Enhancement of solubility and dissolution rate of ebastine fast-disintegrating tablets by solid dispersion method

Islam, Nayyer; Irfan, Muhammad; Abbas, Nasir; Syed, Haroon Khalid; Iqbal, Muhammad Shahid; Khan, Ikram Ullah; Rasul, Akhtar; Inam, Sana; Hussain, Amjad; Mohsin, Noor ul Amin; Arshad, Mohammad Sohail; Ali, Mohsin

doi:10.4314/tjpr.v19i9.1

Cited by 6 publications

(4 citation statements)

References 23 publications

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“…Previously, hydroxypropyl methylcellulose (HPMC-K15M) was investigated for the development of oral films [ 23 , 24 ]. The main reason for selecting HPMC is that it provides appropriate mechanical strength to the films [ 25 , 26 , 27 ]. The significance of current research work is that transfersomes-loaded oral films offer more absorptive properties than existing EBT formulations.…”

Section: Introductionmentioning

confidence: 99%

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

et al. 2021

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The main objective of this research work was the development and evaluation of transfersomes integrated oral films for the bioavailability enhancement of Ebastine (EBT) to treat allergic rhinitis. The flexible transfersomes, consisting of drug (EBT), lipid (Phosphatidylcholine) and edge activator (EA) Polyoxyethylene sorbitan monooleate or Sorbitan monolaurate, were prepared with the conventional thin film hydration method. The developed transfersomes were further integrated into oral films using the solvent casting method. Transfersomes were evaluated for their size distribution, surface charge, entrapment efficiency (EE%) and relative deformability, whereas the formulated oral films were characterized for weight, thickness, pH, folding endurance, tensile strength, % of elongation, degree of crystallinity, water content, content uniformity, in vitro drug release and ex vivo permeation, as well as in vivo pharmacokinetic and pharmacodynamics profile. The mean hydrodynamic diameter of transfersomes was detected to be 75.87 ± 0.55 nm with an average PDI and zeta potential of 0.089 ± 0.01 and 33.5 ± 0.39 mV, respectively. The highest deformability of transfersomes of 18.52 mg/s was observed in the VS-3 formulation. The average entrapment efficiency of the transfersomes was about 95.15 ± 1.4%. Transfersomal oral films were found smooth with an average weight, thickness and tensile strength of 174.72 ± 2.3 mg, 0.313 ± 0.03 mm and 36.4 ± 1.1 MPa, respectively. The folding endurance, pH and elongation were found 132 ± 1, 6.8 ± 0.2 and 10.03 ± 0.4%, respectively. The ex vivo permeability of EBT from formulation ETF-5 was found to be approximately 2.86 folds higher than the pure drug and 1.81 folds higher than plain film (i.e., without loaded transfersomes). The relative oral bioavailability of ETF-5 was 2.95- and 1.7-fold higher than that of EBT-suspension and plain film, respectively. In addition, ETF-5 suppressed the wheal and flare completely within 24 h. Based on the physicochemical considerations, as well as in vitro and in vivo characterizations, it is concluded that the highly flexible transfersomal oral films (TOFs) effectively improved the bioavailability and antihistamine activity of EBT.

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Section: Introductionmentioning

confidence: 99%

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

et al. 2021

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“…These results indicate that the bilosystem (either bilosome or biloparticle) is able to increase the solubility and to control the release of the incorporated drug. Furthermore, these data revealed the significant dominance of the bilosystem to enhance the intestinal passage of budesonide, possibly due to the ability of these nanocarriers to improve the intestinal permeability of the encapsulated drugs [42][43][44][45][46][47][48][49][50][51][52][53][54][55][56].…”

Section: In Vitro and Ex Vivo Studiesmentioning

confidence: 97%

Bilosomes and Biloparticles for the Delivery of Lipophilic Drugs: A Preliminary Study

Sguizzato,

Ferrara,

Baraldo

et al. 2023

Antioxidants

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In this study, bile acid-based vesicles and nanoparticles (i.e., bilosomes and biloparticles) are studied to improve the water solubility of lipophilic drugs. Ursodeoxycholic acid, sodium cholate, sodium taurocholate and budesonide were used as bile acids and model drugs, respectively. Bilosomes and biloparticles were prepared following standard protocols with minor changes, after a preformulation study. The obtained systems showed good encapsulation efficiency and dimensional stability. Particularly, for biloparticles, the increase in encapsulation efficiency followed the order ursodeoxycholic acid < sodium cholate < sodium taurocholate. The in vitro release of budesonide from both bilosytems was performed by means of dialysis using either a nylon membrane or a portion of Wistar rat small intestine and two receiving solutions (i.e., simulated gastric and intestinal fluids). Both in gastric and intestinal fluid, budesonide was released from bilosystems more slowly than the reference solution, while biloparticles showed a significant improvement in the passage of budesonide into aqueous solution. Immunofluorescence experiments indicated that ursodeoxycholic acid bilosomes containing budesonide are effective in reducing the inflammatory response induced by glucose oxidase stimuli and counteract ox-inflammatory damage within intestinal cells.

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“…EB has a partition coefficient (Log P) of 6.8 and a melting point of 86°C. 8,9 Theoretical rules for the formation of ebastine cocrystals 1. pKa rule Benzamide (Pka 14.5) was used as a conformer to prepare cocrystal with EB (Pka 8.19) since according to the "pKa rule," ΔpKa = pKa (acceptor (EB)) À pKa (donor (BENZ)) 13,14 The ΔpKa = -6.31, supposing the formation of cocrystal 15 2. Gibbs free energy and ΔpKa…”

Section: Introductionmentioning

confidence: 99%

Designing and evaluation of ebastine–benzamide cocrystals

Salih,

Al-Khedairy

2023

F1000Res

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Background: Ebastine (EB) is a selective nonsedating H1 antihistamine belonging to Class II(BCS); it has inadequate oral bioavailability due to its poor water solubility. Cocrystal is one of the most recent methods that has been utilized to improve some physicochemical characteristics of a drug, such as solubility and dissolution rate. This research's main objective was to design and evaluate EB cocrystal as a trial to enhance its solubility. Methods: Various techniques were employed to formulate cocrystals, such as solvent evaporation, slurry, and drop asset grinding using benzamide (BENZ) as a co-former in different molar ratios. The prepared formulas were characterized by percentage yield, drug content, saturation solubility, in vitro dissolution studies, infrared spectroscopy (FTIR), Raman spectroscopy, powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC), Results: Solubility enhanced by 347 fold in distilled water with enhanced dissolution profile. Conclusions: Co-crystallization is a potential solid formation method due to its ability to enhance physicochemical and mechanical characteristics. Co-crystals have been successfully formed from a variety of medicines and co-former, using distinct hydrogen bond synthon motifs.

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Enhancement of solubility and dissolution rate of ebastine fast-disintegrating tablets by solid dispersion method

Cited by 6 publications

References 23 publications

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

Bilosomes and Biloparticles for the Delivery of Lipophilic Drugs: A Preliminary Study

Designing and evaluation of ebastine–benzamide cocrystals

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