In Silico Docking of Alkylphosphocholine Analogs to Human Serum Albumin Predicts Partitioning and Pharmacokinetics.

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：:The objective of this work was to investigate the feasibility of using a novel granulation technique, namely, fluidized hot melt granulation (FHMG), to prepare gastroretentive extended-release floating granules. In this study we have utilized FHMG, a solvent free process in which granulation is achieved with the aid o...

journal_title：Molecular pharmaceutics

authors： Zhai H,Jones DS,McCoy CP,Madi AM,Tian Y,Andrews GP

更新日期：2014-10-06 00:00:00

abstract：:Gold nanoparticles (AuNPs) have a number of physical properties that make them appealing for medical applications. For example, the attenuation of X-rays by gold nanoparticles has led to their use in computed tomography imaging and as adjuvants for radiotherapy. AuNPs have numerous other applications in imaging, thera...

journal_title：Molecular pharmaceutics

authors： Mieszawska AJ,Mulder WJ,Fayad ZA,Cormode DP

更新日期：2013-03-04 00:00:00

abstract：:An artificial stomach duodenum (ASD) model has been used to demonstrate the performance difference between two formulations of LY2300559, a low-solubility acidic developmental drug. The two formulations investigated were a conventional high-shear wet granulation (HSWG) formulation and a solid dispersion formulation. A...

journal_title：Molecular pharmaceutics

authors： Polster CS,Wu SJ,Gueorguieva I,Sperry DC

更新日期：2015-04-06 00:00:00

abstract：:Amphotericin B (AmB) loaded polymer lipid hybrid nanoparticles (AmB-PLNs) comprised of lecithin (anionic lipid) and gelatin (Type A, cationic below its isoelectric point 7.0-9.0) were prepared by a two-step desolvation method to improve the oral bioavailability of AmB. The optimized AmB-PLNs were found to have particl...

journal_title：Molecular pharmaceutics

authors： Jain S,Valvi PU,Swarnakar NK,Thanki K

更新日期：2012-09-04 00:00:00

abstract：:To predict the outcome of intestinal drug transporter induction on pharmacokinetics, signaling of the DNA message along with messenger RNA (mRNA) transcription and protein translation leading to transporter function must be understood. We quantified the gene expression of PXR and CAR, gene expression and protein abund...

journal_title：Molecular pharmaceutics

authors： Brueck S,Bruckmueller H,Wegner D,Busch D,Martin P,Oswald S,Cascorbi I,Siegmund W

更新日期：2019-09-03 00:00:00

abstract：:Simvastatin is known to exist in at least three polymorphic forms. The nature of polymorphism in simvastatin is ambiguous, as the crystal structures of the polymorphs do not show any significant change in crystal packing or molecular conformation. We utilize terahertz time-domain spectroscopy to characterize each of t...

journal_title：Molecular pharmaceutics

authors： Tan NY,Zeitler JA

更新日期：2015-03-02 00:00:00

abstract：:A redox-sensitive prodrug, octreotide(Phe)-polyethene glycol-disulfide bond-paclitaxel [OCT(Phe)-PEG-ss-PTX], was successfully developed for targeted intracellular delivery of PTX. The formulation emphasizes long-circulation-time polymer-drug conjugates, combined targeting based on EPR and OCT-receptor mediated endocy...

journal_title：Molecular pharmaceutics

authors： Yin T,Wu Q,Wang L,Yin L,Zhou J,Huo M

更新日期：2015-08-03 00:00:00

abstract：:Robust deposition of extracellular matrix is a significant barrier for delivery of nanotherapeutics and small-molecule anticancer drugs to different tumors including pancreatic ductal adenocarcinoma. Here, we investigated permeation and total uptake of polystyrene nanoparticles of different diameters in 3D multicellul...

journal_title：Molecular pharmaceutics

authors： Durymanov M,Kroll C,Permyakova A,Reineke J

更新日期：2019-03-04 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：:A combination of microbubbles (MBs) and ultrasound (US) is an emerging method for noninvasive and targeted enhancement of anti-cancer drug uptake. This method showed an increase local drug extravasation in tumor tissue while reducing the systemic adverse effects in various tumor models. The present study aims to evalu...

journal_title：Molecular pharmaceutics

authors： Bressand D,Novell A,Girault A,Raoul W,Fromont-Hankard G,Escoffre JM,Lecomte T,Bouakaz A

更新日期：2019-09-03 00:00:00

abstract：:Poly(ethylene glycol)-block-poly(D,L-lactic acid) (PEG-b-PLA) micelles have a proven capacity for drug solubilization and have entered phase III clinical trials as a substitute for Cremophor EL in the delivery of paclitaxel in cancer therapy. PEG-b-PLA is less toxic than Cremophor EL, enabling a doubling of paclitaxel...

journal_title：Molecular pharmaceutics

authors： Shin HC,Alani AW,Cho H,Bae Y,Kolesar JM,Kwon GS

更新日期：2011-08-01 00:00:00

abstract：:The human organic anion-transporting polypeptides OATP1B1 (SLCO1B1) and OATP1B3 (SLCO1B3) are liver-enriched membrane transporters of major importance to hepatic uptake of numerous endogenous compounds, including bile acids, steroid conjugates, hormones, and drugs, including the 3-hydroxy-3-methylglutaryl Co-A reducta...

journal_title：Molecular pharmaceutics

authors： DeGorter MK,Ho RH,Leake BF,Tirona RG,Kim RB

更新日期：2012-04-02 00:00:00

abstract：:Glioblastoma multiforme (GBM) is the most commonly encountered subtype of deadly brain cancer in human adults. It has a high recurrence rate and shows aggressive proliferation. The novel cytotoxic agent temozolomide (TMZ) is now frequently applied as the first-line chemotherapeutic treatment for GBM; however, a consid...

journal_title：Molecular pharmaceutics

authors： Bi Y,Li H,Yi D,Sun Y,Bai Y,Zhong S,Song Y,Zhao G,Chen Y

更新日期：2018-11-05 00:00:00

abstract：:Dual-targeted imaging agents have shown improved targeting efficiencies in comparison to single-targeted entities. The purpose of this study was to quantitatively assess the tumor accumulation of a dual-labeled heterobifunctional imaging agent, targeting two overexpressed biomarkers in pancreatic cancer, using positro...

journal_title：Molecular pharmaceutics

authors： Luo H,England CG,Goel S,Graves SA,Ai F,Liu B,Theuer CP,Wong HC,Nickles RJ,Cai W

更新日期：2017-05-01 00:00:00

abstract：:We have identified and characterized a new solid form of trehalose, the δ form (Tδ) using (13)C solid-state NMR spectroscopy (SSNMR). Tδ is formed from dehydrations of trehalose dihydrate (T(h)) performed at or below 100 °C, and it is generated concurrently with the α form of trehalose (Tα) and amorphous trehalose (T(...

journal_title：Molecular pharmaceutics

authors： Pyszczynski SJ,Munson EJ

更新日期：2013-09-03 00:00:00

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：:To overcome the P-glycoprotein (P-gp)-induced multidrug resistance (MDR) of cancer cells, a novel copolymer, chitosan-graft-D-α-tocopheryl polyethylene glycol 1000 (TPGS) (CT) was synthesized for doxorubicin (DOX) delivery by the P-gp inhibiting virtue of TPGS. DOX-loaded CT nanoparticles (NPs) were fabricated by a mo...

journal_title：Molecular pharmaceutics

authors： Guo Y,Chu M,Tan S,Zhao S,Liu H,Otieno BO,Yang X,Xu C,Zhang Z

更新日期：2014-01-06 00:00:00

abstract：:Fexofenadine is a nonsedative antihistamine that exhibits good oral bioavailability despite its zwitterionic chemical structure and efflux by P-gp. Evidence exists that multiple uptake and efflux transporters play a role in hepatic disposition of fexofenadine. However, the roles of specific transporters and their inte...

journal_title：Molecular pharmaceutics

authors： Ming X,Knight BM,Thakker DR

更新日期：2011-10-03 00:00:00

abstract：:Our objective was to design a polymeric micelle-based doxorubicin and lapatinib combination therapy for treating multidrug resistant (MDR) breast cancers. Poly(ethylene glycol)-block-poly(2-methyl-2-benzoxycarbonylpropylene carbonate) (PEG-PBC) polymers were synthesized for preparing doxorubicin and lapatinib loaded m...

journal_title：Molecular pharmaceutics

authors： Wang H,Li F,Du C,Wang H,Mahato RI,Huang Y

更新日期：2014-08-04 00:00:00

abstract：:The mechanism of cell death in A2780 human ovarian carcinoma cells induced by free doxorubicin (DOX) and N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-bound DOX [P-(GFLG)-DOX] was investigated. In particular, the involvement of the Fas receptor system in drug-induced apoptosis was evaluated. P-(GFLG)-DOX was show...

journal_title：Molecular pharmaceutics

authors： Malugin A,Kopecková P,Kopecek J

更新日期：2004-05-01 00:00:00

abstract：:Targeted delivery of anticancer drugs to brain tumors, especially glioblastoma multiforme, which is the most frequent and aggressive type, is one of the important objectives in nanomedicine. Vascular endothelial growth factor (VEGF) and its receptor type II (VEGFR2) are promising targets because they are overexpressed...

journal_title：Molecular pharmaceutics

authors： Shein SA,Kuznetsov II,Abakumova TO,Chelushkin PS,Melnikov PA,Korchagina AA,Bychkov DA,Seregina IF,Bolshov MA,Kabanov AV,Chekhonin VP,Nukolova NV

更新日期：2016-11-07 00:00:00

abstract：:Drug self-delivery systems consisting of small-molecule active drugs with nanoscale features for intracellular delivery without the need for additional polymeric carriers have drawn much attention recently. In this work, we proposed a highly efficient strategy to fabricate protonized and reduction-responsive self-asse...

journal_title：Molecular pharmaceutics

authors： Dong S,He J,Sun Y,Li D,Li L,Zhang M,Ni P

更新日期：2019-09-03 00:00:00

abstract：:PLGA was functionalized with PEG and biotin using click chemistry to generate a biotin receptor targeted copolymer (biotinylated-PEG-PLGA) which in turn was used to fabricate ultrafine nanoparticles (BPNP) of doxorubicin hydrochloride (DOX) for effective delivery in 4T1 cell induced breast cancer. However, adequate en...

journal_title：Molecular pharmaceutics

authors： Singh Y,Durga Rao Viswanadham KK,Kumar Jajoriya A,Meher JG,Raval K,Jaiswal S,Dewangan J,Bora HK,Rath SK,Lal J,Mishra DP,Chourasia MK

更新日期：2017-08-07 00:00:00

abstract：:Polymer therapeutics have shown promise as tumor-targeted drug delivery systems in mice. The multivalency of polymers allows the attachment of different functional agents to a polymeric backbone, including chemotherapeutic and antiangiogenic drugs, as well as targeting moieties, such as the bone-targeting agent alendr...

journal_title：Molecular pharmaceutics

authors： Miller K,Eldar-Boock A,Polyak D,Segal E,Benayoun L,Shaked Y,Satchi-Fainaro R

更新日期：2011-08-01 00:00:00

abstract：:Poly(ethylcyanoacrylate) (PECA) nanoparticles containing the bioactive d-Lys(6)-GnRH were manufactured by an in situ interfacial polymerization process using a w/o-microemulsion template containing the peptide in the dispersed aqueous pseudophase of the microemulsion. Polymeric nanoparticles were characterized using P...

journal_title：Molecular pharmaceutics

authors： Kafka AP,Kleffmann T,Rades T,McDowell A

更新日期：2009-09-01 00:00:00

abstract：:This paper develops a structure-activity relationship understanding of the way in which surfactant-like dendrons with hydrophilic spermine surface groups and a variety of lipophilic units at their focal points can self-assemble and subsequently bind to DNA with high affinity. The choice of functional group at the foca...

journal_title：Molecular pharmaceutics

authors： Jones SP,Gabrielson NP,Wong CH,Chow HF,Pack DW,Posocco P,Fermeglia M,Pricl S,Smith DK

更新日期：2011-04-04 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 particular characteristics of the tumor microenvironment have the potential to strongly promote tumor growth, metastasis and angiogenesis and induce drug resistance. Therefore, the development of effective, systemic therapeutic approaches specifically based on the tumor microenvironment is highly desirable. Hypoxi...

journal_title：Molecular pharmaceutics

authors： Liu XQ,Xiong MH,Shu XT,Tang RZ,Wang J

更新日期：2012-10-01 00:00:00

abstract：:Antiviral drugs often suffer from poor intestinal permeability, preventing their delivery via the oral route. The goal of this work was to enhance the intestinal absorption of the low-permeability antiviral agents zanamivir heptyl ester (ZHE) and guanidino oseltamivir (GO) utilizing an ion-pairing approach, as a criti...

journal_title：Molecular pharmaceutics

authors： Miller JM,Dahan A,Gupta D,Varghese S,Amidon GL

更新日期：2010-08-02 00:00:00