Exploiting the Buccal Mucosa as an Alternative Route for the Delivery of Donepezil Hydrochloride

Caon, Thiago; Pan, Yijun; Simões, Cláudia Maria Oliveira; Nicolazzo, Joseph A.

doi:10.1002/jps.23950

Cited by 11 publications

(5 citation statements)

References 47 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The oral mucosa is an attractive route for drug delivery since it offers a non-invasive way for drug administration and becomes an alternative route when the enteral administration is compromised [59]. In addition, the oral mucosa exhibits a high vascularized area that facilitates the absorption of compounds through the jugular vein that surrounds this site [60], hence bypassing the hepatic first pass metabolism, leading to a possible systemic effect once the active compound is in the bloodstream [35,60,61].…”

Section: Resultsmentioning

confidence: 99%

Buccal Bullfrog (Rana catesbeiana Shaw) Oil Emulsion: A Mucoadhesive System Intended for Treatment of Oral Candidiasis

et al. 2018

View full text Add to dashboard Cite

Oral candidiasis (OC) is an infectious disease caused by microorganisms of the genus Candida, leading to lesions in the buccal cavity. Its treatment consists of the administration of topical or systemic antifungal agents, which may compromise the patient compliance due to its side effects, highlighting the need for alternative treatments. In this scenario, bullfrog oil, an animal oil composed of a pool of saturated and unsaturated fatty acids, is introduced as a potential antifungal raw material. Thus, the aim of this work was to produce a mucoadhesive emulsified system able to deliver the bullfrog oil in the buccal cavity to treat the OC. The emulsion was produced and characterized by visual inspection, droplet size, polydispersity index (PdI), and zeta potential over the course of 60 days. In addition, its mucoadhesive ability was evaluated using an in vitro mucin model. The antifungal activity, evaluated by the broth microdilution assay and the biocompatibility, performed against human erythrocytes, were also carried out. The emulsion showed a droplet size of 320.79 ± 35.60 nm, a PdI of 0.49 ± 0.08, and a zeta potential of −38.53 ± 6.23 mV, with no significant changes over 60 days. The mucoadhesive properties of the system was improved by the use of pharmaceutical excipients. The antifungal activity showed that the bullfrog oil and the emulsion were able to inhibit the growth of different Candida species. Furthermore, the emulsion showed no significant hemolytic effect. Overall, the system showed suitable physicochemical characteristics and biocompatibility, with substantial in vitro antifungal activity, suggesting that this system can be further investigated for OC treatment.

show abstract

Section: Resultsmentioning

confidence: 99%

Buccal Bullfrog (Rana catesbeiana Shaw) Oil Emulsion: A Mucoadhesive System Intended for Treatment of Oral Candidiasis

et al. 2018

View full text Add to dashboard Cite

show abstract

“…The failure of OA to enhance NAR delivery compared with the other solvents studied (Table 1) might reflect ionic complexation between the ternary amine group of naratriptan and the carboxylic group of OA. The reduction in the permeation of the basic drug, donepezil, through porcine buccal tissue in the presence of OA has been attributed to a similar interaction with OA (Caon et al, 2014).…”

Section: Permeation From Single Solventsmentioning

confidence: 98%

“…Almost twice the amount of naratriptan permeated from PEG 200 compared with PEG 400 (t-test, p < 0.05). PEG 400 has also been shown to retard the buccal permeation of donazepil in a concentrationdependent manner (Caon et al, 2014). This was attributed to a direct interaction between the drug and PEG 400 and its effects on the thermodynamic activity of the molecule.…”

Section: Permeation From Single Solventsmentioning

confidence: 99%

Oral transmucosal delivery of naratriptan

Sattar

Lane

2016

International Journal of Pharmaceutics

View full text Add to dashboard Cite

Naratriptan (NAR) is currently used as the hydrochloride salt (NAR.HCl) for the treatment of migraine and is available in tablet dosage forms for oral administration. Buccal drug delivery offers a number of advantages compared with conventional oral delivery including rapid absorption, avoidance of first pass metabolism and improved patient compliance. We have previously prepared and characterised the base form of NAR and shown that it has more favourable properties for buccal delivery compared with NAR.HCl. This study describes the design and evaluation of a range of formulations for oral transmucosal delivery of NAR base. Permeation studies were conducted using excised porcine buccal tissue mounted in Franz cells. Of the neat solvents examined, Transcutol P (TC) showed the greatest enhancement effects and was the vehicle in which NAR was most soluble. The mechanisms by which TC might promote permeation were further probed using binary systems containing TC with either buffer or Miglyol 812 (MG). Mass balance studies were also conducted for these systems. The permeation of TC as well as NAR was also monitored for TC:MG formulations. Overall, TC appears to promote enhanced membrane permeation of NAR because of its rapid uptake into the buccal tissue. Synergistic enhancement of buccal permeation was observed when TC was combined with MG and this is attributed to the increased thermodynamic activity of NAR in these formulations. Significantly enhanced permeation of NAR was achieved for TC:MG and this was also associated with less TC remaining on the tissue or in the tissue at the end of the experiment. To our knowledge this is the first report where both enhancer and active have been monitored in buccal permeation studies. The findings underline the importance of understanding the fate of vehicle components for rational formulation design of buccal delivery systems.

show abstract

“…Among them, non-invasive buccal drug delivery is considered a promising alternative route to enhance patient compliance, particularly in pediatric patients with central precocious puberty [ 12 ]. The buccal mucosa has good accessibility and physical robustness while bypassing hepatic and intestinal metabolism, making it a favorable route for delivering therapeutic peptides and proteins [ 13 ]. Moreover, the buccal mucosa is a well-vascularized tissue through which blood vessels drain directly into the jugular vein.…”

Section: Introductionmentioning

confidence: 99%

Nanonization and Deformable Behavior of Fattigated Peptide Drug in Mucoadhesive Buccal Films

Kim,

Ngo,

Nguyen

et al. 2024

Pharmaceutics

View full text Add to dashboard Cite

This study was tasked with the design of mucoadhesive buccal films (MBFs) containing a peptide drug, leuprolide (LEU), or its diverse nanoparticles (NPs), for enhanced membrane permeability via self-assembled nanonization and deformable behavior. An LEU-oleic acid conjugate (LOC) and its self-assembled NPs (LON) were developed. Additionally, a deformable variant of LON (d-LON) was originally developed by incorporating l-α-phosphatidylcholine into LON as an edge activator. The physicochemical properties of LON and d-LON, encompassing particle size, zeta potential, and deformability index (DI), were evaluated. MBFs containing LEU, LOC, and NPs (LON, d-LON) were prepared using the solvent casting method by varying the ratio of Eudragit RLPO and hydroxypropyl methylcellulose, with propylene glycol used as a plasticizer. The optimization of MBF formulations was based on their physicochemical properties, including in vitro residence time, dissolution, and permeability. The dissolution results demonstrated that the conjugation of oleic acid to LEU exhibited a more sustained LEU release pattern by cleaving the ester bond of the conjugate, as compared to the native LEU, with reduced variability. Moreover, the LOC and its self-assembled NPs (LON, d-LON), equivalent to 1 mg LEU doses in MBF, exhibited an amorphous state and demonstrated better permeability through the nanonization process than LEU alone, regardless of membrane types. The incorporation of lauroyl-L-carnitine into the films as a permeation enhancer synergistically augmented drug permeability. Most importantly, the d-LON-loaded buccal films showed the highest permeability, due to the deformability of NPs. Overall, MBF-containing peptide NPs and permeation enhancers have the potential to replace parenteral LEU administration by improving LEU druggability and patient compliance.

show abstract

Exploiting the Buccal Mucosa as an Alternative Route for the Delivery of Donepezil Hydrochloride

Cited by 11 publications

References 47 publications

Buccal Bullfrog (Rana catesbeiana Shaw) Oil Emulsion: A Mucoadhesive System Intended for Treatment of Oral Candidiasis

Buccal Bullfrog (Rana catesbeiana Shaw) Oil Emulsion: A Mucoadhesive System Intended for Treatment of Oral Candidiasis

Oral transmucosal delivery of naratriptan

Nanonization and Deformable Behavior of Fattigated Peptide Drug in Mucoadhesive Buccal Films

Contact Info

Product

Resources

About