Browsing by Author "El-Leithy E.S."

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Lipid nanocarriers for tamoxifen citrate/coenzyme Q10 dual delivery
(Editions de Sante, 2017) El-Leithy E.S.; Abdel-Rashid R.S.; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Cairo; Egypt; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; Helwan University; Ain Helwan; Cairo; 11795; Egypt
Nanotechnology based combinatorial therapy has emerged as an effective strategy for cancer treatment due to its synergistic activity, suppression of multi-drug resistance and successful delivery to target site. The objective of this work was to develop and characterize tamoxifen citrate (TC) and coenzyme Q10 (CoQ10) lipid nanocarriers for oral breast cancer chemotherapy. Stearic acid (2%w/v) and poloxamer188 (3%w/v) were selected as optimal lipid matrix and surfactant for development of solid lipid nanocarriers (SLNs). Incorporation of lecithin into lipid matrix (SLN9) significantly reduced particle size to 180 nm and increased %EE of CoQ10 (45%). Nanostructured lipid carriers containing 10% Labrafac oil showed further decrease in particle size reaching only 81 nm and increased %EE up to 94% and 56% for TC and CoQ10, respectively. Lipid nanocapsules showed more prominent effect on decreasing particle size (36 nm). Lipid nanocarriers offered controlled drug release profiles. The study showed that lipid carriers significantly improved drugs permeation through rabbit intestinal mucosa and suggested them as potential delivery systems for improving the bioavailability of TC/CoQ10 therapeutic molecules. Subsequent studies will be performed in order to elucidate the cytotoxicity and genotoxicity of selected lipid nanocarriers formulas on MCF-7 (adenocarcinoma breast cancer cells) versus normal cells (WISH cell line). � 2017 Elsevier B.V.
Optimization of nutraceutical coenzyme Q10 nanoemulsion with improved skin permeability and anti-wrinkle efficiency
(Taylor and Francis Ltd., 2018) El-Leithy E.S.; Makky A.M.; Khattab A.M.; Hussein D.G.; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Cairo; Egypt; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; Helwan University; Ain Helwan; Cairo; Egypt; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; Cairo University; Cairo; Egypt; National Organization for Drug Control and Research; Cairo; Egypt
Coenzyme Q10 (CoQ10) is an insoluble, poorly permeable antioxidant with great biological value which acts as anti-aging and anti-wrinkle agent. To improve its permeability through topical application, the current study aimed at formulating oil/water (o/w) nanoemulsion (NE) as an efficient vehicle for delivering (CoQ10) through the skin barriers. The solubility of (CoQ10) was tested for various oils, surfactants (S), and co-surfactants (CoS). The NE region was determined by constructing pseudoternary phase diagrams. NE formulae containing 1, 2, and 3% w/w drug have been subjected to thermodynamic stability test. The formulae that passed thermodynamic stability tests were characterized by physical properties as pH, viscosity, refractive index, droplet size, zeta-potential, TEM, electroconductivity, in vitro release, and ex vivo permeation. The formula F2 containing 10% w/w isopropyl myristate (oil phase), 60% w/w of Tween 80: Transcutol HP mixture (S/CoSmix) at ratio 2:1, 30% w/w water and 2% w/w drug was evaluated for its anti-wrinkle efficiency using an animal model. The F2 formula showed 11.76 1.1 nm droplet size, 1.4260 0.0016 refractive index, 0.228 PDI, ?14.7 1.23 mv zeta potential, 7.06 0.051 pH, 199.05 0.35 cp viscosity, and the highest percentage of drug release in the selected dissolution media. About 47.21% of the drug was released in phosphate buffer 7.4 containing 5% w/v Labrasol and 5% w/v isopropyl alcohol through 24 h. It also showed the highest drug flux (Jss = 3.164 g/cm2/h), enhancement ratio (Er = 8.32), and permeability coefficient (Kp = 22.14 10?4 cm2/h). CoQ10 NE reduced the skin wrinkles and gave the skin smooth appearance. Our investigation suggests the potential use of NE as a vehicle for enhancing solubility and permeability of CoQ10 and thus improving its anti-wrinkle efficiency. 2017 Informa UK Limited, trading as Taylor & Francis Group.
Tamoxifen citrate/Coenzyme Q10 as smart nanocarriers Bitherapy for Breast Cancer: Cytotoxicity, genotoxicity, and antioxidant activity
(Editions de Sante, 2019) El-Leithy E.S.; Hassan S.A.; Abdel-Rashid R.S.; Department of Pharmaceutics and Industrial Pharmacy; Faculty of Pharmacy; Helwan University; Cairo; Egypt; Faculty of Pharmacy; Department of Pharmaceutics and Industrial Pharmacy; MSA University; Cairo; Egypt; Therapeutic Chemistry Dept; National Research Center; Cairo; Egypt
Nanotechnology-based bitherapy has recently emerged as an effective strategy to overcome biomedical barriers against successful anticancer therapy. The study aimed to evaluate lipid nanocarriers loaded with tamoxifen citrate/coenzyme Q10 (TC/CoQ10) as bitherapy for selective targeting of breast cancer. Based on a previous study, four formulations of lipid nanocarriers were selected for in-vitro cell viability estimation using both MCF-7 and normal WISH cell lines. Oxidative status, cytopathological changes, and genetoxicity were also investigated. The results showed 100% mortality for tested cells without selectivity even at very low concentration for free drugs. On the other hand lipid nanocarriers revealed an increase in % cell viability for normal WISH cell line reaching 100% at 0.25 ?g/ml. The lipid nanocarrier formulated from stearic acid and lecithin showed LC 50 on MCF-7 cell line (1.6 ?g/ml) compared to (4.8 ?g/ml) on WISH cell line. The cell death pathway for unformulated bitherapy depended on necrosis rather than apoptosis. The Malondialdehyde concentration was decreased, while Glutathione level increased to near normal values in both MCF-7 and WISH cells. The results demonstrated a promising synergistic and selective action of TC/CoQ10 bitherapy on breast cancer cells when administered in lipid nanocarriers delivery system. � 2019 Elsevier B.V.