Formulation and Characterization of Native and Crosslinked Hyaluronic Acid Microspheres for Dermal Delivery of Sodium Ascorbyl Phosphate: A Comparative Study

Fallacara, Arianna; Marchetti, Filippo; Pozzoli, Michele; Citernesi, Ugo Raffaello; Manfredini, Stefano; Vertuani, And Silvia

doi:10.3390/pharmaceutics10040254

Cited by 27 publications

(18 citation statements)

References 62 publications

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“…The thermal analysis (Figure 6) of the HA microparticles presented three stages, consisting of an initial mass loss corresponding to dehydration (20-150 • C), a second stage corresponding to partial breakage of the molecular structure (200-270 • C) and a third stage related to degradation of the hyaluronan residues (270-400 • C) [48,49]. The TGA thermogram of HAUR microparticles presented a dehydration step at 20-150 • C with an additional step that can be attributed to the presence of unreacted urea or related chemicals formed from the degradation of crosslinks appearing at 150-223 • C. The twostage degradation of the polysaccharide was also observed for HAUR microparticles [50]. The moisture evaporation of the HAGA microparticles was observed at 20-150 • C and the degradation of the backbone of the HAGA microparticles started at 200 • C. The obtained results indicate that the microparticle structures in principle could tolerate heating to the inlet temperature used in spray drying (100-120 • C) without a significant impact.…”

Section: Thermogravimetric Analysis (Tga)mentioning

confidence: 82%

Hyaluronic Acid Hydrogels for Controlled Pulmonary Drug Delivery—A Particle Engineering Approach

et al. 2021

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Hydrogels warrant attention as a potential material for use in sustained pulmonary drug delivery due to their swelling and mucoadhesive features. Herein, hyaluronic acid (HA) is considered a promising material due to its therapeutic potential, the effect on lung inflammation, and possible utility as an excipient or drug carrier. In this study, the feasibility of using HA hydrogels (without a model drug) to engineer inhalation powders for controlled pulmonary drug delivery was assessed. A combination of chemical crosslinking and spray-drying was proposed as a novel methodology for the preparation of inhalation powders. Different crosslinkers (urea; UR and glutaraldehyde; GA) were exploited in the hydrogel formulation and the obtained powders were subjected to extensive characterization. Compositional analysis of the powders indicated a crosslinked structure of the hydrogels with sufficient thermal stability to withstand spray drying. The obtained microparticles presented a spherical shape with mean diameter particle sizes from 2.3 ± 1.1 to 3.2 ± 2.9 μm. Microparticles formed from HA crosslinked with GA exhibited a reasonable aerosolization performance (fine particle fraction estimated as 28 ± 2%), whereas lower values were obtained for the UR-based formulation. Likewise, swelling and stability in water were larger for GA than for UR, for which the results were very similar to those obtained for native (not crosslinked) HA. In conclusion, microparticles could successfully be produced from crosslinked HA, and the ones crosslinked by GA exhibited superior performance in terms of aerosolization and swelling.

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Section: Thermogravimetric Analysis (Tga)mentioning

confidence: 82%

Hyaluronic Acid Hydrogels for Controlled Pulmonary Drug Delivery—A Particle Engineering Approach

et al. 2021

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“…The earlier scientific evidence confirms that HA is utilized in the distribution of drugs to the respiratory organ and also its sustained release of the drug makes biocompatibility, half-life extension, solubility enhancement, the possibility of high drug loading, less toxicity and increased drug retention time. Moreover, it is proposed that HA-HCQ drug conjugate enters into the lower respiratory tract cell through CD44 receptor, then under the influence of hydrolytic enzymes released from the lysosome, splits the HA-HCQ ester covalent bond and releases the HCQ drug into the target cell to interact with the SARS-COV-2 viral protein targets [37] , [38] , [39] .…”

Section: Resultsmentioning

confidence: 99%

Molecular insights of hyaluronic acid-hydroxychloroquine conjugate as a promising drug in targeting SARS-CoV-2 viral proteins

Thirumalaisamy¹,

Aroulmoji²,

Iqbal

et al. 2021

Journal of Molecular Structure

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In-silico anti-viral activity of Hydroxychloroquine (HCQ) and its Hyaluronic Acid-derivative (HA-HCQ) towards different SARS-CoV-2 protein molecular targets were studied. Four different SARS-CoV-2 proteins molecular target i.e., three different main proteases and one helicase were chosen for In-silico anti-viral analysis. The HA-HCQ conjugates exhibited superior binding affinity and interactions with all the screened SAR-CoV-2 molecular target proteins with the exception of a few targets. The study also revealed that the HA-HCQ conjugate has multiple advantages of efficient drug delivery to its CD44 variant isoform receptors of the lower respiratory tract, highest interactive binding affinity with SARS-CoV-2 protein target. Moreover, the HA-HCQ drug conjugate possesses added advantages of good biodegradability, biocompatibility, non-toxicity and non-immunogenicity. The prominent binding ability of HA-HCQ conjugate towards Mpro (PDB ID 5R82 ) and Helicase (PDB ID 6ZSL ) target protein as compared with HCQ alone was proven through MD simulation analysis. In conclusion, our study suggested that further in-vitro and in-vivo examination of HA-HCQ drug conjugate will be useful to establish a promising early stage antiviral drug for the novel treatment of COVID-19 .

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“…Finally, the molecular structure of either scaffold was degraded entirely after the 450°C. 49 As a result, cQSM-dS has shown better thermal stability due to the crosslinking process compared to QSM-dS.…”

Section: Effect Of Crosslinking Process On Mechanical and Thermal Feamentioning

confidence: 99%

Bioengineered three-dimensional physical constructs from quince seed mucilage for human adipose-derived mesenchymal stem cells

Şimşek

Karaca

Arslan

2020

Journal of Bioactive and Compatible Polymers

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In this study, we aimed at fabricating a novel porous physical construct from quince seed mucilage for translational medicine applications. To achieve this goal, quince seed mucilage was extracted, molded, and freeze-dried. After being freeze-dried, the molded constructs were chemically crosslinked with 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide/N-hydroxysuccinimide to maintain the mechanical integrity of the structure. The fabricated scaffolds were characterized in-depth by scanning electron microscopy, Fourier transform infrared spectroscopy, Brunauer–Emmett–Teller analysis, thermogravimetric analysis, and dynamic mechanical analysis in addition to the swelling, liquid uptake, and porosity tests. The extraction yield of mucilage was calculated to be 6.28% ± 0.40% (n = 3). The swelling ratio of crosslinked quince seed mucilage–derived scaffolds was found to be 12,677.50% ± 388.82% (n = 3), whereas the porosity of crosslinked quince seed mucilage–derived scaffolds was 83.43% ± 2.84% (n = 3). The analyses confirmed the crosslinked quince seed mucilage–derived scaffolds to be possessed interconnected, highly porous structure. Afterward, human adipose-derived mesenchymal stem cells were seeded on the crosslinked quince seed mucilage–derived scaffolds, and the cell viability on the scaffolds was assessed with 3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay. The MTT results revealed the scaffolds not to be possessed any cytotoxic effect on seeded cells. Human adipose-derived mesenchymal stem cells adhesion and migration on the crosslinked quince seed mucilage–derived scaffolds were also evaluated histologically using hematoxylin and eosin staining in addition to scanning electron microscopy analysis. In conclusion, we believe that crosslinked quince seed mucilage–derived scaffolds have the potential to be an alternative to routinely used polysaccharides in regenerative medicine applications.

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Formulation and Characterization of Native and Crosslinked Hyaluronic Acid Microspheres for Dermal Delivery of Sodium Ascorbyl Phosphate: A Comparative Study

Cited by 27 publications

References 62 publications

Hyaluronic Acid Hydrogels for Controlled Pulmonary Drug Delivery—A Particle Engineering Approach

Hyaluronic Acid Hydrogels for Controlled Pulmonary Drug Delivery—A Particle Engineering Approach

Molecular insights of hyaluronic acid-hydroxychloroquine conjugate as a promising drug in targeting SARS-CoV-2 viral proteins

Bioengineered three-dimensional physical constructs from quince seed mucilage for human adipose-derived mesenchymal stem cells

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