Tableted hydrophilic electrospun nanofibers to promote meloxicam dissolution rate

Pisani, Silvia; Friuli, Valeria; Conti, Bice; Bruni, Giovanna; Maggi, Lauretta

doi:10.1016/j.jddst.2021.102878

Cited by 6 publications

(7 citation statements)

References 17 publications

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Section: Resultsmentioning

confidence: 77%

“…Similar results were obtained by using PVP-based nanofibers, where the dissolution rate of meloxicam was improved. These results imply that nanofibers could be an effective carrier, to speed up the dissolution of substances [25]. A very important property from the point of view of the effectiveness of therapy, is the release of active compounds from the formulation.…”

Section: Resultsmentioning

confidence: 89%

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Mechanochemical Properties of Mucoadhesive Tablets Based on PVP/HPβCD Electrospun Nanofibers as Local Delivery of Polygoni cuspidati Extract for Treating Oral Infections

Paczkowska-Walendowska

Szymanowska

Cielecka‐Piontek

2023

Pharmaceuticals

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This study investigated the ability of PVP/HPβCD-based electrospun nanofibers to enhance the dissolution rate of poorly soluble polydatin and resveratrol, the main active components of Polygoni cuspidati extract. To make a solid unit dosage form that would be easier to administer, extract-loaded nanofibers were ground. SEM examination was used to analyze the nanostructure of the fibers, and the results of the cross-section of the tablets showed that they had maintained their fibrous structure. The release of the active compounds (polydatin and resveratrol) in the mucoadhesive tablets was complete and prolonged in time. Additionally, the possibility of staying on the mucosa for a prolonged time has also been proven for both tablets from PVP/HPβCD-based nanofibers and powder. The appropriate physicochemical properties of the tablets, along with the proven antioxidant, anti-inflammatory, and antibacterial properties of P. cuspidati extract, highlight the particular benefits of the mucoadhesive formulation for use as a drug delivery system for periodontal diseases.

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Section: Resultsmentioning

confidence: 77%

Section: Resultsmentioning

confidence: 89%

Mechanochemical Properties of Mucoadhesive Tablets Based on PVP/HPβCD Electrospun Nanofibers as Local Delivery of Polygoni cuspidati Extract for Treating Oral Infections

Paczkowska-Walendowska

Szymanowska

Cielecka‐Piontek

2023

Pharmaceuticals

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“…Some studies [ 13 , 14 , 15 , 16 ] have shown that electrospun drug-loaded fibre mats can be manually compressed after direct loading of the fibre mat into the tablet die. Other authors have ground the fibre mats to effect size reduction and mixed them with large quantities of conventional tabletting excipients prior to compression, reflecting a more conventional oral tablet formulation [ 17 , 18 , 19 , 20 , 21 , 22 ]. Two recent studies have focussed on the mixing step in the conversion of electrospun drug-loaded fibre mats into tablets.…”

Section: Introductionmentioning

confidence: 99%

Development of Robust Tablet Formulations with Enhanced Drug Dissolution Profiles from Centrifugally-Spun Micro-Fibrous Solid Dispersions of Itraconazole, a BCS Class II Drug

et al. 2023

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Fibre-based oral drug delivery systems are an attractive approach to addressing low drug solubility, although clear strategies for incorporating such systems into viable dosage forms have not yet been demonstrated. The present study extends our previous work on drug-loaded sucrose microfibres produced by centrifugal melt spinning to examine systems with high drug loading and investigates their incorporation into realistic tablet formulations. Itraconazole, a model BCS Class II hydrophobic drug, was incorporated into sucrose microfibres at 10, 20, 30, and 50% w/w. Microfibres were exposed to high relative humidity conditions (25 °C/75% RH) for 30 days to deliberately induce sucrose recrystallisation and collapse of the fibrous structure into powdery particles. The collapsed particles were successfully processed into pharmaceutically acceptable tablets using a dry mixing and direct compression approach. The dissolution advantage of the fresh microfibres was maintained and even enhanced after humidity treatment for drug loadings up to 30% w/w and, importantly, retained after compression into tablets. Variations in excipient content and compression force allowed manipulation of the disintegration rate and drug content of the tablets. This then permitted control of the rate of supersaturation generation, allowing the optimisation of the formulation in terms of its dissolution profile. In conclusion, the microfibre-tablet approach has been shown to be a viable method for formulating poorly soluble BCS Class II drugs with improved dissolution performance.

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“…The improvement of the dissolution rate and/or solubility of the loaded drugs are achieved by the high surface-to-volume ratio of the electrospun nanofibers, the potential amorphization of the active and enhancement of its wettability. Moreover, the main feature of this technique is its ability to include a wide variety of drugs into polymeric carriers [ 19 ] to obtain loaded fibers able to enhance the drug dissolution rate and eventually their bioavailability. The production of electrospun fibers for drug delivery applications starts with polymer dissolution in a suitable solvent.…”

Section: Introductionmentioning

confidence: 99%

“…The work aimed to produce HPMC-AS electrospun nanofibers to demonstrate the ability of the electrospun system in increasing the release rate of two model drugs having different pH-dependent solubility in different physiological pH conditions: meloxicam (solubility 4.4 × 10 −3 mg/mL in water at 25 °C; pKa: 4.08 [ 19 ]) and carvedilol (solubility 1.1·10 −2 mg/mL in water at 37 °C; pKa: 7.8 [ 39 ]).…”

Section: Introductionmentioning

confidence: 99%

Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility

et al. 2022

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A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmental pHs. The best approach is to increase the dissolution rate of the drugs at the different pHs and only then modify its release behavior from the pharmaceutical form. This work aims to demonstrate the ability of properly designed polymeric nanofibers in enhancing the release rate of model drugs with different pH-dependent solubility in the different physiological pHs of the gastrointestinal tract. Polymeric nanofibers loaded with meloxicam and carvedilol were prepared using the electrospinning technique and were then included in properly designed tablet formulations to obtain fast or sustained release dosage forms. The nanofibers and the tablets were characterized for their morphological, physico-chemical and dissolution properties. The tablets are able to deliver the dose according to the expected release behavior, and zero-order, first-order, Higuchi, Korsmeyer–Peppas and Hixon–Crowell kinetics models were used to analyze the prevailing release mechanism of the tablets. This study shows that the electrospun fibers can be advantageously included in oral dosage forms to improve their release performances.

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Tableted hydrophilic electrospun nanofibers to promote meloxicam dissolution rate

Cited by 6 publications

References 17 publications

Mechanochemical Properties of Mucoadhesive Tablets Based on PVP/HPβCD Electrospun Nanofibers as Local Delivery of Polygoni cuspidati Extract for Treating Oral Infections

Mechanochemical Properties of Mucoadhesive Tablets Based on PVP/HPβCD Electrospun Nanofibers as Local Delivery of Polygoni cuspidati Extract for Treating Oral Infections

Development of Robust Tablet Formulations with Enhanced Drug Dissolution Profiles from Centrifugally-Spun Micro-Fibrous Solid Dispersions of Itraconazole, a BCS Class II Drug

Tablet Formulations of Polymeric Electrospun Fibers for the Controlled Release of Drugs with pH-Dependent Solubility

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