In vitro and in vivo evaluation of a melamine dendrimer as a vehicle for drug delivery.

Abstract:

:Cell-based and acute and subchronic in vivo toxicity profiles of a dendrimer based on melamine reveal that this class of molecules warrants additional study as vehicles for drug delivery. In cell culture, a substantial decrease in viability was observed at 0.1 mg/mL. For the acute studies, mice were administered 2.5, 10, 40 and 160 mg/kg of dendrimer via i.p. injection. At 160 mg/kg, 100% mortality was seen 6-12 h after injection. For the other cohorts, blood chemistry work revealed no renal damage was taking place at 48 h. Liver enzyme activity nearly doubled for the mice treated at 40 mg/kg suggesting hepatotoxicity. For the subchronic studies, three i.p. injections of 2.5-40 mg/kg of dendrimers were administered at 3-week intervals. No mortality was observed. Forty-eight hours following the last administration, blood chemistry revealed no renal damage, but liver damage was indicated by elevated serum enzyme activity at the highest dose. Histopathological data further confirms that doses up to 10 mg/kg show no hepatic damage at subchronic doses. However, subchronic doses at 40 mg/kg lead to extensive liver necrosis.

journal_name

Int J Pharm

authors

Neerman MF,Zhang W,Parrish AR,Simanek EE

doi

10.1016/j.ijpharm.2004.04.023

keywords:

subject

Has Abstract

pub_date

2004-08-20 00:00:00

pages

129-32

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378517304002790

journal_volume

281

pub_type

杂志文章,评审
  • Development of machine learning models of β-cyclodextrin and sulfobutylether-β-cyclodextrin complexation free energies.

    abstract::A new set of 142 experimentally determined complexation constants between sulfobutylether-β-cyclodextrin and diverse organic guest molecules, and 78 observations reported in literature, were used for the development of the QSPR models by the two machine learning regression methods - Cubist and Random Forest. Similar m...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.03.065

    authors: Merzlikine A,Abramov YA,Kowsz SJ,Thomas VH,Mano T

    更新日期:2011-10-14 00:00:00

  • Efficient incorporation and protection of lansoprazole in cyclodextrin metal-organic frameworks.

    abstract::Lansoprazole (LPZ) is an acid pump inhibitor, which readily degrades upon acidic or basic conditions and under heating. We investigated here LPZ stability upon incorporation in particles made of cyclodextrin metal-organic frameworks (CD-MOFs). LPZ loaded CD-MOFs were successfully synthesized, reaching high LPZ payload...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119442

    authors: Li X,Porcino M,Martineau-Corcos C,Guo T,Xiong T,Zhu W,Patriarche G,Péchoux C,Perronne B,Hassan A,Kümmerle R,Michelet A,Zehnacker-Rentien A,Zhang J,Gref R

    更新日期:2020-07-30 00:00:00

  • Improvement of antischistosomal activity of praziquantel by incorporation into phosphatidylcholine-containing liposomes.

    abstract::Praziquantel (PZQ) is effective against all known species of Schistosomes that infect humans. The failure of mass treatment of schistosomiasis has been attributed to the fact that therapy is not sufficiently long-lasting. This effect may be due to the low bioavailability of PZQ that has a low hydrosolubility and fast ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2005.02.009

    authors: Mourão SC,Costa PI,Salgado HR,Gremião MP

    更新日期:2005-05-13 00:00:00

  • Effect of varying the restriction degree of 4-aminopyridine release from HPMC matrices on the mechanism controlling the process.

    abstract::Among different technological variables that influence drug release from hydrophilic matrices, different proportions of the polymer and a water-soluble excipient have been used to control the drug release properties. These variables were used to modify the drug release rate and to examine its effect on the mechanism c...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(03)00150-9

    authors: Martínez-González I,Villafuerte-Robles L

    更新日期:2003-05-12 00:00:00

  • Polymorphism and stability of ibuprofen/nicotinamide cocrystal: The effect of the crystalline synthesis method.

    abstract::The development over the past decade of design strategies for cocrystal preparation have led to numerous methods for the synthesis of cocrystal without take care of their influence on the precise structure and stability of cocrystalline states. On the other hand the mechanism of cocrystal formation remains widely uncl...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119454

    authors: Guerain M,Guinet Y,Correia NT,Paccou L,Danède F,Hédoux A

    更新日期:2020-06-30 00:00:00

  • Controlled dual release of basic fibroblast growth factor and indomethacin from heparin-conjugated polymeric micelle.

    abstract::This work describes the development of heparinized polymeric micelle as a novel injectable carrier for the dual drug delivery that can simultaneously release basic fibroblast growth factor (bFGF) and indomethacin (IMC), which can promote the regeneration of damaged tissue and prevent the inflammatory response after im...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2007.06.025

    authors: Lee JS,Bae JW,Joung YK,Lee SJ,Han DK,Park KD

    更新日期:2008-01-04 00:00:00

  • Terahertz pulsed spectroscopy and imaging for pharmaceutical applications: a review.

    abstract::The terahertz region of the electromagnetic spectrum spans the frequency range between the infrared and the microwave. Traditionally the exploitation of this spectral region has been difficult owing to the lack of suitable source and detector. Over the last ten years or so, terahertz technology has advanced considerab...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2011.01.012

    authors: Shen YC

    更新日期:2011-09-30 00:00:00

  • Tailoring microstructural, drug release properties, and antichagasic efficacy of biocompatible oil-in-water benznidazol-loaded nanoemulsions.

    abstract::This study explored the transition of lamellar-type liquid crystal (LLC) to biocompatible oil-in-water nanoemulsions able to modify benznidazole (BNZ) release and target the drug to cells infected with the T. cruzi parasite. Three cosolvents (2methylpyrrolidone [NMP], polyethylene glycol [POL], and propylene glycol [P...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2018.11.041

    authors: Streck L,Sarmento VHV,de Menezes RPRPB,Fernandes-Pedrosa MF,Martins AMC,da Silva-Júnior AA

    更新日期:2019-01-30 00:00:00

  • Compression of pellets coated with various aqueous polymer dispersions.

    abstract::Pellets coated with a new aqueous polyvinyl acetate dispersion, Kollicoat SR 30 D, could be compressed into tablets without rupture of the coating providing unchanged release profiles. In contrast, the compression of pellets coated with the ethylcellulose dispersion, Aquacoat ECD 30, resulted in rupture of the coating...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.03.019

    authors: Dashevsky A,Kolter K,Bodmeier R

    更新日期:2004-07-26 00:00:00

  • Macromolecular prodrugs: X. Kinetics of fenoprofen release from PHEA-fenoprofen conjugate.

    abstract::The kinetics of fenoprofen release from poly[alpha,beta-(N-2-hydroxyethyl-DL-aspartamide)]-fenoprofen conjugate (PHEA-Fen) in aqueous buffer solutions (pH 10 and 1.1), simulated gastric (SGF) and intestinal fluids (SIF) was studied. In borate buffer pH 10, the following rate constants were obtained: k=0.2659 (t=60 deg...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(02)00197-7

    authors: van der Merwe T,Boneschans B,Zorc B,Breytenbach J,Zovko M

    更新日期:2002-07-25 00:00:00

  • 3D printing of tablets using inkjet with UV photoinitiation.

    abstract::Additive manufacturing (AM) offers significant potential benefits in the field of drug delivery and pharmaceutical/medical device manufacture. Of AM processes, 3D inkjet printing enables precise deposition of a formulation, whilst offering the potential for significant scale up or scale out as a manufacturing platform...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.06.085

    authors: Clark EA,Alexander MR,Irvine DJ,Roberts CJ,Wallace MJ,Sharpe S,Yoo J,Hague RJM,Tuck CJ,Wildman RD

    更新日期:2017-08-30 00:00:00

  • Data-smart machine learning methods for predicting composition-dependent Young's modulus of pharmaceutical compacts.

    abstract::The ability to predict mechanical properties of compacted powder blends of Active Pharmaceutical Ingredients (API) and excipients solely from component properties can reduce the amount of 'trial-and-error' involved in formulation design. Machine Learning (ML) can reduce model development time and effort with the imper...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.120049

    authors: Thomas S,Palahnuk H,Amini H,Akseli I

    更新日期:2021-01-05 00:00:00

  • Preparation and evaluation of anti-neuroexcitation peptide (ANEP) loaded N-trimethyl chitosan chloride nanoparticles for brain-targeting.

    abstract::Anti-neuroexcitation peptide (ANEP) is a promising candidate for the treatment of neuroexcitation-associated diseases. N-Trimethyl chitosan (TMC) with different degrees of quaternization was synthesized, characterized and evaluated as a brain-targeting delivery vehicle for ANEP. ANEP-loaded TMC nanoparticles were prep...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2009.11.002

    authors: Wang S,Jiang T,Ma M,Hu Y,Zhang J

    更新日期:2010-02-15 00:00:00

  • Occlusion effect on transcutaneous NSAID delivery from conventional and carrier-based formulations.

    abstract::We studied skin occlusion effects in vitro and in vivo on local and systemic delivery of ketoprofen across the organ, using the drug in a conventional non-occlusive topical gel (Togal Mobil-Gel), an occlusive tape (Mohrus), and the new targeted analgesic (Diractin), comprising ultradeformable, hydrophilic carriers in ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.04.005

    authors: Cevc G,Mazgareanu S,Rother M,Vierl U

    更新日期:2008-07-09 00:00:00

  • Transferosomes as nanocarriers for drugs across the skin: Quality by design from lab to industrial scale.

    abstract::Transferosomes, also known as transfersomes, are ultradeformable vesicles for transdermal applications consisting of a lipid bilayer with phospholipids and an edge activator and an ethanol/aqueous core. Depending on the lipophilicity of the active substance, it can be encapsulated within the core or amongst the lipid ...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2019.118817

    authors: Fernández-García R,Lalatsa A,Statts L,Bolás-Fernández F,Ballesteros MP,Serrano DR

    更新日期:2020-01-05 00:00:00

  • Nanohybrid biodegradable scaffolds for TGF-β3 release for the chondrogenic differentiation of human mesenchymal stem cells.

    abstract::An ideal scaffold for bone tissue engineering should have chondroinductive, biodegradable, and biocompatible properties, as well as the ability to absorb and slowly release the biological molecules. In order to develop such a system to support bone tissue regeneration, in the present study, we developed a three-dimens...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2020.119248

    authors: Qasim M,Le NXT,Nguyen TPT,Chae DS,Park SJ,Lee NY

    更新日期:2020-05-15 00:00:00

  • Vesicles as antibiotic carrier: State of art.

    abstract::Antimicrobial resistance (AMR) has become a global health problem. Bacteria are able to adapt to different environments, with the presence or absence of a host, forming colonies and biofilms. In fact, biofilm formation confers chemical protection to the microbial cells, thus making most of the conventional antibiotics...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2020.119478

    authors: Marchianò V,Matos M,Serrano-Pertierra E,Gutiérrez G,Blanco-López MC

    更新日期:2020-07-30 00:00:00

  • On the selection of an opioid for local skin analgesia: Structure-skin permeability relationships.

    abstract::Recent studies demonstrated that post-herpetical and inflammatory pain can be locally managed by morphine gels, empirically chosen. Aiming to rationalize the selection of the most suitable opioid for the cutaneous delivery, we studied the in vitro penetration through human epidermis of eight opioids, evidencing the cr...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2015.04.071

    authors: Musazzi UM,Matera C,Dallanoce C,Vacondio F,De Amici M,Vistoli G,Cilurzo F,Minghetti P

    更新日期:2015-07-15 00:00:00

  • Search for technological reasons to develop a capsule or a tablet formulation with respect to wettability and dissolution.

    abstract::Proquazone, a poorly wettable compound, was used as a model drug in the search for reasons to develop a capsule or tablet formulation. The capsules were filled with proquazone as active ingredient, with lactose monohydrate (200 mesh) as filler and with magnesium stearate as lubricant. The tablet was made out of a gran...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2004.09.006

    authors: von Orelli J,Leuenberger H

    更新日期:2004-12-09 00:00:00

  • Sterilization of implantable polymer-based medical devices: A review.

    abstract::This review article is focused on the sterilization techniques used for polymer-based implantable medical devices as well as the regulatory aspects governing sterile medical devices. Polymeric materials are increasingly used in implantable devices due to their biodegradable and biocompatible nature. Patients and medic...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2017.12.003

    authors: Tipnis NP,Burgess DJ

    更新日期:2018-06-15 00:00:00

  • Importance of in vitro dissolution conditions for the in vivo predictability of an amorphous solid dispersion containing a pH-sensitive carrier.

    abstract::The present study investigated the influence of in vitro dissolution conditions on the in vivo predictability of an amorphous solid dispersion of celecoxib (CCX) in the pH-sensitive polymer Eudragit® S 100. Different doses of a 25:75w/w% CCX:Eudragit® S 100 amorphous solid dispersion (CCX:EUD) were investigated. Durin...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.08.078

    authors: Wendelboe J,Knopp MM,Khan F,Chourak N,Rades T,Holm R

    更新日期:2017-10-05 00:00:00

  • Hydrodynamic size characterization of a self-emulsifying lipid pharmaceutical excipient by Taylor dispersion analysis with fluorescent detection.

    abstract::In this work, the sizing of microemulsion droplets of a lipid-based pharmaceutical excipient (Labrasol® ALF) is performed by Taylor dispersion analysis (TDA) using fluorescent detection. An hydrophobic fluorescent marker is used to tag the microemulsion droplet and to increase the sensitivity of detection (compared to...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2016.09.016

    authors: Chamieh J,Jannin V,Demarne F,Cottet H

    更新日期:2016-11-20 00:00:00

  • Lysozyme-loaded, electrospun chitosan-based nanofiber mats for wound healing.

    abstract::In this study, a blend mixture of chitosan-ethylenediaminetetraacetic acid (CS 2 wt%-EDTA) at a weight ratio of 30/70 and polyvinyl alcohol (PVA) solution (10 wt%) was electrospun to produce fibrous mats with lysozyme (10, 20 and 30 wt%) used for wound healing. The morphology and diameter of the electrospun fiber mats...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2012.02.010

    authors: Charernsriwilaiwat N,Opanasopit P,Rojanarata T,Ngawhirunpat T

    更新日期:2012-05-10 00:00:00

  • Mesoporous silica nanoparticles as a promising skin delivery system for methotrexate.

    abstract::The systemic administration of methotrexate (MTX), a commonly used, antineoplastic drug which is also used in cutaneous disorders, is primarily associated with prolonged retention in the body and consequently with side effects. Innovative drug delivery techniques and alternative administration routes would therefore c...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.07.058

    authors: Sapino S,Oliaro-Bosso S,Zonari D,Zattoni A,Ugazio E

    更新日期:2017-09-15 00:00:00

  • Entrapment and release of saquinavir using novel cationic solid lipid nanoparticles.

    abstract::Cationic solid lipid nanoparticles (CSLNs) with entrapped saquinavir (SQV) were fabricated by microemulsion method. Here, CSLNs were stabilized by polysorbate 80, and the lipid phase contained cationic stearylamine (SA) and dioctadecyldimethyl ammonium bromide (DODAB) and nonionic Compritol 888 ATO (CA) and cacao butt...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2008.08.050

    authors: Kuo YC,Chen HH

    更新日期:2009-01-05 00:00:00

  • Designing optimal formulations for hot-melt coating.

    abstract::Hot-melt coating (HMC) as a solvent-free technology grants faster and more economic coating processes with reduced risk of dissolving the drug during the process. Moreover, traditional coating equipment can be modified to enable the HMC process. Despite the indubitable advantages and feasibility of the process, HMC is...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2017.08.086

    authors: Lopes DG,Salar-Behzadi S,Zimmer A

    更新日期:2017-11-30 00:00:00

  • Generation of Toxoplasma gondii GRA1 protein and DNA vaccine loaded chitosan particles: preparation, characterization, and preliminary in vivo studies.

    abstract::Chitosan microparticles as carriers for GRA-1 protein vaccine were prepared and characterized with respect to loading efficiency and GRA-1 stability after short-term storage. Chitosan nanoparticles as carriers for GRA-1 pDNA vaccine were prepared and characterized with respect to size, zeta potential, and protection o...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/s0378-5173(03)00377-6

    authors: Bivas-Benita M,Laloup M,Versteyhe S,Dewit J,De Braekeleer J,Jongert E,Borchard G

    更新日期:2003-11-06 00:00:00

  • Melt extrusion with poorly soluble drugs - An integrated review.

    abstract::Over the last few decades, hot melt extrusion (HME) has emerged as a successful technology for a broad spectrum of applications in the pharmaceutical industry. As indicated by multiple publications and patents, HME is mainly used for the enhancement of solubility and bioavailability of poorly soluble drugs. This revie...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章,评审

    doi:10.1016/j.ijpharm.2017.10.056

    authors: Repka MA,Bandari S,Kallakunta VR,Vo AQ,McFall H,Pimparade MB,Bhagurkar AM

    更新日期:2018-01-15 00:00:00

  • Distribution of salicylic acid in human stratum corneum following topical application in vivo: a comparison of six different formulations.

    abstract::Distribution of salicylic acid in human stratum corneum from treatment of six different formulations was assessed by quantitation of drug content in sequentially tape-stripped stratum corneum after a single 2-h dose was applied unoccluded to skin on the ventral forearm of four female subjects. The profile and total am...

    journal_title:International journal of pharmaceutics

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1016/s0378-5173(99)00217-3

    authors: Tsai J,Chuang S,Hsu M,Sheu H

    更新日期:1999-10-25 00:00:00

  • Ibuprofen-phospholipid solid dispersions: improved dissolution and gastric tolerance.

    abstract::Solid dispersions of ibuprofen with various phospholipids were prepared, and the effect of phospholipids on the in vitro dissolution and in vivo gastrointestinal toxicity of ibuprofen was evaluated. Most phospholipids improved the dissolution of ibuprofen; dimyristoylphosphatidyl-glycerol (DMPG) had the greatest effec...

    journal_title:International journal of pharmaceutics

    pub_type: 杂志文章

    doi:10.1016/j.ijpharm.2011.11.011

    authors: Hussain MD,Saxena V,Brausch JF,Talukder RM

    更新日期:2012-01-17 00:00:00