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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
Thu Oct 26 2023
Journal Name
Farmacia
THE DEVELOPMENT OF A BRAIN TARGETED MUCOADHESIVE AMISULPRIDE LOADED NANOSTRUCTURED LIPID CARRIER
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Publication Date
Wed Jan 12 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of Community Pharmacists Knowledge, Attitude and Practice towards Modified Release Dosage Forms
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Purpose:To evaluate knowledge, practice and attitude of community pharmacists in Basra regarding modified release dosage forms which are widely used for many therapeutic purposes in pharmacy practice.

Methods:The current study was conducted among certified pharmacists in Basra governorate- south of Iraq. Data collection was carried out by a questionnaire.

Results:A total number of 175 community pharmacists responded to the questionnaire. The majority worked in OTC based dispensing pharmacies located in the center of the city. Most respondents missed K1 and were unable to state the difference between different types of modified products. There was a major positive agreemen

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Publication Date
Wed Jul 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Evaluation of Fast Dissolving Tablets of Taste-Masked Ondansetron Hydrochloride by Solid Dispersion
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Ondansetron hydrochloride (ONH) is a very bitter, potent antiemetic drug used for the treatment and/or prophylaxis of chemotherapy or radiotherapy or postoperative induced emesis. The objective of this study is to formulate and evaluate of taste masked fast dissolving tablet (FDTs) of ONH to increase patient compliance.

 ONH taste masked granules were prepared by solid dispersion technique using Eudragit E100 polymer as an inert carrier. Solvent evaporation and fusion melting methods were used for such preparation.

Completely taste masking with zero release of drug in phosphate buffer pH 6.8was obtained from granules prepared by solvent evaporation method using drug: polymer ratio of 1:2, from which four formulas pas

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Publication Date
Tue Jun 15 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Solubility and Dissolution Enhancement of Ebastine by Surface Solid Dispersion Technique
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Ebastine (EBS) is a non-sedating antihistamine with a long duration of action. This drug has predominantly hydrophobic property causing a low solubility and low bioavailability. Surface solid dispersions (SSD) is an effective technique for improving the solubility and dissolution rate of poorly soluble drugs by using hydrophilic water insoluble carriers.

The present study aims to enhance the solubility and dissolution rate of EBS by using surface solid dispersion technique. Avicel® PH101, Avicel® PH 102, croscarmellose sodium(CCS) and sodium starch glycolate(SSG) were used as water insoluble hydrophilic carriers.

The SSD formulations of EBS were prepared by the solvent evaporation method in different drug:  carrier

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Publication Date
Tue Jan 01 2019
Journal Name
Malaysian Journal Of Biochemistry & Molecular Biology
Evaluation influence of extract of Terfezia claveryi desert truffle, pezizaceae, against Streptococcus pneumoniae, in vivo
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Publication Date
Mon Sep 01 2025
Journal Name
Journal Of Cancer Research Updates
Hematological Parameters in Liver Metastasis: A Comprehensive Clinical Evaluation for Early Detection in Iraqi Patients
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Background: Liver metastasis significantly complicates cancer prognosis, yet easily accessible markers for its early detection and monitoring remain crucial. This study aimed to comprehensively evaluate key hematological parameters as potential indicators for liver metastasis in Iraqi patients. Methods: We conducted a cross-sectional study comparing hematological profiles between 90 patients (presumably with liver metastasis) and 30 healthy controls. White Blood Cell (WBC) count, Lymphocyte percentage, Neutrophil percentage, and Neutrophil-to-Lymphocyte Ratio (NLR) were analyzed. Given non-normal data distributions (confirmed by the Shapiro-Wilk test), group comparisons were performed using the non-parametric Mann-Whitney U test.

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Publication Date
Tue Jun 11 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and In-Vitro Evaluation as an Oral Microsponge Tablet of Baclofen
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The aim of the present study is to formulate floating effervescent microsponge tablet of the narrow absorption window drug, Baclofen (BFN) for controlling drug release and thereby decrease the side effect of the drug. The microsponges of BFN were prepared by non-aqueous emulsion solvent diffusion method (oil in oil emulsion method). The effects of drug: polymer ratio, stirring time and type of Eudragit polymer  on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selected microsponge formula was incorporated into the floating effervescent gastro-retentive tablet. The prepared fl

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Publication Date
Sat Dec 11 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and in-vitro Evaluation of Carvedilol Gastroretentive Capsule as (Superporous Hydrogel)
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  The preferred route of drug administration is the oral route, but drugs with narrow absorption window in the gastrointestinal tract are still challenging. The ability to extend and monitor the gastric emptying time is a valuable tool for processes remaining in the stomach longer than other traditional dosage forms.

The purpose of this study was to formulate and evaluate gastroretentive superporous hydrogel (SPH) of carvedilol with view to improve its solubility and increase gastric residence time in order to get sustained release formulas via utilization of various kinds and concentrations of hydrophilic polymers then after, incorporate the best prepared formula into capsules.

 Sixteenth formulae of SPH h

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Publication Date
Sat Jun 19 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and In-Vitro Evaluation of Meloxicam Solid Dispersion using Natural Polymers.
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Meloxicam (MLX) is non-steroidal anti -inflammatory, poorly water soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Solid dispersion (SD) is an effective technique for enhancing the solubility and dissolution rate of such drug.

    The present study aims to enhance the solubility and the dissolution rate of MLX by SD technique by solvent evaporation method using sodium alginate (SA), hyaluronic acid (HA), collagen and xyloglucan (XG) as gastro-protective hydrophilic natural polymers.

Twelve formulas were prepared in different drug: polymer ratios and evaluated for their, percentage yield, drug content,  water so

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Publication Date
Sun Mar 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and Characterization of Montelukast Sodium ( SMLT ) as a Dual Sustained Release Buccal Strips
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An oral bi layer  sustained release (SR) strips of Sodium  Montelukast SMLT , which is selective  leukotriene  antagonist  , used  for  patients  suffered from mid-night asthma , were prepared successfully ,using different polymers, like guar  gum , carrageenan , and xanthan gum , by solvent casting method .

The results obtained by this study revealed  ,that best  fast  dissolving  film of  SMLT was  loaded  in carrageenan   polymer 57%  w\w (30mg.) ,  with  acceptable  physical properties, like film thickness , elastic endurance and  surface pH  .

Besides  to that , the  disintegration  t

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