Browsing by Author "Morsi N.M."

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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.
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
Insulin Mucoadhesive Liposomal Gel for Wound Healing: a Formulation with Sustained Release and Extended Stability Using Quality by Design Approach
(Springer New York LLC, 2019) Dawoud M.H.S.; Yassin G.E.; Ghorab D.M.; Morsi N.M.; Department of Pharmaceutics; Faculty of Pharmacy; October University for Modern Sciences and Arts; (MSA University); Giza; Egypt; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; Al-Azhar University; Cairo; Egypt; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; Cairo University; Cairo; Egypt
The present study deals with the formulation of topical insulin for wound healing with extended stability and sustained release, by applying quality by design concepts. Insulin has been promoted as a promising therapeutic wound healing agent. Topical formulation of insulin faced major problems, as it cannot be delivered safely to the wound with a controlled rate. Formulation of insulin-loaded vesicles in optimized bio-adhesive hydrogels has been explored to ensure a safe delivery of insulin to wounds in a controlled manner. Quality by design (QbD) was applied to study the effect of several critical process parameters on the critical quality attributes. Ishikawa diagram was used to identify the highest risk factors, which were screened by a fractional factorial design and augmented by Box�Behnken design. The optimized formula was incorporated into a mucoadhesive gel, which was further subjected to stability and clinical studies. An optimized formula was obtained with a particle size of 257.751�nm, zeta potential ? 20.548�mv, 87.379% entrapment efficiency, and a release rate of 91.521�?g/cm2/h. The results showed that liposomal insulin remained stable for 6�months in aqueous dispersion state at 4�C. Moreover, the release was sustained up to 24�h. The clinical study showed an improvement in the wound healing rate, 16 times, as the control group, with magnificent reduction in the erythema of the ulcer and no signs of hypoglycemia. Insulin-loaded liposomal chitosan gel showed a promising drug delivery system with high stability and sustained release. � 2019, American Association of Pharmaceutical Scientists.
Response surface optimization and in-vitro evaluation of sustained release topical insulin liposomal spray for wound healing
(Open Science Publishers LLP Inc., 2018) Dawoud M.H.S.; Yassin G.E.; Ghorab D.M.; Morsi N.M.; Department of Pharmaceutics; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA University); Cairo; Egypt; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; Al-Azhar University; Cairo; Egypt; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; Cairo University; Cairo; Egypt
Chronic wounds are considered a major health care concern, that represents a life-threatening problem worldwide. Insulin has proven its great efficiency as a wound healing agent, especially with diabetic ulcers. However; insulin suffers degradation at the application site due to proteases, moreover; when wounds are painful the patient fails to apply any remedy frequently. In the present study, insulin has been formulated as a spray in liposomes, which protects it at the wound area and sustains its release and thus reducing the application frequency, furthermore; the spray reducing the direct contact of the applicator with the skin, thus, reducing the probability of infection. The full-factorial design has been applied in the preparation optimization of liposomes, where the effects of the cholesterol, method of preparation and sonication have been tested on the particle size and the entrapment efficiency. The present study shows how the thin film hydration method in the absence of cholesterol and sonication were the best conditions for insulin. liposomal formulation, that satisfies the target of the study. Liposomes showed a sustained release of insulin up to 24 hours and were successfully formulated into a spray dosage form. In conclusion, topical insulin liposomal spray offers a protective method from insulin degradation with an expected increase in the patient compliance. � 2018 Marwa H. S. Dawoud et al.