A comprehensive study of the basic formulation of supersaturated self-nanoemulsifying drug delivery systems (SNEDDS) of albendazolum

Alothaid, Hani; Aldughaim, Mohammed S.; Yusuf, Azeez; Yezdani, Umama; Alhazmi, Alaa; Habibullah, Mahmoud M.; Khan, Mohammad Gayoor

doi:10.1080/10717544.2021.1986601

Cited by 12 publications

(11 citation statements)

References 43 publications

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“…The samples were stored at −20℃ in the refrigerator for 48 h, and then stored at 25℃ in a water bath for another 48 h. 43 Those IVA-SNEDDS which showed good performance in accelerated physical stability experiments, with no phase separation, drug precipitation or any droplet size as well as PDI (polymer dispersity index) changes were used for further studies on self-emulsification efficiency. 44 …”

Section: Methodsmentioning

confidence: 99%

Reduced the Food Effect and Enhanced the Oral Bioavailability of Ivacaftor by Self-Nanoemulsifying Drug Delivery System (SNEDDS) Using a New Oil Phase

Miao¹,

Song²,

Zuo³

et al. 2022

DDDT

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Purpose The purpose of this work was to develop an ivacaftor self-nanoemulsion drug delivery system (IVA-SNEDDS) using the newly developed double headed miscellaneous lipid (DHML) as oil phase to reduce the food effect and inter-individual absorption variability of IVA. Methods The lipids with the greatest solubility to IVA were selected as the oil phase of IVA-SNEDDS by saturation solubility method. Then, among different surfactants and co-surfactants, those with good emulsifying ability for the selected oil phase were selected, and the proportion of surfactant and co-surfactant was further selected by pseudo-ternary phase diagram. The prepared IVA-SNEDDS were screened and evaluated in vitro and in beagle dogs. Results The optimized IVA-SNEDDS formulation consisting of DHML, Tween 80, and Transcutol HP with the weight ratio of 2:2:1 was physically stable and it was easy to disperse in water, pH 1.2 hydrochloric acid and pH 6.8 phosphate buffer solution, and generated a fine homogeneous nanoemulsion, with mean globule size less than 75 nm regardless of dilution ratio. In vitro drug release studies showed that the drug in IVA-SNEDDS could be completely released in a short time, while the drug release in IVA-suspension was less than 1% at 60 min. In vivo, using IVA-suspension (Fed) as a reference, the relative oral bioavailability of IVA-suspension (Fasted), IVA-SNEDDS (Fasted), and IVA-SNEDDS (Fed) were 23.35%, 153.63%, and 149.89%, respectively. This showed that IVA-SNEDDS could eliminate the positive food effect, improve the oral bioavailability, and reduce the IVA absorption difference between individuals. Conclusion As the oil phase of SNEDDS, DHML can significantly improve the drug solubility and drug loading of IVA-SNEDDS. Moreover, DHML was easily emulsified and can effectively form a nanoemulsion in vivo and in vitro. The prepared IVA-SNEDDS can reduce the inter-individual absorption variability of IVA, eliminate its food effect and improve its oral bioavailability.

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Section: Methodsmentioning

confidence: 99%

Reduced the Food Effect and Enhanced the Oral Bioavailability of Ivacaftor by Self-Nanoemulsifying Drug Delivery System (SNEDDS) Using a New Oil Phase

Miao¹,

Song²,

Zuo³

et al. 2022

DDDT

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“…System settings regarding sample name, dispersing media, and gate time were set up using the software. Subsequently, "Start Measurement" was clicked to start the analysis process [25].…”

Section: Analysis Using Particle Size Analyzer (Psa)mentioning

confidence: 99%

Modifying Fraction Extracted From Sesewanua (Clerodendrum Fragrans Wild) Leaves in Snedds Preparations: Characterization and Bioavailability Test

SAPIUN,

IMRAN,

ASWAD

et al. 2024

Int J App Pharm

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Objective: This study aimed to determine the effect of compound modification using acyl chloride derivatives on n-hexane: ethyl acetate fraction of sesewanua leaves, focusing on the characteristics and pharmacokinetics profile in Self-Nano-emulsifying Drug Delivery System (SNEDDS) preparations. Methods: A quasi-experimental method was used with six SNEDDS formulas, namely F0 (without active substance), F1 (acetyl chloride fraction), F2 (propanoyl chloride fraction), F3 (butyryl chloride fraction), and F4 (pentanoyl chloride fraction) and F5 (piperine compound). The fractions were subjected to characterization tests, including particle size, polydispersity index, and zeta potential as well as determination of pharmacokinetics profile using the modified crane and Wilson method. Results: The results showed that the characterization tests of particle size using Particle Size Analyzer (PSA) for F0-F5 on gastric fluid included 15.8, 17,367, 20,367, 15.8, 28.233, and 21.533 nm. The polydispersity index values were 0.211, 0.438, 0.311, 0.383, 0.394, and 0.397, while the Zeta Potential values were-22,267,-22.2,-23.5,-24,033,-22,967, and-21.6 mV, respectively. The pharmacokinetics profile of AUC0-∞ was as follows: F0 0 μg, F1 492.83, F2 492.83, F3 245.98, F4 492.94, and F5 843.38 μg. Fraction five (F5) as a control had a higher AUC0-∞ value than compared to the fractions modified with acyl chloride derivatives. The T1/2 elimination values were F0 0 h, F1 22.5 h, F2 10.811 h, F3 35.54 h, F4 231.01 h, and F5 15.469 h. Conclusion: Based on the results, the addition of acetyl, propanoyl, butyryl, and penthanoyl chloride affected Particle Size Characterization Analysis and pharmacokinetics profile of SNEDDS preparation of n-hexane: ethyl acetate fraction. Structural modification showed the ability to alter the bioavailability of the active ingredient according to the desired therapeutic goal.

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“…Phase diagrams were drawn using the OriginLab program. With one apex representing the water, one representing the oil, and one representing Smix at a fixed weight ratio, the shaded area was believed to be a visually clear area in a triangle plot (12) .…”

Section: Pseudo-ternary Phase Diagrams Studymentioning

confidence: 99%

Design, Optimization and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Bilastine

Abbas,

Shaimaa Nazar Abd-AlHammid

2023

IJPS

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Self-nanoemulsifying drug delivery systems are innovative methods that have the potential to resolve a variety of drug formulation issues, including solubility, stability and bioavailability. Bilastine is a potent and highly selective H1-antihistamine. The aim of this study is to develop bilastine as an oral self-nanoemulsion to enhance its permeability from prepared formulas and possibility of lymphatic transport. Based on the solubility investigations of bilastine in some oils, surfactants and cosurfactants, fifteen formulae of liquid SNEDDS were created utilizing oleic acid, tween 60 and transcutol as oil, surfactant and co-surfactant respectively. Pseudoternary phase diagrams were used to evaluate the component phase behavior and the area of the nanoemulsion. The prepared formulas were evaluated for particle size, polydispersity index, zetapotential, self-emulsification time, drug content, and robustness to dilution. When compared to the pure drug powder, the produced SMEDDS formulations showed enhanced drug release. This study's findings showed that a formula 8 with a 20% oleic acid, 40% tween 60, and 40% transcutol composition exhibited lower particle size and higher zetapotential with acceptable drug content compared to other formulas and better in-vitro drug release characteristics than pure bilastine powder. All of these criteria favor the development of self-nano emulsifying drug delivery systems as a potential approach to enhance the bioavailability of drugs like bilastine that are poorly soluble. Keywords: Bilastine, SNEDDS

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A comprehensive study of the basic formulation of supersaturated self-nanoemulsifying drug delivery systems (SNEDDS) of albendazolum

Cited by 12 publications

References 43 publications

Reduced the Food Effect and Enhanced the Oral Bioavailability of Ivacaftor by Self-Nanoemulsifying Drug Delivery System (SNEDDS) Using a New Oil Phase

Reduced the Food Effect and Enhanced the Oral Bioavailability of Ivacaftor by Self-Nanoemulsifying Drug Delivery System (SNEDDS) Using a New Oil Phase

Modifying Fraction Extracted From Sesewanua (Clerodendrum Fragrans Wild) Leaves in Snedds Preparations: Characterization and Bioavailability Test

Design, Optimization and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Bilastine

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