Conventional forms of drug administration generally rely on pills, eye drops, ointments, and intravenous solutions. Recently, a number of novel drug delivery approaches have been developed. These approaches include drug modification by chemical means, drug entrapment in small vesicles that are injected into the bloodstream, and drug entrapment within pumps or polymeric materials that are placed in desired bodily compartments (for example, the eye or beneath the skin). These techniques have already led to delivery systems that improve human health, and continued research may revolutionize the way many drugs are delivered.

http://science.sciencemag.org/content/sci/249/4976/1527.full.pdf

New methods of drug delivery.

This study aimed to review the literature describing and quantifying time lags in the health research translation process. Papers were included in the review if they quantified time lags in the development of health interventions. The study identified 23 papers. Few were comparable as different studies use different measures, of different things, at different time points. We concluded that the current state of knowledge of time lags is of limited use to those responsible for R&D and knowledge transfer who face difficulties in knowing what they should or can do to reduce time lags. This effectively ‘blindfolds’ investment decisions and risks wasting effort. The study concludes that understanding lags first requires agreeing models, definitions and measures, which can be applied in practice. A second task would be to develop a process by which to gather these data.

The Answer Is 17 Years, What Is the Question

Caco-2 monolayers in experimental and theoretical predictions of drug transport

Lyophilization and development of solid protein pharmaceuticals

Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs.

Prodrugs are molecules with little or no pharmacological activity that are converted to the active parent drug in vivo by enzymatic or chemical reactions or by a combination of the two. Prodrugs have evolved from being serendipitously discovered or used as a salvage effort to being intentionally designed. Such efforts can avoid drug development challenges that limit formulation options or result in unacceptable biopharmaceutical or pharmacokinetic performance, or poor targeting. In the past 10 years, the US Food and Drug Administration has approved at least 30 prodrugs, which accounts for more than 12% of all approved small-molecule new chemical entities. In this Review, we highlight prodrug design strategies for improved formulation and pharmacokinetic and targeting properties, with a focus on the most recently marketed prodrugs. We also discuss preclinical and clinical challenges and considerations in prodrug design and development.

The expanding role of prodrugs in contemporary drug design and development

Development of a supersaturable SEDDS (S-SEDDS) formulation of paclitaxel with improved oral bioavailability

Effects of buffer composition and processing conditions on aggregation of bovine IgG during freeze-drying

The importance of water sorption on solid state stability of proteins can be addressed through an understanding of properties of the sorbed water and its impact on the properties of the protein. Most decomposition reactions are minimal at or below the monolayer level of hydration. Sorption of water beyond that of the monolayer generally results in increased rates of decomposition due to the increased conformational flexibility of the protein and the ability of the less tightly bound water to mobilize reactants. In many cases the rates of decomposition can be influenced by the addition of excipients. An understanding of how such excipients can influence water sorption and stability will allow for improved development strategies to minimize the decomposition of proteins in the solid state.

The role of moisture in protein stability

Recent debates have emerged on whether it is water activity (a W ) or the state of the system as dictated by the glass transition temperature (T g ) that impacts the rates of chemical reactions in reduced-moisture solid systems. Previously, model systems could not evaluate the effects of water activity and glass transition independently. By using poly(vinylpyrrolidone) (PVP) of different molecular weights, the effect of water activity and glass transition on chemical reactions can be studied independently and at a constant temperature. The kinetics of aspartame degradation, via its rearrangement into diketopiperazine, was evaluated in the PVP model system. Reaction rates at constant water activity, but different T g values, were not significantly different

Differentiating between the Effects of Water Activity and Glass Transition Dependent Mobility on a Solid State Chemical Reaction: Aspartame Degradation

Michael J. Hageman

Papers

The expanding role of prodrugs in contemporary drug design and development

Development of a supersaturable SEDDS (S-SEDDS) formulation of paclitaxel with improved oral bioavailability

Effects of buffer composition and processing conditions on aggregation of bovine IgG during freeze-drying

The role of moisture in protein stability

Differentiating between the Effects of Water Activity and Glass Transition Dependent Mobility on a Solid State Chemical Reaction: Aspartame Degradation