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

Author(s):  
Juan Carlos Flores-Arriaga ◽  
Daniel Chavarría-Bolaños ◽  
Amaury de Jesús Pozos-Guillén ◽  
Vladimir Alonso Escobar-Barrios ◽  
Bernardino Isaac Cerda-Cristerna

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.

RSC Advances ◽  
2020 ◽  
Vol 10 (33) ◽  
pp. 19587-19599 ◽  
Author(s):  
Zhiping Fan ◽  
Ping Cheng ◽  
Min Liu ◽  
Sangeeta Prakash ◽  
Jun Han ◽  
...  

Polysaccharides-polypeptide derived biohydrogels were formed using hydrazone chemistry as crosslinking strategy, which have controllable drug release rate and many other potential applications, especially in sustained drug delivery and cell scaffold.


2021 ◽  
Vol 6 (2) ◽  
pp. 29-36
Author(s):  
Ritu Jain ◽  
Ritesh Tiwari ◽  
Rama Shankar Dubey ◽  
Aarti Tiwari ◽  
Ajay Kumar Shukla

RSC Advances ◽  
2017 ◽  
Vol 7 (84) ◽  
pp. 53401-53406 ◽  
Author(s):  
Ke Ma ◽  
Yiping Qiu ◽  
Yaqin Fu ◽  
Qing-Qing Ni

Six kinds of nanoscale application are designed in this study. A significant increase of drug release rate can be observed at the gastric site.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2143
Author(s):  
Marija Jovanović ◽  
Miloš Petrović ◽  
Sandra Cvijić ◽  
Nataša Tomić ◽  
Dušica Stojanović ◽  
...  

Gelatin-polyvinylpyrrolidone (PVP) and gelatin-poly(vinyl alcohol) (PVA) mucoadhesive buccal films loaded with propranolol hydrochloride (PRH) were prepared by semi-solid extrusion 3D printing. The aim of this study was to evaluate the effects of the synthetic polymers PVP and PVA on thermal and mechanical properties and drug release profiles of gelatin-based films. The Fourier-transform infrared spectroscopy showed that hydrogen bonding between gelatin and PVP formed during printing. In the other blend, neither the esterification of PVA nor gelatin occurred. Differential scanning calorimetry revealed the presence of partial helical structures. In line with these results, the mechanical properties and drug release profiles were different for each blend. Formulation with gelatin-PVP and PRH showed higher tensile strength, hardness, and adhesive strength but slower drug release than formulation with gelatin-PVA and PRH. The in silico population simulations indicated increased drug bioavailability and decreased inter-individual variations in the resulting pharmacokinetic profiles compared to immediate-release tablets. Moreover, the simulation results suggested that reduced PRH daily dosing can be achieved with prolonged-release buccal films, which improves patient compliance.


2019 ◽  
Vol 2019 ◽  
pp. 1-9 ◽  
Author(s):  
Nagaraja SreeHarsha ◽  
Chandramouli Ramnarayanan ◽  
Bandar E. Al-Dhubiab ◽  
Anroop B. Nair ◽  
Jagadeesh G. Hiremath ◽  
...  

Sitagliptin (MK–0431) is a widely and commonly used oral hypoglycemic drug in the treatment of type 2 diabetes mellitus; patients typically take higher doses of this drug (50 mg, twice daily). One drawback is that only 38% of the drug is bound reversibly to plasma proteins and 79% is excreted in urine without being metabolized. To overcome this issue, there is a need for a better drug-delivery method to improve its efficacy in patients. It has been found that in existing formulations, the drug content is 72.5% ± 5% and the percentage yield is 84.9% ± 3%. In this study, sitagliptin nanoparticles (sizes ranging from 210 to 618 nm) were developed. The bioadhesion properties of the nanoparticles, as well as the swelling of the nanoparticles on the mucus membrane aided in sustained drug release. The pattern of drug release was in accordance with the Peppas model. Fourier-transform infrared (FTIR) spectroscopy demonstrated that there were no significant interactions between sitagliptin and chitosan. Differential scanning calorimetry (DSC) results showed an absence of drug peaks due to the fact that the drug was present in an amorphous state. Mucoadhesive nanoparticles were formulated using sitagliptin and were effective for about 12 hours in the gastrointestinal tract. When compared to conventional sitagliptin administration, use of a nanoparticle delivery system demonstrated greater benefits for use in oral delivery applications. This is the first time that a drug-delivery method based on the mucoadhesive properties of nanoparticles could prolong the drug-release time of sitagliptin.


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