Pharmacokinetic Evaluation of a Single 5-Gram Bolus of Creatine Monohydrate Versus Two Other Creatine-Containing Investigational Products.

The purpose of this study was to determine the relative pharmacokinetics of creatine monohydrate delivered as a formula or as a pure powder (all mixed in solution). A single 5 g bolus of creatine monohydrate was ingested as CreaBev 1, CreaBev 2, or creatine monohydrate. Participants we assigned a test product and monitored in a supervised laboratory setting for ingestion and all blood draws starting 30 min post-ingestion to the 6-h mark. Standard pharmacokinetic analysis was undertaken to determine relative maximum concentration (Cmax), time to maximum concentration (Tmax), and area under the curve (AUC) for the products. Cmax data indicate that CreaBev 1 10.55±4.10, CreaBev 2 15.45±5.48, and creatine monohydrate 12.77±4.0 nmol/h/µL. The Tmax analysis demonstrated CreaBev 1 1.20±1.01, CreaBev 2 1.23±0.65, and creatine monohydrate 0.91±0.2 h. The AUC data indicate that CreaBev 1 22.90±9.17, CreaBev 2 33.92±9.52, and creatine monohydrate 29.58±11.93 nmol/h/µL. When examining the data for pharmacokinetics, the AUC and Cmax pharmacokinetics were greatest for CreaBev 2 (p<0.021 and 0.020). Within the confines of this study, CreaBev 2 produced the highest blood concentrations of creatine as compared to creatine monohydrate and CreaBev 1.

Nano-carriers for targeted delivery and biomedical imaging enhancement.

Theranostic approaches using nanotechnology have been a hot research area for the past decade. All nano drug delivery techniques and architectures have some limitations, as do diagnostic nano-approaches. Thus, combining nano drug delivery strategies with diagnostic techniques using nanoparticles for improving imaging modalities has been the key to fill up those gaps. In the past decade, lots of approaches have been made with different combinations of biomaterials fabricated/synthesized to nanostructures with modified surface functionalization to improve their overall theranostic properties. This article summarizes recent research works based on the biomaterials used for fabricating these nanostructures. Their combinations with other biomaterials have been demonstrated with their overall advantages and limitations.

Improved pharmacokinetics and enhanced tumor growth inhibition using a nanostructured lipid carrier loaded with doxorubicin and modified with a layer-by-layer polyelectrolyte coating.

A nanostructured lipid carrier (NLC) loaded with doxorubicin (DOX) has been shown to be cytotoxic against the human cancer cell lines A549 and MCF-7/Adr. In attempts to improve formulation characteristics, enhance pharmacokinetics and antitumor effects, we modified the surface of these NLC with an alternating layer-by-layer (LbL) assembly of polycation and polyanion polyelectrolytes and an additional coating with PEG using a simple method of core shell attachment. The formulation had a narrow size distribution, longer residence in the blood, lower accumulation in the liver, higher accumulation in tumors and a significant tumor growth inhibition effect. Thus, NLC-DOX nanopreparations complexes modified by LbL coating have the potential to enhance the anticancer effects of DOX against tumors.

Layer-by-layer nanoencapsulation of camptothecin with improved activity.

160 nm nanocapsules containing up to 60% of camptothecin in the core and 7-8 polyelectrolyte bilayers in the shell were produced by washless layer-by-layer assembly of heparin and block-copolymer of poly-l-lysine and polyethylene glycol. The outer surface of the nanocapsules was additionally modified with polyethylene glycol of 5 kDa or 20 kDa molecular weight to attain protein resistant properties, colloidal stability in serum and prolonged release of the drug from the capsules. An advantage of the LbL coated capsules is the preservation of camptothecin lactone form with the shell assembly starting at acidic pH and improved chemical stability of encapsulated drug at neutral and basic pH, especially in the presence of albumin that makes such formulation more active than free camptothecin. LbL nanocapsules preserve the camptothecin lactone form at pH 7.4 resulting in triple activity of the drug toward CRL2303 glioblastoma cell.