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Doaa Ahmed El-Setouhy

Bio: Doaa Ahmed El-Setouhy is an academic researcher from Cairo University. The author has contributed to research in topics: Bioavailability & Transdermal. The author has an hindex of 12, co-authored 25 publications receiving 437 citations.

Papers
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Journal ArticleDOI
TL;DR: Findings suggest that the fast orodispersible film containing tianeptine is likely to become one of choices for acute treatment of depression.
Abstract: The present investigation was undertaken with the objective of formulating orodispersible film(s) of the antidepressant drug tianeptine sodium to enhance the convenience and compliance by the elderly and pediatric patients. The novel film former, lycoat NG73 (granular hydroxypropyl starch), along with different film-forming agents (hydroxypropyl methyl cellulose, hydroxyethyl cellulose, and polyvinyl alcohol), in addition to three film modifiers; namely, maltodextrin, polyvinyl pyrrolidone K90 and lycoat RS780 (pregelatinized hydroxypropyl starch) were evaluated. Eight formulae were prepared by the solvent-casting method; and were evaluated for their in vitro dissolution characteristics, in vitro disintegration time, and their physico-mechanical properties. The promising orodispersible film based on lycoat NG73 (F1); showing the greatest drug dissolution, satisfactory in vitro disintegration time and physico-mechanical properties that are suitable for orodispersible films, was evaluated for its bioavailability compared with a reference marketed product (Stablon® tablets) in rabbits. Statistical analysis revealed no significant difference between the bioavailability parameters (C max (ng/ml), t max (h), AUC0–t (ng h ml−1), and AUC0–∞ (ng h ml−1)] of the test film (F1) and the reference product. The mean ratio values (test/reference) of C max (89.74%), AUC0–t (110.9%), and AUC0–∞ (109.21%) indicated that the two formulae exhibited comparable plasma level-time profiles. These findings suggest that the fast orodispersible film containing tianeptine is likely to become one of choices for acute treatment of depression.

134 citations

Journal ArticleDOI
TL;DR: Permeation experiments showed that skin permeation was mainly affected by weight of proniosomes and that Span 60 proniosomal gels showed higher permeation enhancing effect than Brij 72, which could constitute a promising approach for transdermal delivery of CAR.
Abstract: The aim of this work was to investigate the effects of formulation variables on development of carvedilol (CAR) proniosomal gel formulations as potential transdermal delivery systems Different non-ionic surfactants; polyoxyethylene alkyl ethers, namely Brij 78, Brij 92, and Brij 72; and sorbitan fatty acid esters (Span 60) were evaluated for their applicability in preparation of CAR proniosomal gels A 23 full factorial design was employed to evaluate individual and combined effects of formulation variables, namely cholesterol content, weight of proniosomes, and amount of CAR added on performance of proniosomes Prepared proniosomes were evaluated regarding entrapment efficiency (EE%), vesicle size, and microscopic examination Also, CAR release through cellulose membrane and permeation through hairless mice skin were investigated Proniosomes prepared with Brij 72 and Span 60 showed better niosome forming ability and higher EE% than those prepared with Brij 78 and Brij 92 Higher EE% was obtained by increasing both weight of proniosomes and amount of CAR added, and decreasing cholesterol content Release rate through cellulose membrane was inversely affected by weight of proniosomes In Span 60 proniosomes, on increasing percent of cholesterol, a decrease in release rate was observed While in Brij 72 proniosomes, an enhancement in release rate was observed on increasing amount of CAR added Permeation experiments showed that skin permeation was mainly affected by weight of proniosomes and that Span 60 proniosomal gels showed higher permeation enhancing effect than Brij 72 Proniosomal gel could constitute a promising approach for transdermal delivery of CAR

66 citations

Journal ArticleDOI
TL;DR: The biodistribution study showed that the transdermal 99mTc-SF hydrogel exhibited a more sustained release pattern and longer circulation duration with pulsatile behavior in the blood and higher brain levels than the oral 99mRq-SF dispersion.
Abstract: Haloperidol (Hal) is one of the widely used antipsychotic drugs. When orally administered, it suffers from low bioavailability due to hepatic first pass metabolism. This study aimed at developing Hal-loaded penetration enhancer-containing spanlastics (PECSs) to increase transdermal permeation of Hal with sustained release. PECSs were successfully prepared using ethanol injection method showing reasonable values of percentage entrapment efficiency, particle size, polydispersity index and zeta potential. The statistical analysis of the ex vivo permeation parameters led to the choice of F1L – made of Span® 60 and Tween® 80 at the weight ratio of 4:1 along with 1% w/v Labrasol® – as the selected formula (SF). SF was formulated into a hydrogel by using 2.5% w/v of HPMC K4M. The hydrogel exhibited good in vitro characteristics. Also, it retained its physical and chemical stability for one month in the refrigerator. The radiolabeling of SF showed a maximum yield by mixing of 100 µl of diluted formula wit...

57 citations

Journal ArticleDOI
TL;DR: The results of the in vivo study revealed that valsartan orodispersible tablets would be advantageous with regards to improved patient compliance, rapid onset of action, and increase in bioavailability.
Abstract: Valsartan orodispersible tablets have been developed at 40-mg dose, with the intention of facilitating administration to patients experiencing problems with swallowing and hopefully, improving its poor oral bioavailability. Work started with selecting drug compatible excipients depending on differential scanning calorimetric analysis. A 33 full factorial design was adopted for the optimization of the tablets prepared by freeze-drying technique. The effects of the filler type, the binder type, and the binder concentration were studied. The different tablet formulas were characterized for their physical properties, weight variation, disintegration time, surface properties, wetting properties, and in vitro dissolution. Amongst the prepared 27 tablet formulas, formula number 6 (consisting of 4:6 valsartan:mannitol and 2% pectin) was selected to be tested in vivo. Oral bioavailability of two 40 mg valsartan orodispersible tablets was compared to the conventional commercial tablets after administration of a single dose to four healthy volunteers. Valsartan was monitored in plasma by high-performance liquid chromatography. The apparent rate of absorption of valsartan from the prepared tablets (Cmax = 2.879 μg/ml, tmax = 1.08 h) was significantly higher than that of the conventional tablets (Cmax = 1.471 μg/ml, tmax = 2.17 h), P ≤ 0.05. The relative bioavailability calculated as the ratio of mean total area under the plasma concentration–time curve for the orodispersible tablets relative to the conventional ones was 135%. The results of the in vivo study revealed that valsartan orodispersible tablets would be advantageous with regards to improved patient compliance, rapid onset of action, and increase in bioavailability.

42 citations

Journal ArticleDOI
TL;DR: Itraconazole (ITZ) crystalline nanoparticles were prepared using relatively simple, low-cost sonoprecipitation technique, in which both the solvent and antisolvent were organic in nature.
Abstract: Itraconazole (ITZ) crystalline nanoparticles were prepared using relatively simple, low-cost sonoprecipitation technique, in which both the solvent and antisolvent were organic in nature. The effect of stabilizer type (hydroxypropyl methylcellulose, hydroxypropyl cellulose, Inutec SP1®, and pluronic F127), drying method (oven and freeze drying) and matrix former used (Avicel PH101, and Aerosil®200) on the dissolution performance as a key characteristic of nanocrystals was evaluated. In 10 min, all of the prepared nanocrystals showed 3.77−8.59 times improvement in percent drug dissolved compared to pure ITZ. Concerning the effect of stabilizer type, the following rank order can be given: pluronic F127 ≥ hydroxypropyl cellulose ≥ hydroxypropyl methylcellulose (HPMC) > inutec SP1. Freeze-dried ITZ nanocrystals containing Avicel PH 101 showed better dissolution rate compared to other nanocrystals. The chemical structure of itraconazole nanocrystals was not changed as revealed by Fourier transform infrared. Stability study of selected nanocrystals (F5, F7, and F8) revealed physical and chemical stability of F7 and F8, while a decrease in dissolution rate of F5 was observed (although being chemically stable) when stored under high relative humidity conditions. Although inutec is less potent than pluronic F127 and HPMC regarding their effect on dissolution rate enhancement, it is equipotent to pluronic F127 in preserving the rapid drug dissolution.

36 citations


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Journal ArticleDOI
TL;DR: The aim of this review is to provide an overview of the critical factors affecting the formulation of thin films, including the physico-chemical properties of polymers and drugs, anatomical and physiological constraints, as well as the characterization methods and quality specifications to circumvent the difficulties associated with formulation design.

332 citations

Journal ArticleDOI
TL;DR: The magnitude of variants of ODF technology and the advantages over conventional dosage forms promise more applications and more marketed products with ODFs in the near future.
Abstract: Introduction: Orodispersible films for oral delivery are gaining popularity. Whereas breath-fresheners and over-the-counter products have already become quite common in the US, the first prescription drug films were introduced into the EU and US markets only very recently. Already considered as a unique Rx (prescription drug) dosage form by the FDA (oral soluble film), such products are not substitutable by conventional oral dosage forms. The official term defined by the European Medicines Agency is orodispersible film (ODF). Areas covered: This review gives an overview on the benefits of ODFs, typical excipients and products already available on the market. ODFs are defined and differentiated from other films and dosage forms. Possible manufacturing methods are described. As ODFs are not yet listed in one of the pharmacopoeias, possible methods for characterization and quality control are discussed. Required characteristics, advantages and disadvantages are elaborated. Biopharmaceutical considerations ar...

277 citations

Journal ArticleDOI
TL;DR: As the drug is directly absorbed into systemic circulation, degradation in gastrointestinal tract and first pass effect can be avoided, these points make this formulation most popular and acceptable among pediatric and geriatric patients and patients with fear of choking.
Abstract: Recently, fast dissolving films are gaining interest as an alternative of fast dissolving tablets. The films are designed to dissolve upon contact with a wet surface, such as the tongue, within a few seconds, meaning the consumer can take the product without need for additional liquid. This convenience provides both a marketing advantage and increased patient compliance. As the drug is directly absorbed into systemic circulation, degradation in gastrointestinal tract and first pass effect can be avoided. These points make this formulation most popular and acceptable among pediatric and geriatric patients and patients with fear of choking. Over-the-counter films for pain management and motion sickness are commercialized in the US markets. Many companies are utilizing transdermal drug delivery technology to develop thin film formats. In the present review, recent advancements regarding fast dissolving buccal film formulation and their evaluation parameters are compiled.

219 citations

Journal ArticleDOI
TL;DR: Orally disintegrating films have potential for business and market exploitation because of their myriad of benefits over orally disintegrating tablets and the market prospect of this innovative dosage form is also targeted.
Abstract: Over the past few decades, tendency toward innovative drug delivery systems has majorly increased attempts to ensure efficacy, safety and patient acceptability. As discovery and development of new chemical agents is a complex, expensive and time consuming process, so recent trends are shifting toward designing and developing innovative drug delivery systems for existing drugs. Out of those, drug delivery system being very eminent among pediatrics and geriatrics is orally disintegrating films (ODFs). These fast disintegrating films have superiority over fast disintegrating tablets as the latter are associated with the risks of choking and friability. This drug delivery system has numerous advantages over conventional fast disintegrating tablets as they can be used for dysphasic and schizophrenic patients and are taken without water due to their ability to disintegrate within a few seconds releasing medication in mouth. Various approaches are employed for formulating ODFs and among which solvent casting and spraying methods are frequently used. Generally, hydrophilic polymers along with other excipients are used for preparing ODFs which allow films to disintegrate quickly releasing incorporated active pharmaceutical ingredient (API) within seconds. Orally disintegrating films have potential for business and market exploitation because of their myriad of benefits over orally disintegrating tablets. This present review attempts to focus on benefits, composition, approaches for formulation and evaluation of ODFs. Additionally, the market prospect of this innovative dosage form is also targeted.

208 citations

Journal ArticleDOI
TL;DR: This pharmaceutical form with a blustering beginning as a breath freshener had an emergent entrance in the Rx market proving its reliable value, and is described and explores the oral film technology from its main component, the polymeric matrices, to the new and possible market applications.

206 citations