Background: Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, several formulations of FVT were prepared. Objective: Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel. Methods: Binary ethosomes were prepared using different concentrations of phospholipid PLH90, ethanol, propylene glycol, and cholesterol by thin film hydration and characterized by particle size, zeta potential, and entrapment efficiency. Furthermore, in-vitro, in-vivo, ex-vivo, pharmacokinetics, and histopathological studies were done. Results: Regarding FVT-loaded BE, formula (F9) demonstrated the best parameters from the other formulas; with the lowest particle size (154.1±4.38 nm), lowest PDI (0.213±0.05), highest zeta potential (-46.94±1.05), and highest entrapment efficiency (89.34 ±2.37%). Regarding gel formulation, G2 showed the best gel formula with drug content (99.82±0.02%) and spreadability (12.88 g/ cm2). In-vitro study results showed that, in the first 30 minutes, around 22.3% of the medication is released, whereas, after 24 hours, about 98.56% is released in G2. Conclusion: Based on enhancing the bioavailability and sustaining the drug release, it can be concluded that the Frovatriptan-Loaded Binary ethosome Gel as nano-delivery was developed as a promising non-invasive drug delivery system for treating migraine.
Lasmiditan (LAS) is a recently developed antimigraine drug and was approved in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability, which is around 40%.
This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased in situ gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension (AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in order to determine its relative bioavailability (F-relative) via using rabbits.
In situ gel can be defined as a polymer solution administered as a liquid and when exposed to some physiologic condition such as thepH, ionic, temperature modulation or solvent and UV induced gelation undergo to phase transition to a semisolid gel. Ketotifenfumarate belongs to the histamine H1 receptor antagonists, and Ketotifen fumarate is used in the treatment of allergic conditions likeconjunctivitis and rhinitis. This work aims to study the natural polymer effects (xanthan gum,gellan gum) on the properties of pH-trigger in situ ocular gel, then compared the drug-releasing rate of optimized formula with the market ketotifen eye drop. Eightformulations (F1-F8) were prepared using different concentrations of xanthan gum, gellan gum with ca
... Show MoreIn the present study, MCM-41 was synthesis as a carrier for poorly drugs soluble in water, by the sol-gel technique. Textural and chemical characterizations of MCM-41 were carried out by X-ray diffraction (XRD), Fourier transform infrared (FTIR), scanning electron microscope (SEM), and thermal gravimetric analysis (TGA). The experimental results were analyzed mesoporous carriers MCM-41. With maximum drug loading efficiency in MCM-41 determined to be 90.74%. The NYS released was prudently studied in simulated body fluid (SBF) pH 7.4 and the results proved that the release of NYS from MCM-41 was (87.79%) after 18 hr. The data of NYS released was found to be submitted a Weibull model with a correlation coefficient of (0.995). The Historical
... Show MoreNimodipine (NMD) is a dihydropyridine calcium channel blocker useful for the prevention and treatment of delayed ischemic effects. It belongs to class ? drugs, which is characterized by low solubility and high permeability. This research aimed to prepare Nimodipine nanoparticles (NMD NPs) for the enhancement of solubility and dissolution rate. The formulation of nanoparticles was done by the solvent anti-solvent technique using either magnetic stirrer or bath sonicator for maintaining the motion of the antisolvent phase. Five different stabilizers were used to prepare NMD NPs( TPGS, Soluplus®, HPMC E5, PVP K90, and poloxamer 407). The selected formula F2, in which Soluplus
has been utilized as a stabilizer, has a par
... Show MoreChitosan-schiff base with three different ratios of para-Dimethyl aminobenzaldehyde& chitosan Schiff base hydrogels have been prepared for controlled drug release study. The synthesized chitosan Schiff base and chitosan Schiff base hydrogel were characterized by FT-IR, UV-Visible, SEM, analysis. Swelling properties of the hydrogel were investigated at three different media pH (2, 7, 10). The swelling degree varied with the pH, amount of crosslinking agent glutaraldehyde and with the amount of paraDimethylaminobenzaldehyde for the hydrogels. All hydrogels were used for controlled drug release system. Aspirin was used as model drug, in three different buffer solution (2, 7, 10) as release media. The rate of release of drugs in the pH2 is m
... Show MoreAlginate is one of the natural biopolymers that is widely used for drug formulations, combination of alginate with other polymers, such as gum acacia, pectin, and carrageenan can increase mechanical strength, therefore, can reduce leakage of the encapsulated active pharmaceutical ingredient from the polymer matrix. Interaction of alginate and these polymers can occur via intermolecular hydrogen bonds causing synergism, which is determined from the viscosity of polymer mixture.
Alginate was combined with gum acacia/pectin/carrageenan in different blending ratios (100:0, 75:25, 50:50, 25:75, and 0:100) with and without addition of CaCl2. The synergism effect is obtained from the design of experimental (DoE), and calculati
... Show MoreSelexipag is an orally selective long-acting prostacyclin receptor agonist, which indicated for the treatment of pulmonary arterial hypertension. It is practically insoluble in water ( class II, according to BCS). This work aims to prepare and optimized Selexipag nanosuspensions to achieve an enhancement in the in vitro dissolution rate. The solvent antisolvent precipitation method was used for the production of nanosuspension, and the effect of formulation parameters (stabilizer type, drug: stabilizer ratio, and use of co-stabilizer) and process parameter (stirring speed) on the particle size and polydispersity index were studied. SLPNS prepared with Soluplus® as amain stabilizer (F15) showed the smallest particle size 47nm wi
... Show MoreFelodipine is a calcium-channel blocker with low aqueous solubility and bioavailability. Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE) is one of the popular methods that has been used to solve the dispersibility problems of many drugs. Felodipine was formulated as a NE utilizing oleic acid as an oil phase, tween 80 and tween 60 as surfactants and ethanol as a co-surfactant. Eight formulas were prepared, and different tests were performed to ensure the stability of the NEs, such as particle size, polydispersity index, zeta potential, dilution test, drug content, viscosity and in-vitro drug release. Result
... Show MoreEpilepsy is considered as one of the common neurological disorders.About 50 million persons have affected by epilepsy .Carbamazepine is one of the common drugs used by pregnant women with epilepsy. The aim of the present study is to investigate the effect of carbamazepine on the process of brain development during day 13 of pregnancy.Fifty pregnant albino mice have been used. They were divided into two groups. The control group that had been orally drenched with normal saline. The other group was treated group that had been given 15 mgKg of Carbamazepine orally. The fetuses have been collected after killing of the mice. Boun’s solution was selected as fixative. 5-8 µm thick sections from the fetuses were cut to be stained with hematoxyli
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