Solubility Enhancement of Ebastine by Formulating Microemulsion Using D-Optimal Mixture Design: Optimization and Characterization

Barve, Apoorva Ratnakar; Kapileshwari, Gauri Ramchandra; DCruz, Cleona Elizabeth Mary; Kumar, Lalit; Bhide, Prashant Jivaji; Mahajan, Anand A.; Arondekar, Asmita Sunil; Weigensberg, Marc J.

doi:10.1089/adt.2022.049

Cited by 3 publications

(1 citation statement)

References 27 publications

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“…1. It has a log P value of 4.8 and related to BCS II class [7,8]. ERT exerts its action by ferroptosis via promotes cystine-glutamate transport receptor (system XC−), the voltage-dependent anion channel, and p53 receptors [3].…”

Section: Introductionmentioning

confidence: 99%

Box-Behnken design-based development of eco-friendly RP-HPLC analytical method for the quantification of erastin from the mesoporous silica nanoparticles

Gupta,

Moorkoth

et al. 2024

Preprint

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The current work aims to optimize, stablish, validate a high-performance liquid chromatography (HPLC) method that possesses sufficient sensitivity and specificity to measure erastin (ERT) in mesoporous silica nanoparticles. The HPLC method was optimized using Design of Experiments (DoE) technique. The Box-Behnken design (BBD) was used and buffer ratio, injection volume, buffer pH, and flow rate were used as the independent factors. The dependent variables were retention time (Rt) of ERT, peak area of ERT, and tailing factor (Tf) of ERT. The optimized chromatographic condition were: buffer ration 80%, buffer pH 3.8 and flow rate 0.9 mL/min, and injection volume 8 µL. The established HPLC method was validated as per ICH Q2 (R1) recommendations. The established method showed the good linearity (R2 = 0.9991) having a range of 12–500 ng/mL and LOD and LOQ was 2.71 ng and 6.25 ng, respectively. The mesoporous silica nanoparticle (MSN) matrix did not affect the specificity of our validated RP-HPLC method of analysis for ERT. Analysing the formulation's surface morphology helped with the confirmation of the synthesized MSNs. The proposed RP-HPLC method was effectively used to calculated the medication loaded in the MSNs as well as to measure the amount of ERT entrapped. The % EE for ERT in MSNs was found to be 76.07% and % DL for ERT in MSNs was found to be 14%, respectively. The established HPLC method was found ecofriendly as per the AGREE analysis.

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Section: Introductionmentioning

confidence: 99%

Box-Behnken design-based development of eco-friendly RP-HPLC analytical method for the quantification of erastin from the mesoporous silica nanoparticles

Gupta,

Moorkoth

et al. 2024

Preprint

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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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Formulation of Felodipine lipid nanoparticle-loaded oral fast-dissolving films

Naik,

DCruz,

Kumar

et al. 2024

Tenside Surfactants Detergents

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Felodipine, a calcium channel blocker used to treat hypertension, is a BCS Class II drug characterized by low solubility, high permeability and significant hepatic metabolism, which limits its bioavailability to 15 %. This study focuses on improving the bioavailability of Felodipine by developing oral fast-dissolving films (OFDFs) incorporating lipid nanoparticles. Felodipine loaded lipid nanoparticles were prepared using glyceryl monooleate (GMO) as lipid and Poloxamer 407 as the surfactant, and then incorporated into OFDFs using the solvent casting technique. A Box-Behnken design with Design Expert Stat-Ease® 360 was used to evaluate the impact of GMO, Poloxamer 407 concentration, and sonication time on particle size and entrapment efficiency. The resulting nanoparticle dispersions had particle sizes ranging from 74.92 nm to 112.1 nm and entrapment efficiencies between 80.43 % and 95.23 %. Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD) confirmed successful drug encapsulation. The OFDF showed optimal mechanical properties, disintegration within (41.33 ± 3.51) s, and an in-vitro drug release of (89.82 ± 2.75) % in 6 min. Scanning electron microscopy (SEM) revealed a smooth, uniform, porous surface and the films remained stable for three months. The study concludes that Felodipine loaded lipid nanoparticles in fast-dissolving OFDFs improve permeability, dissolution, and onset of action, making them a promising approach for antihypertensive therapy.

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Solubility Enhancement of Ebastine by Formulating Microemulsion Using D-Optimal Mixture Design: Optimization and Characterization

Cited by 3 publications

References 27 publications

Box-Behnken design-based development of eco-friendly RP-HPLC analytical method for the quantification of erastin from the mesoporous silica nanoparticles

Box-Behnken design-based development of eco-friendly RP-HPLC analytical method for the quantification of erastin from the mesoporous silica nanoparticles

Designing and evaluation of ebastine–benzamide cocrystals

Formulation of Felodipine lipid nanoparticle-loaded oral fast-dissolving films

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