scholarly journals 3D Printed Buccal Films for Prolonged-Release of Propranolol Hydrochloride: Development, Characterization and Bioavailability Prediction

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.

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.


Polymers ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 691
Author(s):  
O. Sánchez-Aguinagalde ◽  
Ainhoa Lejardi ◽  
Emilio Meaurio ◽  
Rebeca Hernández ◽  
Carmen Mijangos ◽  
...  

Chitosan (CS) and poly (vinyl alcohol) (PVA) hydrogels, a polymeric system that shows a broad potential in biomedical applications, were developed. Despite the advantages they present, their mechanical properties are insufficient to support the loads that appear on the body. Thus, it was proposed to reinforce these gels with inorganic glass particles (BG) in order to improve mechanical properties and bioactivity and to see how this reinforcement affects levofloxacin drug release kinetics. Scanning electron microscopy (SEM), X-ray diffraction (XRD), swelling tests, rheology and drug release studies characterized the resulting hydrogels. The experimental results verified the bioactivity of these gels, showed an improvement of the mechanical properties and proved that the added bioactive glass does affect the release kinetics.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 455
Author(s):  
Emilia Szymańska ◽  
Katarzyna Woś-Latosi ◽  
Julia Jacyna ◽  
Magdalena Dąbrowska ◽  
Joanna Potaś ◽  
...  

Microparticles containing water-soluble zidovudine were prepared by spray-drying using chitosan glutamate and beta-glycerophosphate as an ion crosslinker (CF). The Box–Behnken design was applied to optimize the microparticles in terms of their drug loading and release behavior. Physicochemical studies were undertaken to support the results from dissolution tests and to evaluate the impact of the crosslinking ratio on the microparticles’ characteristics. The zidovudine dissolution behavior had a complex nature which comprised two phases: an initial burst effect followed with a prolonged release stage. The initial drug release, which can be modulated by the crosslinking degree, was primarily governed by the dissolution of the drug crystals located on the microparticles’ surfaces. In turn, the further dissolution stage was related to the drug diffusion from the swollen polymer matrix and was found to correlate with the drug loading. Differential Scanning Calorimetry (DSC) studies revealed the partial incorporation of a non-crystallized drug within the polymer matrix, which correlated with the amount of CF. Although CF influenced the swelling capacity of chitosan glutamate microparticles, surprisingly a higher amount of CF did not impact the time required for 80% of the drug to be released markedly. The formulation with the lowest polymer:CF ratio, 3:1, was selected as optimal, providing satisfactory drug loading and displaying a moderate burst effect within the first 30 min of the study, followed with a prolonged drug release of up to 210 min.


2018 ◽  
Vol 244 (4) ◽  
pp. 283-293 ◽  
Author(s):  
Stephen J. Jones ◽  
Annette F. Taylor ◽  
Paul A Beales

Nanomedicines for controlled drug release provide temporal and spatial regulation of drug bioavailability in the body. The timing of drug release is usually engineered either for slow gradual release over an extended period of time or for rapid release triggered by a specific change in its physicochemical environment. However, between these two extremes, there is the desirable possibility of adaptive nanomedicines that dynamically modulate drug release in tune with its changing environment. Adaptation and response through communication with its environment is a fundamental trait of living systems; therefore, the design of biomimetic nanomedicines through the approaches of bottom-up synthetic biology provides a viable route to this goal. This could enable drug delivery systems to optimize release in synchronicity with the body’s natural biological rhythms and the personalized physiological characteristics of the patient, e.g. their metabolic rate. Living systems achieve this responsiveness through feedback-controlled biochemical processes that regulate their functional outputs. Towards this goal of adaptive drug delivery systems, we review the general benefits of nanomedicine formulations, provide existing examples of experimental nanomedicines that encapsulate the metabolic function of enzymes, and give relevant examples of feedback-controlled chemical systems. These are the underpinning concepts that hold promise to be combined to form novel adaptive release systems. Furthermore, we motivate the advantages of adaptive release through chronobiological examples. By providing a brief review of these topics and an assessment of the state of the art, we aim to provide a useful resource to accelerate developments in this field. Impact statement The timing and rate of release of pharmaceuticals from advanced drug delivery systems is an important property that has received considerable attention in the scientific literature. Broadly, these mostly fall into two classes: controlled release with a prolonged release rate or triggered release where the drug is rapidly released in response to an environmental stimulus. This review aims to highlight the potential for developing adaptive release systems that more subtlety modulate the drug release profile through continuous communication with its environment facilitated through feedback control. By reviewing the key elements of this approach in one place (fundamental principles of nanomedicine, enzymatic nanoreactors for medical therapies and feedback-controlled chemical systems) and providing additional motivating case studies in the context of chronobiology, we hope to inspire innovative development of novel “chrononanomedicines.”


Polymers ◽  
2018 ◽  
Vol 10 (10) ◽  
pp. 1178 ◽  
Author(s):  
Yanping Liu ◽  
Hanghang Wei ◽  
Zhen Wang ◽  
Qian Li ◽  
Nan Tian

The mechanical properties of poly (lactic acid) (PLA) nanofibers with 0%, 5%, 10%, and 20% (w/w) poly (vinyl alcohol) (PVA) were investigated at the macro- and microscale. The macro-mechanical properties for the fiber membrane revealed that both the modulus and fracture strain could be improved by 100% and 70%, respectively, with a PVA content of 5%. The variation in modulus and fracture strain versus the diameter of a single electrospun fiber presented two opposite trends, while simultaneous enhancement was observed when the content of PVA was 5% and 10%. With a diameter of 1 μm, the strength and toughness of the L95V5 and L90V10 fibers were enhanced to over 3 and 2 times that of pure PLA, respectively. The structural evolution of electrospun nanofiber was analyzed by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). Although PLA and PVA were still miscible in the concentration range used, the latter could crystallize independently after electrospinning. According to the crystallization behavior of the nanofibers, a double network formed by PLA and PVA—one microcrystal/ordered structure and one amorphous structure—is proposed to contribute to the simultaneous enhancement of strength and toughness, which provides a promising method for preparing biodegradable material with high performance.


2021 ◽  
Vol ahead-of-print (ahead-of-print) ◽  
Author(s):  
Nehad N. Rozik ◽  
Emad Saad Shafik ◽  
Salwa L. Abd-El-Messieh

Purpose This study aims to polymerize of 1-butyl-3-vinylimidazolium bromide (PIL). PIL was embedded into PVA with a different content ratio by casting method. This research also deals with the effect of adding PIL in different proportions to PVA on the electrical and mechanical properties properties in addition to the morphology of the prepared samples. Design/methodology/approach 1-Butyl-3-vinylimidazolium bromide was synthesized through quaternization and free radical polymerization. The resulting polymer was characterized by Fourier transform infrared (FTIR) spectroscopy, thermogravimetric analysis and differential scanning calorimetry. In addition to the morphology of PVA, PVA/PIL was investigated by polarizing microscope. Also, the effect of PIL content on the electrical and mechanical properties was evaluated. Findings The findings of this study might lead to new applications for PVA and PILs in electrical and dielectrics. The mechanical results revealed that the tensile strength increased slightly with increasing polyionic liquid (PIL) content and decreased above 10% PIL. While the elongation at break increased significantly with increasing PIL content and begin to decrease above 10% PIL. Also, the electrical property of the poly(vinyl alcohol) (PVA)/PIL blends was improved because of the strong plasticizing effect of PIL. Also, the electrical conductivity of these polymer electrolytes is greatly increased. This indicates that the imidazolium-based PIL has an effective approach that leads to an increase in the conductivity of the polymer. The PILs/PVA design will not only enrich the chemical structure but also will contribute to green manufacturing techniques and a processing methodology that enables green membrane manufacture. Originality/value This study contributes to green manufacturing techniques and a processing methodology that enables “green” membrane manufacture.


Author(s):  
Mohammad K. Hossain ◽  
Samira N. Shaily ◽  
Hadiya J. Harrigan ◽  
Terrie Mickens

A completely biodegradable composite was fabricated from an herbal polymer, soy protein concentrate (SPC) resin. Soy protein was modified by adding 30 wt% of glycerol and 5 wt% of poly vinyl alcohol (PVA) to enhance its mechanical as well as thermal property. 3%, 5%, 10%, and 20% nanoclay (NC) were infused into the system. To evaluate its mechanical properties, crystallinity, thermal properties, bonding interaction, and morphological evaluation, tensile, X-ray diffraction (XRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR) tests, and optical microscopy (OM) and scanning electron microscopy (SEM) evaluation were performed. Tensile tests showed that the addition of nanoclay improved the mechanical properties of the modified resin. Soy protein is hydrophilic due to the presence of amino acids that contain various polar groups such as amine, carboxyl, and hydroxyl. As a result, polar nanoclay particles that are exfoliated can be evenly dispersed in the SPC resin. From experimental results, it is clear that adding of nanoclay with SPC resin significantly increased the stiffness of the SPC resin. A combination of 5% clay, 30% glycerol, and 5% PVA with the modified SPC resulted in the maximum stress of 18 MPa and Young modulus of 958 MPa. The modified SPC showed a reduced failure strain as well. X-ray diffraction curves showed an improvement of crystallinity of the prepared resin with increasing amount of nanoclay. Interaction among soy, glycerol, PVA, and nanoclay was clearly demonstrated from the FTIR analysis. Optical microscopy (OM) and scanning electron microscopy (SEM) micrographs revealed rougher surface in the nanoclay infused SPC samples compared to that of the neat one. SEM evaluation revealed rougher fracture surface in the NC infused samples.


e-Polymers ◽  
2010 ◽  
Vol 10 (1) ◽  
Author(s):  
Qun Wang ◽  
Lu Qi

AbstractA group of films mainly composed of sericin and poly(vinyl alcohol) (PVA), using boric acid (BA) as a modifier, were prepared by a technique of solution casting. In this work, the effect of BA and sericin on the mechanical properties and water resistance of the films was analyzed, the interior morphology of the films were described by a scanning electron microscopy (SEM), the thermal stability of the films was characterized by differential scanning calorimetry (DSC), and the reaction mechanism was proposed according to the previous literature and the test of Fourier transform infrared spectrum (FTIR). Results indicated that, the properties of the membrane were the functions of the blend ratio of sercin to PVA and the content of BA. The use of BA increased the tensile strength, improved the water resistance and the thermal stability, and varied the interior morphology of the films. The content of sericin greatly influenced the combination of properties of the films, especially the mechanical properties, interior morphology, thermal stability, and water resistance reducing with the increasing of sericin content. The films have potential to be used in materials, such as skin-care coatings for beauty, percutaneous drug delivery systems for exterior intact skin, due to the characteristics of the components and the good mechanical properties of the films.


2021 ◽  
Vol 20 (11) ◽  
pp. 2241-2248
Author(s):  
M. Yasmin Begum ◽  
Ali Alqahtani

Purpose: To formulate and characterize tizanidine hydrochloride (TZN) and piroxicam (PRX)-loaded bilayer mucoadhesive buccal films with an intention to improve the bioavailability and patient compliance in pain management.Methods: Bilayer buccal films were prepared by solvent evaporation technique using hydroxypropyl methylcellulose (HPMC) 15cps and polyvinylpyrrolidone (PVP K30 as immediate release (IR) layer forming polymers and HPMC K15 M, PVP K 90 along with various muco adhesive polymers (Carbopol P934, sodium alginate, etc), as sustained release (SR) layer forming polymers. The prepared films werecharacterized for thickness, weight variation, folding endurance, surface pH, swelling index,mucoadhesive strength, in vitro residence time, in vitro drug release, ex vivo permeation and drug release kinetics.Results: The prepared films were of largely uniform thickness, weight and drug content. Moisture loss (%) and folding endurance were satisfactory. Surface pH was compatible with salivary fluid. Disintegration time was 85 s for F1 and 115 s for F2 of IR films. In vitro dissolution studies showed 99.12 ± 1.2 % (F1) and 90.36 ± 1.8 % (F2) were released in 45 min. Based on the above results, F1 was chosen as the optimum formulation to be combined with SR layer of TZN. Amongst the SR layers of TZN in vitro drug release. The findings show that of F2 was 98.38 ± 0.82 % and correlated with ex vivo release. Drug release followed zero order release kinetics and mechanism of drug release was non-Fickian type diffusion. In vitro residence time was greater than 5 h.Conclusion: The findings show that the bilayer buccal films demonstrate the dual impact of deliveringPRX instantly from the IR layer, with good controlled release and permeation of TZN from the SR layer, thus providing enhanced therapeutic efficacy, drug bioavailability and patient compliance.


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