On the Road to Development of an in Vitro Permeation Test (IVPT) Model to Compare Heat Effects on Transdermal Delivery Systems: Exploratory Studies with Nicotine and Fentanyl.

Abstract:

PURPOSE:At elevated temperatures, the rate of drug release and skin permeation from transdermal delivery systems (TDS) may be higher than at a normal skin temperature. The aim of this study was to compare the effect of heat on the transdermal delivery of two model drugs, nicotine and fentanyl, from matrix-type TDSs with different formulations, using in vitro permeation tests (IVPT). METHODS:IVPT experiments using pig skin were performed on two nicotine and three fentanyl TDSs. Both continuous and transient heat exposures were investigated by applying heat either for the maximum recommended TDS wear duration or for short duration. RESULTS:Continuous heat exposure for the two nicotine TDSs resulted in different effects, showing a prolonged heat effect for one product but not the other. The Jmax enhancement ratio due to the continuous heat effect was comparable between the two nicotine TDS, but significantly different (p < 0.05) among the three fentanyl TDSs. The Jmax enhancement ratios due to transient heat exposure were significantly different for the two nicotine TDSs, but not for the three fentanyl TDSs. Furthermore, the transient heat exposure affected the clearance of drug from the skin depot after TDS removal differently for two drugs, with fentanyl exhibiting a longer heat effect. CONCLUSIONS:This exploratory work suggests that an IVPT study may be able to discriminate differences in transdermal drug delivery when different TDS are exposed to elevated temperatures. However, the clinical significance of IVPT heat effects studies should be further explored by conducting in vivo clinical studies with similar study designs.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Shin SH,Ghosh P,Newman B,Hammell DC,Raney SG,Hassan HE,Stinchcomb AL

doi

10.1007/s11095-017-2189-0

subject

Has Abstract

pub_date

2017-09-01 00:00:00

pages

1817-1830

issue

9

eissn

0724-8741

issn

1573-904X

pii

10.1007/s11095-017-2189-0

journal_volume

34

pub_type

杂志文章
  • Diffusion studies of nanometer polymersomes across tissue engineered human oral mucosa.

    abstract:PURPOSE:To measure the diffusion of nanometer polymersomes through tissue engineered human oral mucosa. METHODS:In vitro models of full thickness tissue engineered oral mucosa (TEOM) were used to assess the penetration properties of two chemically different polymersomes comprising two of block copolymers, PMPC-PDPA an...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-009-9882-6

    authors: Hearnden V,Lomas H,Macneil S,Thornhill M,Murdoch C,Lewis A,Madsen J,Blanazs A,Armes S,Battaglia G

    更新日期:2009-07-01 00:00:00

  • Biodistribution and Toxicity of X-Ray Iodinated Contrast Agent in Nano-emulsions in Function of Their Size.

    abstract:PURPOSE:This study aimed to investigate the impact of the size of X-ray iodinated contrast agent in nano-emulsions, on their toxicity and fate in vivo. METHODS:A new compound, triiodobenzoate cholecalciferol, was synthetized, formulated as nano-emulsions, and followed after i.v. administration in mice by X-ray imaging...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1813-0

    authors: Attia MF,Anton N,Akasov R,Chiper M,Markvicheva E,Vandamme TF

    更新日期:2016-03-01 00:00:00

  • Biodegradable nanoparticles containing doxorubicin-PLGA conjugate for sustained release.

    abstract:PURPOSE:Doxorubicin was chemically conjugated to a terminal end group of poly(D,L-lactic-co-glycolic acid) [PLGA] and the doxorubicin-PLGA conjugate was formulated into nanoparticles to sustain the release of doxorubicin. METHODS:A hydroxyl terminal group of PLGA was activated by p-nitrophenyl chloroformate and reacte...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018908421434

    authors: Yoo HS,Oh JE,Lee KH,Park TG

    更新日期:1999-07-01 00:00:00

  • Controlled delivery systems for proteins using polyanhydride microspheres.

    abstract::A method to provide near-constant sustained release of high molecular weight, water-soluble proteins from polyanhydride microspheres is described. The polyanhydrides used were poly(fatty acid dimer) (PFAD), poly(sebacic acid) (PSA), and their copolymers [P(FAD-SA)]. P(FAD-SA) microspheres containing proteins of differ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018929531410

    authors: Tabata Y,Gutta S,Langer R

    更新日期:1993-04-01 00:00:00

  • Gamma irradiation of active self-healing PLGA microspheres for efficient aqueous encapsulation of vaccine antigens.

    abstract:PURPOSE:To investigate the effect of γ-irradiation of poly(lactic-co-glycolic acid) (PLGA)/Al(OH)₃/0 or 5 wt% diethyl phthalate (DEP) microspheres for active self-healing encapsulation of vaccine antigens. METHODS:Microspheres were irradiated with ⁶⁰Co at 2.5 and 1.8 MRad and 0.37 and 0.20 MRad/h. Encapsulation of tet...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-013-1019-2

    authors: Desai KG,Kadous S,Schwendeman SP

    更新日期:2013-07-01 00:00:00

  • Route of administration and sex differences in the pharmacokinetics of aspirin, administered as its lysine salt.

    abstract::One thousand milligrams of aspirin, as its lysine salt was administered intravenously, orally, and intramuscularly to nine male and nine female young healthy adult volunteers. After intravenous injection mean (+/- SD) values of clearance, steady-state volume of distribution, and terminal half-life were 12.2 +/- 2.2 ml...

    journal_title:Pharmaceutical research

    pub_type: 临床试验,杂志文章

    doi:10.1023/a:1015978104017

    authors: Aarons L,Hopkins K,Rowland M,Brossel S,Thiercelin JF

    更新日期:1989-08-01 00:00:00

  • Microdialysis sampling for determination of plasma protein binding of drugs.

    abstract::The use of microdialysis sampling to study the binding of drugs to plasma proteins was evaluated. Microdialysis sampling is accomplished by placing a short length of dialysis fiber in the sample and perfusing the fiber with a vehicle. Small molecules in the sample, such as drugs, diffuse into the fiber and are transpo...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015955503708

    authors: Herrera AM,Scott DO,Lunte CE

    更新日期:1990-10-01 00:00:00

  • Prodrugs of peptides. 11. Chemical and enzymatic hydrolysis kinetics of N-acyloxymethyl derivatives of a peptide-like bond.

    abstract::Various carboxylic acid esters of the N-hydroxymethyl derivative of N-benzyloxycarbonylglycine benzylamide, used as a peptide-like model, were prepared and their decomposition kinetics studied in aqueous solution and in human plasma solutions. These N-acyloxymethylamide derivatives were found to undergo a facile decom...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015839426229

    authors: Bundgaard H,Rasmussen GJ

    更新日期:1991-10-01 00:00:00

  • Different Efflux Transporter Affinity and Metabolism of 99mTc-2-Methoxyisobutylisonitrile and 99mTc-Tetrofosmin for Multidrug Resistance Monitoring in Cancer.

    abstract:BACKGROUND:Little is known about the affinity and stability of 99mTc-labeled 2-methoxyisobutylisonitrile (99mTc-MIBI) and tetrofosmin (99mTc-TF) for imaging of multiple drug resistance transporters in cancer. We examined the affinity of 99mTc-labeled compounds for these transporters and their stability. METHODS:99mTc-...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2548-5

    authors: Kobayashi M,Tsujiuchi T,Okui Y,Mizutani A,Nishi K,Nakanishi T,Nishii R,Fukuchi K,Tamai I,Kawai K

    更新日期:2018-11-29 00:00:00

  • Renin inhibitor: transport mechanism in rat small intestinal brush-border membrane vesicles.

    abstract::The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The up...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018900124257

    authors: Hashimoto N,Fujioka T,Toyoda T,Muranushi N,Hirano K

    更新日期:1994-10-01 00:00:00

  • Protamine sulfate enhances the transduction efficiency of recombinant adeno-associated virus-mediated gene delivery.

    abstract:PURPOSE:The purpose of this study was to evaluate glucose responsiveness in HepG2 human hepatoma cells transduced by a recombinant adeno-associated virus (rAAV) vector containing the insulin gene promoter. and to investigate the effect of protamine sulfate on rAAV-mediated gene delivery. METHODS:Recombinant AAV vector...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1010923924844

    authors: Yang YW,Hsieh YC

    更新日期:2001-07-01 00:00:00

  • In vitro and in vivo-release of nitroglycerin from a new transdermal therapeutic system.

    abstract::A new transdermal therapeutic system (TTS) for nitroglycerin is presented that controls release of the active substance by means of desorption and diffusion. The drug release, in the dosage range examined under sink conditions, is independent of electrolytes and pH of the aqueous acceptor medium, but it does depend on...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/A:1016361921803

    authors: Wolff M,Cordes G,Luckow V

    更新日期:1985-01-01 00:00:00

  • In Vivo Toxicity and Immunological Characterization of Detoxified Recombinant Botulinum Neurotoxin Type A.

    abstract:PURPOSE:A double-mutant E224A/E262A full-length botulinum neurotoxin (BoNT) Type A with structural similarity to native BoNT/A but lacking the endopeptidase activity provides an ideal surrogate for testing pharmacokinetics and immunochemical characteristics of BoNT. METHODS:We determined lethality (LD50) of deactivate...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1816-x

    authors: Ravichandran E,Janardhanan P,Patel K,Riding S,Cai S,Singh BR

    更新日期:2016-03-01 00:00:00

  • Buccal absorption. III. Simultaneous diffusion and metabolism of an aminopeptidase substrate in the hamster cheek pouch.

    abstract::The simultaneous diffusion and metabolism of the D- and L-isomers of the aminopeptidase substrate, leucine-p-nitroanilide (LPNA), were examined in vitro in the hamster cheek pouch. L-LPNA was completely hydrolyzed during diffusion across the cheek pouch, whereas D-LPNA crossed the cheek pouch intact. The metabolic bar...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015949614437

    authors: Garren KW,Topp EM,Repta AJ

    更新日期:1989-11-01 00:00:00

  • The metastatic stage-dependent mucosal expression of sialic acid is a potential marker for targeting colon cancer with cationic polymers.

    abstract:PURPOSE:Locoregional recurrence is the most common complication after adenocarcinoma resection in the colon, despite adjuvant chemotherapy. Therapy efficacy could be improved if designed to target malignant cells by incorporating specific recognition factors in the drugs or the drug vehicles. The aim of this study was ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-007-9330-4

    authors: Azab AK,Kleinstern J,Srebnik M,Rubinstein A

    更新日期:2008-02-01 00:00:00

  • Designer gene delivery vectors: molecular engineering and evolution of adeno-associated viral vectors for enhanced gene transfer.

    abstract::Gene delivery vectors based on adeno-associated virus (AAV) are highly promising due to several desirable features of this parent virus, including a lack of pathogenicity, efficient infection of dividing and non-dividing cells, and sustained maintenance of the viral genome. However, several problems should be addresse...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-007-9431-0

    authors: Kwon I,Schaffer DV

    更新日期:2008-03-01 00:00:00

  • Polymer chemistry influences monocytic uptake of polyanhydride nanospheres.

    abstract:PURPOSE:To demonstrate that polyanhydride copolymer chemistry affects the uptake and intracellular compartmentalization of nanospheres by THP-1 human monocytic cells. METHODS:Polyanhydride nanospheres were prepared by an anti-solvent nanoprecipitation technique. Morphology and particle diameter were confirmed via scan...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-008-9760-7

    authors: Ulery BD,Phanse Y,Sinha A,Wannemuehler MJ,Narasimhan B,Bellaire BH

    更新日期:2009-03-01 00:00:00

  • Nasal Administration of Cationic Nanoemulsions as Nucleic Acids Delivery Systems Aiming at Mucopolysaccharidosis Type I Gene Therapy.

    abstract:PURPOSE:This study demonstrates the nasal administration (NA) of nanoemulsions complexed with the plasmid encoding for IDUA protein (pIDUA) as an attempt to reach the brain aiming at MPS I gene therapy. METHODS:Formulations composed of DOPE, DOTAP, MCT (NE), and DSPE-PEG (NE-PEG) were prepared by high-pressure homogen...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2503-5

    authors: Schuh RS,Bidone J,Poletto E,Pinheiro CV,Pasqualim G,de Carvalho TG,Farinon M,da Silva Diel D,Xavier RM,Baldo G,Matte U,Teixeira HF

    更新日期:2018-09-26 00:00:00

  • In situ intestinal absorption of a poorly water-soluble drug from mixed micellar solutions of bile salt and lipolysis products in rats.

    abstract::The role of a bile salt (sodium taurocholate) and lipolysis products (monoglyceride and fatty acid) in the intestinal absorption of a poorly water-soluble drug, diazepam, was investigated. Absorption rates and bioavailabilities were determined with the in situ rat gut technique of Doluisio et al. and analyzing the dia...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/A:1016312827680

    authors: Serajuddin AT,Rosoff M,Goldberg AH

    更新日期:1985-09-01 00:00:00

  • A Microfluidic Diffusion Cell for Fast and Easy Percutaneous Absorption Assays.

    abstract:PURPOSE:Percutaneous absorption assays of molecules for pharmaceutical and cosmetology purposes are important to determine the bioavailability of new compounds, once topically applied. The current method of choice is to measure the rate of diffusion through excised human skin using a diffusion cell. This method however...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1654-x

    authors: Provin C,Nicolas A,Grégoire S,Fujii T

    更新日期:2015-08-01 00:00:00

  • Overcoming the blood-brain barrier in chemotherapy treatment of pediatric brain tumors.

    abstract::Pediatric brain tumors are most common cancers in childhood and among the leading causes of death in children. Chemotherapy has been used as adjuvant (i.e. after) or neoadjuvant (i.e. before) therapy to surgery and radiotherapy for the management of pediatric brain tumors for more than four decades and gained more att...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-013-1196-z

    authors: Wu L,Li X,Janagam DR,Lowe TL

    更新日期:2014-03-01 00:00:00

  • Curcumin Delivery by Poly(Lactide)-Based Co-Polymeric Micelles: An In Vitro Anticancer Study.

    abstract:PURPOSE:This work describes the synthesis of block co-polymeric micelles, methoxy-poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA) to encapsulate Curcumin (CUR), thereby improving the dispersibility and chemical stability of curcumin, prolonging its cellular uptake and enhancing its bioavailability. METHODS:CUR-mPEG...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1830-z

    authors: Kumari P,Swami MO,Nadipalli SK,Myneni S,Ghosh B,Biswas S

    更新日期:2016-04-01 00:00:00

  • Development of a Two-Dimensional Model for Predicting Transdermal Permeation with the Follicular Pathway: Demonstration with a Caffeine Study.

    abstract:PURPOSE:The development of a new two-dimensional (2D) model to predict follicular permeation, with integration into a recently reported multi-scale model of transdermal permeation is presented. METHODS:The follicular pathway is modelled by diffusion in sebum. The mass transfer and partition properties of solutes in li...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-017-2209-0

    authors: Kattou P,Lian G,Glavin S,Sorrell I,Chen T

    更新日期:2017-10-01 00:00:00

  • Grapefruit juice activates P-glycoprotein-mediated drug transport.

    abstract:PURPOSE:Grapefruit juice (GJ) is known to increase the oral bioavailability of many CYP3A-substrates by inhibiting intestinal phase-I metabolism. However, the magnitude of AUC increase is often insignificant and highly variable. Since we earlier suggested that CYP3A and P-glycoprotein (P-gp) form a concerted barrier to...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011902625609

    authors: Soldner A,Christians U,Susanto M,Wacher VJ,Silverman JA,Benet LZ

    更新日期:1999-04-01 00:00:00

  • Promoted Antitumor Activity of Myricetin against Lung Carcinoma Via Nanoencapsulated Phospholipid Complex in Respirable Microparticles.

    abstract:PURPOSE:Myricetin (MYR) flavonoid is well-recognized for its antioxidant, anti-inflammatory and anti-tumor potential. Introducing nanomedicine was the ultimate resort to solve the imperfections of this nutraceutical, namely solubility, stability and delivery issues. The study, thus, aims at developing inhalable micropa...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-020-02794-z

    authors: Nafee N,Gaber DM,Elzoghby AO,Helmy MW,Abdallah OY

    更新日期:2020-04-14 00:00:00

  • Structure-activity relationships and organ specificity in the induction of GST and NQO1 by alkyl-aryl isothiocyanates.

    abstract:PURPOSE:To compare the ability of alkyl-aryl isothiocyanates (ITCs) to increase the activities of the Phase 2 detoxification enzymes NAD[P]H:quinone acceptor oxidoreductase 1 (NQO1) and glutathione S-transferases (GST) in rat tissues in vivo and in cells in vitro. MATERIALS AND METHODS:Twelve alkyl-aryl ITCs and the f...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-008-9595-2

    authors: Munday R,Zhang Y,Munday CM,Bapardekar MV,Paonessa JD

    更新日期:2008-09-01 00:00:00

  • Near-infrared image-guided delivery and controlled release using optimized thermosensitive liposomes.

    abstract:PURPOSE:To engineer optimized near-infrared (NIR) active thermosensitive liposomes to potentially achieve image-guided delivery of chemotherapeutic agents. METHODS:Thermosensitive liposomes were surface-coated with either polyethylene glycol or dextran. Differential scanning calorimetry and calcein release studies wer...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0738-0

    authors: Turner DC,Moshkelani D,Shemesh CS,Luc D,Zhang H

    更新日期:2012-08-01 00:00:00

  • Simultaneous in vivo visualization and localization of solid oral dosage forms in the rat gastrointestinal tract by magnetic resonance imaging (MRI).

    abstract:PURPOSE:Bioavailability of orally administered drugs is much influenced by the behavior, performance and fate of the dosage form within the gastrointestinal (GI) tract. Therefore, MRI in vivo methods that allow for the simultaneous visualization of solid oral dosage forms and anatomical structures of the GI tract have ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1012161630481

    authors: Christmann V,Rosenberg J,Seega J,Lehr CM

    更新日期:1997-08-01 00:00:00

  • Development of Vancomycin Dose Individualization Strategy by Bayesian Prediction in Patients Receiving Continuous Renal Replacement Therapy.

    abstract:PURPOSE:Vancomycin (VCM) concentration is often out of therapeutic range (10-20 μg/ml) in patients receiving continuous renal replacement therapy (CRRT). The purposes of this study were to develop a practical VCM population pharmacokinetic (PPK) model and to evaluate the potential of Bayesian prediction-based therapeut...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-020-02820-0

    authors: Oda K,Jono H,Kamohara H,Nishi K,Tanoue N,Saito H

    更新日期:2020-05-28 00:00:00

  • Adhesion of powders for inhalation: an evaluation of drug detachment from surfaces following deposition from aerosol streams.

    abstract:PURPOSE:To evaluate micronized powder retention and detachment from inhaler surfaces following reproducible deposition by impaction, coupled with centrifugal particle detachment (CPD). METHODS:Micronized albuterol sulfate (AS) and beclomethasone dipropionate (BDP) were aerosolized as dry powders and deposited by casca...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1014451203619

    authors: Clarke MJ,Peart J,Cagnani S,Byron PR

    更新日期:2002-03-01 00:00:00