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 Resjournal_title
Pharmaceutical researchauthors
Shin SH,Ghosh P,Newman B,Hammell DC,Raney SG,Hassan HE,Stinchcomb ALdoi
10.1007/s11095-017-2189-0subject
Has Abstractpub_date
2017-09-01 00:00:00pages
1817-1830issue
9eissn
0724-8741issn
1573-904Xpii
10.1007/s11095-017-2189-0journal_volume
34pub_type
杂志文章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
更新日期:2009-07-01 00:00:00
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
更新日期:2016-03-01 00:00:00
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
更新日期:1999-07-01 00:00:00
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
更新日期:1993-04-01 00:00:00
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
更新日期:2013-07-01 00:00:00
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
更新日期:1989-08-01 00:00:00
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
更新日期:1990-10-01 00:00:00
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
更新日期:1991-10-01 00:00:00
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
更新日期:2018-11-29 00:00:00
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
更新日期:1994-10-01 00:00:00
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
更新日期:2001-07-01 00:00:00
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
更新日期:1985-01-01 00:00:00
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
更新日期:2016-03-01 00:00:00
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
更新日期:1989-11-01 00:00:00
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
更新日期:2008-02-01 00:00:00
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
更新日期:2008-03-01 00:00:00
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
更新日期:2009-03-01 00:00:00
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
更新日期:2018-09-26 00:00:00
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
更新日期:1985-09-01 00:00:00
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
更新日期:2015-08-01 00:00:00
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
更新日期:2014-03-01 00:00:00
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
更新日期:2016-04-01 00:00:00
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
更新日期:2017-10-01 00:00:00
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
更新日期:1999-04-01 00:00:00
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
更新日期:2020-04-14 00:00:00
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
更新日期:2008-09-01 00:00:00
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
更新日期:2012-08-01 00:00:00
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
更新日期:1997-08-01 00:00:00
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
更新日期:2020-05-28 00:00:00
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
更新日期:2002-03-01 00:00:00