Buccal Transmucosal Delivery System of Enalapril for Improved Cardiac Drug Delivery: Preparation and Characterization

He, Weiyang; Xiong, Hao-Wei; Xi, Dan; Luo, Tao; Lü, Hao; Li, Menghao; Liu, Jicheng; Guo, Zhigang

doi:10.4314/tjpr.v15i1.2

Cited by 4 publications

(2 citation statements)

References 29 publications

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“…The design of a buccal drug delivery system involves the successful application of the optimized formulation to the buccal mucosa and the absorption of the drug either rapidly or in a controlled manner over a stipulated period. The immediate microenvironment of the buccal mucosa region plays a vital role in modulating the drug release with matrix swelling via hydration in the dissolution medium, diffusion and erosion of the polymer matrix as the main mechanisms of a controlled release formulation [41,42]. Human saliva therefore plays a major role in the release mechanism of a buccal drug delivery system and it is vital in functional characterization of swelling and in vitro release studies to consider the components i.e., presence of electrolytes such as sodium, calcium, potassium, chloride, phosphate, bicarbonate, and magnesium.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Clay-Functionalized Wafers and Films for Nicotine Replacement Therapy via Buccal Mucosa

Boateng

Okeke

2019

Pharmaceutics

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The functional physicochemical properties of nicotine (NIC)-loaded composite freeze-dried wafers and solvent-evaporated films comprising hydroxypropylmethylcellulose (HPMC) and sodium alginate (SA), stabilized with magnesium aluminium silicate (MAS), have been reported. The formulations were characterized for swelling capacity, mucoadhesion, in vitro drug dissolution properties in simulated saliva (SS) and PBS at pH 6.8, and ex vivo and in vitro permeation using pig buccal mucosa membrane and EpiOralTM buccal tissue culture, respectively; finally, the cell viability of the EpiOralTM tissues after contact with the NIC-loaded formulations was investigated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and the functional characteristics compared with those of commercially available NIC strips. Swelling and NIC release from the HPMC–SA wafers were more prolonged (30 min) compared to the commercially available NIC strips which disintegrated rapidly and released the drug within 5 min. Generally, swelling, mucoadhesion, and drug release was faster in PBS than in SS, and the presence of MAS was essential for maintaining a high dose recovery compared to non-MAS formulations and commercial NIC strips, which showed lower percentage of NIC content, possibly due to evaporation during analysis. Permeation studies showed that the NIC released was able to cross both porcine buccal membrane and the EpiOralTM buccal tissue, with the latter showing higher permeation flux for all the formulations tested. All the NIC-loaded, MAS-stabilized formulations showed high tissue viability, with values above 80%, showing their great potential for use as buccal delivery platforms for NIC replacement therapy to aid smoking cessation.

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Section: Discussionmentioning

confidence: 99%

Evaluation of Clay-Functionalized Wafers and Films for Nicotine Replacement Therapy via Buccal Mucosa

Boateng

Okeke

2019

Pharmaceutics

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“…60% of the absorbed amount), its oral bioavailability is only around 40%. To improve this ratio, there have been several attempts to administer it through the buccal route [32][33][34][35].…”

Section: Introductionmentioning

confidence: 99%

Quality by Design-Guided Systematic Development and Optimization of Mucoadhesive Buccal Films

Hassan,

Kristó,

Ibrahim

et al. 2023

Pharmaceutics

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Mucoadhesive buccal films have found increased popularity in pharmaceutical drug delivery due to the several advantages that they possess. The present study strives to develop and optimize chitosan-based mucoadhesive buccal films by relying on quality-by-design (QbD) principles. Previous knowledge and experience were employed to firstly identify the critical quality attributes (CQAs), followed by a thorough risk assessment, which led to the selection of seven critical material attributes and process parameters, namely, the polymer grade and concentration, the plasticizer type and concentration, the citric acid (CA) concentration, the amount of the casted solution, and the drying condition. Their effects on the breaking hardness and mucoadhesivity, selected as CQAs, were investigated in three steps by three designs of the experiment (DoE). The medium molecular weight of chitosan (CH) was the preferred choice in the optimized formulation, and its concentration was the most important factor affecting the CQAs, thickness, and moisture content of the films. It was found that 0.364 g/cm2 was the suitable amount of the casting solution, and its optimum drying conditions were presented in the form of a design space. Glycerol (Gly) was the best choice as a plasticizer, and a design space representing several combinations of CH and CA concentrations that produce films with the required quality was constructed at a fixed concentration of 35% Gly. A formula from this design space was selected and employed to load with two model drugs to test its drug-carrying properties for drugs with different physicochemical characteristics. Uniform drug distribution with an immediate release profile was achieved in both drugs, although one of the CQAs was outside of the specifications in the case of lidocaine-containing film. To summarize, the obtention of the optimum mucoadhesive buccal film based on CH was efficiently facilitated by the rational application of QbD principles and the DoE approach.

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Buccal films: A review of therapeutic opportunities, formulations & relevant evaluation approaches

Shipp

Liu

Kerai

et al. 2022

Journal of Controlled Release

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Buccal Transmucosal Delivery System of Enalapril for Improved Cardiac Drug Delivery: Preparation and Characterization

Cited by 4 publications

References 29 publications

Evaluation of Clay-Functionalized Wafers and Films for Nicotine Replacement Therapy via Buccal Mucosa

Evaluation of Clay-Functionalized Wafers and Films for Nicotine Replacement Therapy via Buccal Mucosa

Quality by Design-Guided Systematic Development and Optimization of Mucoadhesive Buccal Films

Buccal films: A review of therapeutic opportunities, formulations & relevant evaluation approaches

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