Abstract:
:AR-12 is a novel small molecule with broad spectrum antifungal activity. Recently, AR-12 was found to be highly active against Trichophyton rubrum, one of the predominantly responsible organisms that cause onychomycosis. The primary objective of this project was to investigate the ability of AR-12 to penetrate into and across the human nail plate followed by improving its trans-ungual permeation using different penetration enhancers. TranScreen-N™, a high throughput screening method was utilized to explore the potential nail penetration enhancers to facilitate the drug delivery through the nail. This screen demonstrated that dexpanthenol and PEG 400 were the most efficient enhancers. The in vitro permeation studies were performed across the human cadaver nail plates for 7 days with three AR-12 (5% w/v) formulations containing 10% w/v dexpanthenol (Formulation A), 10% w/v PEG 400 (Formulation B), and a combination of 10% w/v dexpanthenol + 10% w/v PEG 400 (Formulation C). The in vitro studies concluded that dexpanthenol and PEG 400 were able to deliver a significant amount of AR-12 into and across the nail plate that was found to be more than MIC 50 level of the drug.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Kushwaha AS,Sharma P,Shivakumar HN,Rappleye C,Zukiwski A,Proniuk S,Murthy SNdoi
10.1208/s12249-017-0752-ysubject
Has Abstractpub_date
2017-10-01 00:00:00pages
2702-2705issue
7issn
1530-9932pii
10.1208/s12249-017-0752-yjournal_volume
18pub_type
杂志文章abstract::The effect of milled and micronized lactose fines on the fluidization and in vitro aerosolization properties of dry powder inhaler (DPI) formulations was investigated, and the suitability of static and dynamic methods for characterizing general powder flow properties of these blends was assessed. Lactose carrier pre-b...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-014-0119-6
更新日期:2014-08-01 00:00:00
abstract::The exudates from the incised trunk of Terminalia randii has been evaluated as controlled release excipient in comparison with xanthan gum and hydroxypropylmethylcellulose (HPMC) using carvedilol (water insoluble) and theophylline (water soluble) as model drugs. Matrix tablets were prepared by direct compression and t...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-011-9712-0
更新日期:2012-03-01 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::Intra-periodontal pocket drug delivery systems, such as liquid crystalline systems, are widely utilized improving the drug release control and the therapy. Propolis is used in the treatment of periodontal diseases, reducing the inflammatory and infectious conditions. Iron oxide magnetic nanoparticles (MNPs) can improv...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1163-4
更新日期:2018-10-01 00:00:00
abstract::Lipid nanoparticles based on solid matrix have emerged as potential drug carriers to improve gastrointestinal (GI) absorption and oral bioavailability of several drugs, especially lipophilic compounds. These formulations may also be used for sustained drug release. Solid lipid nanoparticle (SLN) and the newer generati...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-010-9563-0
更新日期:2011-03-01 00:00:00
abstract::Griseofulvin, an antifungal agent, is a BCS class II drug slowly, erratically, and incompletely absorbed from the gastrointestinal tract in humans. The clinical failure of the conventional oral therapy of griseofulvin is most likely attributed to its poor solubility and appreciable inter- and intra-subject variation i...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,随机对照试验
doi:10.1208/s12249-011-9722-y
更新日期:2012-03-01 00:00:00
abstract::An acid-buffering bioadhesive vaginal tablet was developed for the treatment of genitourinary tract infections. From the bioadhesion experiment and release studies it was found that polycarbophil and sodium carboxymethylcellulose is a good combination for an acid-buffering bioadhesive vaginal tablet. Sodium monocitrat...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt0804109
更新日期:2007-12-14 00:00:00
abstract::Transcutaneous immunization using a microneedle device presents a promising alternative to syringe-based injection of vaccines. The aim of this study was to investigate the effective immune response elicited after application of tetanus toxoid antigen-loaded dissolvable microneedles (TT-MN) in mice model. Dissolvable ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1471-3
更新日期:2019-07-22 00:00:00
abstract::A feasibility evaluation of the addition of fumed silica (SiO2) into an agitated dryer to aid spray-dried solid dispersion intermediate (SDSDi) flow during secondary drying and discharge is described. The quantity of SiO2 to enhance the flow character of SDSDi was assessed by measuring particle size distribution, bulk...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1392-1
更新日期:2019-05-03 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 aim of the present study was to develop and evaluate a buccal adhesive tablet containing ondansetron hydrochloride (OH). Special punches and dies were fabricated and used while preparing buccal adhesive tablets. The tablets were prepared using carbopol (CP 934), sodium alginate, sodium carboxymethylcellulose low v...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-009-9304-4
更新日期:2009-01-01 00:00:00
abstract::Direct pulmonary delivery is a promising step in developing effective gene therapies for respiratory disease. Gene therapies can be used to treat the root cause of diseases, rather than just the symptoms. However, developing effective therapies that do not cause toxicity and that successfully reach the target site at ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1215-9
更新日期:2019-01-02 00:00:00
abstract::The impact of pharmaceutical materials properties on drug product quality and manufacturability is well recognised by the industry. An ongoing effort across industry and academia, the Manufacturing Classification System consortium, aims to gather the existing body of knowledge in a common framework to provide guidance...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-018-1198-6
更新日期:2018-11-01 00:00:00
abstract::Hydroxypropyl methylcellulose (HPMC) tablets containing nicotine-magnesium aluminum silicate (NCT-MAS) complex particles and pH modifiers, namely, sodium chloride, citric acid, and magnesium hydroxide, were prepared using the direct compression method. The effects of HPMC viscosity grades and pH modifiers on NCT relea...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-012-9790-7
更新日期:2012-06-01 00:00:00
abstract::Bimatoprost is widely used for the management of glaucoma. Currently, it is delivered via eye drop solution, which is highly inefficient due to low bioavailability. To control the release of ocular drugs, contact lenses are used by scientists. However, the conventional soaking method showed high burst release due to a...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-1622-6
更新日期:2020-01-13 00:00:00
abstract::In a systematic effort to develop a dual-function intravaginal spermicide as well as a drug delivery vehicle against sexually transmitted pathogens, a submicron particle size (30-80 nm), lipophilic and spermicidal gel-microemulsion (viz GM-144) containing the pharmaceutical excipients propylene glycol, Captex 300, Cre...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt020205
更新日期:2001-04-09 00:00:00
abstract::The aim of this study was to identify trends in deficiencies raised during the EU evaluation of the quality part of dossiers for marketing authorisation applications of biosimilar medicinal products. All adopted day 120 list of questions on the quality module of 22 marketing authorisation applications for biosimilars ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0892-0
更新日期:2018-02-01 00:00:00
abstract::Pharmaceutical excipients contain reactive groups and impurities due to manufacturing processes that can cause decomposition of active drug compounds. The aim of this investigation was to determine if commercially available oral disintegrating tablet (ODT) platforms induce active pharmaceutical ingredient (API) degrad...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-0015-5
更新日期:2013-12-01 00:00:00
abstract::The purpose of this study was to develop and validate a rapid, sensitive, and specific reversed-phase high-performance liquid chromatography method for the quantitative determination of native tenofovir (TNF) for various applications. Different analytical performance parameters such as linearity, precision, accuracy, ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-011-9735-6
更新日期:2012-03-01 00:00:00
abstract::Transdermal drug delivery is an emerging field in the pharmaceutical remit compared with conventional methods (oral and parenteral). Microneedle (MN)-based devices have gained significant interest as a strategy to overcome the skin's formidable barrier: the stratum corneum. This approach provides a less invasive, more...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-019-1560-3
更新日期:2019-12-05 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::Low solubility of active pharmaceutical compounds (APIs) remains an important challenge in dosage form development process. In the manuscript, empirical models were developed and analyzed in order to predict dissolution of bicalutamide (BCL) from solid dispersion with various carriers. BCL was chosen as an example of ...
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
abstract::The performance of dioctyl sodium sulfosuccinate (aerosol OT) in the development of a pharmaceutically acceptable, stable, self-emulsifying water continuous microemulsion with high dilution efficiency was assessed. A pseudoternary microemulsion system was constructed using aerosol OT/medium-chain triglycerides with ol...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt040111
更新日期:2003-01-01 00:00:00
abstract::Chemical penetration enhancers (CPEs) are frequently incorporated into transdermal delivery systems (TDSs) to improve drug delivery and to reduce the required drug load in formulations. However, the minimum detectable effect of formulation changes to CPE-containing TDSs using in vitro permeation tests (IVPT), a widely...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1130-0
更新日期:2018-10-01 00:00:00
abstract::The hydrophobicity of bioactive molecules poses a considerable problem in the pharmaceutical and the food industry. Using food-based protein nanocarriers is one promising way to deliver hydrophobic molecules. These types of protein possess many functional properties such as surface activity, water-binding capacity, em...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-020-01641-z
更新日期:2020-03-09 00:00:00
abstract::The stability of the 37-amino acid peptide pramlintide, in aqueous solution, was studied as a function of pH and temperature. Samples of pramlintide formulated as a parenteral product were exposed to elevated temperatures and to realistic storage conditions for as long as 30 months. Pramlintide degradation was monitor...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt010207
更新日期:2000-03-18 00:00:00
abstract::The aim of this work was to test innovative approach for enhancing ascorbyl palmitate stability in microemulsions for topical application by addition of newly synthesized co-antioxidant 4-(tridecyloxy)benzaldehyde oxime (TDBO) and to investigate its antioxidant activity and finally to evaluate cytotoxicity of TDBO-loa...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-010-9507-8
更新日期:2010-09-01 00:00:00
abstract::The aim of this study was to compare the densification of powder mixtures on eccentric and rotary tablet presses and to establish relationships with the halving properties of the resulting scored tablets. This is an important problem because the recent guidelines of EU require verification of the equal masses of table...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-009-9225-2
更新日期:2009-01-01 00:00:00
abstract::Pentoxifylline (PTX), an anti-hemorrhage drug used in the treatment of intermittent claudication, is extensively metabolized by the liver resulting in a reduction of the therapeutic levels within a short duration of time. Self-nano-emulsifying drug delivery system (SNEDDS) is well reported to enhance the bio-absorptio...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01644-w
更新日期:2020-04-21 00:00:00
abstract::The objective of this study was to design a time-controlled pulsatile release (TCPR) system containing propranolol (PNH) as an active pharmaceutical ingredient. Here, the developed dosage forms were coated with hydroxypropyl-methylcellulose (HPMC) and other excipients as barrier layer using dry-coated technology. The ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0746-9
更新日期:2017-10-01 00:00:00