Pharmaceutical Research

Qiu, Li; Bae, You

doi: 10.1007/s11095-005-9046-2pmid: 16392022

Polymers occupy a major portion of materials used for controlled release formulations and drug-targeting systems because this class of materials presents seemingly endless diversity in topology and chemistry. This is a crucial advantage over other classes of materials to meet the ever-increasing requirements of new designs of drug delivery formulations. The polymer architecture (topology) describes the shape of a single polymer molecule. Every natural, seminatural, and synthetic polymer falls into one of categorized architectures: linear, graft, branched, cross-linked, block, star-shaped, and dendron/dendrimer topology. Although this topic spans a truly broad area in polymer science, this review introduces polymer architectures along with brief synthetic approaches for pharmaceutical scientists who are not familiar with polymer science, summarizes the characteristic properties of each architecture useful for drug delivery applications, and covers recent advances in drug delivery relevant to polymer architecture.

Ahmed, Osama; Pourzand, Charareh; Blagbrough, Ian

doi: 10.1007/s11095-005-8717-3pmid: 16382281

The dienoic fatty acyl spermine conjugate N 4 , N 9 -dilinoleoyl spermine efficiently condenses DNA and achieves the highest transfection levels among the studied lipopolyamines in cultured cells.

Zhao, Chunyan; Zhang, Haixia; Zhang, Xiaoyun; Zhang, Ruisheng; Luan, Feng; Liu, Mancang; Hu, Zhide; Fan, Botao

doi: 10.1007/s11095-005-8716-4pmid: 16308669

The classification accuracy of training set and test set for SVM was 90.63 and 90.00%, respectively. The total accuracy for SVM was 90.48%, which was higher than that of LDA (77.78%). Comparison of the two methods shows that the performance of SVM was better than that of LDA, which implies that the SVM method is an effective tool in evaluating the risk of drugs when experimental M/P ratios have not been investigated.

Jonassen, Ib; Havelund, Svend; Ribel, Ulla; Plum, Anne; Loftager, Mette; Hoeg-Jensen, Thomas; Volund, Aage; Markussen, Jan

doi: 10.1007/s11095-005-9047-1pmid: 16362452

NN344 is a candidate for a neutral soluble basal insulin that might offer people with diabetes a prolonged duration, smooth, and predictable basal insulin supplement.

Persson, Kajsa; Ekehed, Susanne; Otter, Charlotta; Lutz, E.; McPheat, Jane; Masimirembwa, Collen; Andersson, Tommy

doi: 10.1007/s11095-005-8812-5pmid: 16328606

Liver slices are a valuable model to study the regulation of a larger number of enzymes by single compounds. The PXR reporter gene assay could be used as a reliable screening method to predict CYP3A induction in vivo .

Fedorov, Sergey; Radchenko, Oleg; Shubina, Larisa; Balaneva, Nadezhda; Bode, Ann; Stonik, Valentin; Dong, Zigang

doi: 10.1007/s11095-005-8813-4pmid: 16320003

Quinones 1 and 3 – 14 demonstrated cancer-preventive activity in JB6 Cl41 cells, which may be attributed to the induction of p53-independent apoptosis. These activities depended on the length of side chains and on the positions of the methoxyl groups in the quinone part of the molecule.

Liu, Xingjun; Wang, Wei; Hu, Han; Tang, Ning; Zhang, Chunling; Liang, Wei; Wang, Minwei

doi: 10.1007/s11095-005-9043-5pmid: 16341574

Our data demonstrate that naringenin can exert antifibrogenic effects by directly or indirectly down-regulating Smad3 protein expression and phosphorylation through TGF-β signaling.

Eichele, Karin; Weinzierl, Ulrike; Ramer, Robert; Brune, Kay; Hinz, Burkhard

doi: 10.1007/s11095-005-8815-2pmid: 16267630

R(+)-MA-induced apoptosis is mediated via a mitochondrial-dependent pathway that becomes activated, at least in part, through up-regulation of the COX-2 enzyme.

Ng, Chee; Stefanich, Eric; Anand, Banmeet; Fielder, Paul; Vaickus, Louis

doi: 10.1007/s11095-005-8814-3pmid: 16308668

TRX1 displayed nonlinear pharmacokinetic behavior and the CD4 receptors on T cells were saturated and down-modulated following treatment with TRX1. Results from in vitro studies using purified human T cells suggested that CD4-mediated internalization may constitute one pathway by which CD4 is down-modulated and TRX1 is cleared in vivo . The developed receptor-mediated PK/PD model adequately described the data. This PK/PD model was used to simulate PK/PD time profiles after different dosing regimens to help guide the dose selection in future clinical studies.

Martanto, Wijaya; Moore, Jason; Kashlan, Osama; Kamath, Rachna; Wang, Ping; O'Neal, Jessica; Prausnitz, Mark

doi: 10.1007/s11095-005-8498-8pmid: 16308670

By partially retracting microneedles after insertion and other methods to overcome flow resistance of dense dermal tissue, protocols can be designed for hollow microneedles to microinfuse fluid at therapeutically relevant rates.