Synthesis of a PVA drug delivery system for controlled release of a Tramadol–Dexketoprofen combination

• DOI: 10.1007/s10856-021-06529-3
• Publication Date: 2021-05-07T13:06:10Z
• Authors: Juan Carlos Flore...; Daniel Chavarría-...; Amaury de Jesús P...; Vladimir Alonso E...; Bernardino Isaac ...
• Keywords: Adult; Male; 0301 basic medicine; Anti-Inflammatory Agents, Non-Steroidal; Membranes, Artificial; Delivery Systems; 3. Good health; Analgesics, Opioid; Drug Combinations; Drug Liberation; 03 medical and health sciences; Drug Delivery Systems; Ketoprofen; Delayed-Action Preparations; Polyvinyl Alcohol; Spectroscopy, Fourier Transform Infrared; Prothrombin Time; Humans; Partial Thromboplastin Time; Tramadol

AbstractThe local administration of analgesic combinations by means of degradable polymeric drug delivery systems is an alternative for the management of postoperative pain. We formulated a Tramadol–Dexketoprofen combination (TDC) loaded in poly(vinyl alcohol) (PVA) film. Films were prepared by the solvent casting method using three different molecular weights of PVA and crosslinking those films with citric acid, with the objective of controlling the drug release rate, which was evaluated by UV–vis spectrometry. Non-crosslinked PVA films were also evaluated in the experiments. Differential scanning calorimetry (DSC) analysis of samples corroborated the crosslinking of PVA by the citric acid. Blank and loaded PVA films were tested in vitro for its impact on blood coagulation prothrombin time (PT) and partial thromboplastin time (PTT). The swelling capacity was also evaluated. Crosslinked PVA films of higher-molecular weight showed a prolonged release rate compared with that of the lower-molecular-weight films tested. Non-crosslinked PVA films released 11–14% of TDC. Crosslinked PVA films released 80% of the TDC loaded (p < 0.05). This suggests that crosslinking films can modify the drug release rate. The blank and loaded PVA films induced PT and PTT in the normal range. The results showed that the polymeric films evaluated here have the appropriate properties to allow films to be placed directly on surgical wounds and have the capacity for controlled drug release to promote local analgesia for the control of postoperative pain.