Browsing by Author "Aboelwafa A.A."

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    Enhancement of the bioavailability of an antihypertensive drug by transdermal protransfersomal system: formulation and in vivo study
    (Taylor and Francis Ltd, 2018) Morsi N.M.; Aboelwafa A.A.; Dawoud M.H.S.; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; Cairo University; Cairo; Egypt; Department of Pharmaceutics; Faculty of Pharmacy; October University for Modern Sciences and Arts; Dokki; Egypt
    Timolol Maleate (TiM), a nonselective ?-adrenergic blocker, is a potent highly effective agent for management of hypertension. The drug suffers from poor oral bioavailability (50%) due to its first pass effect and a short elimination half-life of 4 h; resulting in its frequent administration. Transdermal formulation may circumvent these problems in the form of protransfersomes. The aim of this study is to develop and optimize transdermal protransfersomal system of Timolol Maleate by film deposition on carrier method where protransfersomes were converted to transfersomes upon skin hydration following transdermal application under occlusive conditions. Two 2 3 full factorial designs were employed to investigate the influence of three formulation variables which were; phosphatidyl choline: surfactant molar ratio, carrier: mixture and the type of SAA each on particle size, drug entrapment efficiency and release rate. The optimized formulation was evaluated regarding permeation through hairless rat skin and compared with oral administration of aqueous solution on male Wistar rats. Optimized protransfersomal system had excellent permeation rate through shaved rat skin (780.69 ?g/cm 2 /h) and showed six times increase in relative bioavailability with prolonged plasma profile up to 72 h. A potential protransfresomal transdermal system was successfully developed and factorial design was found to be a smart tool in its optimization. � 2017 Informa UK Limited, trading as Taylor & Francis Group.
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    Formulation and evaluation of ergotamine tartrate Lyophilized nasal insert
    (2014) El-Telbany D.F.; Tayel S.A.; El-Nabarawi M.A.; Tag R.; Aboelwafa A.A.; Pharmaceutics and Industrial Pharmacy; MSA University; Egypt; Pharmaceutics and Industrial Pharmacy; Cairo University; Egypt
    Lyophilized nasal inserts represent an alternative route for the administration of drugs. The aim of this study is to prepare a firm single dose unit of nasal insert containing ergotamine tartrate which allows easy administration in the nasal cavity and prevent first pass metabolism leading to increased bioavailability. The insert was prepared by applying freeze drying technique using 2% w/w of different polymers.The prepared inserts were evaluated for appearance, bioadhesion potential, water uptake, in vitro drug release and imaged by scanning electron microscopy.The results showed that the prepared nasal inserts have a smooth surface and a spongy-like appearance. No interaction occurred between the drug and different polymers as revealed in DSC and FT-IR. Higher viscosity of the polymer causes a greater degree of water uptake and high bioadhesion potential; this in turn reduces the drug release, as the diffusional path length of drug becomes longer. The study revealed an inverse relationship between water uptake, bioadhesion potential and in vitro drug release. The order of drug release from different inserts is HPMC E5 > PVP K90 > Sodium aliginate > Carrageenan > NaCMC > Xanthan Gum > Chitosan.
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    Improved bioavailability of timolol maleate via transdermal transfersomal gel: Statistical optimization, characterization, and pharmacokinetic assessment
    (Elsevier, 2016) Morsi N.M.; Aboelwafa A.A.; Dawoud M.H.S.; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; Cairo University; Cairo; Egypt; Department of Pharmaceutics; Faculty of Pharmacy; Modern Sciences and Arts University; Cairo; Egypt
    Timolol maleate (TiM), a nonselective ?-adrenergic blocker, is a potent highly effective agent for management of hypertension. The drug suffers from extensive first pass effect, resulting in a reduction of oral bioavailability (F%) to 50% and a short elimination half-life of 4 h; parameters necessitating its frequent administration. The current study was therefore, designed to formulate and optimize the transfersomal TiM gel for transdermal delivery. TiM loaded transfersomal gel was optimized using two 23 full factorial designs; where the effects of egg phosphatidyl choline (PC): surfactant (SAA) molar ratio, solvent volumetric ratio, and the drug amount were evaluated. The formulation variables; including particle size, drug entrapment efficiency (%EE), and release rate were characterized. The optimized transfersomal gel was prepared with 4.65:1 PC:SAA molar ratio, 3:1 solvent volumetric ratio, and 13 mg drug amount with particle size of 2.722 ?m, %EE of 39.96%, and a release rate of 134.49 ?g/cm2/h. The permeation rate of the optimized formulation through the rat skin was excellent (151.53 ?g/cm2/h) and showed four times increase in relative bioavailability with prolonged plasma profile up to 72 h compared with oral aqueous solution. In conclusion, a potential transfersomal transdermal system was successfully developed and the factorial design was found to be a smart tool, when optimized. � 2016