A combined-modification method of carboxymethyl β-cyclodextrin and lignin for nano-hydroxyapatite to reinforce poly(lactide-co-glycolide) for bone materials.

Lignin is the second most abundant natural biomacromolecule. A new surface-modification for nano-hydroxyapatite (n-HA) by carboxymethyl β-cyclodextrin (CM-β-CD) and lignin and its reinforce effect for poly(lactide-co-glycolide) (PLGA) were investigated by Fourier transformation infrared (FTIR), X-ray diffraction pattern (XRD), transmission electron microscopy (TEM), thermal gravimetric analysis (TGA), dispersion images, the tensile tests, scanning electron microscope (SEM), differential scanning calorimeter (DSC) and polarized optical microscopy (POM), compared to the singled-modification of CM-β-CD or lignin. The results showed that the appropriate combined-modified n-HA displayed excellent synergistic effects for increasing the dispersion, yielding good interfacial bonding between n-HA with PLGA matrix.

Comparison of uptake transporter functions in hepatocytes in different species to determine the optimal model for evaluating drug transporter activities in humans.

A thorough understanding of species-dependent differences in hepatic uptake transporters is critical for predicting human pharmacokinetics (PKs) from preclinical data. In this study, the activities of organic anion transporting polypeptide (OATP/Oatp), organic cation transporter 1 (OCT1/Oct1), and sodium-taurocholate cotransporting polypeptide (NTCP/Ntcp) in cultured rat, dog, monkey and human hepatocytes were compared. The activities of hepatic uptake transporters were evaluated with respect to culture duration, substrate and species-dependent differences in hepatocytes.

CYP Suppression in Human Hepatocytes by Monomethyl Auristatin E, the Payload in Brentuximab Vedotin (Adcetris), is Associated with Microtubule Disruption.

Background And Objectives: Monomethyl auristatin E (MMAE), the toxin linked to CD30-specific monoclonal antibody of Adcetris (brentuximab vedotin), is a potent anti-microtubule agent. Brentuximab vedotin has been approved for the treatment of relapsed or refractory Hodgkin lymphoma and anaplastic large cell lymphoma. Cytochrome P450 (CYP) induction assessment of MMAE was conducted in human hepatocytes to assess DDI potentials and its translation to clinic.

The use of a rapid MS-based method for the quantification of the CYP 3A4 protein directly from hepatocyte cell lysate for CYP induction studies.

Background: Most P450 protein quantitation methods involved the time-consuming preparation of microsomes and therefore are not amenable for high-throughput analysis. We here report a new method to measure P450 CYP3A4 protein levels directly from cell lysates.

Results: A direct sample preparation method from hepatocyte cell lysate has been developed for the quantification of CYP3A4 protein levels by combining a modified semi-automated precipitation with a filter-aided sample preparation.