Development of a buccal bioadhesive nicotine tablet formulation for smoking cessation

Ikinci, Gulcan; Şenel, Sevda; Wilson, Clive G.; Şumnu, Murat

doi:10.1016/j.ijpharm.2003.10.040

Cited by 54 publications

(17 citation statements)

References 9 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In order to enhance the intrinsic mucoadhesive properties, the mechanical characteristics, to modulate the swelling behaviour and to improve the biocompatibility of different mucoadhesive systems polymers, transmucosal dosage forms can be composed by combining different polymers [102][103][104][105]. New mucoadhesive materials are prepared by the association of pharmaceutical polymers in solid state or in solution.…”

Section: Polymers Association and Complexesmentioning

confidence: 99%

See 1 more Smart Citation

Mucoadhesive Polymers for Oral Transmucosal Drug Delivery: A Review

Bagán¹,

Paderni²,

Termine³

et al. 2012

CPD

View full text Add to dashboard Cite

Abstract:The oral mucosa offers an interesting site for the application of dosage forms that release drugs within/throughout the oral mucosa, by assuring a high drug bioavailability for topic and systemic effects. However, the relative permeability of the oral mucosa and the washing effect related to the oral fluids and mechanical stresses must be considered in the formulation of oral dosage forms. Since a sustained drug release can be guaranteed only if dosage forms remain in contact with the oral site of absorption/application for a prolonged time, the development of mucoadhesive dosage forms is mandatory. The mucoadhesion is a complex phenomenon and the mucoadhesive bond consists of two different parts, the mucoadhesive polymers and the mucous substrate. In addition to factors related to the oral mucosa and oral environment features, the physical-chemical characteristics of mucoadhesive polymers must be also considered as factors influencing the mucoadhesive bonds. While it is not possible to modify the mucosal features or it is possible to modify or inhibit only in part certain mucosal processes, the knowledge of polymer properties influencing mucoadhesive bonds allows to modify or to control these properties in developing increasingly effective mucoadhesive systems. The aims of this review are to discuss the several mechanisms and factors behind the phenomenon of mucoadhesion with particular reference to the features of the oral environment, oral mucosa, and polymeric compounds influencing mucoadhesion process. Finally, a brief mention to the main mucoadhesive dosage forms designed for oral transmucosal drug delivery is made.

show abstract

Section: Polymers Association and Complexesmentioning

confidence: 99%

“…Several bioadhesive tablet systems have been the subject of a growing interest [103,[106][107][108][109] in order to improve bioavailability of drug administered across buccal mucosa. Adhesive tablets are small, flat and oval with a diameter approximately of 5-8 mm and about 2 mm in thickness [44].…”

Section: Adhesive Tabletsmentioning

confidence: 99%

Mucoadhesive Polymers for Oral Transmucosal Drug Delivery: A Review

Bagán¹,

Paderni²,

Termine³

et al. 2012

CPD

View full text Add to dashboard Cite

show abstract

“…SA has been widely used as a food and pharmaceutical additive as well as a tablet disintegrant and gelling agent. Additionally, it has been employed as a bioadhesive material and drug release modifier for intraoral drug delivery dosage forms such as tablets (12)(13)(14)(15)(16) and films (17).…”

Section: Introductionmentioning

confidence: 99%

“…NCT is a candidate for buccal delivery due to its low bioavailability after oral administration (1) and its ability to permeate across the buccal mucosa (2,19,20). For these reasons, buccal tablets using NCT hydrogen tartrate, a salt form of NCT with high solubility in water, were previously developed (16,21). Thus, it is interesting that usage of NCT-MAS complex particles as drug carriers in SA tablets offers several advantages.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Nicotine–Magnesium Aluminum Silicate Complex-Loaded Sodium Alginate Matrix Tablets for Buccal Delivery

Kanjanabat

2011

AAPS PharmSciTech

View full text Add to dashboard Cite

Abstract. Nicotine (NCT) buccal tablets consisting of sodium alginate (SA) and nicotine-magnesium aluminum silicate (NCT-MAS) complexes acting as drug carriers were prepared using the direct compression method. The effects of the preparation pH levels of the NCT-MAS complexes and the complex/SA ratios on NCT release, permeation across mucosa, and mucoadhesive properties of the tablets were investigated. The NCT-MAS complex-loaded SA tablets had good physical properties and zero-order release kinetics of NCT, which indicate a swelling/erosion-controlled release mechanism. Measurement of unidirectional NCT release and permeation across porcine esophageal mucosa using a modified USP dissolution apparatus 2 showed that NCT delivery was controlled by the swollen gel matrix of the tablets. This matrix, which controlled drug diffusion, resulted from the molecular interactions of SA and MAS. Tablets containing the NCT-MAS complexes prepared at pH 9 showed remarkably higher NCT permeation rates than those containing the complexes prepared at acidic and neutral pH levels. Larger amounts of SA in the tablets decreased NCT release and permeation rates. Additionally, the presence of SA could enhance the mucoadhesive properties of the tablets. These findings suggest that SA plays the important role not only in controlling release and permeation of NCT but also for enhancing the mucoadhesive properties of the NCT-MAS complex-loaded SA tablets, and these tablets demonstrate a promising buccal delivery system for NCT.KEY WORDS: buccal tablets; magnesium aluminum silicate; nicotine; release and permeation; sodium alginate.

show abstract

“…Currently chewing gums, transdermal patches and sublingual tablets for smoking cessation are available in the market (Lewis, Subramanian, Pandey, & Udupa, 2006), however, a number of practical problems are associated with each nicotine product. A low oral bioavailability is exhibited in the buccal administration of drugs, while sublingual tablets and chewing gums might be swallowed before being absorbed (Ìkinci, Şenel, Wilson, & Şumnu, 2004). Nasal spray of nicotine is the quickest way of NRT to allow nicotine to reach the brain and enter into the bloodstream.…”

Section: Potential Therapeutic Role Of Nicotine Inhalersmentioning

confidence: 99%

Development of Nicotine Loaded Chitosan Nanoparticles for Lung Delivery

Wang¹

View full text Add to dashboard Cite

Cigarette smoking has become one of the leading causes of preventable deaths all over the world, causing a serious threat to human wellbeing and a tremendous economic burden to governments. The currently available treatment options for smoking cessation are not efficient. The pulmonary delivery of drugs by methods such as dry powder inhaler (DPI) has been recognized as one of the most efficient routes of drug delivery to the targeted area. The lung delivery of nicotine in this way would be expected to mimic the effects of tobacco smoking and could significantly reduce the negative health effects of smoking that result from nicotine addiction.The aim of this study is to develop nanoparticles with controlled physicochemical properties using biodegradable polymer of chitosan (CS) loaded with nicotine salt for pulmonary delivery as DPI formulations. The outcomes of this project are expected to be a safe and effective CS-based nicotine formulation for pulmonary delivery to treat nicotine dependence. This thesis specially addresses the research questions: (1) how to develop a feasible process to manufacture the nanoparticles suitable for pulmonary drug delivery using biodegradable polymer of CS containing nicotine salt; (2) how to develop an animal model for pulmonary drug delivery from DPI formulation using a nose-only inhalation device.The current therapeutic options for treatment of smoking addiction have been reviewed, and current advancements of technology in pulmonary drug delivery are summarised. Buccal administration of drugs exhibits a low oral bioavailability, and sublingual tablets and chewing gums can be swallowed before being absorbed.Although nasal spray of nicotine is a fast way to deliver nicotine into the bloodstream, Development of Nicotine Loaded Chitosan Nanoparticles for Lung Delivery iii the rate of absorption is still not as rapid as cigarette smoking. Therefore, it is proposed that delivery of nicotine with sustained drug release profile direct into the deep lung is likely to more effectively mimic the rapid effects of cigarette smoking on a physiological level, which could eliminate patient craving and allow the tapering of nicotine level over time to improve patients' compliance.Water in oil (w/o) emulsion crosslinking method has been used to fabricate nicotine hydrogen tartrate (NHT)-loaded CS nanoparticles which separate as solid microaggregates. The physicochemical properties of particles are characterized by a series of techniques. Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) shows that the prepared particles are spherical in morphology with rough surface after loading CS particles with NHT. Dynamic Light Scattering (DLS)by Zetasizer determined nanoparticle size ranging from 167.6 nm to 411 nm, while DLS by Mastersizer demonstrated that the microaggregates of these nanoparticles are in the respirable range (<5µm). The surface positive charge as measured by zeta potential tends to decrease with increase of mass ratios of NHT to CS, which is in contr...

show abstract

Development of a buccal bioadhesive nicotine tablet formulation for smoking cessation

Cited by 54 publications

References 9 publications

Mucoadhesive Polymers for Oral Transmucosal Drug Delivery: A Review

Mucoadhesive Polymers for Oral Transmucosal Drug Delivery: A Review

Preparation and Characterization of Nicotine–Magnesium Aluminum Silicate Complex-Loaded Sodium Alginate Matrix Tablets for Buccal Delivery

Development of Nicotine Loaded Chitosan Nanoparticles for Lung Delivery

Contact Info

Product

Resources

About