Development and in vitro/in vivo evaluation of famotidine hydrochloride bioadhesive sustained release suspension.

To develop a new kind of famotidine-resin microcapsule for gastric adhesion sustained release by screening out suitable excipients and designing reasonable prescriptions to improve patient drug activities to achieve the expected therapeutic effect. The famotidine drug resin was prepared using the water bath method with carbomer 934 used as coating material. Microcapsules were prepared using the emulsified solvent coating method and appropriate excipients were used to prepare famotidine sustained release suspension. Pharmacokinetics of the developed microcapsules were studied in the gastrointestinal tract of rats. The self-made sustained-release suspension of famotidine hydrochloride effectively reduced the blood concentration and prolonged the action time. The relative bioavailability of the self-made suspension of the famotidine hydrochloride to the commercially available famotidine hydrochloride was 146.44%, with an average retention time of about 5h longer, which indicated that the new suspension had acceptable adhesion properties. The findings showed that the newly developed famotidine-resin microcapsule increased the bioavailability of the drug with a significant sustained-release property.

Fabrication of ticagrelor bioadhesive solid dispersion based on coaxial electrostatic spray to improve drug release and enhance oral bioavailability.

Due to the low solubility and poor bioavailability of Ticagrelor (TIC), the current study developed a structured bioadhesive core-shell drug delivery system to address it. Ticagreior solid dispersion (T-SD) was fabricated using the uniaxial electrostatic spray method. Ticagrelor bio adhesive solid dispersion (T-BSD) was also prepared using the coaxial electrostatic spray technique. The adhesion of T-BSD to each intestinal segment was determined using biological adhesion test. The compartment model was used to study the plasma concentration-time curve and related pharmacokinetic parameters. The results of bioadhesion tests showed a positive adhesion effect of T-BSD in each intestinal segment. The maximum plasma concentration (Cmax) of T-BSD was increased to 777.08ng/mL compared with the free drug (367ng/mL). Similarly, t1/2, MRT and Tmax of T-BSD (12.1h, 9.4h, 4h) were higher than the free drug (11.2h, 8.6h, 1h), respectively. The relative bioavailability of T-BSD was further increased to 430% compared with the free drug. The findings collectively revealed that the coaxial-electrospray technique could be a promising way to improve the bioavailability of TIC.

Preparation and in vitro/in vivo evaluation of 6-Gingerol TPGS/PEG-PCL polymeric micelles.

6-Gingerol, an active herbal ingredient of ginger has various bioactivities such as anti-neurodegenerative disease, anti-inflammatory and so on. The aim of the present study was to enhance the oral bioavailability and brain distribution of 6-Gingerol via polymeric micelles. A polymeric micelles drug delivery system of 6-Gingerol consisting of D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) and Poly (ethylene glycol)-poly (ε-caprolactone) (PEG-PCL) was prepared via solvent injection method. The developed 6-Gingerol-loaded TPGS/PEG-PCL micelles (6-GTPMs) were characterized based on particle size, polydispersity index (PDI), zeta potential, encapsulation efficiency (EE), drug loading (DL) and in vitro release profile. The pharmacokinetics and tissue distribution studies were also evaluated. The nanoformulation produced a particle size of 73.24 ± 2.84 nm with acceptable PDI (0.129 ± 0.03), zeta potential (-2.74 ± 0.92 mV), DL (4.64%) and EE (79.68%). The in vitro release profile showed that the 6-GTPMs enhanced the solubility of 6-Gingerol, while the pharmaceutical analysis in rats indicated that 6-GTPMs significantly improved the oral bioavailability of 6-Gingerol (about 3 folds) in circulation. The 6-GTPMs exhibited remarkable brain targetability in the tissue distribution analysis. Collectively, a 6-Gingerol polymeric micelle with enhanced oral bioavailability coupled with excellent brain distribution was successfully developed.