Biopharmaceutic In Vitro In Vivo Extrapolation (IVIV_E) Informed Physiologically-Based Pharmacokinetic Model of Ritonavir Norvir Tablet Absorption in Humans Under Fasted and Fed State Conditions.

abstract：:The objective was to determine the disposition of polymer nanoparticles and an associated, lipophilic, model "active" component on and within the skin following topical application. Polystyrene and poly(methyl methacrylate) nanoparticles containing covalently bound fluorescein methacrylate and dispersed Nile Red were ...

journal_title：Molecular pharmaceutics

authors： Wu X,Price GJ,Guy RH

更新日期：2009-09-01 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：:The formation mechanism of drug nanoparticles was investigated using solid-state nuclear magnetic resonance (NMR) techniques for the efficient discovery of an optimized nanoparticle formulation. The cogrinding of nifedipine (NIF) with polymers, including hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (P...

journal_title：Molecular pharmaceutics

authors： Ueda K,Higashi K,Moribe K

更新日期：2016-03-07 00:00:00

abstract：BACKGROUND:For the development of novel buccoadhesive formulations, their physicochemical properties, strength of the interfacial joint, and residence time on the buccal mucosa are considered as a measure for their in vivo mucoadhesive properties. Focusing on these parameters, the predictive power of established in vit...

journal_title：Molecular pharmaceutics

authors： Baus RA,Haug MF,Leichner C,Jelkmann M,Bernkop-Schnürch A

更新日期：2019-06-03 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：:Interactions of a lyophilized peptide with water and excipients in a solid matrix were explored using photolytic labeling. A model peptide "KLQ" (Ac-QELHKLQ-NHCH3) was covalently labeled with NHS-diazirine (succinimidyl 4,4'-azipentanoate), and the labeled peptide (KLQ-SDA) was formulated and exposed to UV light in bo...

journal_title：Molecular pharmaceutics

authors： Chen Y,Topp EM

更新日期：2019-03-04 00:00:00

abstract：:Fenretinide, a chemotherapeutic agent for cancer, is water-insoluble and has a very low oral bioavailability. Hence, the objective was to deliver it as an injectable depot and improve the drug solubility and release behavior from poly(lactide-co-glycolide) (PLGA) microspheres by incorporating nonionic surfactants with...

journal_title：Molecular pharmaceutics

authors： Zhang Y,Wischke C,Mittal S,Mitra A,Schwendeman SP

更新日期：2016-08-01 00:00:00

abstract：:For efficient and receptor-specific siRNA delivery, a new post-PEGylation strategy was established to provide siRNA polyplexes with targeting and shielding agents. For this purpose, core nanoparticles were formed by complexing siRNA with sequence-defined cationic lipo-oligomers. The T-shaped bis-oleoyl-oligoethanamino...

journal_title：Molecular pharmaceutics

authors： Müller K,Kessel E,Klein PM,Höhn M,Wagner E

更新日期：2016-07-05 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 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：:The aim of the research work was to develop and characterize a concanavalin-A (Con-A) conjugated gastroretentive multiparticulate delivery system of clarithromycin (CM) for the effective treatment of colonization of Helicobacter pylori (H. pylori). Ethylcellulose (EC) microspheres containing CM were prepared using emu...

journal_title：Molecular pharmaceutics

authors： Jain SK,Jangdey MS

更新日期：2009-01-01 00:00:00

abstract：:Most anticancer drugs are poorly soluble and nonspecific, which restricts their clinical application. Drug conjugates, as a prodrug strategy, provide the possibility to overcome these shortcomings, especially combined with nanotechnology. Drug conjugate nanoparticles possess the advantages of high drug loading capacit...

journal_title：Molecular pharmaceutics

authors： Song Q,Wang X,Wang Y,Liang Y,Zhou Y,Song X,He B,Zhang H,Dai W,Wang X,Zhang Q

更新日期：2016-01-04 00:00:00

abstract：:The particle shape of the drug delivery systems had a strong impact on their in vitro and in vivo performance, but there was limited availability of techniques to produce the specific shaped drug carriers. In this article, the novel methotrexate (MTX) decorated MPEG-PLA nanobacillus (MPEG-PLA-MTX NB) was prepared by t...

journal_title：Molecular pharmaceutics

authors： Cui F,Lin J,Li Y,Li Y,Wu H,Yu F,Jia M,Yang X,Wu S,Xie L,Ye S,Luo F,Hou Z

更新日期：2015-04-06 00:00:00

abstract：:Because of its biocompatibility and ability to accommodate a variety of payloads from poorly soluble drugs to biomolecules, porous silicon (PSi) is a lucrative material for the development of carriers for particle-mediated drug delivery. We report a successful direct one-step (18)F-radiolabeling of three types of PSi ...

journal_title：Molecular pharmaceutics

authors： Sarparanta M,Mäkilä E,Heikkilä T,Salonen J,Kukk E,Lehto VP,Santos HA,Hirvonen J,Airaksinen AJ

更新日期：2011-10-03 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：:Formulation of a cocrystal into a solid pharmaceutical dosage form entails numerous processing steps during which there is risk of dissociation. In an effort to reduce the number of unit operations, we have attempted the in situ formation of an indomethacin-saccharin (INDSAC) cocrystal during high-shear wet granulatio...

journal_title：Molecular pharmaceutics

authors： Tanaka R,Duggirala NK,Hattori Y,Otsuka M,Suryanarayanan R

更新日期：2020-01-06 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：:In women with human epidermal growth factor 2 (HER2)-positive breast cancer, the improved control of systemic disease with new therapies has unmasked brain metastases that historically would have remained clinically silent. The efficacy of therapeutic agents against brain metastases is limited by their inability to pe...

journal_title：Molecular pharmaceutics

authors： Wyatt EA,Davis ME

更新日期：2020-02-03 00:00:00

abstract：:The killing efficacy of doxorubicin from liposome-based delivery carriers has been shown to correlate strongly with its intracellular trafficking and, in particular, its fast and extensive release from the delivery carrier. However, previously explored pH-triggered mechanisms that were designed to become activated dur...

journal_title：Molecular pharmaceutics

authors： Mamasheva E,O'Donnell C,Bandekar A,Sofou S

更新日期：2011-12-05 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：: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：:Accumulating evidence suggests that EphB4 plays key roles in cancer progression in numerous cancer types. In fact, therapies focusing on EphB4 have become potentially important components of various cancer treatment strategies. However, tumor sensitivity to EphB4 suppression may not be uniform for different cancers. I...

journal_title：Molecular pharmaceutics

authors： Li D,Liu S,Liu R,Park R,Hughes L,Krasnoperov V,Gill PS,Li Z,Shan H,Conti PS

更新日期：2013-01-07 00:00:00

abstract：:The maytansinoid antibody-drug conjugates (ADCs) in clinical development for cancer therapy each contain a derivative of the microtubule-targeting agent, maytansine, covalently attached to the antibody via an engineered linker. A sample of any of these conjugates contains molecules with different numbers of maytansino...

journal_title：Molecular pharmaceutics

authors： Goldmacher VS,Amphlett G,Wang L,Lazar AC

更新日期：2015-06-01 00:00:00

abstract：:Effective penetration of drug-carrying nanoparticles into solid tumors is a major challenge in cancer therapy. Exploration of the physicochemical properties of nanoparticles that affect penetration efficiency is required to achieve maximum therapeutic effects. Here, we used confocal laser scanning microscopy to evalua...

journal_title：Molecular pharmaceutics

authors： Takechi-Haraya Y,Goda Y,Sakai-Kato K

更新日期：2017-06-05 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：:There is evidence that encapsulating glucocorticoids into nucleic acid-containing nanoparticles reduces the inflammatory toxicities of the nanoparticles. Herein, using betamethasone acetate (BA), a glucocorticoid, and a solid lipid nanoparticle formulation of siRNA, we confirmed that coencapsulating BA into the siRNA ...

journal_title：Molecular pharmaceutics

authors： O'Mary HL,Hanafy MS,Aldayel AM,Valdes SA,Alzhrani RF,Hufnagel S,Koleng JJ,Cui Z

更新日期：2019-11-04 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：:Liposomes are widely used for systemic delivery of chemotherapeutic agents to reduce their nonspecific side effects. Gemcitabine (Gem) makes a great candidate for liposomal encapsulation due to the short half-life and nonspecific side effects; however, it has been difficult to achieve liposomal Gem with high drug load...

journal_title：Molecular pharmaceutics

authors： Tamam H,Park J,Gadalla HH,Masters AR,Abdel-Aleem JA,Abdelrahman SI,Abdelrahman AA,Lyle LT,Yeo Y

更新日期：2019-07-01 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：:Gemcitabine, a clinically effective nucleoside anticancer agent, is a polar drug with low membrane permeability and is administered intravenously. Further, extensive degradation of gemcitabine by cytidine deaminase to an inactive metabolite in the liver affects its activity adversely. Thus, strategies that provide bot...

journal_title：Molecular pharmaceutics

authors： Song X,Lorenzi PL,Landowski CP,Vig BS,Hilfinger JM,Amidon GL

更新日期：2005-03-01 00:00:00