Cell uptake, cytoplasmic diffusion and nuclear access of a 6.5 nm diameter dendrimer.

Abstract:

:Macromolecular crowding and the presence of organelles in the cytosol present barriers to particle mobility, such that it is unclear how nano-carriers can deliver their active agents to the nucleus. In this work a sixth generation amino terminated polyamide polylysine dendrimer (Gly-Lys(63) (NH(2))(64)) (MW 8149, diameter 6.5 nm) which is fluorescent allowed the study of nuclear uptake and mobility in living lung carcinoma (SK/MES-1) and colon adenocarcinoma (Caco-2) cells. The dendrimer is found within 25-45 min of incubation inside the cell nuclei. Living cells were then used to develop a method for the dynamic nuclear uptake study using confocal microscopy. The dynamic uptake of the dendrimer demonstrated here allowed the apparent cytoplasmic diffusion coefficient (D) of the dendrimer to be calculated. Values were found in the range 5.99 x 10(-11)cm(2)s(-1) (SK/MES-1 cells) to 9.82 x 10(-11)cm(2)s(-1) (Caco-2 cells). The difference must reflect variation in the intracellular architecture of the cell types.

journal_name

Int J Pharm

authors

Ruenraroengsak P,Al-Jamal KT,Hartell N,Braeckmans K,De Smedt SC,Florence AT

doi

10.1016/j.ijpharm.2006.12.012

subject

Has Abstract

pub_date

2007-03-01 00:00:00

pages

215-9

issue

2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(06)01061-1

journal_volume

331

pub_type

杂志文章
  • Squalenoyl-gemcitabine/edelfosine nanoassemblies: Anticancer activity in pediatric cancer cells and pharmacokinetic profile in mice.

    abstract::Despite the great advances accomplished in the treatment of pediatric cancers, recurrences and metastases still exacerbate prognosis in some aggressive solid tumors such as neuroblastoma and osteosarcoma. In view of the poor efficacy and toxicity of current chemotherapeutic treatments, we propose a single multitherape...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119345

    authors: Rodríguez-Nogales C,Mura S,Couvreur P,Blanco-Prieto MJ

    更新日期:2020-05-30 00:00:00

  • New silica nanostructure for the improved delivery of topical antibiotics used in the treatment of staphylococcal cutaneous infections.

    abstract::In this paper, we report the synthesis, characterization (FT-IR, XRD, BET, HR-TEM) and bioevaluation of a novel γ-aminobutiric acid/silica (noted GABA-SiO₂ or γ-SiO₂) hybrid nanostructure, for the improved release of topical antibiotics, used in the treatment of Staphylococcus aureus infections. GABA-SiO₂ showed IR ba...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.07.016

    authors: Grumezescu AM,Ghitulica CD,Voicu G,Huang KS,Yang CH,Ficai A,Vasile BS,Grumezescu V,Bleotu C,Chifiriuc MC

    更新日期:2014-03-25 00:00:00

  • Uptake and biodistribution of rizatriptan to blood and brain following different routes of administration in rats.

    abstract::The objective of the present study was to investigate the biodistribution profiles of rizatriptan in the blood and brain of Wistar rats after peroral, subcutaneous, intranasal and intratracheal administration with a particular view to determining the applicability of inhalation delivery to achieve rapid and high avail...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.12.039

    authors: Wang C,Quan LH,Guo Y,Liu CY,Liao YH

    更新日期:2007-06-07 00:00:00

  • Polymer particle erosion controlling drug release. I. Factors influencing drug release and characterization of the release mechanism.

    abstract::The present study deals with controlled drug delivery from hydrocolloid tablets by polymer particle erosion. The influence of excipients and formulation factors on the dissolution behaviour of the methyl hydroxyethyl cellulose (MHEC)-tablets is investigated. Linear drug release with low susceptibility to hydrodynamic ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(01)00596-8

    authors: Zuleger S,Lippold BC

    更新日期:2001-04-17 00:00:00

  • Ethanol effects on drug release from Verapamil Meltrex, an innovative melt extruded formulation.

    abstract::The potential effect of ethanol to accelerate drug release from sustained release (SR) oral formulations is a general concern. Marketed Verapamil is a calcium channel blocker, mainly used as antihypertensive and anti-anginal drug and available in various dose and dosage forms. One is Verapamil Meltrex, combining an in...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.09.052

    authors: Roth W,Setnik B,Zietsch M,Burst A,Breitenbach J,Sellers E,Brennan D

    更新日期:2009-02-23 00:00:00

  • Functionalized single-walled carbon nanotubes: cellular uptake, biodistribution and applications in drug delivery.

    abstract::The unique properties of single-walled carbon nanotubes (SWNTs) enable them to play important roles in many fields. One of their functional roles is to transport cargo into cell. SWNTs are able to traverse amphipathic cell membranes due to their large surface area, flexible interactions with cargo, customizable dimens...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2017.03.017

    authors: Li Z,de Barros ALB,Soares DCF,Moss SN,Alisaraie L

    更新日期:2017-05-30 00:00:00

  • Interaction of gatifloxacin with efflux transporters: a possible mechanism for drug resistance.

    abstract::The purpose of the study is to screen the interactions of fourth generation fluoroquinolone-gatifloxacin with efflux pumps, i.e., P-gp, MRP2 and BCRP. Mechanism of gatifloxacin interaction with efflux transporters may explain its acquired resistance. Such clarification may lead to the development of strategies to over...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.05.027

    authors: Kwatra D,Vadlapatla RK,Vadlapudi AD,Pal D,Mitra AK

    更新日期:2010-08-16 00:00:00

  • Determination of n-octanol/water partition and membrane binding of cationic porphyrins.

    abstract::Porphyrin and their derivatives are being systematically studied as photosensitizers for photodynamic therapy. The ability to predict their membrane partition properties is of key importance to unveil their in vivo activity and applications. Several n-octanol/water partition coefficients (logP(OW)) of porphyrin deriva...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2006.08.008

    authors: Engelmann FM,Rocha SV,Toma HE,Araki K,Baptista MS

    更新日期:2007-02-01 00:00:00

  • Spray-dried chitinosans. Part II: in vitro drug release from tablets made from spray-dried chitinosans.

    abstract:PURPOSE:Application of spray-dried chitinosans as excipients for use in drug delivery systems was explored. METHODS:Spray- and tray-dried chitinosans previously N-deacetylated and depolymerized were used. Directly compressed tablets (200mg) containing tetracycline, chitinosan, and magnesium stearate were prepared. The...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00605-1

    authors: Rege PR,Garmise RJ,Block LH

    更新日期:2003-02-18 00:00:00

  • Effects of gefitinib treatment on cellular uptake of extracellular vesicles in EGFR-mutant non-small cell lung cancer cells.

    abstract::Extracellular vesicles (exosomes, EVs) are cell membrane particles (30-200 nm) secreted by virtually all cells. During intercellular communication in the body, secreted EVs play crucial roles by carrying functional biomolecules (e.g., microRNAs and enzymes) into other cells to affect cellular function, including disea...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118762

    authors: Takenaka T,Nakai S,Katayama M,Hirano M,Ueno N,Noguchi K,Takatani-Nakase T,Fujii I,Kobayashi SS,Nakase I

    更新日期:2019-12-15 00:00:00

  • Positively charged microemulsions for topical application.

    abstract::The study reports pig-skin permeation and skin accumulation of miconazole nitrate (MCZ) from positively charged microemulsions containing water, 1-decanol/1-dodecanol (2:1, w/w), lecithin and/or decyl polyglucoside at different weight ratios, propylene glycol, 1,2 hexanediol and a cationic charge-inducing agent (stear...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.05.065

    authors: Peira E,Carlotti ME,Trotta C,Cavalli R,Trotta M

    更新日期:2008-01-04 00:00:00

  • Dipeptide prodrug approach to evade efflux pumps and CYP3A4 metabolism of lopinavir.

    abstract::Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Moreover, LPV is extensively metabolized by CYP3A4 enzymes. In the present study, dipeptide prodrug approach was employed to circumvent efflux p...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.09.035

    authors: Patel M,Sheng Y,Mandava NK,Pal D,Mitra AK

    更新日期:2014-12-10 00:00:00

  • Novel pH-sensitive microgels prepared using salt bridge.

    abstract::pH-sensitive microgels were prepared by crosslinking carboxymethylcellulose (CMC) and polymeric beta-cyclodextrin (PbetaCD) using (2-hydroxyethyl)trimethylammonium chloride benzoate (TMACB) as a crosslinker. PbetaCD was prepared by reacting epichlorohydrin and beta-CD in an aqueous phase (NaOH solution, 30% (w/w)). TM...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.12.035

    authors: Yang X,Kim JC

    更新日期:2010-03-30 00:00:00

  • General procedure to aid the development of continuous pharmaceutical processes using multivariate statistical modeling - an industrial case study.

    abstract::Streamlining the manufacturing process has been recognized as a key issue to reduce production costs and improve safety in pharmaceutical manufacturing. Although data available from earlier developmental stages are often sparse and unstructured, they can be very useful to improve the understanding about the process un...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2013.01.018

    authors: Tomba E,De Martin M,Facco P,Robertson J,Zomer S,Bezzo F,Barolo M

    更新日期:2013-02-28 00:00:00

  • Preparation, characterization and in vivo pharmacodynamic evaluation of thymopentin loaded poly(lactide acid)/poly(lactide-co-glycolide acid) implants.

    abstract::To avoid the clinical inconvenience of repeated injection of the immune modulator thymopentin (TP5), biodegradable implants comprising a mixed polymer matrix of poly(lactide acid) (PLA) and poly(lactide-co-glycolide acid) (PLGA) were produced using a simple extrusion method. Drug release from these TP5-loaded implants...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.07.036

    authors: Wei G,Jin L,Xu L,Liu Y,Lu W

    更新日期:2010-10-15 00:00:00

  • Stability and activity of hydroxyethyl starch-coated polyplexes in frozen solutions or lyophilizates.

    abstract::Despite their great potential, gene delivery polyplexes have a number of limitations, including their tendency for aggregation in vivo or upon storage. In previous studies, we could show that hydroxyethyl starch (HES)-decoration of polyplexes reduces aggregation in vitro and in vivo. The current study investigates the...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.04.020

    authors: Noga M,Edinger D,Wagner E,Winter G,Besheer A

    更新日期:2014-07-20 00:00:00

  • Isomalt and its diastereomer mixtures as stabilizing excipients with freeze-dried lactate dehydrogenase.

    abstract::The purpose of this research was to study isomalt as a protein-stabilizing excipient with lactate dehydrogenase (LDH) during freeze-drying and subsequent storage and compare it to sucrose, a standard freeze-drying excipient. Four different diastereomer mixtures of isomalt were studied. The stability of the protein was...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2018.01.015

    authors: Tuderman AK,Strachan CJ,Juppo AM

    更新日期:2018-03-01 00:00:00

  • Preparation and evaluation of identifiable quick response (QR)-coded orodispersible films using 3D printer with directly feeding nozzle.

    abstract::3D-printing technology is growing in importance due to increased availability and a wider range of applications. Here, we prepared and evaluated a hot melt pneumatic (HMP) 3D-printed QR (Quick Response)-coded orodispersible film (QRODF) containing a poorly water-soluble aripiprazole (ARP). Moreover, QRODF was formulat...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119405

    authors: Oh BC,Jin G,Park C,Park JB,Lee BJ

    更新日期:2020-06-30 00:00:00

  • Crystal structures, dissolution and pharmacokinetic study on a novel phosphodiesterase-4 inhibitor chlorbipram cocrystals.

    abstract::Cocrystallization of chlorbipram (ChBP), a novel phosphodiesterase-4 (PDE) inhibitor with water insoluble property developed in our lab, was performed to improve the physicochemical properties and bioavailability in the present study. Three new cocrystals with fumaric aicd (FA), gentisic acid (GA) and salicylic acid (...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118984

    authors: Zhou J,Li L,Zhang H,Xu J,Huang D,Gong N,Han W,Yang X,Zhou Z

    更新日期:2020-02-25 00:00:00

  • Multi-modal detection of colon malignancy by NIR-tagged recognition polymers and ultrasound contrast agents.

    abstract::To increase colonoscopy capability to discriminate benign from malignant polyps, we suggest combining two imaging approaches based on targeted polymeric platforms. Water-soluble cationized polyacrylamide (CPAA) was tagged with the near infrared (NIR) dye IR-783-S-Ph-COOH to form Flu-CPAA. The recognition peptide VRPMP...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.11.066

    authors: Bloch M,Jablonowski L,Yavin E,Moradov D,Djavsarov I,Nyska A,Wheatley M,Rubinstein A

    更新日期:2015-01-30 00:00:00

  • Effect of poly(amidoamine) (PAMAM) dendrimer on skin permeation of 5-fluorouracil.

    abstract::The aim of present study is to investigate the effect of poly(amidoamine) (PAMAM) dendrimer on skin permeation of 5-fluorouracil (5FU). Permeation studies were performed using excised porcine skin in a Franz diffusion cell and (14)C labeled 5FU samples were analyzed using liquid scintillation counter. Three different ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.05.034

    authors: Venuganti VV,Perumal OP

    更新日期:2008-09-01 00:00:00

  • GSH responsive nanomedicines self-assembled from small molecule prodrug alleviate the toxicity of cardiac glycosides as potent cancer drugs.

    abstract::Cardiac glycosides (CGs) have been used to treat cancer for hundreds of years. However, the narrow therapeutic window and system toxicity have hindered their wide clinical applications. Herein, the small molecule prodrug strategy and nanotechnology were integrated into one drug delivery system with enhanced therapeuti...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2019.118980

    authors: Zhang H,Zhu Y,Sun C,Xie Y,Adu-Frimpong M,Deng W,Yu J,Xu X,Han Z,Qi G

    更新日期:2020-02-15 00:00:00

  • Development and evaluation of a dimensionless mechanistic pan coating model for the prediction of coated tablet appearance.

    abstract::A mathematical, mechanistic tablet film-coating model has been developed for pharmaceutical pan coating systems based on the mechanisms of atomisation, tablet bed movement and droplet drying with the main purpose of predicting tablet appearance quality. Two dimensionless quantities were used to characterise the produc...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.05.060

    authors: Niblett D,Porter S,Reynolds G,Morgan T,Greenamoyer J,Hach R,Sido S,Karan K,Gabbott I

    更新日期:2017-08-07 00:00:00

  • Microprocessor controlled transdermal drug delivery.

    abstract::Transdermal drug delivery via iontophoresis is reviewed with special focus on the delivery of lidocaine for local anesthesia and fentanyl for patient controlled acute therapy such as postoperative pain. The role of the microprocessor controller in achieving dosimetry, alternating/reverse polarity, pre-programmed, and ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2006.03.053

    authors: Subramony JA,Sharma A,Phipps JB

    更新日期:2006-07-06 00:00:00

  • Novel methods of drug administration for the treatment and care of older patients.

    abstract::The number of older people globally is increasing, contributing to a growing burden of morbidity and mortality. With this shift in population demographic, comes a new challenge in terms of appropriate healthcare for the over 65 years age group. As medication is the principal therapeutic intervention, it is essential t...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2016.01.050

    authors: Quinn HL,Hughes CM,Donnelly RF

    更新日期:2016-10-30 00:00:00

  • Evaluation of the transdermal permeation of different paraben combinations through a pig ear skin model.

    abstract::Although parabens have several features of ideal preservatives, different studies have shown that they may affect human health due to their estrogenic activity. Therefore, various strategies have been applied to reduce their skin penetration. However, the effect of paraben combinations on transdermal permeation has no...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2010.02.006

    authors: Caon T,Costa AC,de Oliveira MA,Micke GA,Simões CM

    更新日期:2010-05-31 00:00:00

  • Preparation and biodisposition of methoxypolyethylene glycol amine-poly(DL-lactic acid) copolymer nanoparticles loaded with pyrene-ended poly(DL-lactic acid).

    abstract::A formyl group-ended poly(DL-lactic acid) (PLA-aldehyde), synthesized in the same manner as reported previously, was utilized to produce the polymeric marker for PLA-related nanoparticles. Namely, pyrene-ended poly(DL-lactic acid) (PLA-pyrene) was prepared as a polymeric marker by the reductive amination of PLA-aldehy...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.03.011

    authors: Sasatsu M,Onishi H,Machida Y

    更新日期:2008-06-24 00:00:00

  • In vitro evaluation of the dissolution behaviour of itraconazole in bio-relevant media.

    abstract::Drugs in the gastrointestinal tract are exposed to a medium of partially digested food, comprising mixtures of fat, protein and carbohydrate. The dissolution behaviour of itraconazole was evaluated in bio-relevant media which were developed to take this into account. Media containing milk with different fat contents, ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.09.003

    authors: Ghazal HS,Dyas AM,Ford JL,Hutcheon GA

    更新日期:2009-01-21 00:00:00

  • Construction and physiochemical characterisation of a multi-composite, potential oral vaccine delivery system (VDS).

    abstract::An increasing human population requires a secure food supply and a cost effective, oral vaccine delivery system for livestock would help facilitate this end. Recombinant antigen adsorbed onto silica beads and coated with myristic acid, was released (∼15% (w/v)) over 24 h at pH 8.8. At pH 2, the myristic acid acted as ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2014.03.046

    authors: Pettit MW,Dyer PD,Mitchell JC,Griffiths PC,Alexander B,Cattoz B,Heenan RK,King SM,Schweins R,Pullen F,Wicks SR,Richardson SC

    更新日期:2014-07-01 00:00:00

  • Roll compaction process modeling: transfer between equipment and impact of process parameters.

    abstract::In this study, the roll compaction of an intermediate drug load formulation was performed using horizontally and vertically force fed roll compactors. The horizontally fed roll compactor was equipped with an instrumented roll technology allowing the direct measurement of normal stress at the roll surface, while the ve...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.02.042

    authors: Souihi N,Reynolds G,Tajarobi P,Wikström H,Haeffler G,Josefson M,Trygg J

    更新日期:2015-04-30 00:00:00