Browsing by Author "Yassin, Ghada E"

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Development of Eplerenone nano sono-crystals using factorial design: Enhanced solubility and dissolution rate via anti solvent crystallization technique
(Informa Healthcare, 2022-12) Yassin, Ghada E; Khalifa, Maha K. A
Objective The purpose of this work was to improve EP solubility by using a sono-crystalization approach to reduce particle size and hence, increase the dissolution rate. Significance Eplerenone (EP) is an antagonist of the aldosterone receptor and is used for the treatment of hypertension and chronic heart failure. EP was classed as biopharmaceutical classification (BCS) class II because of its poor solubility and high permeability, which retards dissolution rate and drug absorption, and decreases bioavailability. Methods Three-factors and two-level (2³) multifactorial design have been employed to study the effect of independent variables which are drug concentration; (X1), stabilizer type (X2), and stabilizer concentration(X3) on responses; saturated solubility of EP in distilled water (Y1), saturated solubility in acidic media pH 1.2 (Y2), particle size (Y3), and polydispersity index, PDI (Y4). Also, they were characterized by Fourier transformed infrared spectroscopy (FTIR), Powder X-ray diffraction (PXRD), Differential scanning calorimetry (DSC), and yield percentage. The optimum formula was further subjected to an in-vitro release study. Results The optimized formulation showed a saturated solubility of EP as 1.29, and 1.86 (mg/ml) in distilled water and acidic media (pH 1.2) respectively. Also, the particle size of 133 nm, and PDI of 0.824 with a small percentage of the difference between the observed and predicted values. Ninety-one percent of EP was released within 10 min., and it was completely released within 45 min. with a significantly higher release rate compared to raw drug. Conclusion This work resulted in a satisfactory enhancement of solubility and dissolution rate which, is suitable for further in-vivo analysis.
Fluconazole-Niosome-Laden Contact Lens: A Promising Therapeutic Approach for Prolonged Ocular Delivery and Enhanced Antifungal Activity
(Springer New York, 2024-07) Yassin, Ghada E; Amer, Mai A; Mannaa, Islam M; Khalifa, Maha Khalifa Ahmed
Background Traditional routes of administration of fluconazole such as eye drops have a low therapeutic efficacy due to insufficient bioavailability. Purpose Herein, a fluconazole noisome-laden contact lens was prepared to control and prolong the drug release and improve its bioavailability. Methods Two methods have been used to prepare fluconazole niosomes: solvent injection method and thin film hydration method utilizing span 60 and cholesterol mixture. Subsequently, formulations were optimized using three factors and a twolevel factorial design and were subjected to in-vitro characterization for the size of niosomes, zeta potential, entrapment efficiency percent, and cytotoxicity study. The optimized fluconazole niosomes were further entrapped in contact lenses by the soaking method and were evaluated according to in-vitro release profile, and antimicrobial activity. Results The results revealed that the investigated fluconazole niosomes are of nano-size ranging from 228.2 to 769.2 nm with zeta-potential values between −18.1 and −60.2 mV. The entrapment efficiency percentage ranged from 51.3 to 75%. Fluconazole was released from fluconazole noisome-laden contact lens and showed a prolonged release up to 48–72 h with a cumulative release of 79.62%. Statistical analysis showed that fluconazole-noisome-laden contact lenses have a significant impressive fungal adhesion reduction as compared to fluconazole-laden contact lenses. Conclusion Fluconazole noisome-laden contact lenses are a promising therapeutic way for effective and prolonged treatment of ocular fungal infection.
Pharmaceutical and Pharmacological Evaluation of the Effect of Nano-Formulated Spironolactone and Progesterone on Inflammation and Hormonal Levels for Managing Hirsutism Experimentally Induced in Rats
(Springer, 7/13/2021) Amer, Reham I; Yassin, Ghada E; Mohamed, Reem A; Fayez, Ahmed M
Hirsutism is a dermatological condition that refers to the excessive growth of hair in androgen-sensitive areas in women. Recently, the enhancement of the visible signs of a hairy female has taken special concern that affected the quality of life. The present study was developed to compare the follicular targeting effect of topical spironolactone (SP) or progesterone (PG)-loaded nanostructured lipid carrier (NLC) on the management of hirsutism. Four NLC formulations were prepared using cold homogenization techniques and pharmaceutically evaluated. SP-NLC and PG-NLC topical hydrogels were prepared to explore their pharmacological effect on letrozole induced polycystic ovarian syndrome (PCOS) in rats. Inflammatory mediators, antioxidant, and hormonal parameters were assayed. Additionally, histopathological examination was carried out to confirm the successful induction of PCOS. Results confirmed that all NLC formulations have a spherical shape with particle size ranged from 225.92 ± 0.41 to 447.80 ± 0.66 nm, entrapment efficiency > 75%, and zeta potential (− 31.4 to − 36.5 mV). F1 and F3 NLCs were considered as selected formulations for SP and PG, respectively. Female Wistar rats treated with F1 formulation for 3 weeks displayed better outcomes as manifested by the measured parameters as compared to the other tested groups. A significant reduction in hair follicle diameter and density was observed after topical application of SP or PG nano-gels. Finally, the outcomes pose a strong argument that the development of topically administered SP- NLC can be explored as a promising carrier over PG-NLC for more effectual improvement in the visible sign of hirsutism.
QUALITY BY DESIGN APPROACH IN FORMULATION & OPTIMIZATION OF INSULIN LOADED LIPOSOMES BY DETERMINING ENCAPSULATION EFFICIENCY
(CAIRO UNIVERSITY, 2016) Yassin, Ghada E; Ghorab, Dalia M; Morsi, Nadia M
The purpose of this study was to extend Quality by Design (QbD) principles to develop insulin-loaded liposomes, to identify and control critical sources of variability in the process, and to understand the impact of formulation and process parameters on the liposomal formulation. Insulin was found to possess an excellent wound healing property.