Optimization and Solubilization Study of Nanoemulsion Budesonide and Constructing Pseudoternary Phase Diagram

Puppala, Raman Kumar; A, Vijaya Lakshmi

doi:10.22159/ajpcr.2019.v12i1.28686

Cited by 5 publications

(3 citation statements)

References 7 publications

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“…The percent weight of oil, S-mix and water in the mixture was calculated to delineate the phase boundaries in each diagram, then plotted using the Original Lab software. The NE's area, which is considered to be visually clear, was the shaded one in a triangle plot with one apex representing the oil, the second one representing water and the third representing the S-mix at a fixed weight ratio [16][17][18]. The method used for the preparation of NE Scientists in a variety of sectors, including pharmaceutical sciences, have paid close attention to the phase inversion composition method (also known as the self-nano emulsification method), which produces NEs at ambient temperature without the need for organic solvents or heat.…”

Section: Productive Of Pseudo-ternary Phase Diagramsmentioning

confidence: 99%

“…Using the plasma concentrationtime curve, we were able to calculate the maximum plasma concentration (Cmax) and the time needed to attain Cmax following oral and intranasal delivery. The elimination half-life time (t1/2) is calculated as 0.693/Ke [37], and the elimination rate constant (Ke) is calculated from the slope of the straight section of the terminal phase (where the slope is equal to Ke/2.303) [16]. where, C19 is the concentration of LAS after 19 hs.…”

Section: Parameters Involved In Pharmacokineticsmentioning

confidence: 99%

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Lasmiditan Nanoemulsion Based in Situ Gel Intranasal Dosage Form: Formulation, Characterization and in Vivo Study

JABER

2023

FARMACIA

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This study aimed to formulate lasmiditan (LAS) as a nanoemulsion in situ gel (NEIG) by utilising nanotechnology in order to escape the problems associated with the poor oral bioavailability of the drug. A study regarding the LAS solubility in different oils, surfactants and co-surfactants, was determined. Different nanoemulsion (NE) formulations were prepared depending on the pseudo-ternary phase diagrams, which were first constructed. Visual characterization, thermodynamic stability study and droplet size were determined for the prepared NEs. Muco-ciliary clearance can be overcome with the in situ gelling agent carbopol 934, a pH-sensitive polymer that was selected to increase the residence time on the nasal mucosa. The gel strength, pH, gelation time and viscosity were predicted for the prepared NEIG. In vitro release and ex vivo nasal permeation were measured for both NE and NEIG formulations. Formula coded-15 (F15) with a droplet size of 58.4 nm provided a maximum in vitro as well as ex vivo permeation to be considered as a selected one, to which 0.5% carbopol 934 was added for the preparation of NEIG2 that exerts comparable release and permeation values as F15 with more residence time in order to overcome the normal nasal physiological clearance. Finally, LAS as NEIG2 was subjected to an in vivo study as a promising intranasal novel formula that exerts rapid onset of action (Tmax 0.75 hours) accompanied by higher bioavailability (2.5 folds) and tissue permeation (4 folds) relative to the oral dosage form (8% aqueous LAS suspension) was considered. RezumatStudiul a avut ca scop formularea lasmiditanului (LAS) sub forma unui gel de tip nanoemulsie in situ (NEIG) prin utilizarea nanotehnologiei, pentru a evita problemele asociate cu biodisponibilitatea orală scăzută a substanței. S-au preparat diferite nanoemulsii (NE) în funcție de diagramele de fază pseudoternare. Caracterizarea vizuală, studiul stabilității termodinamice și dimensiunea picăturilor au fost determinate pentru NE-urile preparate. Clearance-ul mucociliar poate fi redus cu ajutorul agentului de gelificare in situ carbopol 934, un polimer sensibil la pH care a fost selectat pentru a crește timpul de rezidență pe mucoasa nazală. Rezistența gelului, pH-ul, timpul de gelifiere și vâscozitatea au fost estimate pentru NEIG preparate. Cedarea in vitro și permeabilitatea nazală ex vivo au fost măsurate pentru ambele formulări NE și NEIG. Formula F15, cu o dimensiune a picăturilor de 58,4 nm, a prezentat o permeabilitate maximă in vitro, precum și ex vivo; la aceasta s-a adăugat 0,5% carbopol 934, rezultând NEIG2, care prezintă valori de cedare și permeabilitate comparabile cu F15, cu un timp de rezidență mai mare, ce depășește clearance-ul fiziologic nazal normal. În cele din urmă, LAS sub formă de NEIG2 a fost supus unui studiu in vivo, fiind considerat o formulă nouă intranazală promițătoare, care exercită un debut rapid al acțiunii (Tmax de 0,75 ore) însoțit de o biodisponibilitate mai mare (de 2,5 ori) și o permeabilitate tisulară (de 4 ori) în compa...

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Section: Productive Of Pseudo-ternary Phase Diagramsmentioning

confidence: 99%

Section: Parameters Involved In Pharmacokineticsmentioning

confidence: 99%

Lasmiditan Nanoemulsion Based in Situ Gel Intranasal Dosage Form: Formulation, Characterization and in Vivo Study

JABER

2023

FARMACIA

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“…Tables 1 and 2 shows the Oil: surfactant and Oil: Smix ratios analyzed. 6 The system with the highest %transmittance was considered for further development of formulation.…”

Section: Phase Diagram (Pseudo Ternary)mentioning

confidence: 99%

Microemulgel Delivery of Ciprofloxacin Hydrochloride

Torambe,

Chabukswar1,

Dhamane

et al. 2023

IJDDT

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Background: Ciprofloxacin hydrochloride is broad spectrum carboxyfluoroquinolone antibiotic from biopharmaceutics classification system (BCS) class IV. The oral dosage form exhibits gastric irritation whereas the topical cream has demonstrated poor penetration and low bioavailability. Objective: To optimize microemulsion-based gel of ciprofloxacin hydrochloride to increase its solubility and permeability through the cutaneous layer for targeting bacterial skin infections. Methods: To develop microemulsion, oil (soya oil, castor oil, oleic acid, isopropyl myristate and vegetable oil), surfactant (cremophore, span 80, tween 80) and cosurfactant (PEG 600 and PEG 400, propylene glycol) were evaluated. To depict the microemulsion formulation pseudo ternary phase diagram was employed. %Transmittance, zeta potential, dissolution study and size analysis were carried out for evaluation of microemulsion. 32 factorial design was used. Two variables i.e concentration of Sepineo P600 and Carbopol 934 effect on microemulgel was evaluated. Evaluation of gel was carried for physical parameters, antimicrobial, in-vitro and ex-vivo release study. Results: Solubility analysis suggested tween 80, oleic acid and propylene glycol for the formulation of microemulsion. Zeta potential for microemulsion batch F1 was -11.3 mV. This indicated good stability. In-vitro release study showed 91.98% percentage cumulative drug release for batch F1 at 8 hours. Microemulsion-based gel (F1) showed 22.96% inhibition against bacteria which proved its antibacterial activity. Conclusion: The obtained results exhibited that the permeability and bioavailability of the drug was increased when given through a topical route.

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Preparation, In-vitro, Ex-vivo, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based In Situ Gel

Jabir,

Rajab

2025

PNT

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background: 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%. objective: 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. method: Two successfully prepared nanoemulsion (NE) formulas, a and b, were selected for the incorporation of different percentages of pH-sensitive in situ gelling polymer (Carbopol 934) to prepare NEIGs 1, 2, 3, 4, 5, and 6. The pH, gelation capacity, gel strength, and viscosity were predicted for the prepared NEIGs. The release (in vitro) and the nasal permeation (ex vivo) were determined for NEIG 2 and 5, and then both were subjected to pharmacokinetics in vivo studies. Eighteen male rabbits weighing 2.0 to 2.5 kg were employed in the parallel design study. The body surface area (BSA) normalization method was applied for LAS dose calculation. Serial blood samples were taken out and subjected to drug analysis using the HPLC method previously developed and validated by L. Santosh Kumar. Primary pharmacokinetics parameters, including maximum drug concentration in plasma (Cmax), time to reach C-max (T-max), and area under the concentration-time curve from time zero to affinity (AUCt0-∞) were calculated. Both NE (a and b), together with NEIG (2 and 5) formulas, were subjected to the stability study. Finally, a nasal ciliotoxicity study was carried out to evaluate the nasal toxicity of developed NEIGs 2 and 5. result: The results showed that NEIGs 2 and 5 could be selected as the optimized NEIGs as both achieved 100% permeation within 20 min and then released within 25 and 35 min, respectively, thus achieving 3.3 folds with higher permeation percentages as compared to the AQS. Both NEIGs 2 and 5 exerted comparable release and permeation values as the corresponding NE a and b with more residence time in order to overcome the normal nasal physiological clearance. The values of C-max, Tmax, and AUC0- ∞ for NEIG 2 and NEIG 5 were 8066±242 ng/ml, 0.75±0.05 h, 19616.86±589 ng. h/ml, and 7975.67±239 ng/ml, 1.0±0.05 h, 17912.36±537 ng. h/ml, respectively, compared to the traditional AQS, which is equal to 4181.09±125 ng/ml, 2±0.2 h, and 8852.27±266 ng. h/ml, respectively. It was discovered that NEIGs 2 and 5 had better intranasal delivery of LAS and could significantly (p<0.05) achieve a higher value of permeability coefficient (3.3 folds) and 2.5 folds improvement in bioavailability when compared to AQS. The NE a, NE b, NEIG2, and NEIG5 formulations showed good stability at various temperatures. According to the nasal ciliotoxicity study, the nasal mucosal membrane, which was treated with NEIG 5, showed irritation with a bit of damage. However, damage was not observed when it was treated with NEIG 2, indicating the biocompatibility of the last one to be selected as the optimum formula. conclusion: NEIG 2 and NEIG 5 are promising new intranasal formulas with a faster onset of action and greater bioavailability than the oral dosage form (AQS). Finally, the selected optimum gold formula that will be ready for further clinical study is NEIG 2.

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Optimization and Solubilization Study of Nanoemulsion Budesonide and Constructing Pseudoternary Phase Diagram

Cited by 5 publications

References 7 publications

Lasmiditan Nanoemulsion Based in Situ Gel Intranasal Dosage Form: Formulation, Characterization and in Vivo Study

Lasmiditan Nanoemulsion Based in Situ Gel Intranasal Dosage Form: Formulation, Characterization and in Vivo Study

Microemulgel Delivery of Ciprofloxacin Hydrochloride

Preparation, In-vitro, Ex-vivo, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based In Situ Gel

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