Artemether Loaded Ethylcellulose Nanosuspensions: Effects of Formulation Variables, Physical Stability and Drug Release Profile

Khalifa, Nasrin E.; Nur, Abubakr O.; Osman, Zuheir

doi:10.22159/ijpps.2017v9i6.18321

Cited by 3 publications

(1 citation statement)

References 18 publications

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“…Nanosuspensions are a well-established method for producing nanoparticles, with their impact on improving the dissolution of drugs with poor water solubility has been extensively investigated in research [7]. Achieving effective intranasal drug delivery requires maintaining the drug within the nasal cavity for sufficient absorption while preventing dripping or reaching the throat [8].…”

Section: Introductionmentioning

confidence: 99%

Enhancing Nose- To- Brain Delivery of Piribedil: Development of a Nanosuspension Dispersed in Nasal in-Situ Gelling System

BHARGAVI,

RAGHUVEER

2024

Int J App Pharm

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Objective: This study focuses on improving the delivery of Piribedil, a poorly soluble drug, to the brain through the nasal route using a nanosuspension in a nasal in-situ gel. Methods: The nanosuspension was prepared using the sonoprecipitation method. Quality-by-Design (QbD) principles were used to optimize both the formulation and process parameters. The optimal process parameters were determined as sonication time (7.09 min), sonication amplitude (83.44%), and infusion rate (2.41 mL/min) with a desirability value of 0.970. Results: The nanosuspension exhibited an average particle size ranging from 46.7 nm to 50.1 nm, and polydispersity index values between 0.393 and 0.425. Zeta potential values ranged from -33.78 ± 1.86 mV to -35.06 ± 2.12 mV, indicating favorable stability. FTIR studies revealed molecular interactions between Piribedil and stabilizers. XRPD and DSC analyses showed the transition from a crystalline to an amorphous state in the nanosuspension. Dissolution studies demonstrated significantly accelerated dissolution for the Piribedil nanosuspension, attributed to its nanosize and improved wettability. Stability assessments confirmed the robustness of the nanosuspension. Conclusion: This innovative approach offers potential solutions for drug solubility challenges and blood-brain barrier penetration, holding promise for effective brain-targeted treatments.

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Section: Introductionmentioning

confidence: 99%

Enhancing Nose- To- Brain Delivery of Piribedil: Development of a Nanosuspension Dispersed in Nasal in-Situ Gelling System

BHARGAVI,

RAGHUVEER

2024

Int J App Pharm

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A comparative study of oregano (Origanum vulgare L.) essential oil-based polycaprolactone nanocapsules/ microspheres: Preparation, physicochemical characterization, and storage stability

Fraj

Jaafar

Martı́

et al. 2019

Industrial Crops and Products

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Fabrication of Nanosuspension Directly Loaded Fast-Dissolving Films for Enhanced Oral Bioavailability of Olmesartan Medoxomil: In Vitro Characterization and Pharmacokinetic Evaluation in Healthy Human Volunteers

2018

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Olmesartan medoxomil (OM) is an antihypertensive drug with poor water solubility and low oral bioavailability (28.6%). Accordingly, this study aimed to formulate and evaluate OM nanosuspension incorporated into oral fast-dissolving films (FDFs) for bioavailability enhancement. OM nanosuspension was prepared by antisolvent-precipitation-ultrasonication method and characterized regarding particle size (122.67 ± 5.03 nm), span value (1.40 ± 0.51), and zeta potential (- 46.56 ± 1.20 mV). Transmission electron microscopy (TEM) of the nanosuspension showed spherical non-aggregating nanoparticles. The nanosuspension was then directly loaded into FDFs by solvent casting technique. A full factorial design (2 × 3) was implemented for optimization of the FDFs using Design-Expert® software. Physical and mechanical characteristics in addition to dissolution profiles of the FDFs were investigated. The optimum formula (FDF1) showed 0.43 ± 0.02 kg/mm tensile strength, 20.50 ± 2.12 s disintegration time, and 87.53 ± 2.50 and 95.99 ± 0.25% OM dissolved after 6 and 10 min, respectively. Accelerated and long-term shelf stability studies confirmed the stability of FDF1. More than 75% OM was dissolved within 10 min from FDF1 compared with 9.80 and 47.80% for films prepared using coarse drug powder and market tablet, respectively. Relative bioavailability of FDF1 compared to market tablet was assessed in healthy human volunteers. The C value increased significantly from 66.62 ± 14.95 to 179.28 ± 23.96 ng/mL for market tablet and FDF1, respectively. Similarly, the AUC value significantly increased from 498.36 ± 217.46 to 1083.67 ± 246.32 ng h/mL for market tablet and FDF1, respectively. Relative bioavailability of FDF1 was 209.28%. The highlighted results verified the effectiveness of OM nanosuspension-loaded FDFs in improving OM bioavailability.

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Artemether Loaded Ethylcellulose Nanosuspensions: Effects of Formulation Variables, Physical Stability and Drug Release Profile

Cited by 3 publications

References 18 publications

Enhancing Nose- To- Brain Delivery of Piribedil: Development of a Nanosuspension Dispersed in Nasal in-Situ Gelling System

Enhancing Nose- To- Brain Delivery of Piribedil: Development of a Nanosuspension Dispersed in Nasal in-Situ Gelling System

A comparative study of oregano (Origanum vulgare L.) essential oil-based polycaprolactone nanocapsules/ microspheres: Preparation, physicochemical characterization, and storage stability

Fabrication of Nanosuspension Directly Loaded Fast-Dissolving Films for Enhanced Oral Bioavailability of Olmesartan Medoxomil: In Vitro Characterization and Pharmacokinetic Evaluation in Healthy Human Volunteers

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