Sodium hyaluronate as a mucoadhesive component in nasal formulation enhances delivery of molecules to brain tissue

Horvát, Sándor; Fehér, A.; Wolburg, Hartwig; Sipos, Péter; Veszelka, Szilvia; Tóth, Anna Zsófia; Kis, Lóránd; Kurunczi, Anita; Balogh, Gábor; Kürti, Levente; Erös, I.; Szabó‐Révész, Piroska; Deli, Mária A.

doi:10.1016/j.ejpb.2008.10.009

Cited by 89 publications

(74 citation statements)

References 37 publications

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“…The aforementioned values prove that hyaluronic acid incorporation was able to enhance the mucoadhesiveness of the nanoemulsion, which is a desirable property for intranasal administration to reduce mucociliary clearance and increase the residence time of the formula in the nasal cavity (Horvát et al, 2009). …”

Section: Measurement Of the Mucoadhesive Strengthmentioning

confidence: 90%

“…On the contrary, the significantly higher levels of the two drugs (p50.05) reaching the brain at various time intervals following the administration of the mucoadhesive formula N9 was observed (about 7-and 9-fold increase in AUC 0-7h for resveratrol and curcumin, respectively), which is attributed to the lipidic matrix of the nanoemulsion. This is expected to have favored the partitioning of the nanoemulsion into the lipid bilayer of the nasal epithelial cells, in addition to its content of the permeation enhancer cremophor RH 40, which is known for its enhancement of cell membrane fluidity (Horvát et al, 2009). In addition to its mucoadhesive nature which delays the mucociliary clearance, hyaluronic acid was Figure 6.…”

Section: In Vivo Quantification Of the Two Polyphenols In The Brainmentioning

confidence: 99%

“…Quantification of the amounts of resveratrol and curcumin reaching the brain following the intranasal administration of the mucoadhesive formula N9. reported to enhance the absorption of drugs via mucosal tissues (Horvát et al, 2009). The combination of cremophor RH 40 and hyaluronic acid was reported to increase the nose to brain transport of fluorescein isothiocyanate through the olfactory pathway (Horvát et al, 2009).…”

Section: In Vivo Quantification Of the Two Polyphenols In The Brainmentioning

confidence: 99%

“…reported to enhance the absorption of drugs via mucosal tissues (Horvát et al, 2009). The combination of cremophor RH 40 and hyaluronic acid was reported to increase the nose to brain transport of fluorescein isothiocyanate through the olfactory pathway (Horvát et al, 2009). The non-significant difference in AUC values for resveratrol and curcumin (p40.05) may be attributed to the close log D values of the two drugs.…”

Section: In Vivo Quantification Of the Two Polyphenols In The Brainmentioning

confidence: 99%

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Development of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery

Nasr

2015

Drug Delivery

164

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RESEARCH ARTICLEDevelopment of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery Maha NasrDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt AbstractThe development of mucoadhesive lipidic nanoemulsion based on hyaluronic acid, co-encapsulating two polyphenols (resveratrol and curcumin) for the transnasal treatment of neurodegenerative diseases was attempted in the current manuscript. Nanoemulsions were prepared by the spontaneous emulsification method, and were characterized for their particle size, zeta potential, mucoadhesive strength and morphology. The selected formula was tested for its antioxidant potential, in vitro and ex vivo release of the two polyphenols, safety on nasal mucosa and in vivo quantification of the two drugs in rat brains. Its stability was tested by monitoring the change in particle size, zeta potential, drugs' content and antioxidant potential upon storage for 3 months. The optimized hyaluronic acid based nanoemulsion formula displayed a particle size of 115.2 ± 0.15 and a zeta potential of À23.9 ± 1.7. The formula displayed a spherical morphology and significantly higher mucoadhesive strength compared to its non mucoadhesive counterpart. In addition, the nanoemulsion was able to preserve the antioxidant ability of the two polyphenols and protect them from degradation. Diffusion controlled release of the two drugs was achievable till 6 hours, with an ex vivo flux across sheep nasal mucosa of 2.86 and 2.09 mg/cm 2 hr for resveratrol and curcumin, respectively. Moreover, the mucoadhesive nanoemulsion was safe on nasal mucosa and managed to increase the amounts of the two polypehnols in the brain (about 7 and 9 folds increase in AUC 0-7 h for resveratrol and curcumin, respectively). Hyaluronic acid based lipidic nanoemulsion proved itself as a successful carrier enhancing the solubility, stability and brain targetability of polyphenols.

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Section: Measurement Of the Mucoadhesive Strengthmentioning

confidence: 90%

Section: In Vivo Quantification Of the Two Polyphenols In The Brainmentioning

confidence: 99%

Section: In Vivo Quantification Of the Two Polyphenols In The Brainmentioning

confidence: 99%

Section: In Vivo Quantification Of the Two Polyphenols In The Brainmentioning

confidence: 99%

See 2 more Smart Citations

Development of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery

Nasr

2015

Drug Delivery

164

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“…Ex vivo excised animal tissue models are frequently utilized for nasal drug absorption studies (Wadell et al 1999(Wadell et al , 2003Schmidt et al 2000). Several in vivo models of rat, rabbit, dog, sheep, and monkey were reported to deliver pharmacons via the nasal route (Chien et al 1992;Costantino et al 2007;Horvát et al 2009). However, there are several disadvantages of the ex vivo tissue and in vivo animal models, including differences between the species in enzyme activities or in cell type distribution, and specialities in many anatomical and physiological features in various animal nasal cavities, compared with those of the human (Chien et al 1992).…”

Section: Introductionmentioning

confidence: 99%

Retinoic acid and hydrocortisone strengthen the barrier function of human RPMI 2650 cells, a model for nasal epithelial permeability

et al. 2012

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The nasal pathway represents an alternative route for non-invasive systemic administration of drugs. The main advantages of nasal drug delivery are the rapid onset of action, the avoidance of the first-pass metabolism in the liver and the easy applicability. In vitro cell culture systems offer an opportunity to model biological barriers. Our aim was to develop and characterize an in vitro model based on confluent layers of the human RPMI 2650 cell line. Retinoic acid, hydrocortisone and cyclic adenosine monophosphate, which influence cell attachment, growth and differentiation have been investigated on the barrier formation and function of the nasal epithelial cell layers. Real-time cell microelectronic sensing, a novel label-free technique was used for dynamic monitoring of cell growth and barrier properties of RPMI 2650 cells. Treatments enhanced the formation of adherens and tight intercellular junctions visualized by electron microscopy, the presence and localization of junctional proteins ZO-1 and b-catenin demonstrated by fluorescent immunohistochemistry, and the barrier function of nasal epithelial cell layers. The transepithelial resistance of the RPMI 2650 cell model reached 50 to 200 X 9 cm 2 , the permeability coefficient for 4.4 kDa FITC-dextran was 9.3 to 17 9 10 -6 cm/s, in agreement with values measured on nasal mucosa from in vivo and ex vivo experiments. Based on these results human RPMI 2650 cells seem to be a suitable nasal epithelial model to test different pharmaceutical excipients and various novel formulations, such as nanoparticles for toxicity and permeability.

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Novel Non‐Injectable Formulation Approaches of Peptides and Proteins

Mao

Cun

Kawashima

2009

Delivery Technologies for Biopharmaceuticals

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Sodium hyaluronate as a mucoadhesive component in nasal formulation enhances delivery of molecules to brain tissue

Cited by 89 publications

References 37 publications

Development of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery

Development of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery

Retinoic acid and hydrocortisone strengthen the barrier function of human RPMI 2650 cells, a model for nasal epithelial permeability

Novel Non‐Injectable Formulation Approaches of Peptides and Proteins

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