abstract：:The objective was to investigate (trans)corneal and transscleral iontophoresis of biolabile amino acid ester prodrugs of aciclovir (ACV-X, X = Arg, Gly and Trp) as a means to increase ocular bioavailability of ACV. Prodrugs displayed tissue-dependent susceptibility to hydrolysis. Iontophoresis of ACV-Arg, ACV-Gly and ...

journal_title：International journal of pharmaceutics

authors： Chen Y,Kalia YN

更新日期：2018-01-30 00:00:00

abstract：:In the pharmaceutical industry, in vitro dissolution testing ofsolid oral dosage forms is a very important tool for drug development and quality control. However, ion-pairing interaction between the ionic drugand surfactants in dissolution medium often occurs, resulting in inconsistent and incomplete drug release. The...

journal_title：International journal of pharmaceutics

authors： Huang Z,Parikh S,Fish WP

更新日期：2018-01-15 00:00:00

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

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

abstract：:Reproducibility of die fill during tablet production is critical to ensure consistent tablet drug content and mechanical attributes. In the production of mini-tablets, tablets smaller than 6mm, achievement of uniform die fill is much more challenging. Powder flow is often associated with die fill accuracy but this rel...

journal_title：International journal of pharmaceutics

authors： Goh HP,Heng PWS,Liew CV

更新日期：2017-12-20 00:00:00

abstract：:A bilayer tablet, which consisted of telmisartan and amlodipine besylate, was formulated based on a Quality by Design (QbD) approach. The control and response factors were determined based on primary knowledge and the target values of the control tablet (Twynsta®). A D-optimal mixture design was used to obtain the opt...

journal_title：International journal of pharmaceutics

authors： Lee AR,Kwon SY,Choi DH,Park ES

更新日期：2017-12-20 00:00:00

abstract：:Systemic delivery of therapeutic proteins to the central nervous system (CNS) is challenging because of the blood-brain barrier restrictions. Direct intrathecal delivery is possible but does not produce stable concentrations. We are proposing an alternative approach for localized delivery into the CNS based on the Tra...

journal_title：International journal of pharmaceutics

authors： Aronson JP,Katnani HA,Pomerantseva I,Shapir N,Tse H,Miari R,Goltsman H,Mwizerwa O,Neville CM,Neil GA,Eskandar EN,Sundback CA

更新日期：2017-12-20 00:00:00

abstract：:The blending process is a key step in the production of dry powder inhaler formulations, but only little is known about the influence of process parameters. This is especially true for high shear blending of ternary formulations. For this reason, this study aims to investigate the influence of high shear mixing proces...

journal_title：International journal of pharmaceutics

authors： Hertel M,Schwarz E,Kobler M,Hauptstein S,Steckel H,Scherließ R

更新日期：2017-12-20 00:00:00

abstract：PURPOSE:Evaluate ex vivo the bacterial metabolism induced degradation rates of mesalamine (negative control), metronidazole and olsalazine in distal ileum and in cecum. METHODS:The contents of distal ileum and cecum were collected during colonoscopy under anaerobic conditions from twelve healthy adults in the fasted a...

journal_title：International journal of pharmaceutics

authors： Karatza E,Goumas C,Muenster U,Reppas C,Vertzoni M

更新日期：2017-12-20 00:00:00

abstract：:Three dimensional printing technology is gaining in importance because of its increasing availability and wide applications. One of the three dimensional printing techniques is Fused Deposition Modelling (FDM) which works on the basis of hot melt extrusion-well known in the pharmaceutical technology. Combination of fu...

journal_title：International journal of pharmaceutics

authors： Jamróz W,Kurek M,Łyszczarz E,Szafraniec J,Knapik-Kowalczuk J,Syrek K,Paluch M,Jachowicz R

更新日期：2017-11-30 00:00:00

abstract：:Self-emulsifying drug delivery systems (SEDDS) are lipid formulations that improve solubility and oral bioavailability of the incorporated drug with poor biopharmaceutical properties. As liquids they are traditionally filled into soft or hard capsules. Transformation of SEDDS into solid dosage form has been extensivel...

journal_title：International journal of pharmaceutics

authors： Mandić J,Zvonar Pobirk A,Vrečer F,Gašperlin M

更新日期：2017-11-30 00:00:00

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

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

更新日期：2017-11-30 00:00:00

abstract：:DNA as a novel biomaterial can be used to fabricate different kinds of DNA nanostructures based on its principle of GC/AT complementary base pairing. Studies have shown that DNA nanostructure is a nice drug carrier to overcome big obstacles existing in cancer therapy such as systemic toxicity and unsatisfied drug effi...

journal_title：International journal of pharmaceutics

authors： Wu D,Wang L,Li W,Xu X,Jiang W

更新日期：2017-11-25 00:00:00

abstract：:The breath-actuated mechanism (BAM) is a mechanical unit included in NEXThaler® with the role of delaying the emission of the drug until the inhalation flow rate of the patient is sufficiently high to detach the drug particles from their carriers. The main objective of this work was to analyse the effect of the presen...

journal_title：International journal of pharmaceutics

authors： Farkas Á,Lewis D,Church T,Tweedie A,Mason F,Haddrell AE,Reid JP,Horváth A,Balásházy I

更新日期：2017-11-25 00:00:00

abstract：:Nanoprecipitation is a simple and increasingly trending method for nanoparticles preparation. The self-assembly feature of poly (ethylene glycol)-poly (lactide-co-glycolic acid) (PEG-PLGA) amphiphilic copolymer into a nanoparticle and its versatile structure makes nanoprecipitation one of the best methods for its prep...

journal_title：International journal of pharmaceutics

authors： Almoustafa HA,Alshawsh MA,Chik Z

更新日期：2017-11-25 00:00:00

abstract：:The focus of the current study was to explore whether immobilization of proteases to microparticles could result in their enhanced penetration into mucus. The proteases papain (PAP) and bromelain (BROM) were covalently attached to a polyacrylate (PAA; Carbopol 971P) via amide bond formation based on carbodiimide react...

journal_title：International journal of pharmaceutics

authors： Mahmood A,Laffleur F,Leonaviciute G,Bernkop-Schnürch A

更新日期：2017-10-30 00:00:00

abstract：:A substantial drug release from poly(lactic-co-glycolic) acid (PLGA) micro- and nanoparticles can occur in the first hours of immersion, which is referred to as burst release. A strong burst release (when not intentional) is to be avoided as it decreases the efficacy of the treatment and could be dangerous to the host...

journal_title：International journal of pharmaceutics

authors： Rodrigues de Azevedo C,von Stosch M,Costa MS,Ramos AM,Cardoso MM,Danhier F,Préat V,Oliveira R

更新日期：2017-10-30 00:00:00

abstract：:Glycerosomes were formulated using 1,2-dimyristoyl-sn-glycero-3-phosphatidycholine (DMPC), diclofenac sodium salt and 10, 20 or 30% glycerol in the water phase, while corresponding liposomes were prepared with the same amount of DMPC and diclofenac, without glycerol. The aim of the present work was to evaluate the eff...

journal_title：International journal of pharmaceutics

authors： Manca ML,Manconi M,Zaru M,Valenti D,Peris JE,Matricardi P,Maccioni AM,Fadda AM

更新日期：2017-10-30 00:00:00

abstract：:Cancer cells increase their metabolism to produce the energy and biomolecules necessary for growth and proliferation. Thus, energy metabolism pathways may serve as targets for anti-cancer therapy. NCL-240 is a second generation anti-cancer drug belonging to the PITenins class of PI3K-Akt inhibitors. Our analysis sugge...

journal_title：International journal of pharmaceutics

authors： Pattni BS,Jhaveri A,Dutta I,Baleja JD,Degterev A,Torchilin V

更新日期：2017-10-30 00:00:00

abstract：:There has been limited research done on the downstream processing of nanosuspensions into solid oral dosage forms. This paper demonstrates the bead layering process with a layering level at 150% and 240%, as well as the selection and justification of the outer phase excipients for tabletability and disintegrating prop...

journal_title：International journal of pharmaceutics

authors： Tan EH,Parmentier J,Low A,Möschwitzer JP

更新日期：2017-10-30 00:00:00

abstract：:Microcrystalline cellulose (MCC) is one of the most important excipients due to its outstanding binding and tableting properties. Owing to the absence of high resolution characterization techniques at the single particle scale, 3D (three dimension) microstructure of MCC and its effects on formulation performance remai...

journal_title：International journal of pharmaceutics

authors： Fang L,Yin X,Wu L,He Y,He Y,Qin W,Meng F,York P,Xu X,Zhang J

更新日期：2017-10-15 00:00:00

abstract：:Rifampicin (Rif) is a broad spectrum antibiotic used as a first line agent in the treatment of mycobacterial infections. However, its low solubility and reduced stability in water limit its bioavailability, thus requiring the use of complex formulations. Here, we present a systematic study of Rif in complex with a met...

journal_title：International journal of pharmaceutics

authors： Angiolini L,Agnes M,Cohen B,Yannakopoulou K,Douhal A

更新日期：2017-10-15 00:00:00

abstract：:Ethionamide (ETH) is a second line antitubercular drug suffering from poor solubility in water and strong tendency to crystallize. These drawbacks were addressed by loading ETH in β-cyclodextrin (βCyD)-based carriers. The drug was incorporated in a molecular state avoiding crystallization even for long-term storage an...

journal_title：International journal of pharmaceutics

authors： Wankar J,Salzano G,Pancani E,Benkovics G,Malanga M,Manoli F,Gref R,Fenyvesi E,Manet I

更新日期：2017-10-15 00:00:00

abstract：:Cyclodextrin-based nanosponges (CD-NSs) are insoluble, highly cross-linked 3D network polymers used in several scientific and technological fields, the main area of investigation concerns the pharmaceutical applications, in which CD-NSs have been mostly employed as drug delivery systems. CD-NSs can be generally groupe...

journal_title：International journal of pharmaceutics

authors： Caldera F,Tannous M,Cavalli R,Zanetti M,Trotta F

更新日期：2017-10-15 00:00:00

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

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

更新日期：2017-10-05 00:00:00

abstract：:Nalbuphine is a semi-synthetic opioid indicated for the relief of moderate to severe pain. Dinalbuphine sebacate (DNS) is a prodrug of nalbuphine for which we have developed long-acting lipophilic formulations in a benzyl benzoate/sesame oil mixture for intramuscular (IM) injection. In this study, we found that the in...

journal_title：International journal of pharmaceutics

authors： Li CJ,Ku MY,Lu CY,Tien YE,Chern WH,Huang JD

更新日期：2017-10-05 00:00:00

abstract：:For drug delivery to the lungs, the aerodynamic size of drug particles plays a predominant role in determining the sites of deposition in the airway, and the particles with the size less than 2μm are highly expected as they will be preferably delivered to the ideal site of alveolar regions. In this paper, a novel plat...

journal_title：International journal of pharmaceutics

authors： Li HY,Xu EY

更新日期：2017-09-15 00:00:00

abstract：:The aim of this study was to investigate the ability of L-leucine (LL) in preventing moisture-induced deterioration in the in vitro aerosolization performance of spray-dried (SD) salbutamol sulfate (SS). Increasing mass fraction of LL (5-80%) were co-spray dried with SS, and the physicochemical properties of the powde...

journal_title：International journal of pharmaceutics

authors： Li L,Leung SSY,Gengenbach T,Yu J,Gao GF,Tang P,Zhou QT,Chan HK

更新日期：2017-09-15 00:00:00

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

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

更新日期：2017-09-15 00:00:00

abstract：:This work reports a novel approach to the assessment of the surface properties of compacts used in Surface Dissolution Imaging (SDI). SDI is useful for determining intrinsic dissolution rate (IDR), an important parameter in early stage drug development. Surface topography, post-compaction and post-SDI run, have been m...

journal_title：International journal of pharmaceutics

authors： Ward A,Walton K,Box K,Østergaard J,Gillie LJ,Conway BR,Asare-Addo K

更新日期：2017-09-15 00:00:00

abstract：:Cyclosporin A (CyA) is an immunosuppressive drug used topically to treat ocular inflammatory disorder such as dry eye disease (DES). It is a lipophilic cyclic peptide with molecular weight of 1202.6Da. The aim of this study was to develop surfactant free aqueous 0.2% (w/v) CyA eye drops where the drug is present in an...

journal_title：International journal of pharmaceutics

authors： Jóhannsdóttir S,Kristinsson JK,Fülöp Z,Ásgrímsdóttir G,Stefánsson E,Loftsson T

更新日期：2017-08-30 00:00:00

abstract：:Chitosan-based nanoparticles prepared by ionotropic gelation are prone to stability issues. The aim of this work is to chemically modify chitosan by grafting to succinate, phthalate, glutarate and phenylsuccinate moieties and to investigate the suitability of the resulting polymers as covalently-crosslinked nanocarrie...

journal_title：International journal of pharmaceutics

authors： Dmour I,Taha MO

更新日期：2017-08-30 00:00:00

abstract：:Docetaxel (DTX) is one of the important antitumor drugs, being used in several common chemotherapies to control leading cancer types. Severe toxicities of the DTX are prominent due to sudden parenteral exposure of desired loading dose to maintain the therapeutic concentration. Field of nanotechnology is leading to res...

journal_title：International journal of pharmaceutics

authors： Choudhury H,Gorain B,Pandey M,Kumbhar SA,Tekade RK,Iyer AK,Kesharwani P

更新日期：2017-08-30 00:00:00

abstract：:A simple and rapid method for radiolabeling of three types of Ag NPs has been performed using 125I isotope, with high labeling yields, >90% without disturbing the optical properties. All the factors affecting labeling yield were studied. In order to monitor the in-vivo tissue uptake of radiolabeled Ag NPs using γ-rays...

journal_title：International journal of pharmaceutics

authors： Farrag NS,El-Sabagh HA,Al-Mahallawi AM,Amin AM,AbdEl-Bary A,Mamdouh W

更新日期：2017-08-30 00:00:00

abstract：:A mechanistic particle scale model is proposed for bilayer tablet compaction. Making bilayer tablets involves the application of first layer compaction pressure on the first layer powder and a second layer compaction pressure on entire powder bed. The bonding formed between the first layer and the second layer particl...

journal_title：International journal of pharmaceutics

authors： Yohannes B,Gonzalez M,Abebe A,Sprockel O,Nikfar F,Kiang S,Cuitiño AM

更新日期：2017-08-30 00:00:00

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

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

abstract：:This study focuses on evaluating the potential of transferring from a batch process to continuous process for manufacturing of the extended release formulation. Metformin hydrochloride (HCl) was used in the model formulation which was intended to contain the high amount of hydrophilic drug. The effects of barrel tempe...

journal_title：International journal of pharmaceutics

authors： Kim SH,Hwang KM,Cho CH,Nguyen TT,Seok SH,Hwang KM,Kim JY,Park CW,Rhee YS,Park ES

更新日期：2017-08-30 00:00:00

abstract：:This work aimed to prove the ability of "ready-to-use" topical vehicles based on alkyl polyglucoside-mixed emulsifier (with/without co-solvent modifications) to replace the conventionally used pharmacopoeial bases (e.g., non-ionic hydrophilic cream) in compounding practice. For this purpose, considering the regulatory...

journal_title：International journal of pharmaceutics

authors： Ilić T,Pantelić I,Lunter D,Đorđević S,Marković B,Ranković D,Daniels R,Savić S

更新日期：2017-08-07 00:00:00

abstract：:The potential of two derivatives of vitamin E, i.e. α-tocopheryl phosphate (TP) and di-α-tocopheryl phosphate (T2P), for the protection and delivery of therapeutics is being investigated in our laboratory and some promising results have been obtained so far. Novel nanocarrier systems containing TP, T2P and different l...

journal_title：International journal of pharmaceutics

authors： Mozafari MR,Javanmard R,Raji M

更新日期：2017-08-07 00:00:00

abstract：:Microporous zeolites of distinct framework types, textural properties and crystal morphologies namely BEA, ZSM and NaX, have been employed as carriers to assess their effect on modulating the dissolution behavior of a BCS II model drug (indomethacin). Preparation of the loaded carriers via the incipient wetness method...

journal_title：International journal of pharmaceutics

authors： Karavasili C,Amanatiadou EP,Kontogiannidou E,Eleftheriadis GK,Bouropoulos N,Pavlidou E,Kontopoulou I,Vizirianakis IS,Fatouros DG

更新日期：2017-08-07 00:00:00

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

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