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Development of Lyophilized Ebastine-Loaded Novasome Tablets: Comprehensive Physicochemical Characterization and In Vitro/In Vivo Release Evaluation
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Introduction/Objective:

Ebastine, a second-generation H1 antihistamine, exhibits poor aqueous solubility and consequently low oral bioavailability, limiting its clinical therapeutic efficacy. Novasome is an advanced vesicular nanocarrier system that offers a promising approach to enhance the solubility and dissolution behavior of a poorly water solubility drug. Therefore, this study aimed to develop, optimize, and characterize ebastine-loaded novasomes and to compress them into tablets to enhance drug solubility, dissolution, and oral bioavailability.

Methods:

Ebastine-loaded novasomes were prepared and optimized, then converted into lyophilized tablets using a suitable cryoprotectant. The optimized formulation was characterized for Particle Size (PS), Polydispersity Index (PDI), Zeta Potential (ZP), and Entrapment Efficiency (EE). Solidstate properties were assessed via Differential Scanning Calorimetry (DSC) and X-Ray Diffraction (XRD), while drug-excipient compatibility was evaluated using Fourier-Transform Infrared Spectroscopy (FTIR). In-vitro release studies were performed under stimulated physiological conditions, and in-vivo pharmacokinetic evaluation was conducted in Wistar rats.

Results:

The selected ebastine-loaded novasome exhibited a mean particle size of 189.9nm, a polydispersity index of 0.31, and an entrapment efficiency of 86.19%. In-vitro release exceeded 90% over 12 hours, significantly surpassing the dissolution profile of pure ebastine. DSC and XRD analyses confirmed amorphization of the drug within the Novasomal matrix, while FTIR revealed no evidence of drug-excipient compatibility. In-vivo studies demonstrated a 493.88% increase in relative oral bioavailability compared to free drug suspension (p < 0.05).

Discussion:

The enhanced dissolution and bioavailability are attributable to drug amorphization, high surface area to volume ratio of the nanovesicles, and protective entrapment of ebastine within the bilayer structure, which together improved gastrointestinal solubilization and oral bioavailability.

Conclusion:

The lyophilized Ebastine-loaded novasome tablet constitutes a stable, effective, and pharmacokinetically superior oral dosage form, offering significant potential for enhance the oral bioavailability of poorly water-soluble drugs.

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Publication Date
Sat Sep 08 2018
Journal Name
International Journal Of Applied Pharmaceutics
PREPARATION AND CHARACTERIZATION OF LAFUTIDINE AS IMMEDIATE RELEASE ORAL STRIP USING DIFFERENT TYPE OF WATER-SOLUBLE POLYMER
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Objective: The objective of the present study was to design and optimize oral fast dissolving film (OFDF) of practically insoluble drug lafutidine in order to enhance bioavailability and patient compliance especially for a geriatric and unconscious patient who are suffering from difficulty in swallowing.Methods: The films were prepared by a solvent casting method using low-grade hydroxyl propyl methyl cellulose (HPMC E5), polyvinyl alcohol (PVA), and sodium carboxymethyl cellulose (SCMC) as film forming polymers. Polyethylene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer to enhance the film forming properties of the polymer. Tween 80 (1% solution) and poloxamer407 were used as a surfactant, citri

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Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and Characterization of Poly (D,L-Lactide-Co-Glycolide) Microspheres for Controlled Release of KSL Peptide
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The purpose of this research was to prepare, characterize, and evaluate the new antimicrobial peptide  KSL peptide encapsulated in poly(D,L-lactide-co-glycolide) (PLGA)composite microspheres. KSL was loaded in poly(acryloyl hydroxyethyl) starch (acHES) micropar-ticles, and then the peptide-containing microparticles were encapsulated in the PLGA matrix by a solvent extraction /evaporation method.

 KSL-loaded PLGA microspheres were also prepared without the starch hydrogel microparticle microspheres for comparison study. KSL peptide microspheres were characterized for drug content, surface morphology, microspheres size determination, polymers stability , in vitro microspheres degradation and in vitro release. KSL peptide

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Publication Date
Wed Dec 30 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation, Characterization and Ex vivo Permeability Study of Transdermal Apixaban O/W Nanoemulsion Based Gel
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This study designed to prepare ultrafine apixaban (APX) o/w nanoemulsion (NE) based gel with droplet size below 50 nm as a good method for transdermal APX delivery without using permeation enhancer, alternatively, the formulation components itself act as permeation enhancer. APX, a potent oral anticoagulant drug that selectively and directly inhibit coagulation factor Xa, was selected as a good candidate for transdermal delivery as it displays poor water solubility (0.028 mg/mL) and low bioavailability (50%). APX-NE gel was prepared using triacetin, triton-x-100 and carbitol as oil phase, surfactant and cosurfactant respectively, while Carbopol 940 used as a gelling agent. Ex vivo permeation of APX-NE gel through human stratum c

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Publication Date
Fri Jun 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Effect Of Comprehensive Income In Market Value Of Company Importance Of Comprehensive Income In Market Value Of
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The study aims (objective ) to clarify the concept of comprehensive income and its usefulness for users, as the study aims to clarify the relationship between the concept of comprehensive income and market value of the company where the measurement of comprehensive income after accounting for net income and by measuring the unrealized gains or losses in the value of securities available for sale, and measurement the unrealized gains or losses on futures contracts, which are financial derivatives, and measurement the unrealized gains or losses from the settlement of foreign currency translation (conversions), and measurement the impact on the market value of companies and of the present study to rise or fall of return on the stock

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Publication Date
Wed Sep 30 2026
Journal Name
Journal Of Baghdad College Of Dentistry
In-Vitro evaluation of load-deflection characteristics and force levels of nickel titanium orthodontic archwires
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Background: Nickel-titanium (NiTi) archwires have become increasingly popular because of their ability to release constant light forces, which are especially useful during initial alignment and leveling phase. The aim of the present study was to investigate and compare the load–deflection characteristics of four commercially available NiTi archwires. Materials and methods: 200 NiTi 0.014, 0.016, 0.018, 0.016x0.022 and 0.019x0.025-inch nickel–titanium archwires from four different manufacturers (3M, Ortho Technology, Jiscop and Astar) were tested. The load-deflection properties of these archwires were evaluated by a full arch bending test in both palatal and gingival directionsat 37°C temperature using a universal material t

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Publication Date
Mon Jan 01 2024
Journal Name
Nanotechnology, Science And Applications
Formulation and Characterization of Intranasal Drug Delivery of Frovatriptan-Loaded Binary Ethosomes Gel for Brain Targeting
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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 paramet

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Publication Date
Wed Jan 24 2024
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Development and Characterization of Hyaluronic Acid-Incorporated Thermosensitive Nasal in situ Gel of Meclizine Hydrochloride
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Background: Meclizine hydrochloride (MCZ) is an antihistamine that is used as an antiemetic to prevent and cure nausea and vomiting. Because of its limited water solubility and first-pass metabolism, it exhibits variable absorption. Objective: To formulate and evaluate MCZ as an intranasal in situ gel with increased residence time and permeability. Methods: We made an inclusion complex of MCZ using various cyclodextrins as a complexing agent to help the drug dissolve better. The complexes were studied, and the ones that were better at dissolving were chosen to be used in the creation of an in situ gel with poloxamer 407 (17–20% w/v) and hyaluronic acid (0.25–0.75% w/v). Prepared formulas were subjected to various evaluation tes

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Publication Date
Fri Feb 09 2024
Journal Name
Pharmacia
Evaluation of types and concentration of bile salts impact on physical properties of nisoldipine-loaded bilosomes
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Background: Bilosomes are lipid vesicles that exhibit flexibility and deformability. They consist of phospholipids and amphiphilic bile salts. Compared to the normal vesicular systems such as liposomes and niosomes, bilosomes provide several notable advantages, including simplified manufacturing, cost-effectiveness, and enhanced stability.

Aim: The main objective of the present work was to evaluate the effect of different bile salts on the physical properties that include entrapment efficiency, vesicle size, and polydispersity index(PDI). In addition, in vitro drug release for nisoldipine (NSD) loaded bilosomes was evaluated.

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Publication Date
Fri Jun 17 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Development of 5-FU Loaded poly lactic-co-glycolic acid Nanoparticles for Treatment of Lung Cancer
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Non-Small Cell Lung Cancer (NSCLC) accounts for about 84% of all lung cancer types diagnosed so far. Every year, regardless of gender, the NSCLC targets many communities worldwide. 5-Fluorouracil (5-FU) is a uracil-analog anticancer compound. This drug tends to annihilate multiple tumour cells. But 5-FU's most significant obstacle is that it gets very easily metabolized in the blood, which eventually leads to lower anticancer activity. Therfore a perfect drug delivery system is needed to overcome all the associated challenges.

In this experiment, an attempt was made to prepare 5-FU loaded poly lactic-co-glycolic acid  nanoparticles using solvent evaporation method and subsequently observed the effect of molecular weight of poly l

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Publication Date
Wed Sep 30 2026
Journal Name
Journal Of Baghdad College Of Dentistry
In Vitro Evaluation of Shear Bond Strength of Sapphire Brackets after Dental Bleaching
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Background: The present study was conducted to evaluate the effects of different bleaching methods on the shear bond strength of orthodontic Sapphire brackets bonded to human premolars teeth using light cured composite resin and to determine the predominant site of bond failure. Materials and Methods: Thirty freshly extracted human premolars were selected and randomly divided into three groups (10 per group). These groups are: control (unbleached) group, hydrogen peroxide group (HP) 37.5% ; which is the in- office bleaching method group, carbamide peroxide group (CP) 16%; which is the at- home bleaching method group. After bleaching process was performed, all the teeth stored in distilled water in a sealed container at room temperature for

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