Polymer Nanocoating of Amorphous Drugs for Improving Stability, Dissolution, Powder Flow, and Tabletability: The Case of Chitosan-Coated Indomethacin.

abstract：:In order to gain molecular level understanding of drug dissolution into aqueous media, we report the first molecular dynamics (MD) simulation of a drug crystal dissolving. The simulation was performed for acetaminophen crystal Form I dissolving in 0.15 M aqueous NaCl solution at 37 °C. The 10 ns simulation revealed in...

journal_title：Molecular pharmaceutics

authors： Gao Y,Olsen KW

更新日期：2013-03-04 00:00:00

abstract：:Folate receptor (FR) targeting is an attractive strategy for nuclear imaging of cancer and activated macrophages through application of folic acid radioconjugates. However, significant renal accumulation of folate radioconjugates and hence exceedingly high emission of radiation from the kidneys may mask uptake of radi...

journal_title：Molecular pharmaceutics

authors： Müller C,Reber J,Schlup C,Leamon CP,Schibli R

更新日期：2013-03-04 00:00:00

abstract：:Recent developments in pharmaceutical technology have facilitated the design and production of modified release formulas for drugs whose physical, chemical or biological properties impede release and thus might compromise their efficacy or safety. One such drug is morphine, whose short half-life requires repeated dose...

journal_title：Molecular pharmaceutics

authors： Morales ME,López G,Gallardo V,Ruiz MA

更新日期：2011-04-04 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：:Intravitreal sustained delivery of corticosteroids such as dexamethasone is an effective means of treating a number of ocular diseases, including diabetic retinopathy, uveitis, and age-related or diabetic macular edema. There are currently marketed devices for this purpose, yet only one, Ozurdex, is degradable. In vit...

journal_title：Molecular pharmaceutics

authors： Amsden BG,Marecak D

更新日期：2016-09-06 00:00:00

abstract：:Dendrimers are being explored in many preclinical studies as drug, gene, and imaging agent delivery systems. Understanding their detailed organ, tissue, cellular uptake, and retention can provide valuable insights into their effectiveness as delivery vehicles and the associated toxicity. This work explores a fluoresce...

journal_title：Molecular pharmaceutics

authors： Lesniak WG,Mishra MK,Jyoti A,Balakrishnan B,Zhang F,Nance E,Romero R,Kannan S,Kannan RM

更新日期：2013-12-02 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：: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：:Improving the therapeutic index of anticancer agents is an enormous challenge. Targeting decreases the side effects of the therapeutic agents by delivering the drugs to the intended destination. Nanocarriers containing the nuclear localizing peptide sequences (NLS) translocate to the cell nuclei. However, the nuclear ...

journal_title：Molecular pharmaceutics

authors： Anajafi T,Yu J,Sedigh A,Haldar MK,Muhonen WW,Oberlander S,Wasness H,Froberg J,Molla MS,Katti KS,Choi Y,Shabb JB,Srivastava DK,Mallik S

更新日期：2017-06-05 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：: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：:Cancer stem cells (CSCs) are a subpopulation of cancer cells that have stem cell-like properties and are thought to be responsible for tumor drug resistance and relapse. Therapies that can effectively eliminate CSCs will, therefore, likely inhibit tumor recurrence. The objective of our study was to determine the susce...

journal_title：Molecular pharmaceutics

authors： Sadhukha T,Niu L,Wiedmann TS,Panyam J

更新日期：2013-04-01 00:00:00

abstract：:In the postprandial stomach, processes such as secretion, digestion, and gastric emptying all occur simultaneously. Therefore, the system is highly heterogeneous and dynamically changing, for instance, in terms of various physicochemical parameters such as pH value or viscosity. Thus, the administration of a drug toge...

journal_title：Molecular pharmaceutics

authors： Schick P,Sager M,Wegner F,Wiedmann M,Schapperer E,Weitschies W,Koziolek M

更新日期：2019-11-04 00:00:00

abstract：:Understanding in vivo drug release kinetics is critical for the development of nanoparticle-based delivery systems. In this study, we developed a fluorescence resonance energy transfer (FRET) imaging approach to noninvasively monitor in vitro and in vivo cargo release from polymeric nanoparticles. The FRET donor dye (...

journal_title：Molecular pharmaceutics

authors： Zou P,Chen H,Paholak HJ,Sun D

更新日期：2013-11-04 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：:Solubility limited compounds require enabling formulations such as amorphous solid dispersions (ASDs) to increase the apparent solubility by dissolving to a concentration higher than the equilibrium solubility of the drug. This may lead to subsequent precipitation and thus the loss of the solubility advantage. Althoug...

journal_title：Molecular pharmaceutics

authors： Han YR,Lee PI

更新日期：2017-01-03 00:00:00

abstract：:As the hearts of tumor cells, the nucleus is the ultimate target of many chemotherapeutic agents and genes. However, nuclear drug delivery is always hampered by multiple intracellular obstacles, such as low efficiency of lysosome escape and insufficient nuclear trafficking. Herein, an N-(2-hydroxypropyl) methacrylamid...

journal_title：Molecular pharmaceutics

authors： Zhong J,Zhu X,Luo K,Li L,Tang M,Liu Y,Zhou Z,Huang Y

更新日期：2016-09-06 00:00:00

abstract：:Powder adhesion or sticking onto punches is one of the outstanding issues in pharmaceutical tablet manufacturing. We show in this work that, at comparable particle sizes, the acesulfame potassium exhibited pronouncedly reduced propensity to punch sticking than acesulfame. Detailed analyses revealed strong correlation ...

journal_title：Molecular pharmaceutics

authors： Paul S,Wang C,Wang K,Sun CC

更新日期：2019-06-03 00:00:00

abstract：:We evaluated the chemical and enzymatic stabilities of prodrugs containing methoxy, ethoxy and propylene glycol linkers in order to find a suitable linker for prodrugs of carboxylic acids with amino acids. l-Valine and l-phenylalanine prodrugs of model compounds (benzoic acid and phenyl acetic acid) containing methoxy...

journal_title：Molecular pharmaceutics

authors： Gupta D,Gupta SV,Lee KD,Amidon GL

更新日期：2009-09-01 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：:The wet form of age-related macular degeneration (AMD) is a leading cause of blindness among elderly Americans and is characterized by abnormal vessel growth, termed choroidal neovascularization (CNV). Integrin α5β1 is a transmembrane receptor that binds matrix macromolecules and proteinases to stimulate angiogenesis....

journal_title：Molecular pharmaceutics

authors： Wang WQ,Wang FH,Qin WX,Liu HY,Lu B,Chung C,Zhu J,Gu Q,Shi W,Wen C,Wu F,Zhang K,Sun XD

更新日期：2016-09-06 00:00:00

abstract：:In this manuscript, we have reported a novel 2D fingerprint-based artificial neural network QSAR (FANN-QSAR) method in order to effectively predict biological activities of structurally diverse chemical ligands. Three different types of fingerprints, namely, ECFP6, FP2 and MACCS, were used in FANN-QSAR algorithm devel...

journal_title：Molecular pharmaceutics

authors： Myint KZ,Wang L,Tong Q,Xie XQ

更新日期：2012-10-01 00:00:00

abstract：:sec-Butylpropylacetamide (SPD) is the amide derivative of valproic acid (VPA). SPD possess a wide-spectrum anticonvulsant profile better than that of VPA and blocks status epilepticus (SE) induced by pilocarpine and organophosphates. The activity of SPD on SE is better than that of benzodiazepines (BZDs) in terms of t...

journal_title：Molecular pharmaceutics

authors： Mawasi H,Bibi D,Shekh-Ahmad T,Shaul C,Blotnik S,Bialer M

更新日期：2016-07-05 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 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：:Herein, we elucidated the mechanisms and key factors for the tumor-targeting ability of nanoparticles that presented high targeting efficiency for liver tumor. We used several different nanoparticles with sizes of 200-300 nm, including liposome nanoparticles (LNPs), polystyrene nanoparticles (PNPs) and glycol chitosan...

journal_title：Molecular pharmaceutics

authors： Na JH,Koo H,Lee S,Han SJ,Lee KE,Kim S,Lee H,Lee S,Choi K,Kwon IC,Kim K

更新日期：2016-11-07 00:00:00

abstract：:Deep generative adversarial networks (GANs) are the emerging technology in drug discovery and biomarker development. In our recent work, we demonstrated a proof-of-concept of implementing deep generative adversarial autoencoder (AAE) to identify new molecular fingerprints with predefined anticancer properties. Another...

journal_title：Molecular pharmaceutics

authors： Kadurin A,Nikolenko S,Khrabrov K,Aliper A,Zhavoronkov A

更新日期：2017-09-05 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：:Current cancer chemotherapies commonly suffer from nonspecificity, drug resistance, poor bioavailability, and narrow therapeutic indices. To achieve the optimum drug efficacy, we designed a polymeric drug delivery system for targeted intracellular delivery of a clinically approved, water-soluble anticancer drug, gemci...

journal_title：Molecular pharmaceutics

authors： Kulhari H,Pooja D,Kota R,Reddy TS,Tabor RF,Shukla R,Adams DJ,Sistla R,Bansal V

更新日期：2016-05-02 00:00:00

abstract：:The purpose of this study was to investigate labetalol as a potential high permeability reference standard for the application of Biopharmaceutics Classification Systems (BCS). Permeabilities of labetalol and metoprolol were investigated in animal intestinal perfusion models and Caco-2 cell monolayers. After isolating...

journal_title：Molecular pharmaceutics

authors： Incecayir T,Tsume Y,Amidon GL

更新日期：2013-03-04 00:00:00