Redox Potential-Sensitive N-Acetyl Cysteine-Prodrug Nanoparticles Inhibit the Activation of Microglia and Improve Neuronal Survival.

abstract：:Amorphous solids and crystalline salts are both of interest as a means of improving the dissolution characteristics and apparent solubility of poorly water soluble active pharmaceutical ingredients which have low bioavailability in humans. The theory and selection of both crystalline drug substance salt forms and amor...

journal_title：Molecular pharmaceutics

authors： Towler CS,Li T,Wikström H,Remick DM,Sanchez-Felix MV,Taylor LS

更新日期：2008-11-01 00:00:00

abstract：:Dysbiosis (alteration of intestinal flora) is associated with various host physiologies, including diseases. The purpose of this study was to clarify the effect of dysbiosis on protein expression levels in mouse liver and kidney by quantitative proteomic analysis, focusing in particular on drug-metabolizing enzymes an...

journal_title：Molecular pharmaceutics

authors： Kuno T,Hirayama-Kurogi M,Ito S,Ohtsuki S

更新日期：2016-08-01 00:00:00

abstract：:Due to overexpression of glycyrrhetinic acid (GA) receptor in liver cancer cells, glycyrrhetinic acid modified recombinant human serum albumin (rHSA) nanoparticles for targeting liver tumor cells may result in increased therapeutic efficacy and decreased adverse effects of cancer therapy. In this study, doxorubicin (D...

journal_title：Molecular pharmaceutics

authors： Qi WW,Yu HY,Guo H,Lou J,Wang ZM,Liu P,Sapin-Minet A,Maincent P,Hong XC,Hu XM,Xiao YL

更新日期：2015-03-02 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：: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

abstract：:A series of poorly soluble BCS class II compounds with "grease ball" characteristics were assessed for solubility and dissolution rate in biorelevant dissolution media (BDM) with the purpose of investigating which molecular structures gain most in solubility when dissolved under physiologically relevant conditions. Th...

journal_title：Molecular pharmaceutics

authors： Fagerberg JH,Tsinman O,Sun N,Tsinman K,Avdeef A,Bergström CA

更新日期：2010-10-04 00:00:00

abstract：:The effective delivery of bioimaging probes to a selected cancerous tissue has extensive significance for biological studies and clinical investigations. Herein, the peptide functionalized NaGdF4 nanodots (termed as, pPeptide-NaGdF4 nanodots) have been prepared for highly efficient magnetic resonance imaging (MRI) of ...

journal_title：Molecular pharmaceutics

authors： Chen H,Li X,Liu F,Zhang H,Wang Z

更新日期：2017-09-05 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：: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：:Current chemotherapy strategies for second-line treatment of relapsed ovarian cancer are unable to effectively treat residual disease post-cytoreduction. The findings presented herein suggest that tissue penetration of drug is not only an issue for large, unresectable tumors, but also for invisible, microscopic lesion...

journal_title：Molecular pharmaceutics

authors： Eetezadi S,De Souza R,Vythilingam M,Lessa Cataldi R,Allen C

更新日期：2015-11-02 00:00:00

abstract：:It is a challenge to formulate polymer based nanoparticles of therapeutic proteins as excipients and process conditions affect stability and structural integrity of the protein. Hence, understanding the protein stability and complex aggregation phenomena is an important area of research in therapeutic protein delivery...

journal_title：Molecular pharmaceutics

authors： Rawat S,Gupta P,Kumar A,Garg P,Suri CR,Sahoo DK

更新日期：2015-04-06 00:00:00

abstract：:The systemic pharmacokinetics and pharmacodynamics of small molecules are determined by subcellular transport phenomena. Although approaches used to study the subcellular distribution of small molecules have gradually evolved over the past several decades, experimental analysis and prediction of cellular pharmacokinet...

journal_title：Molecular pharmaceutics

authors： Zheng N,Tsai HN,Zhang X,Rosania GR

更新日期：2011-10-03 00:00:00

abstract：:Ultrasound-targeted microbubble destruction (UTMD) is a promising technique to facilitate the delivery of chemotherapy in cancer treatment. However, the process typically uses nonspecific microbubbles, leading to low tumor-to-normal tissue uptake ratio and adverse side effects. In this study, we synthesized the LHRH r...

journal_title：Molecular pharmaceutics

authors： Pu C,Chang S,Sun J,Zhu S,Liu H,Zhu Y,Wang Z,Xu RX

更新日期：2014-01-06 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：:Itraconazole is a drug of choice for the treatment of severe fungal infections and parasitic diseases, but its use is limited by its low water solubility and varying bioavailability. New self-emulsifying drug delivery systems (SEDDS) based on PEGylated bile acids (BA-PEGs) were designed and prepared, where the number ...

journal_title：Molecular pharmaceutics

authors： Le Dévédec F,Strandman S,Hildgen P,Leclair G,Zhu XX

更新日期：2013-08-05 00:00:00

abstract：:Efficient drug delivery to the skin is essential for the treatment of major dermatologic diseases, such as eczema, psoriasis and acne. However, many compounds penetrate the skin barrier poorly and require optimized formulations to ensure their bioavailability. Here, stimulated Raman scattering (SRS) microscopy, a rece...

journal_title：Molecular pharmaceutics

authors： Saar BG,Contreras-Rojas LR,Xie XS,Guy RH

更新日期：2011-06-06 00:00:00

abstract：:In this work, we demonstrated that the simple substitution of the 1,2,4-triazole moiety in 5-( 4H-1,2,4-triazol-4-yl)isophthalic acid (5-TIA) by the 1 H-1,2,3-triazol-5-yl unit enables the preparation of a hydrogelator (click-TIA). In sharp contrast to 5-TIA, its isostere click-TIA undergoes self-assembly in water upo...

journal_title：Molecular pharmaceutics

authors： Häring M,Rodríguez-López J,Grijalvo S,Tautz M,Eritja R,Martín VS,Díaz Díaz D

更新日期：2018-08-06 00:00:00

abstract：:In this study, the polymer-free electrospinning was performed in order to produce cyclodextrin/ibuprofen inclusion complex nanofibers, which could have potential as the fast dissolving oral drug delivery system. Ibuprofen is a poorly water-soluble nonsteroidal anti-inflammatory drug; however, the water solubility of i...

journal_title：Molecular pharmaceutics

authors： Celebioglu A,Uyar T

更新日期：2019-10-07 00:00:00

abstract：:The molecular mechanisms of autophagy in polyethylenimine (PEI)-treated cells are not well understood because of the use of nonspecific autophagy inhibitors. Here, we applied autophagy-related gene expression analysis to pinpoint the molecular mechanisms of autophagy in PEI-treated wild-type and atg5 gene knockout (at...

journal_title：Molecular pharmaceutics

authors： Lin CW,Jan MS,Kuo JH

更新日期：2014-09-02 00:00:00

abstract：:This work demonstrates the way to achieve efficient and target specific delivery of a graphene quantum dot (GQD) using hyaluronic acid (HA) (GQD-HA) as a targeting agent. HA has been anchored to a GQD that accepts the fascinating adhesive properties of the catechol moiety, dopamine hydrochloride, conjugated to HA, whi...

journal_title：Molecular pharmaceutics

authors： Abdullah-Al-Nahain,Lee JE,In I,Lee H,Lee KD,Jeong JH,Park SY

更新日期：2013-10-07 00:00:00

abstract：:Tumor hypoxia plays a major role in radio- and chemotherapy resistance in solid tumors. Carbonic Anhydrase IX (CAIX) is an endogenous hypoxia-related protein, which is associated with poor patient outcome. The quantitative assessment of CAIX expression of tumors may steer cancer treatment by predicting therapy respons...

journal_title：Molecular pharmaceutics

authors： Huizing FJ,Hoeben BAW,Franssen GM,Boerman OC,Heskamp S,Bussink J

更新日期：2019-02-04 00:00:00

abstract：:We present an in situ hydrophobic salt forming technique for the encapsulation of weakly hydrophobic, ionizable active pharmaceutical ingredients (API) into stable nanocarriers (NCs) formed via a rapid precipitation process. Traditionally, NC formation via rapid precipitation has been difficult with APIs in this class...

journal_title：Molecular pharmaceutics

authors： Pinkerton NM,Grandeury A,Fisch A,Brozio J,Riebesehl BU,Prud'homme RK

更新日期：2013-01-07 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：: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：: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：:Bacterial capsular polysaccharides are components of many modern vaccines, but they are weakly immunogenic. Herein, we describe the delivery of pneumococcal capsular polysaccharide serotype-1 (PCP-1) in polylactide polymeric particles to enhance its immunogenicity. Immunization with PCP-1-entrapped particles elicited ...

journal_title：Molecular pharmaceutics

authors： Anish C,Khan N,Upadhyay AK,Sehgal D,Panda AK

更新日期：2014-03-03 00:00:00

abstract：:Iron oxide nanoparticles have great potential as diagnostic and therapeutic agents in cancer and other diseases; however, biological aggregation severely limits their function in vivo. Aggregates can cause poor biodistribution, reduced heating capability, and can confound their visualization and quantification by magn...

journal_title：Molecular pharmaceutics

authors： Hurley KR,Ring HL,Etheridge M,Zhang J,Gao Z,Shao Q,Klein ND,Szlag VM,Chung C,Reineke TM,Garwood M,Bischof JC,Haynes CL

更新日期：2016-07-05 00:00:00

abstract：:Our work has focused on defining the utility of fluorine (19F)-labeled bile acid analogues and magnetic resonance imaging (MRI) to identify altered bile acid transport in vivo. In the current study, we explored the ability of this approach to differentiate fibroblast growth factor-15 (FGF15)-deficient from wild-type (...

journal_title：Molecular pharmaceutics

authors： Metry M,Felton J,Cheng K,Xu S,Ai Y,Xue F,Raufman JP,Polli JE

更新日期：2018-11-05 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：: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