Abstract：
PURPOSE:In this study, we aimed to illustrate the utility of fractional radiofrequency (RF) that generated microchannels in the skin, allowing delivery of peptide and siRNA via the skin. The mechanisms involved in the correlation between macromolecule permeation and skin structure were also elucidated. METHODS:The morphology of the skin was examined by transmission electron microscopy (TEM), higher harmonic generation microscopy (HGM), and physiological factors. In vivo skin distribution of macromolecules was assessed by fluorescence and confocal microscopies. RESULTS:RF thermolysis selectively created an array of micropores deep into the epidermis without significant removal of the stratum corneum (SC). With energy of 30 mJ, a pore depth of 35 μm was achieved. The bipolar RF resulted in a 3-fold increase of transepidermal water loss (TEWL) compared with intact skin. The respective skin accumulation and flux of the peptide with a molecular weight (MW) of 2335 Da was 3- and 23-fold greater for the RF-treated group than for the non-treatment group. RF enhanced skin accumulation of siRNAs with MW of 10 and 15 kDa by 6.2- and 2.6-fold, respectively. Cutaneous penetration of the macromolecules with an MW of at least 40 kDa could be accomplished by RF. Confocal microscopy imaging revealed that RF could effectively deliver the peptide up to at least a 74-μm depth. The penetration depth of siRNA by RF irradiation was about 50 μm. CONCLUSIONS:The novel RF device efficiently delivered macromolecules into the skin while reserving SC layers to support some barrier functions. In this work, for the first time the assistance of fractional RF on peptide and siRNA transport was demonstrated.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Lee WR,Shen SC,Sun CK,Aljuffali IA,Suen SY,Lin YK,Wang JJ,Fang JYdoi
10.1007/s11095-014-1568-zsubject
Has Abstractpub_date
2015-05-01 00:00:00pages
1704-13issue
5eissn
0724-8741issn
1573-904Xjournal_volume
32pub_type
杂志文章abstract：PURPOSE:To provide the physicochemical properties of vitrified trehalose for predicting its recrystallization. METHODS:Thin films of vitrified trehalose solutions were prepared at room temperature and exposed to various humid and temperature atmospheres. The in-situ amount of retained water in the vacuum-dried trehalo...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2420-7
更新日期：2018-05-10 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：:A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption. This analysis uses a transp...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016212804288
更新日期：1995-03-01 00:00:00
abstract：PURPOSE:Critical steps in the subcellular processing of poly(ethylene imine)/nucleic acid complexes, especially endosomal/lysosomal escape, were visualized by using living cell confocal laser scanning microscopy (CSLM) to obtain an insight into their mechanism. METHODS:Living cell confocal microscopy was used to exami...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1014212630566
更新日期：2002-02-01 00:00:00
abstract：:Celiac disease (CD) is an immune-mediated enteropathy triggered by the ingestion of gluten-containing grains that affects ~1% of the white ethnic population. In the last decades, a rise in prevalence of CD has been observed that cannot be fully explained by improved diagnostics. Genetic predisposition greatly influenc...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0951-x
更新日期：2013-03-01 00:00:00
abstract：PURPOSE:Gastroduodenal and intestinal permeability were compared after single doses of sustained release and regular release flurbiprofen in the rat to assess possible site-specific formulation-dependent toxicity. METHODS:Pharmacokinetics was assessed and gastrointestinal permeability was evaluated using sucrose and 5...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1012134503107
更新日期：1997-11-01 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：PURPOSE:Nonlinear conjugation metabolic rate of valproic acid (VPA) has been speculated previously from plasma elimination and liver concentration of VPA in guinea pigs. The purposes of the present study were to assess our speculation by direct measurement of VPA glucuronidation rate in vitro. METHODS:VPA at various c...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016028707130
更新日期：1996-08-01 00:00:00
abstract：:Fibers were spun by the downward configuration of the wet spinning technique. This configuration is capable of encapsulating nonspherical and/or coarse particles. We examined encapsulation of propranolol hydrochloride and the ability of the fibers to act as a sustained-release delivery system for propranolol hydrochlo...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015982521706
更新日期：1989-12-01 00:00:00
abstract：:Biotherapeutics, including recombinant or plasma-derived human proteins and antibody-based molecules, have emerged as an important class of pharmaceuticals. Aggregation and immunogenicity are among the major bottlenecks during discovery and development of biotherapeutics. Computational tools that can predict aggregati...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0414-9
更新日期：2011-05-01 00:00:00
abstract：PURPOSE:Monocarboxylate transporter (MCT) inhibition represents a potential treatment strategy for γ-hydroxybutyric acid (GHB) overdose by blocking its renal reabsorption in the kidney. This study further evaluated the effects of a novel, highly potent MCT inhibitor, AR-C155858, on GHB toxicokinetics/toxicodynamics (TK...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1583-0
更新日期：2015-06-01 00:00:00
abstract：PURPOSE:The United States Pharmacopoeia (USP) imposes strict requirements on the geometry and operating conditions of the USP Dissolution Testing Apparatus II. A previously validated Computational Fluid Dynamics (CFD) approach was used here to study the hydrodynamics of USP Apparatus II when the impeller was placed at ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9477-z
更新日期：2008-02-01 00:00:00
abstract：PURPOSE:To examine the transport characteristics of the multidrug resistance-associated protein (MRP) substrate fluorescein across the isolated rat small intestinal segments. METHODS:The transport of fluorescein was studied in side-by-side diffusion chambers under short-circuited conditions at physiological pH. RESUL...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000022410.89709.c3
更新日期：2004-04-01 00:00:00
abstract：:Since ancient times, natural products, herbs and spices have been used for preventing several diseases, including cancer. The term chemoprevention was coined in the late 1970s and referred to the prevention of cancer by selective use of phytochemicals or their analogs. The field utilizes experimental carcinogenesis mo...
journal_title：Pharmaceutical research
pub_type： 历史文章,杂志文章,评审
doi：10.1007/s11095-010-0085-y
更新日期：2010-06-01 00:00:00
abstract：PURPOSE:Novel therapeutics are greatly needed that target specific pathological receptors and pathways involved in Neuropathic Pain (NP). Extending our previous work published in this Journal on Group I metabotropic glutamate receptor (mGluR) modulators, we now investigate the therapeutic potential of niclosamide in mo...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2027-9
更新日期：2016-12-01 00:00:00
abstract：PURPOSE:To characterize factor(s) contained in apical medium of primary cultured rat alveolar epithelial type II cell-like monolayers (RAECM-II) that enhance insulin absorption across alveolar epithelial cells. MATERIALS AND METHODS:Primary rat alveolar epithelial cell monolayers cultured on Transwells in the presence...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9301-9
更新日期：2007-09-01 00:00:00
abstract：:Semitelechelic poly[N-(2-hydroxypropyl)methacrylamide]s (ST-PHPMA) containing one amino end-group and differing in molecular weight were synthesized by radical polymerization in the presence of 2-aminoethanethiol (AET) as chain transfer agent. These polymers were covalently attached via amide bonds to the surface of n...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016247206531
更新日期：1995-05-01 00:00:00
abstract：PURPOSE:A novel bioequivalence limit is proposed taking into account the therapeutic window. METHODS:The therapeutic range is introduced as the ratios maximum tolerated dose/therapeutic dose (MTD/D) and the therapeutic dose/lowest effective dose. The performance of the new acceptance range was compared with the method...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9680-6
更新日期：2008-11-01 00:00:00
abstract：PURPOSE:To develop and subsequently evaluate a novel phase inversion-based method used to formulate lipidic nanocapsules. METHODS:Mechanical properties of emulsions prepared by multiinversion phase processes were investigated using a drop tensiometer. Based on the results obtained, a formulation process was developed ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016121319668
更新日期：2002-06-01 00:00:00
abstract：PURPOSE:The in-situ particle size of delavirdine mesylate in dry mix and tablets was determined. METHODS:Optical microscopy and fluorescence microscopy combined with image analysis were used for qualitative and quantitative measurements. RESULTS:Using optical microscopy, it was demonstrated qualitatively that fragmen...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018875130152
更新日期：1999-04-01 00:00:00
abstract：:An alternative procedure for the simultaneous determination of trimethoprim and sulfamethoxazole in an intravenous pharmaceutical formulation is presented. Infrared spectra of 14 calibration and 6 validation samples were collected using Fourier transform-infrared/attenuated total reflectance (FT-IR/ATR). Partial least...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015957632242
更新日期：1989-07-01 00:00:00
abstract：PURPOSE:Predicting human skin permeability of chemical compounds accurately and efficiently is useful for developing dermatological medicines and cosmetics. However, previous work have two problems; 1) quality of databases used, and 2) methods for prediction models. In this paper, we attempt to solve these two problems...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1629-y
更新日期：2015-07-01 00:00:00
abstract：PURPOSE:Type I collagen accumulates during liver fibrosis primarily because α-complex protein-2 (αCP(2)), encoded by the poly(rC) binding protein 2 (PCBP2) gene, binds to the 3' end of the collagen mRNA and increases its half-life. This study aimed to reverse the pro-fibrogenic effect of alcohol on hepatic stellate cel...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0475-9
更新日期：2011-12-01 00:00:00
abstract：PURPOSE:To design, synthesize, and test synthetic glycopeptide-based delivery systems for gene targeting to hepatocytes by systemic administration. METHODS:All peptides were synthesized by the solid phase method developed using Fmoc chemistry on a peptide synthesizer. The binding of galactosylated peptides to HepG2 ce...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1007533121682
更新日期：2000-04-01 00:00:00
abstract：:Esmolol hydrochloride degrades in aqueous solutions by the hydrolysis of a labile aliphatic carboxyester group. The products are methanol and ASL-8123. The resulting aliphatic carboxylic acid moiety (ASL-8123) has a pK of 4.80, which is within 1 pH unit of the pH of the formulation. ASL-8123 therefore acts as a "secon...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015973425708
更新日期：1988-08-01 00:00:00
abstract：PURPOSE:Study on curcumin dissolved in natural deep eutectic solvents (NADES) was aimed at exploiting their beneficial properties as drug carriers. METHODS:The concentration of dissolved curcumin in NADES was measured. Simulated gastrointestinal fluids were used to determine the concentration of curcumin and quantum c...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2643-2
更新日期：2019-06-03 00:00:00
abstract：:The pharmacokinetics of and biologic response modification by recombinant human interferon-beta ser (rIFN-beta ser) were evaluated in 12 healthy male volunteers. Subjects received a single intravenous (iv) injection of 90 x 10(6) IU of rIFN-beta ser followed by a single or eight consecutive daily 90 x 10(6) IU subcuta...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018902120023
更新日期：1993-04-01 00:00:00
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:The purpose of this study was to develop a new computational fluid dynamics (CFD)-based model of the complex transport and droplet drying kinetics within a laboratory-scale spray dryer, and relate CFD-predicted drying parameters to powder aerosolization metrics from a reference dry powder inhaler (DPI). METHOD...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02806-y
更新日期：2020-05-21 00:00:00
abstract：PURPOSE:Desmopressin acetate (DDAVP) is used parenterally and intranasally in the control of several diseases. Oral administration of DDAVP, while most desirable, is not practical presently due to low bioavailability. The objective of the present study was to explore the feasibility for employing oil-in-water MucoAdhes...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016023111248
更新日期：1996-07-01 00:00:00
