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

Abstract

The 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.

Chitosan-Based Thermo-Responsive Scaffold for Wound Heal-ing Provides Dexketoprofen Trometamol Controlled Release for 24 Hour-Use

“…2b) shows a crystalline endotherm at 156.45 °C that seems to correspond with citric acid melting point (154.11 °C). On the other hand, F2 shows a shift in PVA endotherm at 194.30 °C to 177.06 °C, which can be due to the polymerization process and crosslinking with citric acid [22]. However, in this formulation, it is not possible to see PVA second endotherm at 323.61 °C or any other related to chitosan and citric acid.…”

“…5.a) showed a reduction in the drug released at 24 hours (88.40 ± 3.94 %) but also reduced burst release compared to F1 (1h: 26,81 ± 3.25 %, 6h: 58.16 ± 3.07 %). This profile can be attributed to the presence of intra-and inter-crosslinked PVA tubules by the citric acid, which reduce porosity, difficult the penetration of water molecules and reduce wettability [22]. Nonetheless, F3 (Fig.…”

“…2 (a and b), it is not possible to identify DKT melting point in the formulations at 107.33 °C as obtained in the DSC analysis for the raw material due to its low concentration. In addition, polymerization phenomena due to the agitation and heating time could have caused a series of shifts in different thermal events from the constituent materials [21,22]. As a result, it is not possible to appreciate chitosan's endotherm at 90.28 °C or close in any of the formulations.…”

SeDeM tool-driven full factorial design for osmotic drug delivery of tramadol HCl: Formulation development, physicochemical evaluation, and in-silico PBPK modeling for predictive pharmacokinetic evaluation using GastroPlus™

“…A study conducted by Palla N et al also reported the absence of interaction between tramadol HCl and HPMC (Palla et al, 2013). Another study suggests that there is no visible interaction between tramadol HCl and commonly used pharmaceutical excipients (Flores-Arriaga et al, 2021).…”

Ultrathin, elastic, and self-adhesive nanofiber bio-tape: An intraoperative drug-loading module for ureteral stents with localized and controlled drug delivery properties for customized therapy

“…In addition, the adhesion strength of the hydrogel to the US is also weakened by its swelling features [ [20] , [21] , [22] ]. Other preparation techniques for drug carriers include 3-D printing [ [23] , [24] , [25] , [26] ], solvent casting [ 27 ], and micro-nano capsules [ [28] , [29] , [30] , [31] ]. However, the drug-loading process (type, dose) is usually carried out before polymer molding and cannot be adjusted in use.…”