Optimization of piribedil mucoadhesive tablets for efficient therapy of Parkinson’s disease: physical characterization and<i>ex vivo</i>drug permeation through buccal mucosa

Çelik, Burak; Özdemir, Samet; Demirkoz, Aslı Barla; Üner, Melike

doi:10.1080/03639045.2017.1349785

Cited by 18 publications

(13 citation statements)

References 42 publications

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“…Buccal tablets were compressed by using a single-punch tablet machine (TDP-5; Shanghai Tianfan Machinery Factory, Shanghai, China) equipped with 7-mm round flat punch set. 20 Tablet weight was kept constant at 100 mg, and the thickness of tablets was adjusted tô2 mm. Tablets were stored in an airtight container away from the light for further studies.…”

Section: Methodsmentioning

confidence: 99%

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Risperidone mucoadhesive buccal tablets: formulation design, optimization and evaluation

Çelik

2017

DDDT

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The aim of this study was to design and optimize risperidone (RIS) mucoadhesive buccal tablets for systemic delivery as an alternative route. Direct compression method was used for the preparation of buccal tablets, and screening studies were conducted with different polymers to determine their effects on tablet characteristics. Carbopol® (CP) and sodium alginate (SA) were selected as two polymer types for further optimization studies by applying response surface methodology. Tablet hardness (TH), ex vivo residence time (RT), and peak detachment force (DF) from buccal mucosa were selected as three important responses. Physicochemical compatibility of formulation excipients and RIS was evaluated by using Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) analysis. In vitro drug release profiles and release kinetics were investigated; swelling index and matrix erosion studies were conducted. Optimum formulation consisted of 16.4% CP and 20.3% SA, which provided 7.67±0.29 hour ex vivo RT, 45.52±4.85 N TH, and 2.12±0.17 N DF. FT-IR spectroscopy and DSC analysis revealed that there was no chemical interaction present between tablet ingredients. Cumulative RIS release of >90% was achieved after 8 hours of in vitro dissolution studies, which was supported by swelling and matrix erosion analysis. Mechanism of RIS release was fitted best to zero-order model, while release exponent (n) value of 0.77 demonstrated an anomalous (non-Fickian) release, indicating combined erosion and swelling mechanism. The results suggested that optimized buccal tablets of RIS would be a promising and alternative delivery system for the treatment of schizophrenia.

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Section: Methodsmentioning

confidence: 99%

“…Mucoadhesive strength of tablets was determined by using a texture analyzer (Middleboro, MA, USA). 20 , 26 Fresh buccal mucosa from the sheep obtained from local slaughterhouse was used as a model membrane. Samples were prepared by separating the underlying adipose tissue, and the obtained mucosal membrane was cut into 2×2 cm pieces.…”

Section: Methodsmentioning

confidence: 99%

Risperidone mucoadhesive buccal tablets: formulation design, optimization and evaluation

Çelik

2017

DDDT

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“…HEC is frequently used in the formulation of gels with mucous administration because it was demonstrated to be similar to the fertile cervical mucus [ 24 , 25 ]. On the other hand, HPMC is used as excipient in more than 80% of the pharmaceutical products with oral administration [ 26 ] and, unlike HEC, has the property of retaining water, structuring the gel in a particular manner without dehydrating the biological substrate when it gets in contact with [ 27 , 28 ], thus providing comfort feel in occlusive state of application. The flexibility and the elasticity of the polymeric films are ensured by plasticizers (e.g., polyethylene glycol, propylene glycol and polysorbates) which often can also act as permeation activators, when they breach into the corneous layer of the epidermis [ 29 , 30 , 31 , 32 , 33 , 34 , 35 , 36 , 37 ].…”

Section: Introductionmentioning

confidence: 99%

Development of Dermal Films Containing Miconazole Nitrate

et al. 2018

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This study aims to develop new antifungal dermal films based on their mechanical properties (elongation, adhesion, behaviour towards vapour moisture) and the in vitro availability of miconazole nitrate, used as a pharmaceutical active ingredient in various concentrations. The three polymeric films prepared were translucent or shiny, with the surface of 63.585 cm2, 0.20–0.30 mm thickness, and content of miconazole nitrate of 3.931 or 15.726 mg·cm2. The mechanical resistance and elongation tests demonstrated that the two films based on hydroxyethyl cellulose (HEC) polymer were more elastic than the one prepared with hydroxypropyl methylcellulose (HPMC). The vapour water absorption and vapour water loss capacity of the films revealed that the HPMC film did not dry very well in the process of preparation by the evaporation of the solvent technique, unlike the HEC films that jellified more evenly in water and had higher drying capacity at 40 °C. The in vitro availability of miconazole nitrate from dermal films was evaluated using the Franz diffusion cell method, through a synthetic membrane (Ø 25 mm × 0.45 µm) and acceptor media with pH 7.4 (phosphate buffer and sodium lauryl sulphate 0.045%), resulting a release rate of up to 70%.

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“…Piribedil was estimated in formulations by Yardimci et al using micellar electrokinetic capillary chromatography [10] . In addition to these analytical methods, few other research articles reported enhancement of dissolution pattern of piribedil [11] , optimization of piribedil mucoadhesive tablets [12] , characterization of piribedil buccal tablets [13] and in vivo evaluation of piribedil solid lipid micro and nanoparticles [14] . No method has so far been reported for the estimation of impurities in piribedil prolonged release tablets.…”

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confidence: 99%

Quality by Design Based Development and Optimization of A Novel, Dual Wavelength HPLC Method for Determination of Impurities in Piribedil Prolonged Release Tablets

Kumar¹,

Dharmalingam²

2020

pharmaceutical-sciences

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Optimization of piribedil mucoadhesive tablets for efficient therapy of Parkinson’s disease: physical characterization andex vivodrug permeation through buccal mucosa

Cited by 18 publications

References 42 publications

Risperidone mucoadhesive buccal tablets: formulation design, optimization and evaluation

Risperidone mucoadhesive buccal tablets: formulation design, optimization and evaluation

Development of Dermal Films Containing Miconazole Nitrate

Quality by Design Based Development and Optimization of A Novel, Dual Wavelength HPLC Method for Determination of Impurities in Piribedil Prolonged Release Tablets

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