Abstract：
:Polymeric films are safe and effective and can be used for vaginal administration of microbicide drug candidates. Dapivirine (DPV), an investigational and clinically advanced antiretroviral drug, was selected as a model compound for this study. We have previously developed and clinically tested a quick-dissolving DPV film using solvent cast (SC) manufacturing technique. As an alternative to current pharmaceutical film manufacturing techniques, we investigated hot melt extrusion (HME) process in this study because it has several benefits, including its capacity as a continuous manufacturing process, lack of solvents, smaller footprint, and ease of scalability. The goal of this work was to evaluate the feasibility of using HME for DPV vaginal film manufacturing and to develop a robust manufacturing process using HME by evaluating the effect of process parameters on film quality and performance. DPV was successfully incorporated into a vaginal film using HME and maintained acceptable characteristics. Three process parameters (zone temperature, screw speed, and feed rate) had an impact on film quality and performance. Of these, the zone temperature was found to most significantly affect weight, thickness, puncture strength, and dissolution of films. Additionally, film manufacturing using HME was highly reproducible. Finally, the DPV HME film was comparable to films manufactured using SC in terms of physicochemical, biological, and safety characteristics including in vitro drug release, mechanical strength, tissue permeability, compatibility with commensal vaginal Lactobacilli, and in vitro bioactivity. These results demonstrate that HME is an effective, robust, and viable manufacturing method to produce vaginal films.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Regev G,Patel SK,Moncla BJ,Twist J,Devlin B,Rohan LCdoi
10.1208/s12249-019-1442-8subject
Has Abstractpub_date
2019-06-26 00:00:00pages
239issue
6issn
1530-9932pii
10.1208/s12249-019-1442-8journal_volume
20pub_type
杂志文章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
abstract：:The purpose of this paper is to describe results from the use of a set of Excel macros written to facilitate the comparison of image analysis (IA) and laser diffraction (LD) particle size analysis (psa) data. Measurements were made on particle systems of differing morphological characteristics including differing aver...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt070369
更新日期：2006-08-18 00:00:00
abstract：:In this study, the use of trimethylchitosan (TMC), by higher solubility in comparison with chitosan, in alginate/chitosan nanoparticles containing cationic β-cyclodextrin polymers (CPβCDs) has been studied, with the aim of increasing insulin uptake by nanoparticles. Firstly, TMCs were synthesized by iodomethane, and C...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0282-9
更新日期：2015-08-01 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：:Spheroid formation mechanisms were investigated using extrusion-spheronization (ES) and rotary processing (RP). Using ES (cross-hatch), ES (teardrop), and RP (teardrop), spheroids with similar mass median diameter (MMD) and span were produced using equivalent formulation and spheronization conditions. During spheroniz...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt0801010
更新日期：2007-02-09 00:00:00
abstract：:Development of palatable formulations for pediatric and geriatric patients involves various challenges. However, an innovative development with beneficial characteristics of marketed formulations in a single formulation platform was attempted. The goal of this research was to develop solid oral flexible tablets (OFTs)...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-016-0666-0
更新日期：2017-08-01 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：: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 purpose of this research was to explore the utility of beta cyclodextrin (betaCD) and beta cyclodextrin derivatives (hydroxypropyl-beta-cyclodextrin [HPbetaCD], sulfobutylether-beta-CD [SBbetaCD], and a randomly methylated-beta-CD [RMbetaCD]) to form inclusion complexes with the antitumoral drug, beta-lapachone (b...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt0803060
更新日期：2007-07-27 00:00:00
abstract：:The purpose of this research was to investigate the measurement and in vitro delivery implications of multimodal distributions, occurring near or in the respirable range, emitted from pressurized metered-dose inhalers (pMDIs). Particle size distributions of solution pMDIs containing hydrofluoroalkane-134a (HFA-134a) a...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt040338
更新日期：2003-01-01 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 aim of this study was to introduce smectite clay matrices as a drug delivery carrier for the development of amorphous solid dispersions (ASD). Indomethacin (IND) was processed with two different smectite clays, magnesium aluminium and lithium magnesium sodium silicates, using hot melt extrusion (HME) to prepare so...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01813-x
更新日期：2020-10-08 00:00:00
abstract：:Drug delivery to deep-seated tissues such as bone has been a major complication till date. This preferential drug delivery is further important in targeting anti-tumour agents to bone metastasis owing to its complexity. The present study involves the formulation of PLGA nanoparticles and conjugation with zolendronic a...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-016-0691-z
更新日期：2017-08-01 00:00:00
abstract：:This work combines several methods in an integrated strategy to develop a matrix for buccal administration. For this purpose, tablets containing selected mucoadhesive polymers loaded with a model drug (omeprazole), free or in a complexed form with cyclodextrins, and in the absence and presence of alkali agents were su...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-010-9546-1
更新日期：2010-12-01 00:00:00
abstract：:Solid dispersion is one of the most effective ways to improve the dissolution of insoluble drugs. When the carrier can highly disperse the drug, it will increase the wettability of the drug and reduce the surface tension, thus improving the solubility, dissolution, and bioavailability. However, amorphous solid dispers...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-020-01802-0
更新日期：2020-09-25 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：:Incorporation of drug-loaded nanoparticles into swellable and respirable microparticles is a promising strategy to avoid rapid clearance from the lung and achieve sustained drug release. In this investigation, a copolymer of polyethylene glycol grafted onto phthaloyl chitosan (PEG-g-PHCs) was synthesized and then self...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0176-x
更新日期：2014-12-01 00:00:00
abstract：:Top-spray fluidized bed granulation with axial fluidization airflow from the bottom of the granulator is well-established in the pharmaceutical industry. The application of swirling airflow for fluidized bed granulation was more recently introduced. This study examined the effects of various process parameters on the ...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-012-9906-0
更新日期：2013-03-01 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 objective of the study was to investigate in vitro transdermal delivery of venlafaxine hydrochloride across the pigskin by passive diffusion and iontophoresis. For passive diffusion, experiments were carried out in Franz diffusion cell whereas for iontophoretic permeation, the diffusion cell was modified to contai...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-008-9111-3
更新日期：2008-01-01 00:00:00
abstract：:The second author's name was incorrectly published as "Niha F. Younes". The correct name is "Nihal Farid Younes" as shown above in the list of authors. ...
journal_title：AAPS PharmSciTech
pub_type： 已发布勘误
doi：10.1208/s12249-019-1321-3
更新日期：2019-02-25 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
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
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：: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
abstract：:Herein, we report the successful development of a novel nanosystem capable of an efficient delivery and temperature-triggered drug release specifically aimed at cancer. The water-soluble 130.1 ± 0.2 nm iron oxide nanoparticles (IONPs) were obtained via synthesis of a monodispersed iron oxide core stabilized with tetra...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-014-0131-x
更新日期：2014-08-01 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：:The purpose of this research was to design and develop hydrogels by esterification of polyvinyl alcohol (PVA) with gelatin. The membranes were characterized by Fourier Transform Infrared (FTIR) spectroscopy, x-ray diffraction (XRD), and differential scanning calorimetry. The viscosity of the esterified product (as sol...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/pt080121
更新日期：2007-03-16 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：:Amylin is a pancreatic hormone that plays important roles in overall metabolism and in glucose homeostasis. The therapeutic restoration of postprandial and basal amylin levels is highly desirable for patients with diabetes who need to avoid glucose excursions. Protein conjugation with polyethylene glycol (PEG) has lon...
journal_title：AAPS PharmSciTech
pub_type： 杂志文章
doi：10.1208/s12249-013-9987-4
更新日期：2013-09-01 00:00:00
