Cannabidiol (CBD), a phytocannabinoid compound of Cannabis sativa, shows limited oral bioavailability due to its lipophilicity and extensive first-pass metabolism. CBD is also known for its high intra- and inter-subject absorption variability in humans. To overcome these limitations a novel self-emulsifying drug delivery system (SEDDS) based on VESIsorb® formulation technology incorporating CBD, as Hemp-Extract, was developed (SEDDS-CBD). The study objective was to evaluate the pharmacokinetic profile of SEDDS-CBD in a randomized, double-blind, cross-over design in 16 healthy volunteers under fasted conditions. As reference formulation, the same Hemp-Extract diluted with medium-chain triglycerides (MCT-CBD) was used. CBD dose was standardized to 25 mg. Pharmacokinetic parameters were analyzed from individual concentration-time curves. Single oral administration of SEDDS-CBD led to a 4.4-fold higher Cmax and a 2.85-/1.70-fold higher AUC0–8h/AUC0–24h compared to the reference formulation. Tmax was substantially shorter for SEDDS-CBD (1.0 h) compared to MCT-CBD (3.0 h). Subgroup analysis demonstrated a higher bioavailability in women compared to men. This difference was seen for MCT-CBD while SEDDS-CBD mitigated this gender effect. Overall, SEDDS-CBD showed a significant improvement for all determined pharmacokinetic parameters: increased CBD plasma values (Cmax), favorably enhanced bioavailability (AUC) and fast absorption (Tmax). No safety concerns were noted following either administration.
Several health promoting effects have been reported for maqui berry, rich in anthocyanins. Direct effects of anthocyanins as well as bioactive metabolites might be involved. Within the study, bioavailability of a proprietary standardized maqui berry extract Delphinol® was investigated based on two selected anthocyanins (delphinidin-3-O-glucoside (DS) + cyanidin-3-O-sambubioside (CS)) and two breakdown products (protocatechuic acid (PCA) + gallic acid (GA)) after a single-dose supplementation in humans. Pharmacokinetic parameters were calculated from individual concentration time curves. In all 12 subjects a significant increase was noted in plasma values of DG and CS after intake of maqui berry extract. Maximum concentration of DG was observed after 1.0 ± 0.3 h and CS after 2.0 ± 1.1 h. Within 8 h, concentrations nearly returned to baseline levels. The results confirm a fast uptake and metabolism of the two selected key substances. Additionally, the phenolic acids GA and PCA were observed as breakdown products of anthocyanins. In summary, the study clearly confirms the bioavailability of maqui berry extract and its specific anthocyanin compounds and related breakdown products in healthy subjects.
Background and Aims: Implants for surgical needs are produced from different materials including metals, alloys, ceramics or polymers. Metal implants are preferred in those disciplines where sufficient mechanical strength is needed, including traumatology, orthopedic or dental surgery. Further, modern tissue engineering techniques require scaffold materials to generate shape and stability for in vitro generated transplants. However, the biocompatibility and surface contact of most implants or scaffold materials to vital bone or other tissues are not optimal. Therefore we investigated the biocompatibility of different polymer surfaces to an osteoblastic cell line as a function of wettability or hydrophobicity to describe some of the surface parameters influencing the cell to implant or cell to scaffold contact. Methods: Glass slides were coated with different polymers and in some cases physically or chemically modified. SAOS-2 osteosarcoma cells were used for the biocompatibility tests on 16 different polymers and modifications thereof. The viability of the adherent cells was investigated by MTT assay. Commercially available tissue culture vessels served as controls. Results: We report that excellent biocompatibility to SAOS-2 osteoblastic cells can be obtained with hydrophobic surfaces generated for instance by epoxy resins. Chemical modification of epoxy resin surfaces yielded even a further increased viability index surpassing the viability index obtained with cell culture vessels. Conclusion: We conclude that modified hydrophobic surfaces represent an interesting group of compounds for coating endoprosthetic implants or scaffolds for the purposes of tissue engineering.
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