Molecular Computations of Preferential Interaction Coefficients of IgG1 Monoclonal Antibodies with Sorbitol, Sucrose, and Trehalose and the Impact of These Excipients on Aggregation and Viscosity.

abstract：:Approximately, 40-70% of active pharmaceutical ingredients (API) are severely limited by their extremely poor aqueous solubility, and consequently, there is a high demand for excipients that can be used to formulate clinically relevant doses of these drug candidates. Here, proof-of-concept studies demonstrate the pote...

journal_title：Molecular pharmaceutics

authors： Hettiarachchi G,Samanta SK,Falcinelli S,Zhang B,Moncelet D,Isaacs L,Briken V

更新日期：2016-03-07 00:00:00

abstract：:Diagnostic imaging of the liver by ultrasound, computed tomography (CT) and magnetic resonance tomography (MRT) is generally limited to the visualization of the morphology. In order to exploit the intriguing liver tropism of the human hepatitis B virus (HBV) for molecular imaging of the liver, peptidic tracers derived...

journal_title：Molecular pharmaceutics

authors： Müller T,Mehrle S,Schieck A,Haberkorn U,Urban S,Mier W

更新日期：2013-06-03 00:00:00

abstract：:Prediction of the rate and extent of drug absorption upon oral dosing needs models that capture the complexities of both the drug molecule and intestinal physiology. We report here the development of a continuous intestinal absorption model based on the convection-diffusion equation. The model includes explicit entero...

journal_title：Molecular pharmaceutics

authors： Nagar S,Korzekwa RC,Korzekwa K

更新日期：2017-09-05 00:00:00

abstract：:Polymer therapeutics offer potential benefits in the treatment of multidrug resistant (MDR) infections; affording targeted delivery of biologically active agents to the site of inflammation, potential decreases in systemic toxicity, and the retention of antimicrobial activity at the target site. As a prototype model, ...

journal_title：Molecular pharmaceutics

authors： Ferguson EL,Azzopardi E,Roberts JL,Walsh TR,Thomas DW

更新日期：2014-12-01 00:00:00

abstract：:The human apical sodium-dependent bile acid transporter (hASBT) is a potential target for drug delivery, but an understanding of hASBT substrate requirements is limited. The objective of this study was to evaluate the influence of ionic character and steric bulk in the C-24 region of bile acid conjugates in governing ...

journal_title：Molecular pharmaceutics

authors： Balakrishnan A,Wring SA,Coop A,Polli JE

更新日期：2006-05-01 00:00:00

abstract：:Superoxide dismutase 1 (SOD1) efficiently catalyzes dismutation of superoxide, but its poor delivery to the target sites in the body, such as brain, hinders its use as a therapeutic agent for superoxide-associated disorders. Here to enhance the delivery of SOD1 across the blood-brain barrier (BBB) and in neurons the e...

journal_title：Molecular pharmaceutics

authors： Tong J,Yi X,Luxenhofer R,Banks WA,Jordan R,Zimmerman MC,Kabanov AV

更新日期：2013-01-07 00:00:00

abstract：:The complement system plays an important role in host innate immunity, and its activation can be exploited as a potential strategy for vaccine adjuvants. Herein, a pH-responsive micellar vaccine platform (COOH-NPs) was developed using a carboxyl-modified diblock copolymer of poly(2-ethyl-2-oxazoline)-poly(d,l-lactide)...

journal_title：Molecular pharmaceutics

authors： Li C,Lu Y,Chen Q,Hu H,Zhao X,Qiao M,Chen D

更新日期：2019-06-03 00:00:00

abstract：:Lipid-core nanocapsules (LCNs) have been proposed as drug carriers to improve brain delivery by modulating drug pharmacokinetics (PK). However, it is not clear whether the LCNs carry the drug through the blood-brain barrier or increase free drug penetration due to changes in the barrier permeability. Quetiapine (QTP) ...

journal_title：Molecular pharmaceutics

authors： Carreño F,Paese K,Silva CM,Guterres SS,Dalla Costa T

更新日期：2016-04-04 00:00:00

abstract：:A wide variety of chemotherapy and radiotherapy agents are available for treating cancer, but a critical challenge is to deliver these agents locally to cancer cells and tumors while minimizing side effects from systemic delivery. Nanomedicine uses nanoparticles with diameters in the range of ∼1-100 nm to encapsulate ...

journal_title：Molecular pharmaceutics

authors： Moore T,Chen H,Morrison R,Wang F,Anker JN,Alexis F

更新日期：2014-01-06 00:00:00

abstract：:The transfection activity and the phase behavior of two novel cationic O-alkyl-phosphatidylcholines, 1,2-dioleoyl- sn-glycero-3-hexylphosphocholine (C6-DOPC) and 1,2-dierucoyl- sn-glycero-3-ethylphosphocholine (di22:1-EPC), have been examined with the aim of more completely understanding the mechanism of lipid-mediate...

journal_title：Molecular pharmaceutics

authors： Koynova R,Wang L,Macdonald RC

更新日期：2008-09-01 00:00:00

abstract：:The most abundant polyphenol in green tea, epigallocatechin-3-gallate (EGCg), has recently received considerable attention due to the discovery of numerous health-promoting bioactivities. Despite reports of its poor oral bioavailability, EGCg has been included in many dietary supplement formulations. Conventional pref...

journal_title：Molecular pharmaceutics

authors： Smith AJ,Kavuru P,Arora KK,Kesani S,Tan J,Zaworotko MJ,Shytle RD

更新日期：2013-08-05 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：:Water-soluble camptothecin (CPT)-polyoxetane conjugates were synthesized using a clickable polymeric platform P(EAMO) that was made by polymerization of acetylene-functionalized 3-ethyl-3-(hydroxymethyl)oxetane (i.e., EAMO). CPT was first modified with a linker 6-azidohexanoic acid via an ester linkage to yield CPT-az...

journal_title：Molecular pharmaceutics

authors： Zolotarskaya OY,Wagner AF,Beckta JM,Valerie K,Wynne KJ,Yang H

更新日期：2012-11-05 00:00:00

abstract：:A deep convolutional generative adversarial network (dcGAN) model was developed in this study to screen and design target-specific novel compounds for cannabinoid receptors. In the adversarial process of training, two models, the discriminator D and the generator G, are iteratively trained. D is trained to discover th...

journal_title：Molecular pharmaceutics

authors： Bian Y,Wang J,Jun JJ,Xie XQ

更新日期：2019-11-04 00:00:00

abstract：:Novel multivalent copper(II)-conjugated phosphorus dendrimers and their corresponding mononuclear copper(II) complexes were synthesized, characterized, and screened for antiproliferative activity against human cancer cell lines. Selected copper ligands were grafted on the surface of phosphorus dendrimers of generation...

journal_title：Molecular pharmaceutics

authors： El Brahmi N,El Kazzouli S,Mignani SM,Essassi el M,Aubert G,Laurent R,Caminade AM,Bousmina MM,Cresteil T,Majoral JP

更新日期：2013-04-01 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：:Cationic poly-L-lysine 3H-dendrimers with either 16 or 32 surface amine groups (BHALys [Lys]4 [3H-Lys]8 [NH2]16 and BHALys [Lys]8 [3H-Lys]16 [NH2]32, generation 3 and 4, respectively) have been synthesized and their pharmacokinetics and biodistribution investigated after intravenous administration to rats. The species...

journal_title：Molecular pharmaceutics

authors： Boyd BJ,Kaminskas LM,Karellas P,Krippner G,Lessene R,Porter CJ

更新日期：2006-09-01 00:00:00

abstract：:In previous studies, we developed a new technique (ionic gelation vibrational jet flow; IGVJF) in order to encapsulate pancreatic β-cells, for insulin in vivo delivery, and diabetes treatment. The fabricated microcapsules showed good morphology but limited cell functions. Thus, this study aimed to optimize the IGVJF t...

journal_title：Molecular pharmaceutics

authors： Mooranian A,Negrulj R,Takechi R,Jamieson E,Morahan G,Al-Salami H

更新日期：2017-08-07 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：:Chemotherapy is an indispensable auxiliary treatment for glioma but highly limited by the existence of both blood-brain barrier (BBB) and blood-brain tumor barrier (BBTB). The dysfunctional brain tumor blood vessels and high interstitial pressure in glioma also greatly hindered the accumulation and deep penetration of...

journal_title：Molecular pharmaceutics

authors： Miao D,Jiang M,Liu Z,Gu G,Hu Q,Kang T,Song Q,Yao L,Li W,Gao X,Sun M,Chen J

更新日期：2014-01-06 00:00:00

abstract：:5P12-RANTES is a recently developed chemokine analogue that has shown high level protection from SHIV infection in macaques. However, the feasibility of using 5P12-RANTES as a long-term HIV prevention agent has not been explored partially due to the lack of available delivery devices that can easily be modified for lo...

journal_title：Molecular pharmaceutics

authors： Wang NX,Sieg SF,Lederman MM,Offord RE,Hartley O,von Recum HA

更新日期：2013-10-07 00:00:00

abstract：:Near-infrared (NIR)-to-visible upconversion nanoparticle (UCNP) has shown promising prospects in photodynamic therapy (PDT) as a drug carrier or energy donor. In this work, a photosensitizer pyropheophorbide a (Ppa) and RGD peptide c(RGDyK) comodified chitosan-wrapped NaYF(4):Yb/Er upconversion nanoparticle UCNP-Ppa-R...

journal_title：Molecular pharmaceutics

authors： Zhou A,Wei Y,Wu B,Chen Q,Xing D

更新日期：2012-06-04 00:00:00

abstract：:The encapsulation of glucocorticoids, such as dexamethasone, in nanoparticles (NPs) faces two main issues: a low drug loading and the destabilization of the nanoparticle suspension due to drug crystallization. Here, we successfully formulated a prodrug of dexamethasone, dexamethasone palmitate (DXP), into nanoparticle...

journal_title：Molecular pharmaceutics

authors： Lorscheider M,Tsapis N,Simón-Vázquez R,Guiblin N,Ghermani N,Reynaud F,Canioni R,Abreu S,Chaminade P,Fattal E

更新日期：2019-07-01 00:00:00

abstract：:Drug transporter expression and function at the blood-brain barrier is altered in Alzheimer's disease (AD). However, the impact of AD on the expression of transporters and metabolizing enzymes in peripheral tissues has received little attention. The current study evaluated the expression of drug transporters and metab...

journal_title：Molecular pharmaceutics

authors： Pan Y,Omori K,Ali I,Tachikawa M,Terasaki T,Brouwer KLR,Nicolazzo JA

更新日期：2018-09-04 00:00:00

abstract：:Metastatic breast cancer is incurable. The goal of this study was to develop a positron emission tomography (PET)/near-infrared fluorescent (NIRF) probe for imaging CD105 expression in breast cancer experimental lung metastasis. TRC105, a chimeric anti-CD105 antibody, was dual-labeled with a NIRF dye (IRDye 800CW) and...

journal_title：Molecular pharmaceutics

authors： Hong H,Zhang Y,Severin GW,Yang Y,Engle JW,Niu G,Nickles RJ,Chen X,Leigh BR,Barnhart TE,Cai W

更新日期：2012-08-06 00:00:00

abstract：:The interaction with cervicovaginal mucus presents the potential to impact the performance of drug nanocarriers. These systems must migrate through this biological fluid in order to deliver their drug payload to the underlying mucosal surface. We studied the ability of dapivirine-loaded polycaprolactone (PCL)-based na...

journal_title：Molecular pharmaceutics

authors： das Neves J,Rocha CM,Gonçalves MP,Carrier RL,Amiji M,Bahia MF,Sarmento B

更新日期：2012-11-05 00:00:00

abstract：:Extracellular β-glucuronidase (β-GUS) in tumors has been investigated as a target enzyme for prodrug therapy. However, despite encouraging preclinical results, animal studies also indicate that the success of prodrug therapy might be limited by the insufficient prodrug-converting enzyme activity, especially in small t...

journal_title：Molecular pharmaceutics

authors： Antunes IF,Haisma HJ,Elsinga PH,Di Gialleonardo V,van Waarde A,Willemsen AT,Dierckx RA,de Vries EF

更新日期：2012-11-05 00:00:00

abstract：:The present study explores the potential of polyelectrolyte-coated liposomes for improving the oral deliverability of doxorubicin (Dox). As a part of formulation strategy, stearyl amine was selected as a formulation component to provide positive charge to liposomes, which were subsequently coated with anionic poly(acr...

journal_title：Molecular pharmaceutics

authors： Jain S,Patil SR,Swarnakar NK,Agrawal AK

更新日期：2012-09-04 00:00:00

abstract：:We report herein on the preparation of thermoresponsive hydrogels by taking advantage of the interaction of cyclodextrins (CDs) and a hydrophobically modified polymer. A hydrophobically modified hydroxypropyl methylcellulose (HM-HPMC) gel formed thermoresponsive hydrogels when small amounts of α-CD were added to the s...

journal_title：Molecular pharmaceutics

authors： Iohara D,Okubo M,Anraku M,Uramatsu S,Shimamoto T,Uekama K,Hirayama F

更新日期：2017-08-07 00:00:00

abstract：:Within the immune system there is an exquisite ability to discriminate between "self" and "non-self" that is orchestrated by antigen-specific T lymphocytes. Genomic plasticity enables differentiation of naive CD4+ T lymphocytes into either regulatory cells (Treg) that express the transcription factor Foxp3 and activel...

journal_title：Molecular pharmaceutics

authors： Park J,Gao W,Whiston R,Strom TB,Metcalfe S,Fahmy TM

更新日期：2011-02-07 00:00:00