更新日期:2019-12-10 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01660-w
更新日期:2020-03-31 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-015-0308-y
更新日期:2015-10-01 00:00:00
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journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt060241
更新日期:2005-10-06 00:00:00
abstract::The scale up of production processes is a major challenge in pharmaceutical industry. Using a quality by design approach, upscaling can be based on the design space, which can be assessed on a small scale. In a previous study, the critical process parameters were identified by a definitive screening design on cetomacr...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1063-7
更新日期:2018-07-01 00:00:00
abstract::Targeted delivery to the lung for controlling lung inflammation is an area that we have explored in this study. The purpose was to use microparticles containing an antisense oligonucleotide (ASO) to NF-κB to inhibit the production of proinflammatory cytokines. Microparticles were prepared using the B-290 Buchi Spray D...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1002-7
更新日期:2018-05-01 00:00:00
abstract::Co-encapsulation of anticancer drugs paclitaxel and imatinib in nanocarriers is a promising strategy to optimize cancer treatment. Aiming to combine the cytotoxic and antiangiogenic properties of the drugs, a liposome formulation targeted to folate receptor co-encapsulating paclitaxel and imatinib was designed in this...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0830-1
更新日期:2018-01-01 00:00:00
abstract::The aim of the present study was to investigate the use of different grades of microcrystalline cellulose (MCC) and lactose in a direct pelletization process in a rotary processor. For this purpose, a mixed 2- and 3-level factorial study was performed to determine the influence of the particle size of microcrystalline...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt060362
更新日期:2005-10-24 00:00:00
abstract::The purpose of this study was to prepare ginkgolide B (GB) lyophilized powder for injection with excellent appearance and stable quality through a formulation screening and by optimizing the freeze-drying process. Cremophor EL as a solubilizer, PEG 400 as a latent solvent, and mannitol as an excipient were mixed to in...
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::Non-invasive administration of insulin is expected for better diabetes mellitus therapy. In this report, we developed intraoral preparation for insulin. Insulin was encapsulated into nanocarrier using self-assembly emulsification process. To increase lipophilicity of insulin, it was dispersed in phospholipid resulted ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-014-0258-9
更新日期:2015-06-01 00:00:00
abstract::The approach documented in this article reviews data from earlier process validation lifecycle stages with a described statistical model to provide the "best estimate" on the number of process performance qualification (PPQ) batches that should generate sufficient information to make a scientific and risk-based decisi...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-015-0409-7
更新日期:2016-08-01 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