Drug delivery

Comparison of In Vitro Corneal Permeation and In Vivo Ocular Bioavailability in Rabbits of Three Marketed Latanoprost Formulations

Background and Objective: All latanoprost formulations currently available for the treatment of glaucoma or ocular hypertension contain the same concentration of latanoprost (0.005%) but differ in excipients, which may affect corneal drug permeability or stability. This study aimed at comparing corneal penetration of three marketed latanoprost solutions with different excipient formulations in in vitro and […]

Mucoadhesive chitosan-poly (lactic-co-glycolic acid) nanoparticles for intranasal delivery of quetiapine – Development & characterization in physiologically relevant 3D tissue models

Quetiapine hemifumarate (QF) delivery to the CNS via conventional formulations is challenging due to poor solubility and lower oral bioavailability (9 %). Similarly, many other second-generation antipsychotics, such as olanzapine, clozapine, and paliperidone, have also shown low oral bioavailability of <50 %. Hence, the present work was intended to formulate QF-loaded biodegradable PLGA-NPs with appropriate […]

Kinetic conversion of BIOGF1K enriched in compound K from in vitro 3-D human tissue model

The purposes of current study were to investigate the effect of ginsenosides from BIOGF1K enriched in compound K (CK) and compound Y (CY) on the skin barrier function, the deposition in in vitro 3-D human tissue model (EpiDermFT™ Full Thickness 400), and to identify and quantify kinetic bioconversion of the ginsenosides in artificial skin by utilizing the […]

Investigating the sonophoresis effect on the permeation of diclofenac sodium using 3D skin equivalent

Ultrasound temporally increases skin permeability by altering stratum corneum SC function (sonophoresis). The objective of this study was to evaluate the effect of variable ultrasound conditions on the permeation of diclofenac sodium DS with range of physicochemical properties through EpiDerm™. Permeation studies were carried out in vitro using Franz diffusion cell. HPLC method was used […]

Expression and Function of ABC Transporters in Human Alveolar Epithelial Cells

ATP-binding cassette (ABC) transporters are a large superfamily of membrane transporters that facilitate the translocation of different substrates. While ABC transporters are clearly expressed in various tumor cells where they can play a role in drug extrusion, the presence of these transporters in normal lung tissues is still controversial. Here, we performed an analysis of […]

Organic Cation Transporters (OCTs/OCTNs) in Human Primary Alveolar Epithelial Cells

Alveolar epithelium, besides exerting a key role in gas exchange and surfactant production, plays important functions in host defense and inflammation. Pathological conditions associated to alveolar dysfunction include Acute Respiratory Distress Syndrome (ARDS), asthma, chronic obstructive pulmonary disease (COPD) and idiopathic pulmonary fibrosis (IPF).The use of predictive in vitro models of human alveolar epithelium is […]

Evaluation of Clay-Functionalized Wafers and Films for Nicotine Replacement Therapy via Buccal Mucosa

The functional physicochemical properties of nicotine (NIC)-loaded composite freeze-dried wafers and solvent-evaporated films comprising hydroxypropylmethylcellulose (HPMC) and sodium alginate (SA), stabilized with magnesium aluminium silicate (MAS), have been reported. The formulations were characterized for swelling capacity, mucoadhesion, in vitro drug dissolution properties in simulated saliva (SS) and PBS at pH 6.8, and ex vivo and […]

A series of in vitro and human studies of a novel lip cream formulation for protecting against environmental triggers of recurrent herpes labialis

Purpose: These studies describe the testing of a novel, daily-use lip cream designed for individuals with lips prone to recurrent herpes labialis (RHL) that protects against environmental triggers. Subjects and methods: In vitro occlusive and in vitro and in vivo photoprotection analyses, a characterization of normal vs dry lips, and a randomized, evaluator-blinded, clinical trial […]

Nintedanib-Cyclodextrin Complex to Improve Bio-Activity and Intestinal Permeability

Cyclodextrin complex of nintedanib was prepared aiming for increased bio-activity and improved transport across intestinal membrane with reduced p-glycoprotein (p-gp) efflux. Based on preliminary phase solubility studies and molecular modeling, sulfobutyl ether derivative of β-cyclodextrin (SBE-β-CD, Captisol®) was selected to prepare inclusion complex. Complexation was confirmed using FTIR, 1H NMR, DSC, and XRD. Bioactivity of […]

IL-22 Increases Permeability of Intestinal Epithelial Tight Junctions by Enhancing Claudin-2 Expression

Dysfunction of the epithelial barrier is a hallmark of inflammatory intestinal diseases. The intestinal epithelial barrier is maintained by expression of tight junctions that connect adjacent epithelial cells and seal the paracellular space. IL-22 is critical for the maintenance of intestinal barrier function through promoting antipathogen responses and regeneration of epithelial tissues in the gut. However, little is […]

Human 3D Gastrointestinal Microtissue Barrier Function As a Predictor of Drug-Induced Diarrhea

Drug-induced gastrointestinal toxicities (GITs) rank among the most common clinical side effects. Preclinical efforts to reduce incidence are limited by inadequate predictivity of in vitro assays. Recent breakthroughs in in vitro culture methods support intestinal stem cell maintenance and continual differentiation into the epithelial cell types resident in the intestine. These diverse cells self-assemble into microtissues with in […]

New Human Organotypic Corneal Tissue Model for Ophthalmic Drug Delivery Studies

PURPOSE. The purpose of the current work was to develop a physiologically relevant, in vitro human three-dimensional (3D) corneal epithelial tissue model for use in ophthalmic drug development. METHODS. Normal human corneal epithelial cells were cultured at the air–liquid interface to produce the 3D corneal tissue model. Corneal barrier was determined by measuring transepithelial electrical resistance (TEER). Quantitative PCR arrays […]

Human Primary Cell-Based Organotypic Microtissues for Modeling Small Intestinal Drug Absorption

Purpose: The study evaluates the use of new in vitro primary human cell-based organotypic small intestinal (SMI) microtissues for predicting intestinal drug absorption and drug-drug interaction. Methods: The microtissues were reconstructed using human intestinal fibroblasts and enterocytes cultured on a permeable support. To evaluate the suitability of the intestinal microtissues to model drug absorption, the permeability coefficients across the microtissues were determined for […]

In Vitro Skin Models and Their Predictability in Defining Normal and Disease Biology, Pharmacology, and Toxicity

In vitro skin model systems are increasingly being used both in the early evaluation of therapeutic drug candidates and in confirmatory mechanistic studies. The most commonly used of these in vitro model systems are reconstituted human epidermis (RHE) models. These RHE skin models consist solely of epidermal keratinocytes, which comes with some limitations but also with the advantage […]

In Vitro Permeation of Latanoprost Eye Drop Formulations in a 3-Dimensional Normal Human Corneal Tissue Model

Permeation of topically applied ocular drugs occurs predominantly through the cornea and therefore absorption studies using corneal tissues play a critical role in ocular drug formulation. The purpose of the study was to evaluate the permeation of Latanoprost eye drops through in vitro reconstructed normal human corneal tissue model. Seven different formulations of Latanoprost eye […]

An in vitro Reconstructed Normal Human Corneal Tissue Model for Corneal Drug Delivery Studies of Ophthalmic Formulations

Purpose: Permeation of topically applied ocular drugs occurs predominantly through the cornea and therefore absorption studies using corneal tissues play a critical role in ocular drug formulation. Currently, most ocular absorption studies use in vivo or ex vivo animal tissues that have many disadvantages including poor standardization, species extrapolation, high cost, and ethical concerns. Methods: […]

A four-organ-chip for interconnected long-term co-culture of human intestine, liver, skin and kidney equivalents

Systemic absorption and metabolism of drugs in the small intestine, metabolism by the liver as well as excretion by the kidney are key determinants of efficacy and safety for therapeutic candidates. However, these systemic responses of applied substances lack in most in vitro assays. In this study, a microphysiological system maintaining the functionality of four organs over 28 […]

Chip-based human liver–intestine and liver–skin co-cultures – A first step toward systemic repeated dose substance testing in vitro

Systemic repeated dose safety assessment and systemic efficacy evaluation of substances are currently carried out on laboratory animals and in humans due to the lack of predictive alternatives. Relevant international regulations, such as OECD and ICH guidelines, demand long-term testing and oral, dermal, inhalation, and systemic exposure routes for such evaluations. So-called human-on-a-chip concepts are […]

AN IN VITRO HUMAN AIRWAY MODEL FOR RAPID TOXICITY AND FORMULATION SCREENING OF NASAL DRUG DELIVERY SYSTEMS.

INTRODUCTION: Purpose: Nasal delivery of protein and other high molecular weight drugs is an attractive option to injection or oral delivery. However, nasal drug delivery is limited by potential irritation/toxicity issues, difficulties in achieving effective doses and rapidity of clearance from the nasal cavity. These difficulties are best addressed early in formulation development prior to […]

IN VITRO AND IN VIVO SCREENING OF INTRANASAL INSULIN FORMULATIONS.

This study by researchers at Nastech Pharmaceuticals demonstrated that Mattek’s EpiAirway in vitro human tissue equivalents can be used by pharmaceutical companies to develop intranasal drug formulations that provide improved permeation in vivo of Active Pharmaceutical Ingredients (API’s). Nasal delivery of insulin provides an attractive option for a non-invasive diabetes treatment. To identify a suitable […]

PERMEABILITY AND CYTOTOXICITY OF MACROMOLECULE FROM NASAL FORMULATION USING EPIAIRWAY TISSUE MODEL.

Hydrophilic macromolecules such as proteins and peptides are poorly absorbed through the nasal mucosa. Nastech Pharmaceuticals has utilized a variety of techniques to improve the nasal absorption of macromolecules with emphasize on achieving safety as well as therapeutic efficacy. EpiAirway, an in vitro epithelial cell membrane model, was employed to screen Nastech formulations and marketed […]

LONG TERM REPRODUCIBILITY OF EPIDERM, AN EPIDERMAL MODEL FOR DERMAL TESTING AND RESEARCH.

This technical reference summarizes Mattek’s 10-plus YEAR EpiDerm tissue reproducibility data. Long-term reproducibility is important not only to Mattek Customers, but also to European (ECVAM) and US (ICCVAM) regulators. Regulators constantly stress the need for superior reproducibility of in vitro tissue equivalents, not only during a specific validation program, but also long after the initial […]

FORMULATION DEVELOPMENT OF siRNAs FOR DRUG DELIVERY: A NEW THERAPEUTIC APPROACH FOR PANDEMIC INFLUENZA.

This study by scientists at Nastech Pharmaceuticals demonstrated how Mattek’s EpiAirway human tracheal/bronchial tissue equivalent can be used to identify lipids that facilitate siRNA uptake in lung tissue. This was part of a program to develop siRNA-based therapeutics designed for direct-to-lung delivery to treat humans infected with H5N1 Pandemic (Bird) Flu. The risk of an […]

NALTREXONE ESTER PRODRUG BIOCONVERSION IN A HUMAN EPIDERMIS EQUIVALENT.

IMPROVEMENTS IN EPIDERM, A HIGHLY DIFFERENTIATED SKIN MODEL, FOR DRUG DELIVERY STUDIES.

The ability to produce skin in vitro with barrier properties equivalent to those of native epidermis remains a much sought after goal. This study by scientists in the Department of Pharmacology and Physiology, UMDNJ-NJMS and Mattek Corp. involves the use of a highly differentiated skin model, EpiDerm™, which has been shown to be useful in […]

Preclinical development and ocular biodistribution of gemini-DNA nanoparticles after intravitreal and topical administration: Towards non-invasive glaucoma gene therapy

Gene therapy could offer improvement in the treatment of glaucoma compared to the current standard of lowering intraocular pressure. We have developed and characterized non-viral gemini surfactant-phospholipid nanoparticles (GL-NPs) for intravitreal and topical administration. Optimized GL-NPs (size range 150-180 nm) were biocompatible with rat retinal ganglion (RGC-5) cells with N95% viability by PrestoBlue™assay. GL-NPs carrying […]

PARTICLE SIZE AND BILAYER RIGIDITY EFFECTS ON SKIN DIFFUSION OF NANOSOMES.

IDENTIFICATION OF TIGHT JUNCTION MODULATING LIPIDS.

Tight junctions (TJs) play an important role in regulating paracellular drug transport. The aim of this study was to identify lipids that rapidly and reversibly alter transepithelial electrical resistance (TER) and/or TJ permeability in epithelial tissue. In this study, we developed a screen for identifying lipids that alter TJ properties. Measurement of TER was used […]

AN IN VITRO MODEL OF HUMAN AIRWAY EPITHELIUM (EPIAIRWAY) FOR IN VITRO METABOLISM, TOXICITY SCREENING AND DRUG DELIVERY APPLICATIONS.

This study by Mattek Corp. scientists demonstrated that the EpiAirway in vitro human tracheal/bronchial tissue equivalent possesses the in vivo-like physical and biochemical attributes necessary for evaluating the delivery of drugs, metabolism, airway irritation, and toxicity potential of environmental/occupational chemicals. In vitro airway models are urgently needed as alternatives to animal testing for compliance with […]

IN VITRO SKIN EQUIVALENT MODELS FOR TOXICITY TESTING.

This technical paper by Mattek scientists documented how Mattek’s EpiDerm, EpiDermFT and MelanoDerm in vitro human skin tissue equivalents can be used to assess the safety of topically applied pharmaceutical and cosmetic products. Prior to human use of new cosmetic or therapeutic products, in vivo animal tests are often conducted in order to screen for […]

DRUG/XENOBIOTIC-METABOLIZING ENZYME (XME) EXPRESSION IN THE EPIAIRWAY IN VITRO HUMAN AIRWAY MODEL: UTILITY FOR ASSESSING TRACHEAL/BRONCHIAL BIOTRANSFORMATION OF INHALED PHARMACEUTICALS AND ENVIRONMENTAL CHEMICALS.

This study by Mattek Corp. scientists demonstrated that Mattek’s EpiAirway human airway tissue equivalent possesses numerous in vivo-like xenobiotic metabolizing enzyme (XME) activities and therefore should be useful for evaluating the airway metabolism of drugs, tobacco smoke and environmental/occupational chemicals. Human tracheal/bronchial epithelium contains xenobiotic metabolizing capabilities provided by a variety of phase I (oxidative) […]

DISCOVERY OF TRANSDERMAL PENETRATION ENHANCERS BY HIGH-THROUGHPUT SCREENING.

Although transdermal drug delivery is more attractive than injection, it has not been applied to macromolecules because of low skin permeability. Here scientists at UC Santa Barbara describe particular mixtures of penetration enhancers that increase skin permeability to macromolecules (~1-10 kDa) by up to ~100-fold without inducing skin irritation. The discovery of these mixtures was […]

NALTREXONE AND NALTREXONE-3-O-VALERATE DIFFUSION AND BIOCONVERSION IN A HUMAN EPIDERMIS EQUIVALENT.

Transdermal naltrexone delivery may help improve patient compliance in the treatment of narcotic dependence and alcoholism. Lipophilic alkyl ester prodrugs increase the delivery rate of naltrexone across human surgical waste skin in vitro. Human skin equivalent models can be useful tools for assessing epidermal drug metabolism and topical/transdermal prodrug metabolic conversion. The purpose of this […]

BARRIER FUNCTION COMPARISON BETWEEN IN VITRO SKIN, ORAL (BUCCAL), AND OCULAR TISSUE MODELS – IMPLICATIONS FOR DRUG DELIVERY STUDIES.

Purpose: Due to the barrier properties of skin, transdermal delivery of therapeutic compounds is often not feasible. As an alternative, delivery through buccal or gingival tissues has been investigated. The current presentation involves use highly differentiated, in vitro tissue models of the epidermis (EpiDerm™), oral tissue (EpiOral™), and cornea tissue (EpiOcular™). The purpose of this […]

NOVEL 3D HUMAN SMALL INTESTINAL TISSUE MODEL (EPIINESTINAL™ ) TO ASSESS DRUG PERMEATION & INFLAMMATION

Purpose:  Drug transport and permeability across the small intestine (SMI) is a key parameter for determining bioavailability of orally administered drugs. The currently available in vitro models are highly dependent on immortalized cell lines (e.g. Caco-2) and have significant deficiencies for drug development applications. Therefore, we developed an in vitro SMI model (EpiIntestinalTM) using normal […]

TRANSCORNEAL IONTOPHORESIS FOR DELIVERY OF CIPROFLOXACIN HYDROCHLORIDE.

Purpose: To investigate the feasibility of utilizing iontophoresis for delivery of ciprofloxacin hydrochloride to the anterior chamber of the eye and to carry out systematic studies to investigate the effect of electrical protocol on the transcorneal drug delivery. Materials and Methods: Effect of current density (0.75 mA/cm2 to 6.25 mA/cm2 applied for 5 minutes) on […]

HYDROGEN PEROXIDE MEDIATED TRANSVAGINAL DRUG DELIVERY.

Simple, safe and effective permeability enhancers are crucial for successful non-invasive drug delivery methods. We seek local permeability augmentation mechanisms for integration into passive or active architectures in order to enable novel therapeutic delivery routes of the target drug while minimizing drug formulation challenges. This study explores the efficacy of hydrogen peroxide (HP) as a […]

EVALUATION OF RECONSTITUTED HUMAN VAGINAL EPITHELIUM AS A MODEL FOR DRUG DELIVERY OF FLUCONAZOLE GEL FOR TREATING VULVOVAGINAL CANDIDIASIS.

Purpose: The goal of this project performed by researchers at the Massachusetts College of Pharmacy and Health Sciences was to evaluate the use of EpiVaginal, a reconstituted human vaginal epithelium, as a model for penetration for an antifungal gel containing fluconazole. A tissue culture based model for vaginal epithelium (EpiVaginal) has been developed by Mattek […]

CANNABIDIOL DIFFUSION ACROSS HUMAN TRACHEO-BRONCHIAL TISSUE (EPIAIRWAY™) AND INTRANASAL ABSORPTION IN RATS.

Some cannabinoids are potentially useful in cancer symptom management to alleviate pain and control chemotherapy-induced nausea and vomiting. The drugs have also been shown to possess anticonvulsant, antianxiety/antipsychotic, and immuno-modulatory effects. The non-psychoactive cannabinoid, cannabidiol (CBD), is a clinical candidate for management of medical conditions where emesis and pain are prevalent. Considering the rapid onset […]

BIOCONVERSION OF NALTREXONE AND ITS 3-O-ALKYL-ESTER PRODRUGS IN A HUMAN SKIN EQUIVALENT.

This study by scientists at the University of Kentucky College of Pharmacy and Mattek Corp. demonstrated that Mattek’s EpiDerm in vitro human skin tissue equivalent can be used as an alternative experimental system to human skin for the prediction of topical/transdermal drug/prodrug bioconversion. The purpose of this study was to compare the percutaneous absorption and […]

PERMEATION OF WIN 55,212-2, A POTENT CANNABINOID RECEPTOR AGONIST, ACROSS HUMAN TRACHEO-BRONCHIAL TISSUE (EPIAIRWAY™) IN VITRO AND RAT NASAL EPITHELIUM IN VIVO.

R-(+)-WIN 55,212-2 is prone to hepatic first-pass metabolism and variable bioavailability following oral administration. The aim of this study was to predict intranasal absorption of the compound using EpiAirway™ tissue culture. Permeation experiments of R-(+)-WIN 55,212-2 mesylate formulations with 2% dimethyl-β-cyclodextrin (DMβCD), 2% randomly methylated-β-cyclodextrin (RAMβCD), 1:1 propylene glycol:saline [PG:S (1:1)] and 1.5% propylene glycol […]

THE EFFICACY OF ECHINACEA IN A 3-D TISSUE MODEL OF HUMAN AIRWAY EPITHELIUM.

This study by researchers at the University of British Columbia and A. Vogel Bioforce AG demonstrated that Mattek’s EpiAirway in vitro 3-D human tracheal/bronchial tissue equivalent can be infected with rhinovirus type 1A (RV1A) and then used to evaluate the antirhinovirus efficacy of Echinacea purpurea. Researchers evaluated the antirhinovirus efficacy of a standardized preparation of […]

DRUG PERMEABILITY ACROSS BOVINE RESPIRATORY TISSUES COMPARED TO A HUMAN TRACHEO/BRONCHIAL CELL CULTURE (EPIAIRWAY™ SYSTEM).

The past three decades have seen the emergence of the nasal mucosa as a viable alternative route for drug delivery. The availability of over 15 drugs meant for systemic action is a testament to its rapidly growing popularity. However, the absence of a good in vitro model precludes the rapid screening of suitable drug compounds […]

RECONSTRUCTION OF NEW ORGANOTYPIC 3D HUMAN SMALL INTESTINE TISSUE MODEL FOR DRUG SAFETY AND TOXICITY.

The epithelial lining of the gastrointestinal (GI) tract is a gatekeeper for entry of orally ingested nutrients and xenobiotics including medicaments. The small intestine has a well organized structure containing proliferative cells which migrate along the crypt-villi axis and differentiate into functionally mature epithelial cells. Currently, the most common in vitro model utilized for study […]

DOPAMINE TRANSPORT ACROSS RESPIRATORY EPITHELIUM.

Dopamine is a catecholamine neurotransmitter implicated in CNS related disorders such as Parkinson’s disease, schizophrenia and Huntington’s disease. It is known to be transported by the dopamine transporter (DAT) in the CNS and an organic cation transporter (OCT) peripherally. It is orally ineffective due to high first pass metabolism and its inability to cross the […]

DAS181, A SIALIDASE FUSION PROTEIN, PROTECTS HUMAN AIRWAY EPITHELIUM AGAINST INFLUENZA VIRUS INFECTION: AN IN VITRO PHARMACODYNAMIC ANALYSIS.

This study by researchers at NexBio and the University of Hong Kong demonstrated that Mattek’s EpiAirway in vitro 3-D human tracheal/bronchial tissue equivalent can be used to model the pharmacodynamics of a new drug formulation that inhibits influenza virus infection. Objectives: The influenza virus (IFV) infection models commonly used to evaluate antiviral agents (e.g. MDCK […]

DEVELOPMENT OF AN INTRANASAL FORMULATION OF THE Y2R AGONIST PEPTIDE YY3-36.

Peptide YY (PYY) was identified in the 1980s as a hormone produced in the gut and as early as 1993 it was demonstrated that peripheral administration of PYY was a satiety factor in mammals and could thus be a potential treatment for obesity. Subsequent research has identified that PYY is released in proportion to the […]

AN IN VITRO MODEL FOR THE RAPID SCREENING OF POTENTIAL COMPONENTS AND FORMULATIONS FOR NASAL DRUG DELIVERY.

Clinical trials have indicated that nasal delivery of a variety of drugs is both possible and, in some cases, superior to either injections or oral delivery. The two main drawbacks of nasal delivery are the limited maximum dose per spray and the rapidity of clearance from the nasal cavity. These difficulties can best be addressed […]

EFFECTS OF ENHANCERS ON MACROMOLECULES FORMULATIONS ON MEMBRANE PENETRATION, CELL VIABILITY AND RESISTANCE USING EPIAIRWAY™ TISSUE MODEL.

Drug delivery by the nasal route provides many advantages and is an attractive alternative for drugs that cannot be delivered orally and hence typically administered by the parenteral route. Nasal delivery provides an attractive alternative not only because it overcomes the above-mentioned problems with oral delivery, but also due to its fast onset of action, […]

RETAINING CELL INTEGRITY DURING ORGANOTYPIC MODEL VIABILITY ASSAYS: ALTERNATIVES TO MTT.

This study by researchers at the State University of New York (SUNY) at Stony Brook documents the effort to the develop an alternative tissue viability endpoint analysis using a non-lytic agent (MTS, Alamar Blue or CalceinAM) in place of the industry-standard MTT for Mattek’s EpiAirway in vitro 3-D human tracheal/bronchial tissue equivalent and Mattek’s EpiDerm […]

VALIDATING MTS AS AN ALTERNATIVE VIABILITY ASSAY TO MTT ON THE HUMAN 3-D TISSUE MODELS, EPIAIRWAY AND EPIDERM.

This study by researchers at the State University of New York (SUNY) at Stony Brook documents the development of an alternative tissue viability endpoint analysis using the non-lytic agent MTS in place of the industry-standard MTT for Mattek’s EpiAirway in vitro 3-D human tracheal/bronchial tissue equivalent and Mattek’s EpiDerm in vitro 3-D human skin tissue […]

IN VITRO FORMULATION OPTIMIZATION OF INTRANASAL GALANTAMINE LEADING TO ENHANCED BIOAVAILABILITY AND REDUCED EMETIC RESPONSE IN VIVO.

This study by researchers at Nastech Pharmaceuticals demonstrated that Mattek’s EpiAirway in vitro human tracheal/bronchial tissue equivalent can be used to accurately assess the drug permeability, tight junction modulation, and cellular toxicity of new intranasal drug formulations. The purpose of the current investigation was to optimize an intranasal (IN) galantamine (an acetylcholinesterase inhibitor used for […]

PEPTIDES AND PEGYLATED PEPTIDES AS INTRANASAL PERMEATION ENHANCERS: COMPARISON TO SMALL MOLECULAR EXCIPIENTS.

This study by scientists at Nastech Pharmaceuticals demonstrated how Mattek’s EpiAirway human tracheal/bronchial tissue equivalent can be used to identify novel permeation enhancers for use in nasal drug delivery. Intranasal delivery as an alternative route for administering drugs, in particular biologically active peptides, is desirable. Earlier studies by Nastech Pharmaceutical Company scientists showed that a […]

THERAPEUTIC UTILITY OF A NOVEL TIGHT JUNCTION MODULATING PEPTIDE FOR ENHANCING INTRANASAL DRUG DELIVERY.

This study by scientists at Nastech Pharmaceuticals demonstrated how Mattek’s EpiAirway human tracheal/bronchial tissue equivalent can be used to test the ability of a novel tight junction modulating (TJM) peptide to enhance the permeability of one low-molecular weight (LMW) drug and three peptides. Previously, a novel tight junction modulating (TJM) peptide was described by Nastech […]

PEPTIDE DRUG PERMEATION ENHANCEMENT BY SELECT CLASSES OF LIPIDS.

This study by researchers at Nastech Pharmaceuticals demonstrated that Mattek’s EpiAirway in vitro human tracheal/bronchial tissue equivalent can be used to identify lipids that rapidly and reversibly alter the tight junction permeability of human epithelial tissues. Tight junctions play an important role in regulating paracellular drug transport. The aim of this Nastech Pharmaceutical Co. study […]

DEVELOPMENT OF A NOVEL HIGH-CONCENTRATION GALANTAMINE FORMULATION SUITABLE FOR INTRANASAL DELIVERY.

This study by researchers at Nastech Pharmaceuticals demonstrated that Mattek’s EpiAirway in vitro human tracheal/bronchial tissue equivalent can be used to assess the drug permeability and cellular toxicity of a novel drug formulation designed for intranasal delivery. The goal of this Nastech Pharmaceutical Co. study was to develop an intranasal formulation of the acetylcholinesterase inhibitor […]

INTRANASAL DELIVERY OF RECOMBINANT HUMAN PARATHYROID HORMONE [HPTH (1–34)], TERIPARATIDE IN RATS.

This study by scientists at the University of Kentucky College of Pharmacy and Mattek Corp. demonstrated that Mattek’s EpiAirway in vitro human tracheal/bronchial tissue equivalent can be used to determine the potential toxicity to humans of drugs to be administered intranasally. The aim of this study was to explore the nasal route as an alternative […]

LOCALIZATION OF P-GLYCOPROTEIN IN HYMAN TRACHEAL/BRONCHIAL EPITHELIAL CELL CULTURE (EPIAIRWAY™)

The development of a human in vitro cell culture system would enhance the ability to study various factors affecting nasal drug delivery. EpiAirway is a cell culture system derived from normal human tracheal/bronchial epithelial cells which is grown on polycarbonate inserts. It shows a well developed epithelial region and retains the ability to secrete mucus. […]

TRANSDERMAL AND BUCCAL DELIVERY OF METHYLXANTHINES THROUGH HUMAN TISSUE IN VITRO.

This study by researchers at Rutgers University (USA) and the University of Strathclyde (Scotland) demonstrated that Mattek’s EpiOral in vitro human buccal (inner cheek) tissue equivalent is an excellent in vitro substitute for testing the buccal permeability of a number of central nervous system stimulants. Researchers examined the in vitro permeation of central nervous system […]

LINKER-BASED LECITHIN MICROEMULSIONS FOR TRANSDERMAL DELIVERY OF LIDOCAINE.

This study by researchers at the University of Toronto demonstrated that Mattek’s EpiDerm in vitro human skin tissue equivalent is an excellent in vitro alternative for examining the transdermal permeation and cytotoxicity characteristics of novel microemulsions. In this work, researchers at the University of Toronto introduce alcohol-free lecithin microemulsions formulated with linkers to produce transdermal […]

IN VITRO SKIN ABSORPTION AND DRUG RELEASE – A COMPARISON OF SIX COMMERCIAL PREDNICARBATE PREPARATIONS FOR TOPICAL USE.

This study by researchers at the Freie Universitat Berlin and Charite–Universitatsmedizin Berlin demonstrated that Mattek’s EpiDerm in vitro human skin tissue equivalent is an excellent in vitro model to study the potential skin metabolism of drugs designed to be applied to and/or penetrate human skin. Reconstructed human epidermis is a useful tool for in vitro […]

Nose-to-brain transport of melatonin from polymer gel suspensions: a microdialysis study in rats

PURPOSE: Exogenous melatonin (MT) has significant neuroprotective roles in Alzheimer’s and Parkinson’s diseases. This study investigates the delivery MT to brain via nasal route as a polymeric gel suspension using central brain microdialysis in anesthetized rats. METHODS: Micronized MT suspensions using polymers [carbopol, carboxymethyl cellulose (CMC)] and polyethylene glycol 400 (PEG400) were prepared and characterized […]

APPLICATION OF ORGANOTYPIC IN VITRO HUMAN CELL CULTURE MODELS FOR RESEARCH AND DEVELOPMENT OF INHALATION PHARMACEUTICAL FORMULATIONS TARGETING THE PROXIMAL AIRWAYS.

Delivery of pharmaceuticals via inhalation is a potentially useful alternative to intravenous injection for drugs that are unstable or poorly absorbed after oral administration; for chronic disease conditions that require frequent administration: or therapeutics for which the airways are the intended target. The proximal airways are common targets for drugs Intended to treat inflammatory conditions […]

IN VITRO PERCUTANEOUS ABSORPTION USING THE Mattek EPI-606X SKIN CONSTRUCT AND HUMAN SKIN.

The rates of absorption of chemicals in human skin can be modeled in the in vitro percutaneous absorption assay. Moreover, the impact of various vehicles on the permeation rates of chemicals can also be evaluated. The reference material, benzoic acid (BA), was prepared in two vehicles (acetone and petrolatum) and was tested in duplicate trials […]

ASSESSMENT OF HUMAN CADAVER AND RECONSTRUCTED SKIN MODELS TO PREDICT PHARMACOKINETICS OF TESTOSTERONE TRANSDERMAL DRUG DELIVERY PATCHES.0

Testosterone TDD patches were compared for in-vitro skin permeation characteristics and in the clinic for in-vivo pharmacokinetic parameters. In-vitro evaluations were conducted using both human cadaver and reconstructed skin models in order to determine a model predictive of in-vivo delivery. HCS was chosen at the model most predictive of testosterone in-vivo delivery. The preliminary IVIVC […]

INTERRELATION OF PERMEATION AND PENETRATION PARAMETERS OBTAINED FROM IN VITRO EXPERIMENTS WITH HUMAN SKIN AND SKIN EQUIVALENTS.

In a comparative study, two different in vitro cutaneous test systems were examined: (1) The Franz diffusion cell (FD-C), a test system to study drug permeation through the skin and to obtain data like steady state flux and lag time as well as permeability and diffusion coefficients. (2) The Saarbruecken penetration model (SB-M), a test […]

COMPARISON OF CUTANEOUS BIOAVAILABILIY OF COSMETIC PREPARATIONS CONTAINING CAFFEINE OR α-TOCOPHEROL APPLIED ON HUMAN SKIN MODELS OR HUMAN SKIN EX VIVO AT FINITE DOSES.

The use of human skin models for performing cutaneous bioavailability studies has been little investigated. For instance, only few studies have been reported on human skin models dealing with vehicle effects on percutaneous penetration. The present study aimed at evaluating the influence on caffeine’s and α-tocopherol’s cutaneous bioavailability of cosmetic vehicles such as a water-in-oil […]

ASSESSMENT OF SKIN ABSORPTION AND METABOLISM OF ARACHIDONIC ACID & GLYCERYL ARACHIDONATE USING IN VITRO DIFFUSION CELL TECHNIQUES.

Arachidonic acid (AA), has been used in cosmetics as a surfactant-cleansing and emulsifying agent. Glyceryl arachidonate (GA), a skin conditioning agent and emollient, may be partially metabolized by ester hydrolysis in skin to AA. Based on the Cosmetic Ingredient Review (CIR) Panel’s concern that there was a lack of dermal absorption data for AA, in […]

RECONSTRUCTED HUMAN EPIDERMIS FOR SKIN ABSORPTION TESTING: RESULTS OF THE GERMAN PREVALIDATION STUDY.

This study by scientists at the Freie Universität Berlin, Across Barriers GmbH, BASF Aktiengesellschaft Experimental Toxicology and Ecology, the Institut für Pharmakologie, Ludwig-Maximilians-Universität München, Cognis Deutschland GmbH & Co. KG, Universität des Saarlandes, ZEBET (Berlin, Germany), and Henkel KGaA demonstrated that Mattek’s EpiDerm in vitro human skin tissue equivalent can be used to predict the […]

RECONSTRUCTED SKIN EQUIVALENTS FOR ASSESSING PERCUTANEOUS DRUG ABSORPTION FROM PHARMACEUTICAL FORMULATIONS.

Excised human skin has so far been considered to be one of the most suitable in vitro methods to evaluate the penetration of dermatologically applied substances. The limited supply and the relatively high donor variability stimulated many research groups to use animal skin as a substitute for human skin. Since nowadays reconstructed skin equivalents are […]

EVALUATION OF HUMAN BIO-ENGINEEREED SKIN EQUIVALENT FOR DRUG PERMEATION STUDIES.

PURPOSE: To test the barrier function of a bio-engineered human skin (BHS) using three model drugs (caffeine, hydrocortisone, and tamoxifen) in vitro. To investigate the lipid composition and microscopic structure of the BHS. METHODS: The human skin substitute was composed of both epidermal and dermal layers, the latter having a bovine collagen matrix. The permeability […]

NEW DRUG DELIVERY SYSTEMS: VALIDATION OF IN VITRO MODELS.

IN VITRO PERMEATION AND IRRITATION OF BENZOYL PEROXIDE – CONTAINING PRODUCTS.

Two in vitro models to measure release of benzoyl peroxide (BPO) from formulations were presented. Franz-type diffusion cells and acetonitrile/water receptor mediums were used in both models. The barrier in one model was silicone sheeting and in the other was cultured human epidermis. The similarity in release profiles, rates of permeation, and diffusion coefficients obtained […]

RECONSTRUCTED EPIDERMIS AND FULL-THICKNESS SKIN FOR ABSORPTION TESTING: INFLUENCE OF THE VEHICLES USED ON STEROID PERMEATION.

This study by researchers at the Free University of Berlin demonstrated that Mattek’s EpiDerm in vitro human skin tissue equivalent and EpiDermFT full-thickness in vitro human skin tissue equivalent can be used in the development of topical dermatics and for hazard analysis of toxic compounds and their formulations. A protocol for percutaneous absorption studies has […]