Buccal Drug Delivery Systems

Smart, John D.; Keegan, Gemma

doi:10.1002/9780470640487.ch11

Cited by 6 publications

(3 citation statements)

References 93 publications

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“…However, the risk of systemic adverse reactions is minimal because the bupivacaine plasma levels in the patients with HNC were well below the toxic threshold, bearing in mind that we have measured the total plasma concentration of bupivacaine and not the free fraction of bupivacaine, which exerts pharmacological and toxicological effects . Patients with HNC often experience a reduced volume of saliva, leading to less saliva washout . The decreased ‘saliva washout’ could be the reason for the larger amount of bupivacaine that is absorbed systemically and thereby has contributed to increased relative bioavailability in patients with HNC compared with healthy individuals.…”

Section: Discussionmentioning

confidence: 99%

Absorption of Bupivacaine after Administration of a Lozenge as Topical Treatment for Pain from Oral Mucositis

Mogensen

Sverrisdóttir

Sveinsdóttir

et al. 2016

Basic Clin Pharma Tox

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Abstract:The aim was to investigate systemic exposure after administration of a novel bupivacaine lozenge in healthy individuals with normal mucosa and in head and neck cancer (HNC) patients with oral mucositis. A lozenge containing 5, 10, 25 and 50 mg bupivacaine, respectively, was administered as single dose to 10 healthy individuals, and a lozenge containing 25 mg bupivacaine was administered as single dose to 10 HNC patients with oral mucositis and as multiple doses to five patients with HNC. Blood samples were collected for 6 hr from the healthy individuals and 3 hr from the patients with HNC, respectively, after administration. The plasma concentration-time profiles of bupivacaine were fitted to pharmacokinetic models using nonlinear mixed-effects modelling, evaluating demographics and health status as covariates. The population pharmacokinetics (PK) of bupivacaine lozenge was best described by a two-compartment distribution model with absorption transit compartments. All the observed plasma concentrations were well below the bupivacaine concentrations (2000-2250 ng/ml) which have caused toxic symptoms. The PK model suggested that relative bioavailability was two times higher in HNC patients with oral mucositis grade 1-2 and three times higher in HNC patients with oral mucositis grade 3-4 than in the healthy individuals. Simulations showed that the plasma concentrations would be below the toxic limit after repeated dosing every second hour with 25 mg bupivacaine for five days. The 25-mg bupivacaine lozenges were safe without systemic toxic levels of bupivacaine or risk of side effects. Based on PK simulations of repeated doses of 25 mg every two hours for 16 hr a day, the lozenges can be administered with minimum risk of exceeding the toxic limit.

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Section: Discussionmentioning

confidence: 99%

Absorption of Bupivacaine after Administration of a Lozenge as Topical Treatment for Pain from Oral Mucositis

Mogensen

Sverrisdóttir

Sveinsdóttir

et al. 2016

Basic Clin Pharma Tox

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“…A commonly used method to manipulate the barrier properties of the oral mucosae is the incorporation of chemical permeation enhancers. These enhancers improve the permeability of the oral mucosae by different mechanisms, namely, increasing the fluidity of the cell membrane, extracting inter/intracellular lipids, altering cellular proteins, or altering the surface of the mucin . The most commonly used permeation enhancers are fatty acids, bile salts, and surfactants .…”

Section: General Considerations In the Development Of Intraoral Drug mentioning

confidence: 99%

“…These enhancers improve the permeability of the oral mucosae by different mechanisms, namely, increasing the fluidity of the cell membrane, extracting inter/intracellular lipids, altering cellular proteins, or altering the surface of the mucin . The most commonly used permeation enhancers are fatty acids, bile salts, and surfactants . Alternative and/or concurrent methods such as sonophoresis, iontophoresis, and electroporation could be employed or developed for improved drug delivery in the oral cavity …”

Section: General Considerations In the Development Of Intraoral Drug mentioning

confidence: 99%

Polymeric drug delivery systems for intraoral site‐specific chemoprevention of oral cancer

Desai

2017

J Biomed Mater Res

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Oral cancer is among the most prevalent cancers in the world. Moreover, it is one of the major health problems and causes of death in many regions of the world. The traditional treatment modalities include surgical removal, radiation therapy, systemic chemotherapy, or a combination of these methods. In recent decades, there has been significant interest in intraoral site-specific chemoprevention via local drug delivery using polymeric systems. Because of its easy accessibility and clear visibility, the oral mucosa is amenable for local drug delivery. A variety of polymeric systems-such as gels, tablets, films, patches, injectable systems (e.g., millicylindrical implants, microparticles, and in situ-forming depots), and nanosized carriers (e.g., polymeric nanoparticles, nanofibers, polymer-drug conjugates, polymeric micelles, nanoliposomes, nanoemulsions, and polymersomes)-have been developed and evaluated for the local delivery of natural and synthetic chemopreventive agents. The findings of in vitro, ex vivo, and in vivo studies and the positive outcome of clinical trials demonstrate that intraoral site-specific drug delivery is an attractive, highly effective and patient-friendly strategy for the management of oral cancer. Intraoral site-specific drug delivery provides unique therapeutic advantages when compared to systemic chemotherapy. Moreover, intraoral drug delivery systems are self-administrable and can be removed when needed, increasing patient compliance. This article covers important aspects and advances related to the design, development, and efficacy of polymeric systems for intraoral site-specific drug delivery. © 2017 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 106B: 1383-1413, 2018.

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