Objectives: Despite having profound therapeutic value, the clinical application of resveratrol is restrained due to its <1% bioavailability, arising from the extensive fast-pass effect along with enterohepatic recirculation. This study aimed to develop a self-emulsifying formulation capable of increasing the bioavailability of resveratrol via lymphatic transport. Methods: The resveratrol–phospholipid complex (RPC) was formed by the solvent evaporation method and characterized by FTIR, DSC, and XRD analyses. The RPC-loaded self-emulsifying drug delivery system (SEDDS) was designed, developed, and optimized using the QbD approach with an emphasis on resveratrol transport through the intestinal lymphatic pathway. The in vivo pharmacokinetic study was investigated in male Wister Albino rats. Results: The FTIR, DSC, and XRD analyses confirmed the RPC formation. The obtained design space provided robustness of prediction within the 95% prediction interval to meet the CQA specifications. An optimal formulation (desirability value of 7.24) provided Grade-A self-emulsion and exhibited a 48-fold bioavailability enhancement compared to the pure resveratrol. The cycloheximide-induced chylomicron flow blocking approach demonstrated that 91.14% of the systemically available resveratrol was transported through the intestinal lymphatic route. Conclusions: This study suggests that an optimal self-emulsifying formulation can significantly increase the bioavailability of resveratrol through lymphatic transport to achieve the desired pharmacological effects.
1 January 2020 in Biomedical Physics & Engineering Express
The application of surgical suture-thread and the systemic analgesics regimens for pain control in the postoperative surgery remain the criterion standard. However, these medications have daunting adverse effects on the body’s innate pain management system. To address this issue, we have developed a local analgesic-loaded suture system which could be efficiently used for surgical repair with localized sedation effect. The drug-loaded conventional suture has modified by adhesive poly-dopamine coating with the local anesthetic lidocaine. The surface modifications have been ascertained by FE-SEM imaging. The tensile strength of suture ensures required elasticity to use in surgical skin closure. In vitro drug release and the in vivo local analgesia was achieved one day after surgery and persisted approximately for one week in 80% of treated animals. Our pre-clinical results suggest that drug-loaded surgical thread may be an effective strategy for improving the overall outcome.