PEGylated bile acids for use in drug delivery systems: enhanced solubility and bioavailability of itraconazole.

abstract：:Delivery of plasmid DNA for protein production in mammalian cells is not an efficient process. In this study, the theory that cellular localization of plasmid DNA increases transfection efficiency is examined with an emphasis on the understanding of the cellular association of the components of a ternary transfection ...

journal_title：Molecular pharmaceutics

authors： Guo C,Gemeinhart RA

更新日期：2004-07-01 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：:Lipid-based drug delivery systems have been vastly investigated as a pharmaceutical method to enhance oral absorption of lipophilic drugs. However, these vehicles not only affect drug bioavailability but may also have an impact on gastric emptying, drug disposition, lymphatic absorption and be affected by lipid digest...

journal_title：Molecular pharmaceutics

authors： Izgelov D,Regev A,Domb AJ,Hoffman A

更新日期：2020-06-01 00:00:00

abstract：:Engineered superparamagnetic iron oxide nanoparticles (SPIONs) have been studied extensively for their localized homogeneous heat generation in breast cancer therapy. However, challenges such as aggregation and inability to produce sub-10 nm SPIONs limit their potential in magnetothermal ablation. We report a facile, ...

journal_title：Molecular pharmaceutics

authors： Alhasan AH,Fardous RS,Alsudir SA,Majrashi MA,Alghamdi WM,Alsharaeh EH,Almalik AM

更新日期：2019-08-05 00:00:00

abstract：:Although nanocarriers hold promise for cancer chemotherapy, their intracellular drug delivery pathways are not fully understood. In particular, the influence of nanocarrier stability on cellular uptake is still uncertain. By physically loading hydrophobic FRET probes, we revealed different intracellular drug delivery ...

journal_title：Molecular pharmaceutics

authors： Lee SY,Tyler JY,Kim S,Park K,Cheng JX

更新日期：2013-09-03 00:00:00

abstract：:In this study, a facile strategy for efficient codelivery of gene and drug was developed. Using a coprecipitation method, doxorubicin hydrochloride (DOX), an antitumor drug, and p53 expression plasmid were encapsulated in alginate/CaCO(3)/DNA/DOX nanoparticles with high encapsulation efficiency. The in vitro cell inhi...

journal_title：Molecular pharmaceutics

authors： Zhao D,Liu CJ,Zhuo RX,Cheng SX

更新日期：2012-10-01 00:00:00

abstract：:The controversy surrounding the use of diphtheria toxin (DT) as a therapeutic agent against tumor cells arises mainly from its unexpected harmfulness to healthy tissues. We encoded the cytotoxic fragment A of DT (DTA) as an objective gene in the Light-On gene-expression system to construct plasmids pGAVPO (pG) and pU5...

journal_title：Molecular pharmaceutics

authors： Xu J,He M,Hou X,Wang Y,Shou C,Cai X,Yuan Z,Yin Y,Lan M,Lou K,Zhao Y,Yang Y,Chen X,Gao F

更新日期：2020-01-06 00:00:00

abstract：:Sodium lauryl sulfate (SLS), as an effective surfactant, is often used as a solubilizer and/or wetting agent in various dosage forms for the purpose of improving the solubility and dissolution of lipophilic, poorly water-soluble drugs. This study aims to understand the impact of SLS on the solution behavior and bioava...

journal_title：Molecular pharmaceutics

authors： Chen Y,Wang S,Wang S,Liu C,Su C,Hageman M,Hussain M,Haskell R,Stefanski K,Qian F

更新日期：2016-08-01 00:00:00

abstract：:Reversible aqueous lipidization (REAL) at the interdisulfide bond has been shown to improve the deliverability of some peptide drugs. Recently, we developed a nonreversible aqueous lipidization method targeted at the interdisulfide bond of salmon calcitonin (sCT). The resultant derivative had comparable hypocalcemic a...

journal_title：Molecular pharmaceutics

authors： Cheng W,Lim LY

更新日期：2008-07-01 00:00:00

abstract：:The impact of the chain length or dispersity of polymers in controlling the crystallization of amorphous active pharmaceutical ingredients (APIs) has been discussed for a long time. However, because of the weak control of these parameters in the majority of macromolecules used in pharmaceutical formulations, the above...

journal_title：Molecular pharmaceutics

authors： Minecka A,Tarnacka M,Jurkiewicz K,Hachuła B,Wrzalik R,Kamiński K,Paluch M,Kamińska E

更新日期：2021-01-04 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：: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：: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：: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：:Understanding protein stability is central to combatting protein aggregation diseases and developing new protein therapeutics. At the high concentrations often present in biological systems, purified proteins can exhibit undesirable high solution viscosities and poor solubilities mediated by short-range electrostatic ...

journal_title：Molecular pharmaceutics

authors： Laber JR,Dear BJ,Martins ML,Jackson DE,DiVenere A,Gollihar JD,Ellington AD,Truskett TM,Johnston KP,Maynard JA

更新日期：2017-10-02 00:00:00

abstract：:Current experimental methodologies used to determine the thermodynamic solubility of an API within a polymer typically involves establishing the dissolution/melting end point of the crystalline API within a physical mixture or through the use of the glass transition temperature measurement of a demixed amorphous solid...

journal_title：Molecular pharmaceutics

authors： Tian Y,Jones DS,Donnelly C,Brannigan T,Li S,Andrews GP

更新日期：2018-04-02 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：:RNA oligonucleotides capable of inducing controlled immunostimulation combined with specific oncogene silencing via an RNA interference (RNAi) mechanism provide synergistic inhibition of cancer cell growth. With this concept, we previously designed a potent immunostimulatory long double stranded RNA, referred to as li...

journal_title：Molecular pharmaceutics

authors： Sajeesh S,Lee TY,Hong SW,Dua P,Choe JY,Kang A,Yun WS,Song C,Park SH,Kim S,Li C,Lee DK

更新日期：2014-03-03 00:00:00

abstract：:BCS classification is a vital tool in the development of both generic and innovative drug products. The purpose of this work was to provisionally classify the world's top selling oral drugs according to the BCS, using in silico methods. Three different in silico methods were examined: the well-established group contri...

journal_title：Molecular pharmaceutics

authors： Dahan A,Wolk O,Kim YH,Ramachandran C,Crippen GM,Takagi T,Bermejo M,Amidon GL

更新日期：2013-11-04 00:00:00

abstract：:Terpenoids represent a diverse class of molecules that provide a wealth of opportunities to address many human health and societal issues. The expansive array of structures and functionalities that have been evolved in nature provide an excellent pool of molecules for use in human therapeutics. While this class of mol...

journal_title：Molecular pharmaceutics

authors： Ajikumar PK,Tyo K,Carlsen S,Mucha O,Phon TH,Stephanopoulos G

更新日期：2008-03-01 00:00:00

abstract：:Delta-like ligand 4 (Dll4) expressed in tumor cells plays a key role to promote tumor growth of numerous cancer types. Based on a novel antihuman Dll4 monoclonal antibody (61B), we developed a (64)Cu-labeled probe for positron emission tomography (PET) imaging of tumor Dll4 expression. In this study, 61B was conjugate...

journal_title：Molecular pharmaceutics

authors： Zhou B,Wang H,Liu R,Wang M,Deng H,Giglio BC,Gill PS,Shan H,Li Z

更新日期：2015-10-05 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：:Preferential interactions of formulation excipients govern their overall interactions with protein molecules, and molecular dynamics simulations allow for the examination of the interactions at the molecular level. We used molecular dynamics simulations to examine the interactions of sorbitol, sucrose, and trehalose w...

journal_title：Molecular pharmaceutics

authors： Cloutier T,Sudrik C,Mody N,Sathish HA,Trout BL

更新日期：2019-08-05 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：:Amphotericin B is a lifesaving polyene antibiotic used in the treatment of systemic mycoses. Unfortunately, the pharmacological applicability of this drug is limited because of its severe toxic side effects. At the same time, the lack of a well-defined mechanism of selectivity hampers the efforts to rationally design ...

journal_title：Molecular pharmaceutics

authors： Grela E,Wieczór M,Luchowski R,Zielinska J,Barzycka A,Grudzinski W,Nowak K,Tarkowski P,Czub J,Gruszecki WI

更新日期：2018-09-04 00:00:00

abstract：:This work aims to elucidate the mechanism by which N-methylpyrrolidone (NMP) enhances the skin permeation of a compound by combining experimental data with molecular dynamic (MD) simulations. The addition of 10% NMP significantly increased the propranolol (PR) permeation through the human epidermis (∼ 15 μg/cm(2) vs ∼...

journal_title：Molecular pharmaceutics

authors： Cilurzo F,Vistoli G,Selmin F,Gennari CG,Musazzi UM,Franzé S,Lo Monte M,Minghetti P

更新日期：2014-03-03 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：:Targeted gene delivery using nonviral vectors is a highly touted scheme to reduce the potential for toxic or immunological side effects by reducing dose. In previous reports, TAT polyplexes with DNA have shown relatively poor gene delivery. The transfection efficiency has been enhanced by condensing TAT/DNA complexes ...

journal_title：Molecular pharmaceutics

authors： Khondee S,Baoum A,Siahaan TJ,Berkland C

更新日期：2011-06-06 00:00:00

abstract：:Lipid-based nanoparticles are considered as promising candidates for delivering siRNA into the cytoplasm of targeted cells. However, in vivo efficiency of these nanoparticles is critically dependent on formulation strategies of lipid-siRNA complexes. Adsorption of serum proteins to lipid-siRNA complexes and its charge...

journal_title：Molecular pharmaceutics

authors： Dar GH,Gopal V,Rao NM

更新日期：2015-02-02 00:00:00