abstract：:A big hurdle for the use of protein-based drugs is that they are easily degraded by proteases in the human body. In an attempt to solve this problem, we show the possibility to functionalize TM encapsulin nanoparticles with an mEETI-II knottin miniprotein from the cysteine-stabilized knot class. The resulting particle...

journal_title：Molecular pharmaceutics

authors： Klem R,de Ruiter MV,Cornelissen JJLM

更新日期：2018-08-06 00:00:00

abstract：:Nanoenabled lipid-based drug delivery systems offer a platform to overcome challenges encountered with current failed leads in the treatment of parasitic and infectious diseases. When prepared with FDA or EMA approved excipients, they can be readily translated without the need for further toxicological studies, while ...

journal_title：Molecular pharmaceutics

authors： Smith L,Serrano DR,Mauger M,Bolás-Fernández F,Dea-Ayuela MA,Lalatsa A

更新日期：2018-07-02 00:00:00

abstract：:Photodynamic therapy, a procedure that uses a photosensitizer to enable light therapy selectively at diseased sites, remains underutilized in oncological clinic. To further improve its cancer selectivity, we developed a polymeric nanosystem by conjugating a photosensitizer IRDye 700DX (IR700) and cancer targeting RGD ...

journal_title：Molecular pharmaceutics

authors： Zhao Y,Li F,Mao C,Ming X

更新日期：2018-07-02 00:00:00

abstract：:Neovascular age-related macular degeneration (wet AMD) results from the pathological angiogenesis of choroidal capillaries, which leak fluid within or below the macular region of the retina. The current standard of care for treating wet AMD utilizes intravitreal injections of anti-VEGF antibodies or antibody fragments...

journal_title：Molecular pharmaceutics

authors： Hutton-Smith LA,Gaffney EA,Byrne HM,Caruso A,Maini PK,Mazer NA

更新日期：2018-07-02 00:00:00

abstract：:Lung cancer is a kind of malignant tumor with high morbidity and metastasis tendency. Gambogic acid (GA) has demonstrated significant antitumor activity in vitro, but its poor water-solubility and adverse effects restrict its application in vivo and in clinic. In this study, a passive-targeting GA delivery system was ...

journal_title：Molecular pharmaceutics

authors： Yang Y,Cai H,Yuan X,Xu H,Hu Y,Rui X,Wu J,Chen J,Li J,Gao X,Yin D

更新日期：2018-05-07 00:00:00

abstract：:Active targeting of nanostructures containing chemotherapeutic agents can improve cancer treatment. Here, a three-way junction pocket DNA nanostructure was developed for efficient doxorubicin (Dox) delivery into cancer cells. The three-way junction pocket DNA nanostructure is composed of three strands of AS1411 aptame...

journal_title：Molecular pharmaceutics

authors： Taghdisi SM,Danesh NM,Ramezani M,Yazdian-Robati R,Abnous K

更新日期：2018-05-07 00:00:00

abstract：:Current experimental methodologies used to determine the thermodynamic solubility of an API within a polymer typically involves establishing the dissolution/melting end point of the crystalline API within a physical mixture or through the use of the glass transition temperature measurement of a demixed amorphous solid...

journal_title：Molecular pharmaceutics

authors： Tian Y,Jones DS,Donnelly C,Brannigan T,Li S,Andrews GP

更新日期：2018-04-02 00:00:00

abstract：:Photodynamic therapy (PDT) has been shown to kill cancer cells and improve survival and quality of life in cancer patients, and numerous new approaches have been considered for maximizing the efficacy of PDT. In this study, a new multifunctional nanophotosensitizer Ce6/GE11-(pH)micelle was developed to target epiderma...

journal_title：Molecular pharmaceutics

authors： Chu WY,Tsai MH,Peng CL,Shih YH,Luo TY,Yang SJ,Shieh MJ

更新日期：2018-04-02 00:00:00

abstract：:Pyropheophorbide-a (Pyro) is a highly promising photosensitizer for tumor photodynamic therapy (PDT), although its very limited tumor-accumulation ability seriously restricts its clinical applications. A higher accumulation of photosensitizers is very important for the treatment of deeply seated and larger tumors. The...

journal_title：Molecular pharmaceutics

authors： Li W,Tan S,Xing Y,Liu Q,Li S,Chen Q,Yu M,Wang F,Hong Z

更新日期：2018-04-02 00:00:00

abstract：:Photostability conditions as prescribed by ICH guidelines induced highly reduction-resistant scrambled disulfides that contribute to the population of apparent nonreducible aggregates in an IgG1 mAb. Photoinduced cross-linked species were isolated under reducing conditions using an organic phase size exclusion chromat...

journal_title：Molecular pharmaceutics

authors： Wecksler AT,Yin J,Lee Tao P,Kabakoff B,Sreedhara A,Deperalta G

更新日期：2018-04-02 00:00:00

abstract：:By the combined use of powder and single-crystal X-ray diffraction, solid-state NMR, and molecular modeling, the crystal structures of two systems containing the unusually large tenapanor drug molecule have been determined: the free form, ANHY, and a dihydrochloride salt form, 2HCl. Dynamic nuclear polarization (DNP) ...

journal_title：Molecular pharmaceutics

authors： Nilsson Lill SO,Widdifield CM,Pettersen A,Svensk Ankarberg A,Lindkvist M,Aldred P,Gracin S,Shankland N,Shankland K,Schantz S,Emsley L

更新日期：2018-04-02 00:00:00

abstract：:The primary cause of mortality for glioblastoma (GBM) is local tumor recurrence following standard-of-care therapies, including surgical resection. With most tumors recurring near the site of surgical resection, local delivery of chemotherapy at the time of surgery is a promising strategy. Herein drug-loaded polymer s...

journal_title：Molecular pharmaceutics

authors： Graham-Gurysh E,Moore KM,Satterlee AB,Sheets KT,Lin FC,Bachelder EM,Miller CR,Hingtgen SD,Ainslie KM

更新日期：2018-03-05 00:00:00

abstract：:Nucleic acid biopharmaceuticals are being investigated as potential therapeutics. They need to be incorporated into a biocompatible carrier so as to overcome several biological barriers. Rational development of suitable nanocarriers requires high-quality characterization techniques. While size, concentration, and stab...

journal_title：Molecular pharmaceutics

authors： Zagato E,Vermeulen L,Dewitte H,Van Imschoot G,Vandenbroucke RE,Demeester J,De Smedt SC,Neyts K,Remaut K,Braeckmans K

更新日期：2018-03-05 00:00:00

abstract：:To develop a radioactive metal complex platform for tumor theranostics, we introduced three radiopharmaceutical derivatives of 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic acid-benzothiazole aniline (DO3A-BTA, L1) labeled with medical radioisotopes for diagnosis (68Ga/64Cu) and therapy (177Lu). The tumor-targeting ...

journal_title：Molecular pharmaceutics

authors： Park JA,Lee JW,Kim HK,Shin UC,Lee KC,Kim TJ,Chang Y,Kim KM,Kim JY,Lee YJ

更新日期：2018-03-05 00:00:00

abstract：:Amino acids derivative are well established molecular probes for diagnosis of a variety of cancer using positron emission tomography (PET). Recently, boramino acid (BAAs) was found as a prospective molecular platform for developing PET tracer. The objective of this study was to develop a 18F-labeled alanine derivative...

journal_title：Molecular pharmaceutics

authors： Liu H,Han Y,Li J,Qin M,Fu Q,Wang C,Liu Z

更新日期：2018-03-05 00:00:00

abstract：:The most promising F508del-CFTR corrector, VX-809, has been unsuccessful as an effective, stand-alone treatment for CF patients, but the rescue effect in combination with other drugs may confer an acceptable level of therapeutic benefit. Targeting cellular factors that modify trafficking may act to enhance the cell su...

journal_title：Molecular pharmaceutics

authors： Perkins LA,Fisher GW,Naganbabu M,Schmidt BF,Mun F,Bruchez MP

更新日期：2018-03-05 00:00:00

abstract：:Multidrug resistance (MDR) is the major obstacle for chemotherapy. In a previous study, we have successfully synthesized a novel doxorubicin (DOX) derivative modified by triphenylphosphonium (TPP) to realize mitochondrial delivery of DOX and showed the potential of this compound to overcome DOX resistance in MDA-MB-43...

journal_title：Molecular pharmaceutics

authors： Liu HN,Guo NN,Wang TT,Guo WW,Lin MT,Huang-Fu MY,Vakili MR,Xu WH,Chen JJ,Wei QC,Han M,Lavasanifar A,Gao JQ

更新日期：2018-03-05 00:00:00

abstract：:The biodistribution of dendronized iron oxides, NPs10@D1_DOTAGA and melanin-targeting NPs10@D1_ICF_DOTAGA, was studied in vivo using magnetic resonance imaging (MRI) and planar scintigraphy through [177Lu]Lu-radiolabeling. MRI experiments showed high contrast power of both dendronized nanoparticles (DPs) and hepatobil...

journal_title：Molecular pharmaceutics

authors： Bordeianu C,Parat A,Piant S,Walter A,Zbaraszczuk-Affolter C,Meyer F,Begin-Colin S,Boutry S,Muller RN,Jouberton E,Chezal JM,Labeille B,Cinotti E,Perrot JL,Miot-Noirault E,Laurent S,Felder-Flesch D

更新日期：2018-02-05 00:00:00

abstract：:Pancreatic ductal adenocarcinoma (PDAC) is highly chemo-resistant and has an extremely poor patient prognosis, with a survival rate at five years of <8%. There remains an urgent need for innovative treatments. Targeting polyamine biosynthesis through inhibition of ornithine decarboxylase with difluoromethylornithine (...

journal_title：Molecular pharmaceutics

authors： Gitto SB,Pandey V,Oyer JL,Copik AJ,Hogan FC,Phanstiel O 4th,Altomare DA

更新日期：2018-02-05 00:00:00

abstract：:Polymeric nanoparticles (NPs) are extremely attractive vaccine adjuvants, able to promote antigen delivery and in some instances, exert intrinsic immunostimulatory properties that enhance antigen specific humoral and cellular immune responses. The poly-ε-caprolactone (PCL)/chitosan NPs were designed with the aim of be...

journal_title：Molecular pharmaceutics

authors： Jesus S,Soares E,Borchard G,Borges O

更新日期：2018-01-02 00:00:00

abstract：:In vitro antibody discovery and/or affinity maturation are often performed using antibody fragments (Fabs), but most monovalent Fabs are reformatted as bivalent IgGs (monoclonal antibodies, mAbs) for therapeutic applications. One problem related to reformatting antibodies is that the bivalency of mAbs can lead to incr...

journal_title：Molecular pharmaceutics

authors： Alam ME,Geng SB,Bender C,Ludwig SD,Linden L,Hoet R,Tessier PM

更新日期：2018-01-02 00:00:00

abstract：:Currently, the most prominent barrier to the success of orally delivered paclitaxel (PTX) is the extremely limited bioavailability of delivered therapeutic. In light of this issue, an amphiphilic sulfhydrylated N-deoxycholic acid-N,O-hydroxyethyl chitosan (TGA-DHC) was synthesized to improve the oral bioavailability o...

journal_title：Molecular pharmaceutics

authors： Yu Y,Huo M,Fu Y,Xu W,Cai H,Yao L,Chen Q,Mu Y,Zhou J,Yin T

更新日期：2017-12-04 00:00:00

abstract：:The tumor microenvironments are often acidic and overexpress specific enzymes. In this work, we synthesized a poly(AA-b-NIPAAm) copolymer (PAA-b-PNIPAAm) using a reversible addition-fragmentation chain transfer (RAFT) polymerization method. PAA-b-PNIPAAm and a cationic protein (protamine) were self-assembled into nano...

journal_title：Molecular pharmaceutics

authors： Don TM,Lu KY,Lin LJ,Hsu CH,Wu JY,Mi FL

更新日期：2017-12-04 00:00:00

abstract：:The potential use of poly(dimethylsiloxane) (PDMS) as an in vitro biomimetic analogue of the passive drug absorption process in the human gastrointestinal tract (GI) is assessed. PDMS is biomimetic because of similarities in small molecule transport, such as mechanism, ionization selectivity, lipophilicity. Nine molec...

journal_title：Molecular pharmaceutics

authors： Sinko PD,Gidley D,Vallery R,Lamoureux A,Amidon GL,Amidon GE

更新日期：2017-12-04 00:00:00

abstract：:There are an increasing number of studies showing the order of drug presentation plays a critical role in achieving optimal combination therapy. Here, a nanoparticle design is presented using ion pairing and drug-polymer conjugate for the sequential delivery of gefitinib (Gi) and doxorubicin (Dox) targeting epidermal ...

journal_title：Molecular pharmaceutics

authors： Zhou Z,Jafari M,Sriram V,Kim J,Lee JY,Ruiz-Torres SJ,Waltz SE

更新日期：2017-12-04 00:00:00

abstract：:The drug-induced accumulation of phospholipids in lysosomes of various tissues is predominantly observed in regular repeat dose studies, often after prolonged exposure, and further investigated in mechanistic studies prior to candidate nomination. The finding can cause delays in the discovery process inflicting high c...

journal_title：Molecular pharmaceutics

authors： Fusani L,Brown M,Chen H,Ahlberg E,Noeske T

更新日期：2017-12-04 00:00:00

abstract：:The effect of a lipidated prodrug of mitomycin C (MLP) on the membrane of a pegylated liposome formulation (PL-MLP), also known as Promitil, was characterized through high-sensitivity differential scanning calorimetry (DSC) and cryo-TEM. The thermodynamic analysis demonstrated that MLP led to the formation of heteroge...

journal_title：Molecular pharmaceutics

authors： Wei X,Patil Y,Ohana P,Amitay Y,Shmeeda H,Gabizon A,Barenholz Y

更新日期：2017-12-04 00:00:00

abstract：:This study determined intraluminal ethanol concentrations (stomach and duodenum) in fed healthy volunteers after the consumption of common alcoholic beverages (beer, wine, and whisky). The results of this study were compared with a previous study in fasted volunteers. Five healthy volunteers were recruited in a crosso...

journal_title：Molecular pharmaceutics

authors： Rubbens J,Riethorst D,Brouwers J,Wolfs K,Adams E,Tack J,Augustijns P

更新日期：2017-12-04 00:00:00

abstract：:Currently, the screening of new drug candidates for intestinal permeation is typically based on in vitro models which give no information regarding regional differences along the gut. When evaluation of intestinal permeability by region is undertaken, two preclinical rat models are commonly used, the Ussing chamber me...

journal_title：Molecular pharmaceutics

authors： Roos C,Dahlgren D,Sjögren E,Tannergren C,Abrahamsson B,Lennernäs H

更新日期：2017-12-04 00:00:00

abstract：:For the purpose of improving the tumor delivery of doxorubicin (DOX), a kind of peptide-DOXO conjugate was designed and prepared, in which the peptide composed of an albumin-binding domain (ABD) and a tumor-specific internalizing sequence (RGDK or RPARPAR) was conjugated to a (6-maleimidocaproyl) hydrazone derivative ...

journal_title：Molecular pharmaceutics

authors： Liu L,Zhang C,Li Z,Wang C,Bi J,Yin S,Wang Q,Yu R,Liu Y,Su Z

更新日期：2017-11-06 00:00:00

abstract：:Although tumor-targeting nanovehicles for hepatocellular carcinoma (HCC) chemotherapy have attracted great research and clinic interest, the poor cancer penetration, inefficient cellular uptake, and slow intracellular drug release greatly compromise their therapeutic outcomes. In this work, a multifunctional mixed mic...

journal_title：Molecular pharmaceutics

authors： Zhang J,Zheng Y,Xie X,Wang L,Su Z,Wang Y,Leong KW,Chen M

更新日期：2017-11-06 00:00:00

abstract：:Bioadhesive nanoparticles based on poly(vinyl methyl ether/maleic anhydride) (PVMMA) and poly(ethylene glycol) methyl ether-b-poly(d,l-lactic acid) (mPEG-b-PLA) were produced by the emulsification solvent evaporation method. Paclitaxel was utilized as the model drug, with an encapsulation efficiency of up to 90.2 ± 4....

journal_title：Molecular pharmaceutics

authors： Wang Q,Li C,Ren T,Chen S,Ye X,Guo H,He H,Zhang Y,Yin T,Liang XJ,Tang X

更新日期：2017-10-02 00:00:00

abstract：:In this work we measured self-diffusion coefficients of 5 drugs (aspirin, caffeine, ethionamide, salicylic acid, and paracetamol) and 11 biologically active compounds of similar structure in deuterated water and 1-octanol by NMR. It has been found that an increase in the van der Waals volume of the molecules of the st...

journal_title：Molecular pharmaceutics

authors： Blokhina SV,Volkova TV,Golubev VA,Perlovich GL

更新日期：2017-10-02 00:00:00

abstract：:Lung-delivered polymer nanoparticles provoked dysfunction of the essential lung surfactant system. A steric shielding of the nanoparticle surface with poloxamers could minimize the unwanted interference of polymer nanoparticles with the biophysical function of lung surfactant. The extent of poly(styrene) and poly(lact...

journal_title：Molecular pharmaceutics

authors： Beck-Broichsitter M,Bohr A,Ruge CA

更新日期：2017-10-02 00:00:00

abstract：:Many cancer therapy regimes still rely heavily on the systemic administration of toxic chemotherapeutic agents. Ultrasound contrast agents consisting of microbubbles (MBs) have emerged as a drug delivery vehicle to overcome the challenges associated with systemic chemotherapy. Here, we describe the development of non-...

journal_title：Molecular pharmaceutics

authors： Jablonowski LJ,Teraphongphom NT,Wheatley MA

更新日期：2017-10-02 00:00:00

abstract：:Understanding protein stability is central to combatting protein aggregation diseases and developing new protein therapeutics. At the high concentrations often present in biological systems, purified proteins can exhibit undesirable high solution viscosities and poor solubilities mediated by short-range electrostatic ...

journal_title：Molecular pharmaceutics

authors： Laber JR,Dear BJ,Martins ML,Jackson DE,DiVenere A,Gollihar JD,Ellington AD,Truskett TM,Johnston KP,Maynard JA

更新日期：2017-10-02 00:00:00

abstract：:Protein drugs play an important role in modern day medicine. Typically, these proteins are formulated as liquids requiring cold chain processing. To circumvent the cold chain and achieve better storage stability, these proteins can be dried in the presence of carbohydrates. We demonstrate that thermal gradient mid- an...

journal_title：Molecular pharmaceutics

authors： Mensink MA,Šibík J,Frijlink HW,van der Voort Maarschalk K,Hinrichs WLJ,Zeitler JA

更新日期：2017-10-02 00:00:00

abstract：:Abnormal tumor vessels impede the transport and distribution of chemotherapeutics, resulting in low drug concentration at tumor sites and compromised drug efficacy. Normalizing tumor vessels can modulate tumor vascular permeability, alleviate tumor hypoxia, increase blood perfusion, attenuate interstitial fluid pressu...

journal_title：Molecular pharmaceutics

authors： Xiao W,Ruan S,Yu W,Wang R,Hu C,Liu R,Gao H

更新日期：2017-10-02 00:00:00

abstract：:We report the development of sponge Haliclona sp. spicules, referred to as SHS, and its topical application in skin delivery of hydrophilic biomacromolecules, a series of fluorescein isothiocyanate-dextrans (FDs). SHS are silicious oxeas which are sharp-edged and rod-shaped (∼120 μm in length and ∼7 μm in diameter). S...

journal_title：Molecular pharmaceutics

authors： Zhang S,Ou H,Liu C,Zhang Y,Mitragotri S,Wang D,Chen M

更新日期：2017-09-05 00:00:00

abstract：:The weak base memantine is actively secreted into urine, however the underlying mechanisms are insufficiently understood. Potential candidates involved in memantine renal secretion are organic cation transporter 2 (OCT2) and multidrug and toxin extrusion proteins (MATE1, MATE2-K). The aim of this in vitro study was th...

journal_title：Molecular pharmaceutics

authors： Müller F,Weitz D,Derdau V,Sandvoss M,Mertsch K,König J,Fromm MF

更新日期：2017-09-05 00:00:00