Percutaneous Delivery of Antihypertensive Agents: Advances and Challenges.

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 PharmSciTech

journal_title

AAPS PharmSciTech

authors

Ita K,Ashong S

doi

10.1208/s12249-019-1583-9

subject

Has Abstract

pub_date

2020-01-06 00:00:00

pages

56

issue

2

issn

1530-9932

pii

10.1208/s12249-019-1583-9

journal_volume

21

pub_type

杂志文章,评审
  • The Influence of Simulated Fasted Gastrointestinal pH Profiles on Diclofenac Sodium Dissolution in a Glass-Bead Flow-Through System.

    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

    authors: Felicijan T,Pišlar M,Vene K,Bogataj M

    更新日期:2018-10-01 00:00:00

  • To Evaluate the Effect of Solvents and Different Relative Humidity Conditions on Thermal and Rheological Properties of Microcrystalline Cellulose 101 Using METHOCEL™ E15LV as a Binder.

    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

    authors: Jagia M,Trivedi M,Dave RH

    更新日期:2016-08-01 00:00:00

  • Pharmaceutical and pharmacokinetic evaluation of a novel fast dissolving film formulation of flupentixol dihydrochloride.

    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

    authors: Abdelbary A,Bendas ER,Ramadan AA,Mostafa DA

    更新日期:2014-12-01 00:00:00

  • Effect of hydrophilic polymers on buccoadhesive Eudragit patches of propranolol hydrochloride using factorial design.

    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

    authors: Patel VM,Prajapati BG,Patel MM

    更新日期:2007-06-22 00:00:00

  • Development and characterization of sorbitan monostearate and sesame oil-based organogels for topical delivery of antimicrobials.

    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

    authors: Singh VK,Pramanik K,Ray SS,Pal K

    更新日期:2015-04-01 00:00:00

  • Preparation and In Vitro-In Vivo Evaluation of Sustained-Release Matrix Pellets of Capsaicin to Enhance the Oral Bioavailability.

    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

    authors: Zhang Y,Huang Z,Omari-Siaw E,Lu S,Zhu Y,Jiang D,Wang M,Yu J,Xu X,Zhang W

    更新日期:2016-04-01 00:00:00

  • Chitosan gels for the vaginal delivery of lactic acid: relevance of formulation parameters to mucoadhesion and release mechanisms.

    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

    authors: Bonferoni MC,Giunchedi P,Scalia S,Rossi S,Sandri G,Caramella C

    更新日期:2006-01-01 00:00:00

  • Estimating the number of droplets and drug particles emitted from MDIs.

    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

    authors: Stein SW

    更新日期:2008-01-01 00:00:00

  • Whey protein/polysaccharide-stabilized emulsions: Effect of polymer type and pH on release and topical delivery of salicylic acid.

    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

    authors: Combrinck J,Otto A,du Plessis J

    更新日期:2014-06-01 00:00:00

  • Stability of a second-generation cephalosporin veterinary mastitis formulation after electron beam irradiation.

    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

    authors: Johns PJ,Turberg M,Willard K,Matagne D,Cheesman D

    更新日期:2001-11-19 00:00:00

  • Antiangiogenic activity of sterically stabilized liposomes containing paclitaxel (SSL-PTX): in vitro and in vivo.

    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

    authors: Huang Y,Chen XM,Zhao BX,Ke XY,Zhao BJ,Zhao X,Wang Y,Zhang X,Zhang Q

    更新日期:2010-06-01 00:00:00

  • Sustained Release of Poorly Water-Soluble Drug from Hydrophilic Polymeric Film Sandwiched Between Hydrophobic Layers.

    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

    authors: Kevadiya BD,Zhang L,Davé RN

    更新日期:2018-08-01 00:00:00

  • Assessment Methodology for Process Validation Lifecycle Stage 3A.

    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

    authors: Sayeed-Desta N,Pazhayattil AB,Collins J,Chen S,Ingram M,Spes J

    更新日期:2017-07-01 00:00:00

  • Studies on mefenamic acid microparticles: formulation, in vitro release, and in situ studies in rats.

    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

    authors: Sevgi F,Yurdasiper A,Kaynarsoy B,Turunç E,Güneri T,Yalçin A

    更新日期:2009-01-01 00:00:00

  • Formulation and release behavior of doxycycline-alginate hydrogel microparticles embedded into pluronic F127 thermogels as a potential new vehicle for doxycycline intradermal sustained delivery.

    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

    authors: Giovagnoli S,Tsai T,DeLuca PP

    更新日期:2010-03-01 00:00:00

  • Nicotine fast dissolving films made of maltodextrins: a feasibility study.

    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

    authors: Cilurzo F,Cupone IE,Minghetti P,Buratti S,Selmin F,Gennari CG,Montanari L

    更新日期:2010-12-01 00:00:00

  • Supercritical assisted atomization: a novel technology for microparticles preparation of an asthma-controlling drug.

    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

    authors: Della Porta G,De Vittori C,Reverchon E

    更新日期:2005-10-22 00:00:00

  • Highly Soluble Glimepiride and Irbesartan Co-amorphous Formulation with Potential Application in Combination Therapy.

    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

    authors: Cruz-Angeles J,Videa M,Martínez LM

    更新日期:2019-03-18 00:00:00

  • Chronological Delivery of Antihypertensive Drugs in Bilayered Core-in-Cup Buccoadhesive Tablets: In Vitro and In Vivo Evaluation.

    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

    authors: Rashad AA,Nageeb El-Helaly S,Abd El Rehim RT,El-Gazayerly ON

    更新日期:2019-12-10 00:00:00

  • Data-Driven Modeling of the Bicalutamide Dissolution from Powder Systems.

    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

    authors: Mendyk A,Pacławski A,Szafraniec-Szczęsny J,Antosik A,Jamróz W,Paluch M,Jachowicz R

    更新日期:2020-03-31 00:00:00

  • Exploring Microstructural Changes in Structural Analogues of Ibuprofen-Hosted In Situ Gelling System and Its Influence on Pharmaceutical Performance.

    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

    authors: Patil SS,Venugopal E,Bhat S,Mahadik KR,Paradkar AR

    更新日期:2015-10-01 00:00:00

  • Excipient selection can significantly affect solid-state phase transformation in formulation during wet granulation.

    abstract::Phase transformations in formulations can lead to instability in physicochemical, biopharmaceutical, and processing properties of products. The influences of formulation design on the optimal dosage forms should be specified. The aim here was to investigate whether excipients with different water sorption behavior aff...

    journal_title:AAPS PharmSciTech

    pub_type: 杂志文章

    doi:10.1208/pt060241

    authors: Airaksinen S,Karjalainen M,Kivikero N,Westermarck S,Shevchenko A,Rantanen J,Yliruusi J

    更新日期:2005-10-06 00:00:00

  • Scale up of Semisolid Dosage Forms Manufacturing Based on Process Understanding: from Lab to Industrial Scale.

    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

    authors: van Heugten AJP,Vromans H

    更新日期:2018-07-01 00:00:00

  • Pulmonary Administration of Microparticulate Antisense Oligonucleotide (ASO) for the Treatment of Lung Inflammation.

    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

    authors: Ubale RV,Shastri PN,Oettinger C,D'Souza MJ

    更新日期:2018-05-01 00:00:00

  • Antiproliferative Activity and VEGF Expression Reduction in MCF7 and PC-3 Cancer Cells by Paclitaxel and Imatinib Co-encapsulation in Folate-Targeted Liposomes.

    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

    authors: Peres-Filho MJ,Dos Santos AP,Nascimento TL,de Ávila RI,Ferreira FS,Valadares MC,Lima EM

    更新日期:2018-01-01 00:00:00

  • Direct pelletization in a rotary processor controlled by torque measurements. III. Investigation of microcrystalline cellulose and lactose grade.

    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

    authors: Kristensen J

    更新日期:2005-10-24 00:00:00

  • Formulation Screening and Freeze-Drying Process Optimization of Ginkgolide B Lyophilized Powder for Injection.

    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

    authors: Liu D,Galvanin F,Yu Y

    更新日期:2018-02-01 00:00:00

  • Intraoral film containing insulin-phospholipid microemulsion: formulation and in vivo hypoglycemic activity study.

    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

    authors: Rachmawati H,Haryadi BM,Anggadiredja K,Suendo V

    更新日期:2015-06-01 00:00:00

  • Stage 2 Process Performance Qualification (PPQ): a Scientific Approach to Determine the Number of PPQ Batches.

    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

    authors: Pazhayattil A,Alsmeyer D,Chen S,Hye M,Ingram M,Sanghvi P

    更新日期:2016-08-01 00:00:00

  • Validation of a new 96-well plate spectrophotometric method for the quantification of compound 48/80 associated with particles.

    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

    authors: Bento D,Borchard G,Gonçalves T,Borges O

    更新日期:2013-06-01 00:00:00