Transbuccal delivery of betahistine dihydrochloride from mucoadhesive tablets with a unidirectional drug flow: in vitro, ex vivo and in vivo evaluation

El-Nabarawi, Mohamed A.; Ali, Adel A.; Aboud, Heba M.; Hassan, Amira H.; Godah, Amany H

doi:10.2147/dddt.s120613

Cited by 28 publications

(18 citation statements)

References 44 publications

(31 reference statements)

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“…Also, the mechanism of drug release from cubosomes was assessed employing the Korsmeyer–Peppas model. The calculated values of n among different formulations ranged from 0.53 to 0.71, indicating the non-Fickian diffusion of drug (0.45 < n < 0.89) and demonstrating anomalous release behavior where the diffusion may be combined with swelling of GMO bilayers (Elgindy et al., 2016 ; El-Nabarawi et al., 2016 ).…”

Section: Methodsmentioning

confidence: 99%

Novel in situ gelling vaginal sponges of sildenafil citrate-based cubosomes for uterine targeting

et al. 2018

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Sildenafil citrate (SIL), a type 5-specific phosphodiesterase inhibitor, demonstrates valuable results in the management of infertility in women; however, the absence of vaginal dosage form in addition to the associated oral adverse effects minimize its clinical performance. The present study is concerned with SIL uterine targeting following intravaginal administration via optimization of cubosomal in situ gelling sponges (CIS). An emulsification method was employed for preparation of cubosomal dispersions incorporating glyceryl monooleate as a lipid phase and poloxamer 407 as a surfactant with or without polyvinyl alcohol as a stabilizer. Cubosomes were estimated regarding entrapment efficiency (EE%), particle size, and in vitro drug release. Chitosan (2% w/w) was incorporated into the optimum formulation and then lyophilized into small sponges. For the CIS, in vivo histopathological and pharmacokinetic studies were conducted on female Wistar rats and compared with intravaginal free SIL sponges (FIS) and oral SIL solution. SIL-loaded cubosomes showed EE% ranging between 32.15 and 72.01%, particle size in the range of 150.81–446.02 nm and sustained drug release over 8 h. Histopathological study revealed a significant enlargement in endometrial thickness with congestion and dilatation of endometrial blood vessels in intravaginal CIS compared to intravaginal FIS and oral-treated groups. The pharmacokinetic study demonstrated higher AUC0–∞ and Cmax with oral administration compared to intravaginal CIS or intravaginal FIS indicating potential involvement of first uterine pass effect after intravaginal administration. Finally, intravaginal CIS could be considered as a promising platform for SIL uterine targeting with minimized systemic exposure and side effects.

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Section: Methodsmentioning

confidence: 99%

Novel in situ gelling vaginal sponges of sildenafil citrate-based cubosomes for uterine targeting

et al. 2018

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“… 14 Mucoadhesion strength varies based on the physicochemical properties of the polymer, characteristics of the biological material, and contact time of the dosage form. 15 , 16 …”

Section: Introductionmentioning

confidence: 99%

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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“…15 Several studies have been carried out to control BDH release and explore a new route for its administration like the transdermal route and mucoadhesive tablets for buccal delivery. 8 , 16 , 17 …”

Section: Introductionmentioning

confidence: 99%

A novel transdermal nanoethosomal gel of betahistine dihydrochloride for weight gain control: in-vitro and in-vivo characterization

El-Menshawe¹,

Ali²,

Halawa³

et al. 2017

DDDT

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BackgroundBetahistine dihydrochloride (BDH) is a histamine analog used to control weight gain, with short elimination half-life and gastric irritation as side effects.ObjectiveThe aim of the current investigation is to formulate and optimize a topical BDH ethosomal gel for weight gain control.Materials and methodsBox–Behnken design was applied to study the effect of independent variables: phosphatidylcholine (PC), propylene glycol (PG), and ethanol on vesicle size; entrapment efficiency; % drug release; and flux. The morphology and zeta potential of the optimized formulation were evaluated. The % drug release, flux, and pharmacodynamics of the optimized formulation gel were studied.ResultsThe size and entrapment efficiency percent had a direct positive relationship with the concentration of PC and negative relationship with ethanol and PG. The % drug release and flux decreased with increasing PC and PG, while ethanol enhanced both responses. Regression modeling indicated a good correlation between dependent and independent variables, where F16 was chosen as the optimized formulation. F16 showed well-defined spherical vesicles and zeta potential of −24 mV, and % release from the gel exceeded 99.5% over 16 h with the flux of 0.28 mg/cm2/h. Food intake and weight gain of rats were significantly decreased after transdermal application of the BDH ethosomal gel when compared with control, placebo, and BDH gel. The histopathological findings proved the absence of inflammation and decrease in adipose tissue.ConclusionResults obtained showed a significant, sustained transdermal absorption of BDH ethosomal gel and, consequently, a decrease in food intake and weight gain.

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Transbuccal delivery of betahistine dihydrochloride from mucoadhesive tablets with a unidirectional drug flow: in vitro, ex vivo and in vivo evaluation

Cited by 28 publications

References 44 publications

Novel in situ gelling vaginal sponges of sildenafil citrate-based cubosomes for uterine targeting

Novel in situ gelling vaginal sponges of sildenafil citrate-based cubosomes for uterine targeting

Risperidone mucoadhesive buccal tablets: formulation design, optimization and evaluation

A novel transdermal nanoethosomal gel of betahistine dihydrochloride for weight gain control: in-vitro and in-vivo characterization

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