Oral Mucosa Models to Evaluate Drug Permeability

Mazzinelli, Elena; Favuzzi, Ilaria; Arcovito, Alessandro; Castagnola, Raffaella; Fratocchi, Giorgia; Mordente, Alvaro; Nocca, Giuseppina

doi:10.3390/pharmaceutics15051559

Cited by 11 publications

(5 citation statements)

References 112 publications

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“…Given that the mucosal barriers in the mouth do reduce the effective absorption of native oxytocin into the peripheral blood stream [ 11 ], there may be advantages in producing formulations with an improved ability to permeate the oral mucosae and thereby more efficiently increase blood concentrations. For example, penetrant enhancers such as fatty acids, surfactants, cholates, lauric acid, and alcohols or emulsions in the form of deformable liposomes and nanoparticles have been used as well as materials such as polyacrylic acid, chitosan, cellulose derivatives, alginate, and hyaluronic acid (see reviews [ 51 , 52 , 53 ]). However, the main issues limiting the passage of oxytocin across mucosal barriers would appear to be its high molecular weight and low lipophilicity [ 11 ], and so the development of peptidomimetic drugs which can circumvent these issues may be a more promising future approach.…”

Section: Discussion and Future Potential Developments And Applicationsmentioning

confidence: 99%

Oromucosal Administration of Oxytocin: The Development of ‘Oxipops’

Xu,

Lan,

Kou

et al. 2024

Pharmaceutics

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The role of the hypothalamic neuropeptide oxytocin in influencing the brain and behavior has been the subject of widespread research over the last few decades due, most notably, to its reported involvement in promoting social cognition and motivation, reducing anxiety, and relieving pain. It is also increasingly being considered as an important therapeutic intervention in a variety of disorders with social dysfunction as a symptom. While, in recent years, studies in humans have administered oxytocin primarily via an intranasal route, since it may partly enter the brain directly this way via the olfactory and trigeminal nerves, there is increasing evidence that many of its functional effects can be peripherally mediated via increasing its concentration in the blood. This has opened up an oromucosal administration route as an alternative, which is beneficial since the oral consumption of peptides is problematic due to their rapid breakdown in the acidic environment of the gastrointestinal system. In this review we will discuss both the methodologies we have developed for administering oxytocin via lingual application and medicated lollipops, ‘oxipops’, in terms of increasing blood concentrations and the bioavailability of the peptide, and also their validation in terms of functional effects on the brain and behavior. While areas under the curve are significantly greater in terms of plasma oxytocin concentrations following intranasally relative to oromucosally administered oxytocin, with the estimated absolute bioavailability of the latter being around 4.4% compared with 11.1% for intranasal administration, the time to peak concentrations (around 30 min) and functional effects on the brain and behavior are broadly similar. We will also discuss potential therapeutic advantages of the oromucosal administration of oxytocin in different clinical contexts and its wider application for other peptides which are increasingly being developed for therapeutic use.

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Section: Discussion and Future Potential Developments And Applicationsmentioning

confidence: 99%

Oromucosal Administration of Oxytocin: The Development of ‘Oxipops’

Xu,

Lan,

Kou

et al. 2024

Pharmaceutics

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“…A variety of drug delivery systems, with the advantages of improving drug availability, improving drug stability, and regulating drug release, have been widely reported [38][39][40]. Alginate is a naturally occurring polyanionic polysaccharide extracted from the cell walls of brown algae and certain bacteria [41].…”

Section: Discussionmentioning

confidence: 99%

CpG ODN/Mangiferin Dual Delivery through Calcium Alginate Hydrogels Inhibits Immune-Mediated Osteoclastogenesis and Promotes Alveolar Bone Regeneration in Mice

Hu²,

Huang

et al. 2023

Biology

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The immune system plays an important role in the skeletal system during bone repair and regeneration. The controlled release of biological factors from the immune system could facilitate and optimize the bone remodeling process through the regulation of the activities of bone cells. This study aimed to determine the effect of the controlled delivery of immunomodulatory biologicals on bone regeneration. Immunostimulatory cytosine-phosphate-guanosine oligodeoxynucleotides (CpG ODN) and glucosylxanthone Mangiferin (MAG)-embedded microbeads were incubated with P. gingivalis-challenged splenocytes, or co-cultured with RAW264.7 cells. The effect of CpG ODN/MAG-containing microbeads on bone regeneration was then tested in vivo in a mouse alveolar bone defect model. The results demonstrated that MAG significantly antagonized P. gingivalis proliferation and reduced the live/dead cell ratio. After the addition of CpG ODN + MAG microbeads, anti-inflammatory cytokines IL-10 and IL-4 were upregulated on day 2 but not day 4, whereas pro-inflammatory cytokine IL-1β responses showed no difference at both timepoints. RANKL production by splenocytes and TRAP+ cell formation of RAW264.7 cells were inhibited by the addition of CpG ODN + MAG microbeads. Alveolar bony defects, filled with CpG ODN + MAG microbeads, showed significantly increased new bone after 4 weeks. In summary, this study evaluated a new hydrogel-based regimen for the local delivery and controlled release of biologicals to repair and regenerate alveolar bony defects. The combined CpG ODN + MAG treatment may promote alveolar bone regeneration through the anti-microbial/anti-inflammatory effects and the inhibition of RANKL-mediated osteoclastogenesis.

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“…The film proved to have very good mucoadhesion and a long release period of viable lactobacilli either at the level of a lesion at the oral mucosa or at the level of the entire oral cavity [78]. To achieve better discharge of active substances, mucoadhesive systems have been improved with solid dispersion of nanoparticles, microemulsions, and liposomes [79][80][81][82][83].…”

Section: Intraoral Mucoadhesive Systemsmentioning

confidence: 99%

Challenges in Optimizing Nanoplatforms Used for Local and Systemic Delivery in the Oral Cavity

Cocoș,

Dumitriu Buzia,

Tatu

et al. 2024

Pharmaceutics

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In this study, we focused on innovative approaches to improve drug administration in oral pathology, especially by transmucosal and transdermal pathways. These improvements refer to the type of microneedles used (proposing needles in the saw), to the use of certain enhancers such as essential oils (which, besides the amplifier action, also have intrinsic actions on oral health), to associations of active substances with synergistic action, as well as the use of copolymeric membranes, cemented directly on the tooth. We also propose a review of the principles of release at the level of the oral mucosa and of the main release systems used in oral pathology. Controlled failure systems applicable in oral pathology include the following: fast dissolving films, mucoadhesive tablets, hydrogels, intraoral mucoadhesive films, composite wafers, and smart drugs. The novelty elements brought by this paper refer to the possibilities of optimizing the localized drug delivery system in osteoarthritis of the temporomandibular joint, neuropathic pain, oral cancer, periodontitis, and pericoronitis, as well as in maintaining oral health. We would like to mention the possibility of incorporating natural products into the controlled failure systems used in oral pathology, paying special attention to essential oils.

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Oral Mucosa Models to Evaluate Drug Permeability

Cited by 11 publications

References 112 publications

Oromucosal Administration of Oxytocin: The Development of ‘Oxipops’

Oromucosal Administration of Oxytocin: The Development of ‘Oxipops’

CpG ODN/Mangiferin Dual Delivery through Calcium Alginate Hydrogels Inhibits Immune-Mediated Osteoclastogenesis and Promotes Alveolar Bone Regeneration in Mice

Challenges in Optimizing Nanoplatforms Used for Local and Systemic Delivery in the Oral Cavity

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