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Introduction
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Publications
Publications (62)
PurposeLetrozole (LTZ), an aromatase inhibitor with poor aqueous solubility, is used as the first line treatment for hormonal sensitive breast cancer in postmenopausal women. The purpose of the current study is to develop hyaluronic acid (HA)/chitosan (Cs)-coated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles for the delivery of LTZ to improve...
The aim was to develop an optimized albendazole (ALB) nanosuspension to improve its solubility and therapeutic activity as an adjuvant localized therapy for treatment of the pinworm infection to enhance oral treatment outcomes using Box-Behnken design. ALB-nanosuspensions were successfully prepared by antisolvent sono-precipitation technique consid...
Skin damage exposes the underlying layers to bacterial invasion, leading to skin and soft tissue infections. Several pathogens have developed resistance against conventional topical antimicrobial treatments and rendered them less effective. Recently, several nanomedical strategies have emerged as a potential approach to improve therapeutic outcomes...
Ionotropic gelation method was used to entrap Ketoprofen (KP) into calcium alginate beads. KP is one of the non steroidal anti-inflammatory drugs (NSAIDs); it has a short half life (1.5-2 h) and deleterious side effects on GIT such as irritation and ulceration. Beads were investigated in-vitro for possible sustained drug release and in-vivo as a ga...
Solid lipid nanoparticles (SLN) have demonstrated favorable properties for oral protein delivery. However, their protein entrapment efficiency (EE%) values remain limited due to their hydrophobic nature. In this study, we reported a new strategy in which two polymeric excipients were incorporated into the double-emulsion based SLN to address this e...
Intravenous delivery of poorly water-soluble anticancer drugs such as docetaxel (DTX) is challenging due to the low bioavailability and the toxicity related to solubilizing excipients. Colloidal nanoparticles are used as alternative carriers, but low drug loading capacity and circulation instability limit their clinical translation. To address thes...
The purpose of the current study is to develop nanostructured lipid carriers (NLCs) for the delivery of the antihyperlipidemic drug simvastatin (SIM) to increase its extremely low oral bioavailability (<5%) and prolong its antihyperlipidemic effect. NLCs were prepared via emulsification-solvent evaporation technique followed by ultrasonication, and...
Objective: To develop and characterize in situ thermosensitive gels for the vaginal administration of sildenafil as a potential treatment of endometrial thinning occurring as a result of using clomiphene citrate for ovulation induction in women with type II eugonadotrophic anovulation. While sildenafil has shown promising results in the treatment o...
We aimed to investigate the effect of adding sildenafil vaginal gel to clomiphene citrate (CC) in infertile women with prior CC failure.
Methods
This is a self- controlled clinical trial. Women with CC failure (in prior 5 cycles) and thin endometrium were recruited (N = 42). In their 6th (CC only) cycle, women continued on CC 100 mg/ day for 5 day...
Objective: To develop and characterize in situ thermosensitive gels for the vaginal administration of sildenafil as a potential treatment of endometrial thinning occurring as a result of using clomiphene citrate for ovulation induction in women with type II eugonadotrophic anovulation. While sildenafil has shown promising results in the treatment o...
Drug delivery using synthetic nanoparticles including porous silicon has been extensively used to overcome the limitations of chemotherapy. However, their synthesis has many challenges such as lack of scalability, high cost, and the use of toxic materials with concerning environmental impact. Nanoscale materials obtained from natural resources are...
The aim of the present work was to prepare and evaluate sublingual fast dissolving films containing metoprolol tartrate-loaded niosomes. Niosomes were utilized to allow for prolonged release of the drug, whereas the films were used to increase the drug’s bioavailability via the sublingual route. Niosomes were prepared using span 60 and cholesterol...
Solid lipid nanoparticles (SLN) have demonstrated good potential for oral peptide delivery. However, their hydrophobic nature generally accounts for low peptide entrapment efficiency (EE%). In this study, a new strategy was adopted to improve peptide EE% by incorporating a hydrophilic viscosity-enhancing agent (VA) within SLN cores to develop visco...
Non-ionic surfactant vesicles containing fluconazole (FLZ) were prepared using, span 60 or span 80 and cholesterol in weight ratios of 1:1, 2:1 and 1:2. The prepared vesicles were characterized for size, entrapment efficiency, and _in vitro_ drug release. The drug encapsulation efficiencies varied from 40.0% to 84.35%. The particle size ranged from...
Nonionic surfactant vesicles containing celecoxib (CXB) as an anti-inflammatory drug were prepared using, Span 60 or Span 40 and cholesterol in the ratios of 1:0, 1:1 and 1:2. Prepared vesicles were characterized for encapsulation efficiency, particle size and drug release. The drug encapsulation efficiencies varied from 60.55 to 80.35 %. The vesic...
Multidrug resistance (MDR), a major cause for chemotherapy failure, has been linked to upregulation of ATP-dependent membrane efflux systems that limit intracellular accumulation of cytotoxic anticancer agents. P-glycoprotein (P-gp) encoded by the human ABCB1 gene was the first efflux transporter identified to contribute to MDR. ABCB1 gene expressi...
Even with the use of double-emulsion technique for preparation, the hydrophobic nature of solid lipid nanoparticles (SLNs) limits their encapsulation efficiency (EE%) for peptides such as insulin. In this study, we hypothesize that inclusion of Methocel into SLN to form Methocel-lipid hybrid nanocarriers (MLNs) will significantly enhance insulin EE...
Niosomes have been reported as a possible approach to improve low skin permeation shown by
conventional vehicles. In this study, a noisome-based delivery system of meloxicam (MX) was
developed and characterized for in vitro performance.
Niosomes were prepared by reverse-phase evaporation method (REV) using different non ionic
surfactants and choles...
In view of the wide clinical use of theophylline, its narrow therapeutic index, repeated daily dosing and gastrointestinal side effects, sustained-release microcapsules of theophylline were prepared by a modified emulsion-solvent evaporation –non solvent addition technique. Two different polymers, namely, cellulose acetate butyrate (CAB) and ethyl...
Background: Bacterial vaginosis (BV) is one of the most common infections in childbearing age.
Aim: To compare the efficacy of metronidazole (once-daily 0.8% MTZ in situ gel) versus twice-daily conventional MTZ vaginal gel in the treatment of bacterial vaginosis (BV).
Material and methods: All patients who presented to Assiut
Women Health Hospital-...
A. Santos, D. Losic, and co-workers demonstrate on page 5107 the preparation of luminescent silicon diatom replicas with unique porous microcapsule structures, by conversion from silica diatoms using a reduction process. These silicon diatoms are biodegradable and have intrinsic luminescence, sensing and drug-releasing properties which make them ou...
Current development of drug microcarriers is mainly based on spherical shapes, which are not biologically favorable geometries for complex interactions with biological systems. Scalable synthesis of drug carriers with nonspherical and anisotropic shapes featuring sustained drug-releasing performances, biocompatibility, degradability, and sensing ca...
Purpose: To develop a safe, lipid-based non-viral gene delivery system that achieves high transfection efficiency in the presence of serum proteins. Methods: Polyplexes with the pAcGFP1-C1 plasmid were formed in phosphate buffered saline, pH 7.4 (PBS)
using the novel poly[N-(2-hydroxypropyl)methacrylamide]-poly(N,N-dimethylaminoethylmethacrylate) d...
Ionotropic gelation method was used to entrap Ketoprofen (KP) into calcium alginate beads. KP is one of the non steroidal anti-inflammatory drugs (NSAIDs); it has a short half life (1.5-2 h) and deleterious side effects on GIT such as irritation and ulceration. Beads were investigated in-vitro for possible sustained drug release and in-vivo as a ga...
Abstract Non-ionic surfactant vesicles were prepared using Span-60 and cholesterol in the mass ratios of 1:1, 2:1, 1:2 and 3:1 for transdermal delivery of an anti-inflammatory drug meloxicam (MXM). The drug encapsulation efficiencies and particle size were observed in the range of 32.9-80.7% and 56.5-133.4 nm, respectively. Three different gel base...
Preclinical Research
The objective of this work was to evaluate liposome‐containing gel formulations for the sustained, site‐specific delivery of celecoxib ( CXB ). Liposomes composed of phosphadtidylcholine (and various amounts of cholesterol ( C h) were prepared using thin film hydration and characterized for encapsulation efficiency, vesicle si...
The aim of this study was to develop and evaluate self-nanoemulsifying drug delivery system (SNEDDS) of tadalafil (TDL) in order to enhance its aqueous solubility and dissolution rate. TDL SNEDDS were developed by aqueous phase titration method via construction of pseudo-ternary phase diagrams. The formulations which passed thermodynamic stability...
The aim of this study was to measure and correlate the temperature dependent solubility data of tadalafil (TDL) in water, ethanol, propylene glycol (PG), polyethylene glycol-400 (PEG-400), and Transcutol from (298.15 to 333.15) K at atmospheric pressure using the shake flask method. The experimental solubilities were regressed by Apelblat equation...
Abstract The aim of this study was to develop liposomal-based (LBGF) and micro-emulsion-based (MBGF) gel formulations of croconazole to compare their topical delivery potential. Conventional gels were also prepared using various polymers such as sodium carboxymethyl cellulose (SCMC), Poloxamer 407, Carbopol 971P and chitosan. The in vitro release o...
Poor solubililty of drugs is the major obstacle associated with formulation development. Application of nanotechnology in the formulation development of poorly soluble drugs as nanosuspensions offers the opportunity to address many of the deficiencies associated with these compounds.
Therefore, the aim of present study was to develop and evaluate n...
Development and characterization of thermosensitive pluronic-based metronidazole in situ gelling formulations for vaginal application
The purpose of this study was to develop pluronic-based in situ gelling formulations of metronidazole (MTZ) for treatment of bacterial vaginosis, aimed at prolonging the residence time, controlling drug release, enha...
In the design of oral delivery, alginates (Alg) have attracted increasing attention. However, due to their hydrophilic character incorporation of small hydrophilic drugs such as tolmetin sodium (TOL) into Alg beads will not provide the desired regular shape as well as delayed drug release. There is no study investigating the effect of methylcellulo...
Lornoxicam is a NSAID of the oxicam class and it has the same side effects of this group when taken orally. In attempts to avoid the systemic side effects of lornoxicam (e.g. gastric irritation) and to achieve sustained release of the drug, several buccal patch formulations containing lornoxicam were prepared using different polymers and were evalu...
This study was designed to evaluate the suitability of chitosan polymer as a vehicle for topical delivery system. Celecoxib, which is a non-steroidal anti-inflammatory drug, was incorporated into the gel vehicles in a concentration of 0.5 % w/v. Gels were prepared using three different concentrations and different molecular weights of chitosan. Vis...
To compare the efficacy of a novel vaginal delivery system for metronidazole (0.8% MTZ in situ gel) versus a conventional MTZ vaginal gel product in the treatment of bacterial vaginosis (BV).
All consecutive patients who presented to a tertiary care hospital with symptoms suggestive of BV were approached to participate in the study. Forty-two eligi...
The objective of this work was to develop suitable film formulations of ketorolac tromethamine (KT) for transdermal use and to investigate the effect of film composition and permeation enhancers on the in-vitro release and skin permeation of the drug. Polyvinyl alcohol (PVA), sodium carboxymethylcellulose (NaCMC), and chitosan were used as film-for...
The objective of this work was to evaluate the efficacy and suitability of different organogel formulations as transdermal delivery systems of meloxicam (MX) compared to hydrogel formulations. Hydrogels and hydroalcoholic gels were prepared using either carbopol 940 or pluronic F-127 as gelling agents. The organogels used glyceryl monostrearate (GM...
The aim of the present study was to develop ibuprofen (IBU) - loaded pellets by melt solidification technique using Gelucire 50/13 (GL) as a lipid carrier in different concentrations. This system was intended to prolong the drug release in order to minimize the drug related adverse effects and improve bioavailability in different gastrointestinal t...
Ketorolac tromethamine (KT) is a non-steroidal anti-inflammatory drug having a half half-life around 6 h. This study aims to formulate sustained release forms of KT by preparing solid dispersion in the matrices of Eudragit polymers (Eud) using coevaporation technique. Tow Eud polymers, namely Eud RS100 and Eud RL100, were used in preparing KT-copre...
The aim of this study was to prepare and characterize solid dispersions of water insoluble non-steroidal anti-inflammatory drug, indomethacin (IND), with polyethylene glycol 4000 (PEG4000) and Gelucire 50/13 (Gelu.) for enhancing the dissolution rate of the drug. The solid dispersions (SDs) were prepared by hot melting method at 1:1, 1:2 and 1:4 dr...
The aim of this study was to prepare and characterize solid dispersions of water insoluble non steroidal anti-inflammatory drug, indomethacin (IND), with polyethylene glycol 4000 (PEG4000) and Gelucire 50/13 (Gelu.) for enhancing the dissolution rate of the drug. The solid dispersions (SDs) were prepared by hot melting method at 1:1, 1:2 and 1:4 dr...
The characteristics of NO donors, NOC5 [3-(2-hydroxy-1-(1-methylethyl-2-nitrosohydrazino)-1-propanamine), NOC12 [N-ethyl-2-(1-ethyl-2-hydroxy-2-nitrosohydrazino)-ethanamine] and SNAP [S-nitroso-N-acetyl-DL-penicillamine] as absorption enhancers for poorly absorbable drugs were examined in rats using an in situ closed loop method. They were compared...
The objective of this study was to estimate the colon-specific delivery of [Asu1,7]-eel calcitonin (ECT) using chitosan capsules in rats. The intestinal absorption of ECT was evaluated by measuring the plasma calcium levels after oral administration of the chitosan capsules containing ECT and different combinations of additives. The same combinatio...
The characteristics of three NO donors, 3-(2-hydroxy-1-(1-methylethyl)-2-nitrosohydrazino)-1-propanamine (NOC5), N-ethyl-2-(1-ethyl-2-hydroxy-2-nitrosohydrazino)-ethanamine (NOC12) and S-nitroso-N-acetyl-DL-penicillamine (SNAP) as absorption enhancers for peptide drugs were examined in rats using a modified Ussing chamber method and an in situ clos...
In general, absorption enhancing effects of various absorption enhancers were greater in the large intestine than those in the small intestinal regions. Therefore, the effectiveness of absorption enhancers is expected to be remarkably observed, if these enhancers can be delivered to the large intestine with some poorly absorbable drugs after oral a...
In attempts to avoid the systemic side effects of piroxicam (PC) (e.g. gastrotoxicity), several buccal gel formulations containing PC were prepared and their effects on the characteristics of the drug permeation through rabbit buccal mucosa in-vitro were evaluated using a Franz-type diffusion cell. The general rank order of the total flux of 0.5% P...