Carvedilol-loaded polyvinylpyrrolidone electrospun nanofiber film for sublingual delivery

Li, Jinghan; Pan, Hao; Ye, Qingzhuo; Shi, Ce; Zhang, Xiangrong; Pan, Weisan

doi:10.1016/j.jddst.2020.101726

Cited by 22 publications

(21 citation statements)

References 37 publications

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“…This accelerated release profile was expected due to the polymer's hydrophilic nature (PVP) that will disintegrate fast upon contact with the buffer (PBS). This finding is consistent with Li et al [53], Sriyanti et al [54], and Moydeen et al's [55] studies on carvedilol-, α-mangostin-, and ciprofloxacin-loaded PVP fibers, respectively. The in vitro release study's trend is summarized as follows: diffusion-dependent drug release occurred at the initial time points (5-15 min) leading to burst release, followed by polymer degradation, which accounted for the full drug release (at about 30 to 120 min).…”

Section: Drug Release Profilesupporting

confidence: 91%

The Delivery of the Novel Drug ‘Halicin’ Using Electrospun Fibers for the Treatment of Pressure Ulcer against Pathogenic Bacteria

et al. 2020

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Pressure ulcer or bedsore is a form of skin infection that commonly occurs with patients admitted to the hospital for an extended period of time, which might lead to severe complications in the absence of medical attention, resulting in infection either by drug-sensitive or drug-resistant bacteria. Halicin, a newly discovered drug effective against several bacterial strains, including multidrug-resistant bacteria, was investigated to reduce bacterial infection burden. This study aims to formulate halicin into electrospun fibers to be applied in bedsores as antibacterial dressing to assess its efficacy against gram-positive (Staphylococcus aureus) and gram-negative bacteria (Escherichia coli and Acinetobacter baumannii) by studying the minimum inhibitory concentration (MIC) and bacterial zone of inhibition assays. The diameters of inhibition growth zones were measured, and the results have shown that the drug-loaded fibers were able to inhibit the growth of bacteria compared to the halicin discs. The release profile of the drug-loaded fibers exhibited a complete release of the drug after 2 h. The results demonstrated that the drug-loaded fibers could successfully release the drug while retaining their biological activity and they may be used as a potential antimicrobial dressing for patients with pressure ulcers caused by multidrug resistant bacteria.

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Section: Drug Release Profilesupporting

confidence: 91%

The Delivery of the Novel Drug ‘Halicin’ Using Electrospun Fibers for the Treatment of Pressure Ulcer against Pathogenic Bacteria

et al. 2020

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“…For PDLA, the average fiber size was already below the micron size. For all the samples, SEM micrographs did not present any visible particles at the surface of the fibers, which could be a qualitative indication of the effective entrapment of CVD into the fibers, in good agreement with previous studies [ 19 , 21 ].…”

Section: Resultssupporting

confidence: 91%

“…Studies based on hydroxypropyl cellulose-based films were designed with CVD, showing a significant improvement in the bioavailability of carvedilol as a buccal monolayer film when compared to the oral route [ 5 ]. Electrospinning was also used to generate electrospun CVD-loaded fibers in water-soluble polymers such as polyethylene oxide (PEO) [ 2 ] and polyvinylpyrrolidone (PVP) [ 19 ], showing faster dissolution rates when compared to pristine CVD, with almost a complete release in the first 30 min for most of the formulations studied. Although these studies are very meaningful, instant release due to fast polymer dissolution may imply an increase in side effects for certain APIs and fluctuations of the therapeutic concentration in plasma [ 20 ].…”

Section: Introductionmentioning

confidence: 99%

Development of an Electrospun Patch Platform Technology for the Delivery of Carvedilol in the Oral Mucosa

Pardo-Figuerez

Teno²,

Lafraya³

et al. 2022

Nanomaterials

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The work herein presented aims to develop and characterize carvedilol (CVD) releasable non-water-soluble monolayers and a multilayer patch made of ultrathin micron and submicron fibers for drug delivery into the sublingual mucosa. Firstly, the developed formulations containing CVD within different biopolymers (PDLA, PCL, and PHB) were characterized by scanning electron microscopy (SEM), attenuated total reflectance Fourier transformed infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC), wide-angle X-ray scattering (WAXS), and for their in vitro drug release. SEM micrographs assessed the fiber morphology attained by adding carvedilol. ATR-FTIR spectra revealed good chemical compatibility between CVD and the tested biopolymers, whereas DSC and WAXS confirmed that CVD was in an amorphous state within the biopolymeric fibers. In vitro release studies showed enhanced CVD release kinetics from the electrospun biopolymer monolayers compared to the dissolution rate of the commercial form of the pure drug, except for the slow-releasing PDLA fibers. Finally, the selected CVD-loaded layer, i.e., electrospun PHB, was built into a three-layer patch to tackle mucosa adhesion and unidirectional release, while retaining the enhanced release kinetics. The patch design proposed here further demonstrates the potential of the electro-hydrodynamic processing technology to render unique mucoadhesive controlled delivery platforms for poorly water-soluble drugs.

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“…Besides, the thin non-keratinized sublingual mucosa and the ample blood supply at the sublingual region allow for optimum drug penetration, resulting in higher plasma drug concentration and faster onset of action [9]. Moreover, it is convenient for the elderly and patients who have difficulty swallowing [6,10]. Clinical study showed that, with sublingual sildenafil, the onset of erection could be efficiently shortened to 15.5 min and not affected by food ingestion [6].…”

Section: Introductionmentioning

confidence: 99%

Exploitation of Design-of-Experiment Approach for Design and Optimization of Fast-Disintegrating Tablets for Sublingual Delivery of Sildenafil Citrate with Enhanced Bioavailability Using Fluid-Bed Granulation Technique

et al. 2021

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Sildenafil citrate undergoes first-pass metabolism, resulting in poor oral bioavailability at 25–41% of the administered dose. This study aimed to design and optimize fast-disintegrating tablets for the sublingual delivery of sildenafil citrate to improve bioavailability and facilitate rapid onset of action. The design-of-experiment (DoE) approach using 32 full factorial design was conducted to develop a new formulation of sildenafil fast-disintegrating sublingual tablets (FDSTs) using the fluid-bed granulation technique. The levels of partially pre-gelatinized starch (5–15%) and microcrystalline cellulose (10–60%) were selected as independent formulation variables. The prepared FDSTs were investigated for physical properties. Further, the optimum formulation was chosen for in vivo study in rabbits. Regression analysis showed that independent variables have a significant (p < 0.05) influence on critical attributes of FDSTs. The optimized formulation showed acceptable mechanical strength (friability <1.0%) with very fast disintegration (14.561 ± 0.84 s) and dissolution (94.734 ± 2.76% after 15 min). Further, the optimized formulation demonstrated a significant increase (p < 0.01) in Cmax and AUC0–∞ with short tmax compared to the market product (Viagra®). Based on these results, using the DoE approach, a high level of assurance was achieved for FDSTs’ product quality and performance.

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Carvedilol-loaded polyvinylpyrrolidone electrospun nanofiber film for sublingual delivery

Cited by 22 publications

References 37 publications

The Delivery of the Novel Drug ‘Halicin’ Using Electrospun Fibers for the Treatment of Pressure Ulcer against Pathogenic Bacteria

The Delivery of the Novel Drug ‘Halicin’ Using Electrospun Fibers for the Treatment of Pressure Ulcer against Pathogenic Bacteria

Development of an Electrospun Patch Platform Technology for the Delivery of Carvedilol in the Oral Mucosa

Exploitation of Design-of-Experiment Approach for Design and Optimization of Fast-Disintegrating Tablets for Sublingual Delivery of Sildenafil Citrate with Enhanced Bioavailability Using Fluid-Bed Granulation Technique

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