Abstract:
:Colorectal cancer is a global concern, and its treatment is fraught with non-selective effects including adverse side effects requiring hospital visits and palliative care. A relatively safe drug formulated in a bioavailability enhancing and targeting delivery platform will be of significance. Metformin-loaded solid lipid nanoparticles (SLN) were designed, optimized, and characterized for particle size, zeta potential, drug entrapment, structure, crystallinity, thermal behavior, morphology, and drug release. Optimized SLN were 195.01 ± 6.03 nm in size, -17.08 ± 0.95 mV with regard to surface charge, fibrous in shape, largely amorphous, and release of metformin was controlled. The optimized size, charge, and shape suggest the solid lipid nanoparticles will migrate and accumulate in the colon tumor preventing its proliferation and subsequently leading to tumor shrinkage and cell death.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Ngwuluka NC,Kotak DJ,Devarajan PVdoi
10.1208/s12249-016-0505-3subject
Has Abstractpub_date
2017-02-01 00:00:00pages
358-368issue
2issn
1530-9932pii
10.1208/s12249-016-0505-3journal_volume
18pub_type
杂志文章abstract::The present work explores inner structuration of in situ gelling system consisting of glyceryl monooleate (GMO) and oleic acid (OA). The system under study involves investigation of microstructural changes which are believed to govern the pharmaceutical performance of final formulation. The changes which are often ter...
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
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 an...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0752-y
更新日期:2017-10-01 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::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::A novel polymer-drug conjugate, polyethylene glycol-N-(acetyl)-glucosamine-doxorubicin (PEG-NAG-DOX) was evaluated in this study for its in vivo potential for treatment of tumours demonstrating improved efficacy and reduced toxicity. The proposed polymer-drug conjugate comprised of polyethylene glycol-maleimide (mPEG-...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0787-0
更新日期:2017-11-01 00:00:00
abstract::Use of higher tableting speeds is gaining increasing importance for pharmaceutical industry. There is a profound lack of new studies of mechanical properties of hypromellose, and none of them evaluate different suppliers. Thus, the objective of this study was to investigate flow and compaction properties of different ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01688-y
更新日期:2020-07-22 00:00:00
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 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 present work was undertaken with the objectives of improving the dissolution velocity, related oral bioavailability, and minimizing the fasted/fed state variability of repaglinide, a poorly water-soluble anti-diabetic active by exploring the principles of nanotechnology. Nanocrystal formulations were prepared by b...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-014-0267-8
更新日期:2015-08-01 00:00:00
abstract:PURPOSE:To develop a novel nanoparticle drug delivery system consisting of chitosan and glyceryl monooleate (GMO) for the delivery of a wide variety of therapeutics including paclitaxel. METHODS:Chitosan/GMO nanoparticles were prepared by multiple emulsion (o/w/o) solvent evaporation methods. Particle size and surface...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-008-9063-7
更新日期:2008-01-01 00:00:00
abstract::The main principles of green chemistry and engineering were extended to pharmaceutical formulations to prepare eco-friendly surfactant-free dry emulsion tablets (SFDETs) devoid of solvents or synthetic surfactants. Surfactant-free emulsions were stabilized by in situ cyclodextrins/sweet almond oil inclusion complexes ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1450-8
更新日期:2019-07-18 00:00:00
abstract::Cancerous invasion yields unusual metabolisms providing a significant amount of peptide albuminomes that modulate albumin stability via binding. The study aimed at the investigation of the thermal stability of human plasma albumin with breast cancer of various stages by means of differential scanning calorimetry (DSC)...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1356-5
更新日期:2019-03-18 00:00:00
abstract::In this paper, linkages between tablet surface roughness, tablet compression forces, material properties, and the tensile strength of tablets were studied. Pure sodium halides (NaF, NaBr, NaCl, and NaI) were chosen as model substances because of their simple and similar structure. Based on the data available in the li...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-014-0104-0
更新日期:2014-06-01 00:00:00
abstract::The objective of this study was to prepare and evaluate terbutaline sulphate (TBS) bi-layer tablets for once-daily administration. The bi-layer tablets consisted of an immediate-release layer and a sustained-release layer containing 5 and 10 mg TBS, respectively. The sustained-release layer was developed by using Comp...
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::A dissolution test for tablets containing 40 mg of olmesartan medoxomil (OLM) was developed and validated using both LC-UV and UV methods. After evaluation of the sink condition, dissolution medium, and stability of the drug, the method was validated using USP apparatus 2, 50 rpm rotation speed, and 900 ml of deaerate...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-010-9421-0
更新日期:2010-06-01 00:00:00
abstract::The purpose of this research was to use inline real-time near-infrared (NIR) to measure the moisture content of granules manufactured using a commercial production scale continuous twin-screw granulator fluid-bed dryer milling process. A central composite response surface statistical design was used to study the effec...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-011-9669-z
更新日期:2011-12-01 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::Celecoxib (CXB) is a poorly aqueous solubility sulfonamide non-steroidal anti-inflammatory drug (NSAID). Hence, the formulation of CXB was selected for solubilization and bioavailability. To find out suitable formulation for microemulsion, the solubility of CXB in triacetin (oil phase), Tween 80 (surfactant), and Tran...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-016-0667-z
更新日期:2017-08-01 00:00:00
abstract::Establishing bioequivalence (BE) of drugs indicated to treat cancer poses special challenges. For ethical reasons, often, the studies need to be conducted in cancer patients rather than in healthy volunteers, especially when the drug is cytotoxic. The Biopharmaceutics Classification System (BCS) introduced by Amidon (...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-014-0195-7
更新日期:2015-02-01 00:00:00
abstract::A combination of analytical and statistical methods is used to improve a tablet coating process guided by quality by design (QbD) principles. A solid dosage form product was found to intermittently exhibit bad taste. A suspected cause was the variability in coating thickness which could lead to the subject tasting the...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-011-9723-x
更新日期:2012-03-01 00:00:00
abstract::The aim of the present study was to develop a spilanthol emulsion and investigate the effect of oil and drug physicochemical properties on drug release and skin retention at molecular level. Formulation factors including oil, emulsifier, and humectant were investigated by in vitro skin retention/permeation study and t...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1454-4
更新日期:2019-06-20 00:00:00
abstract::The objectives of this study are to enhance cellular accumulation of gemcitabine with chitosan/glyceryl monooleate (GMO) nanostructures, and to provide significant increase in cell death of human pancreatic cancer cells in vitro. The delivery system was prepared by a multiple emulsion solvent evaporation method. The n...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-010-9393-0
更新日期:2010-03-01 00:00:00
abstract::For polymer-based controlled release drug products (e.g. microspheres and implants), active pharmaceutical ingredient distribution and microporosity inside the polymer matrix are critical for product performance, particularly drug release kinetics. Due to the decreasing domain size and increasing complexity of such pr...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01741-w
更新日期:2020-07-14 00:00:00
abstract::Posaconazole is a triazole antifungal drug that with extremely poor aqueous solubility. Up to now, this drug can be administered via intravenous injection and oral suspension. However, its oral bioavailability is greatly limited by the dissolution rate of the drug. This study aimed to improve water solubility and diss...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-016-0497-z
更新日期:2017-01-01 00:00:00
abstract::The objective of the present study was to investigate the effects of processing variables and formulation factors on the characteristics of hot-melt extrudates containing a copolymer (Kollidon® VA 64). Nifedipine was used as a model drug in all of the extrudates. Differential scanning calorimetry (DSC) was utilized on...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-014-0226-4
更新日期:2015-04-01 00:00:00
abstract::The purpose of this research was to develop and evaluate different preparations of sustained delivery systems, using Carbopols as carriers, in the form of matrices and three-layer tablets with isosorbite mononitrate. Matrix tablets were prepared by direct compression whereas three-layer tablets were prepared by compre...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-008-9084-2
更新日期:2008-01-01 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::While polyethylene oxide (PEO)-based matrix tablets are frequently used as abuse-deterrent dosage forms, there is limited information available regarding how the selection of formulation components and manufacturing processes affect the resulting abuse-deterrent properties. The objective of the current study was to ev...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1565-y
更新日期:2019-12-19 00:00:00
abstract::The aim of this study was to apply quality by design (QbD) for pharmaceutical development of felodipine solid mixture (FSM) containing hydrophilic carriers and/or polymeric surfactants, for easier development of controlled-release tablets of felodipine. The material attributes, the process parameters (CPP), and the cr...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-011-9646-6
更新日期:2011-09-01 00:00:00
abstract::To ensure consistency of clinical outcomes, orally inhaled therapies must exhibit consistent delivered dose and aerosol properties at the time of manufacturing, throughout storage, and during various patient-use conditions. Achieving consistency across these scenarios has presented a significant challenge, especially ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0891-1
更新日期:2018-02-01 00:00:00