abstract：:Today, about 50% of men and 15-30% of women suffer from hair loss as well as the associated psychological impact. Drug therapy, especially through topical administration, is the main treatment strategy for stimulating hair regrowth. However, challenges exist due to the skin barrier that hinders drug penetration. To th...

journal_title：Molecular pharmaceutics

authors： Yang G,Chen G,Gu Z

更新日期：2021-02-01 00:00:00

abstract：:Resveratrol (RES) is a nutraceutical with promising anti-inflammatory properties for the treatment of inflammatory bowel diseases (IBD). However, the clinical effectiveness of resveratrol as an oral anti-inflammatory agent is hindered by its extremely poor solubility and poor stability. In this study, we encapsulated ...

journal_title：Molecular pharmaceutics

authors： Pujara N,Wong KY,Qu Z,Wang R,Moniruzzaman M,Rewatkar P,Kumeria T,Ross BP,McGuckin M,Popat A

更新日期：2021-02-01 00:00:00

abstract：:Influenza viruses cause seasonal epidemics and represent a pandemic risk. With current vaccine methods struggling to protect populations against emerging strains, there is a demand for a next-generation flu vaccine capable of providing broad protection. Recombinant biotechnology, combined with nanomedicine techniques,...

journal_title：Molecular pharmaceutics

authors： Sia ZR,Miller MS,Lovell JF

更新日期：2021-02-01 00:00:00

abstract：:Deferoxamine mesylate (DFO) is an FDA-approved, hexadentate iron chelator routinely used to alleviate systemic iron burden in thalassemia major and sickle cell patients. Iron accumulation in these disease states results from the repeated blood transfusions required to manage these conditions. Iron accumulation has als...

journal_title：Molecular pharmaceutics

authors： Farr AC,Xiong MP

更新日期：2021-02-01 00:00:00

abstract：:Heart transplantation (HT) is an effective treatment for end-stage heart disease. However, acute rejection (AR) is still the main cause of death within one year after HT. AR is an acute immune response mediated by T lymphocytes, mainly CD4+ T lymphocytes. This study innovatively develops a radiolabeled probe 99mTc-HYN...

journal_title：Molecular pharmaceutics

authors： Li H,Chen Y,Jin Q,Wu Y,Deng C,Gai Y,Sun Z,Li Y,Wang J,Yang Y,Lv Q,Zhang Y,An R,Lan X,Zhang L,Xie M

更新日期：2021-01-28 00:00:00

abstract：:Photodynamic therapy (PDT) is promising for clinical cancer therapy; however, the efficacy was limited as an individual treatment regimen. Here, an approach synergistically combining PDT and nitric oxide (NO) gas therapy along with destruction of the tumor extracellular matrix (ECM) was presented to eliminate cancer. ...

journal_title：Molecular pharmaceutics

authors： Sun Z,Wang X,Liu J,Wang Z,Wang W,Kong D,Leng X

更新日期：2021-01-11 00:00:00

abstract：:DEK protein is critical to the formation of neutrophil extracellular traps (NETs) in rheumatoid arthritis (RA). Blocking DEK using the aptamer DTA via articular injection has been shown to have robust anti-inflammatory efficacy in a previous study. However, DTA is prone to nuclease degradation and renal clearance in v...

journal_title：Molecular pharmaceutics

authors： Cao J,Su J,An M,Yang Y,Zhang Y,Zuo J,Zhang N,Zhao Y

更新日期：2021-01-04 00:00:00

abstract：:Cold crystallization of amorphous pharmaceuticals is an important aspect in the search to stabilize amorphous or glassy compounds used as amorphous pharmaceutical ingredients (APIs). In the present work, we report results for the isothermal crystallization of the compound GDC-0276 based on differential scanning calori...

journal_title：Molecular pharmaceutics

authors： Cheng S,Chakravarty P,Nagapudi K,McKenna GB

更新日期：2021-01-04 00:00:00

abstract：:In this work, we have developed covalent and low molecular weight docetaxel delivery systems based on conjugation with N-acetyl-d-galactosamine and studied their properties related to hepatocellular carcinoma cells. The resulting glycoconjugates have an excellent affinity to the asialoglycoprotein receptor (ASGPR) in ...

journal_title：Molecular pharmaceutics

authors： Petrov RA,Mefedova SR,Yamansarov EY,Maklakova SY,Grishin DA,Lopatukhina EV,Burenina OY,Lopukhov AV,Kovalev SV,Timchenko YV,Ondar EE,Ivanenkov YA,Evteev SA,Vaneev AN,Timoshenko RV,Klyachko NL,Erofeev AS,Gorelkin PV,Bel

更新日期：2021-01-04 00:00:00

abstract：:We present a new approach for characterizing drug-polymer interactions in aqueous media, using sedimentation velocity analytical ultracentrifugation (AUC). We investigated the potential interaction of ketoconazole (KTZ), a poorly water-soluble drug, with polyacrylic acid (PAA) and a polyvinyl caprolactam-polyvinyl ace...

journal_title：Molecular pharmaceutics

authors： Amponsah-Efah KK,Demeler B,Suryanarayanan R

更新日期：2021-01-04 00:00:00

abstract：:The N-glycosylation pattern of Asn-297 may have impacts on monoclonal antibody (mAb) drug plasma clearance, antibody-dependent cell mediated cytotoxicity (ADCC), and complement-dependent cytotoxicity (CDC). Notably, the changes in the relative abundance of certain minor glycans, like the afucosylation, high-mannose, o...

journal_title：Molecular pharmaceutics

authors： Zhuo Y,Keire DA,Chen K

更新日期：2021-01-04 00:00:00

abstract：:The impact of the chain length or dispersity of polymers in controlling the crystallization of amorphous active pharmaceutical ingredients (APIs) has been discussed for a long time. However, because of the weak control of these parameters in the majority of macromolecules used in pharmaceutical formulations, the above...

journal_title：Molecular pharmaceutics

authors： Minecka A,Tarnacka M,Jurkiewicz K,Hachuła B,Wrzalik R,Kamiński K,Paluch M,Kamińska E

更新日期：2021-01-04 00:00:00

abstract：:Topical delivery of small interfering RNA (siRNA) can be an attractive method for the treatment of skin diseases and improving the quality of life of patients. However, it is difficult for siRNA to pass through the two major barriers of the skin: the stratum corneum (SC) and tight junctions. We have previously reporte...

journal_title：Molecular pharmaceutics

authors： Kawai M,Ibaraki H,Takashima Y,Kanazawa T,Okada H

更新日期：2021-01-04 00:00:00

abstract：:It is well established that polymers adopt a range of conformations and solution-state organization in response to varying solution environments, although very little work has been done to understand how these effects might impact the physical stability and bioavailability of spray-dried amorphous dispersions (SDDs). ...

journal_title：Molecular pharmaceutics

authors： Defrese MK,Farmer MA,Long Y,Timmerman LR,Bae Y,Marsac PJ

更新日期：2020-12-07 00:00:00

abstract：:Infantile neural ceroid lipofuscinosis (INCL) is a lysosomal storage disorder characterized by mutations in the CLN1 gene that leads to lack of the lysosomal enzyme palmitoyl-protein thioesterase-1 (PPT1), which causes the progressive death of cortical neurons. Enzyme replacement therapy (ERT) is one of the most promi...

journal_title：Molecular pharmaceutics

authors： Santi M,Finamore F,Cecchettini A,Santorelli FM,Doccini S,Rocchiccioli S,Signore G

更新日期：2020-12-07 00:00:00

abstract：:Conventional drug solubilization strategies limit the understanding of the full potential of poorly water-soluble drugs during drug screening. Here, we propose a screening approach in which poorly water-soluble drugs are entrapped in poly(2-(methacryloyloxyethyl phosphorylcholine)-poly(2-(diisopropylaminoethyl methacr...

journal_title：Molecular pharmaceutics

authors： Sola-Barrado B,M Leite D,Scarpa E,Duro-Castano A,Battaglia G

更新日期：2020-12-07 00:00:00

abstract：:Polysorbate 20 (PS20) is a commonly used surfactant in biopharmaceutical formulations. It is a heterogeneous surfactant containing a distribution of fatty acid esters, which are subject to hydrolytic degradation, generating free fatty acids (FFAs). The FFAs can form visible or subvisible particles in drug product on s...

journal_title：Molecular pharmaceutics

authors： Doshi N,Martin J,Tomlinson A

更新日期：2020-11-02 00:00:00

abstract：:Interest in the use of 225Ac for targeted alpha therapies has increased dramatically over the past few years, resulting in a multitude of new isotope production and translational research efforts. However, 225Ac radioimmunoconjugate (RIC) research is still in its infancy, with most prior experience in hematologic mali...

journal_title：Molecular pharmaceutics

authors： Lakes AL,An DD,Gauny SS,Ansoborlo C,Liang BH,Rees JA,McKnight KD,Karsunky H,Abergel RJ

更新日期：2020-11-02 00:00:00

abstract：:This study describes a novel nonlinear variant of the well-known Yalkowsky general solubility equation (GSE). The modified equation can be trained with small molecules, mostly from the Lipinski Rule of 5 (Ro5) chemical space, to predict the intrinsic aqueous solubility, S0, of large molecules (MW > 800 Da) from beyond...

journal_title：Molecular pharmaceutics

authors： Avdeef A,Kansy M

更新日期：2020-10-05 00:00:00

abstract：:We have developed a macromolecular prodrug platform based on poly(l-lysine succinylated) (PLS) that targets scavenger receptor A1 (SR-A1), a receptor expressed by myeloid and endothelial cells. We demonstrate the selective uptake of PLS by murine macrophage, RAW 264.7 cells, which was eliminated upon cotreatment with ...

journal_title：Molecular pharmaceutics

authors： Stevens DM,Adiseshaiah P,Dasa SSK,Potter TM,Skoczen SL,Snapp KS,Cedrone E,Patel N,Busman-Sahay K,Rosen EP,Sykes C,Cottrell M,Dobrovolskaia MA,Estes JD,Kashuba ADM,Stern ST

更新日期：2020-10-05 00:00:00

abstract：:Cyclic RGD (cRGD) peptide-conjugated boronated albumin was developed to direct toward integrin αvβ3, which overexpresses on many cancer cells. A stepwise conjugation of c[RGDfK(Mal)] and maleimide-conjugated closo-dodecaborate (MID) to bovine serum albumin (BSA) afforded cRGD-MID-BSA, which was noncytotoxic toward bot...

journal_title：Molecular pharmaceutics

authors： Kawai K,Nishimura K,Okada S,Sato S,Suzuki M,Takata T,Nakamura H

更新日期：2020-10-05 00:00:00

abstract：:Drug repositioning is an important drug development strategy as it saves the time and efforts exerted in drug discovery. Since reepithelization of the cornea is a critical problem, we envisioned that the anticonvulsant phenytoin sodium can promote reepithelization of corneal ulcers as it was repurposed for skin wound ...

journal_title：Molecular pharmaceutics

authors： Mahmoud DB,Afifi SA,El Sayed NS

更新日期：2020-10-05 00:00:00

abstract：:Dissolution is a crucial process for the oral delivery of drug products. Before being absorbed through epithelial cell membranes to reach the systemic circulation, drugs must first dissolve in the human gastrointestinal (GI) tract. In vivo and in vitro dissolutions are complex because of their dependency upon the drug...

journal_title：Molecular pharmaceutics

authors： Salehi N,Al-Gousous J,Mudie DM,Amidon GL,Ziff RM,Amidon GE

更新日期：2020-10-05 00:00:00

abstract：:Preferential interactions of formulation excipients govern their impact on the stability properties of proteins in solution. The ability to predict these interactions without the need to perform experiments would enable formulation design to begin early in the development of a new antibody therapeutic. With that in mi...

journal_title：Molecular pharmaceutics

authors： Cloutier TK,Sudrik C,Mody N,Sathish HA,Trout BL

更新日期：2020-09-08 00:00:00

abstract：:Erythropoietin (EPO), a hematopoietic growth factor and a promising therapy for Alzheimer's disease, has low permeability across the blood-brain barrier. The transferrin receptor antibody fused to EPO (TfRMAb-EPO) is a chimeric monoclonal antibody that ferries EPO into the brain via the transvascular route. However, T...

journal_title：Molecular pharmaceutics

authors： Yang J,Sun J,Castellanos DM,Pardridge WM,Sumbria RK

更新日期：2020-08-03 00:00:00

abstract：:The effect of tertiary butyl alcohol (TBA) as a cosolvent on the phase behavior of mannitol in frozen and freeze-dried systems was characterized using differential scanning calorimetry (DSC) and X-ray diffractometry (XRD; laboratory and synchrotron sources). Solutions of mannitol (2 and 5% w/w) in TBA-water systems of...

journal_title：Molecular pharmaceutics

authors： Sonje J,Thakral S,Suryanarayanan R

更新日期：2020-08-03 00:00:00

abstract：:Subcutaneous allergen-specific immunotherapy (SCIT) qualifies as a promising approach for the permanent cure of IgE-mediated airway allergies, which can often manifest into allergic rhinitis and other allergic respiratory diseases. SCIT entails repeated administration of a high allergen dose into the subcutaneous (sc)...

journal_title：Molecular pharmaceutics

authors： Shakya AK,Lee CH,Gill HS

更新日期：2020-08-03 00:00:00

abstract：:Antibody-based near-infrared photoimmunotherapy (NIR-PIT) is an attractive strategy for cancer treatment. Tumor cells can be selectively and efficiently killed by the targeted delivery of an antibody-photoabsorber complex followed by exposure to NIR light. Glycoprotein A33 antigen (GPA33) is highly expressed in most h...

journal_title：Molecular pharmaceutics

authors： Wei D,Tao Z,Shi Q,Wang L,Liu L,She T,Yi Q,Wen X,Liu L,Li S,Yang H,Jiang X

更新日期：2020-07-06 00:00:00

abstract：:Ritonavir is a well-known CYP3A4 and CYP2D6 enzyme inhibitor, frequently used to assess the drug-drug interaction (DDI) liability of susceptible drugs. It is also used as a pharmacokinetic booster to increase exposure to CYP3A4 substrates. This study aimed to develop a mechanistic absorption and disposition model to d...

journal_title：Molecular pharmaceutics

authors： Arora S,Pansari A,Kilford P,Jamei M,Gardner I,Turner DB

更新日期：2020-07-06 00:00:00

abstract：:Graphene-based tumor cell nuclear targeting fluorescent nanoprobes (GTTNs) were synthesized in our laboratory as a kind of nanomaterial and showed good performance for both in vivo and in vitro imaging. GTTNs directly cross the cell membrane and specifically target the tumor cell nucleus via a cell membrane permeabili...

journal_title：Molecular pharmaceutics

authors： Gao W,Zhang J,Xue Q,Yin X,Yin X,Li C,Wang Y

更新日期：2020-07-06 00:00:00

abstract：:Helicobacter pylori inhabits the gastric epithelium and can promote the development of gastric disorders, such as peptic ulcers, acute and chronic gastritis, mucosal lymphoid tissue (MALT), and gastric adenocarcinomas. To use nanotechnology as a tool to increase the antibacterial activity of silver I [Ag(I)] compounds...

journal_title：Molecular pharmaceutics

authors： Almeida Furquim de Camargo B,Soares Silva DE,Noronha da Silva A,Campos DL,Machado Ribeiro TR,Mieli MJ,Borges Teixeira Zanatta M,Bento da Silva P,Pavan FR,Gallina Moreira C,Resende FA,Menegário AA,Chorilli M,Vieira de Godoy Nett

更新日期：2020-07-06 00:00:00

abstract：:Intra-articular (IA) injection of thermoresponsive hydrogels coupled with microparticles (MPs) possess the benefit of sustaining the anti-inflammatory drug effect within the joint cavity for rheumatoid arthritis treatment. Star-shaped thermoresponsive poly(polyethylene glycol) methacrylate [Poly(PEGMA)] copolymers wer...

journal_title：Molecular pharmaceutics

authors： Abou-ElNour M,Soliman ME,Skouras A,Casettari L,Geneidi AS,Ishak RAH

更新日期：2020-06-01 00:00:00

abstract：:We report on tailored lipid-polymer hybrid nanoparticles (NPs) delivering nitric oxide (NO) under the control of visible light as a tool for overcoming doxorubicin (DOX) resistance. The NPs consist of a polymeric core and a coating. They are appropriately designed to entrap DOX in the poly(lactide-co-glycolide) core a...

journal_title：Molecular pharmaceutics

authors： Fraix A,Conte C,Gazzano E,Riganti C,Quaglia F,Sortino S

更新日期：2020-06-01 00:00:00

abstract：:The formulation of drug/polymer amorphous solid dispersions (ASDs) is one of the most successful strategies for improving the oral bioavailability of poorly soluble active pharmaceutical ingredients (APIs). Hot-melt extrusion (HME) is one method for preparing ASDs that is growing in importance in the pharmaceutical in...

journal_title：Molecular pharmaceutics

authors： Pisa E,Hughes LP,Wren SAC,Booth J,McCabe JF,Whittaker DTE,Mantle MD

更新日期：2020-06-01 00:00:00

abstract：:This work was designed to clarify the absolute abundances of transporters and receptors at different cerebral regions of the blood-brain barriers (BBB) and blood-spinal cord barrier (BSCB) in humans and rats, using physiologically relevant units (pmol/g tissue and fmol/cm2); 39 and 29 proteins including tight-junction...

journal_title：Molecular pharmaceutics

authors： Uchida Y,Yagi Y,Takao M,Tano M,Umetsu M,Hirano S,Usui T,Tachikawa M,Terasaki T

更新日期：2020-06-01 00:00:00

abstract：:The toxicity of Amphotericin B (AmB) is contributed by the small, water-soluble aggregates of the drug. Hence, AmB lipid polymer hybrid nanoparticles (LIPOMER), comprising stearate lipids with a hydrophilic polymer Gantrez (GZ), and solid lipid nanoparticles (SLN), comprising only stearates, were prepared with the obj...

journal_title：Molecular pharmaceutics

authors： Das S,Devarajan PV

更新日期：2020-06-01 00:00:00

abstract：:Lipid-based drug delivery systems have been vastly investigated as a pharmaceutical method to enhance oral absorption of lipophilic drugs. However, these vehicles not only affect drug bioavailability but may also have an impact on gastric emptying, drug disposition, lymphatic absorption and be affected by lipid digest...

journal_title：Molecular pharmaceutics

authors： Izgelov D,Regev A,Domb AJ,Hoffman A

更新日期：2020-06-01 00:00:00

abstract：:The rapid absorptive clearance of drugs delivered to the airways of the lungs means that many inhaled medicines have a short duration of action. The aim of this study was to investigate whether forming polar ion-pairs can modify drug absorption to slow down clearance from the airways. Salbutamol was used as a model dr...

journal_title：Molecular pharmaceutics

authors： Dutton B,Woods A,Sadler R,Prime D,Barlow DJ,Forbes B,Jones SA

更新日期：2020-05-04 00:00:00

abstract：:Diabetic wounds are a worldwide health problem causing extremely heavy public health burden and require effective treatment. Optimal strategies for treating nonhealing diabetic wounds include stem-cell-based therapy and delivery of novel drug substances, such as functional microRNAs (miRNAs); however, miRNA easily deg...

journal_title：Molecular pharmaceutics

authors： Lv Q,Deng J,Chen Y,Wang Y,Liu B,Liu J

更新日期：2020-05-04 00:00:00

abstract：:Positron emission tomography (PET) imaging using 68Ga-labeled bisphosphonates to target bone metastasis could be a valuable tool in cancer diagnosis and monitoring therapeutic treatment. A 68Ga labeled ligand, N,N'-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N'-diacetic acid (HBED-CC) containing one bisphos...

journal_title：Molecular pharmaceutics

authors： Zha Z,Wu Z,Choi SR,Ploessl K,Smith M,Alexoff D,Zhu L,Kung HF

更新日期：2020-05-04 00:00:00