Development of a Solid Supersaturable Micelle of Revaprazan for Improved Dissolution and Oral Bioavailability Using Box-Behnken Design

Goo, Yoon Tae; Sa, Cheol-Ki; Choi, Ji Yeh; Kim, Min Song; Kim, Chang‐Hyun; Kim, Hyeon Kyun; Choi, Young Wook

doi:10.2147/ijn.s298450

Cited by 15 publications

(2 citation statements)

References 54 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Based on Table 3, the observed and predicted values were in good agreement, indicating the validity of the model. This was also confirmed by the low (< 5%) prediction error (58,59), calculated by comparing the observed and predicted values (Prediction (error% = observed value − predicted value predicted value × 100 ) (60). It must be mentioned that the milling time used to prepare the optimized formulation was about 18-fold less than that of the previous study (23).…”

Section: Discussionsupporting

confidence: 60%

The Impact of Process and Formulation Parameters on the Fabrication of Efavirenz Nanosuspension to Improve Drug Solubility and Dissolution

2022

View full text Add to dashboard Cite

Background: Efavirenz nanosuspensions (EZ-NSs) were developed by the wet milling method as the most promising top-down nanosizing technique. Different process and formulation parameters were studied and optimized to produce appropriate EZ-NS in suitable conditions to enhance drug dissolution. Methods: In the preliminary studies, various polymeric stabilizers, including Pluronic F68, sodium carboxymethylcellulose (CMC), hydroxypropyl methylcellulose (HPMC), and polyvinyl alcohol (PVA), as well as different sizes and weight of milling beads were used to prepare NSs. The effect of sodium lauryl sulfate (SLS) concentration on the NS properties was also evaluated. The influence of other formulation and process parameters, including polymer concentration, milling speed, and milling time, on the particle size and distribution of NSs were investigated using Box-Behnken design. The optimized freeze-dried nanosuspension was characterized by redispersibility, physicochemical properties, and stability. Results: A combination of PVA and SLS was selected as steric and electrostatic stabilizers. The optimum EZ-NS displayed a uniform size distribution with mean particle size and zeta potential of 254.4 nm and 21.1 mV, respectively. The solidified nanosuspension was well redispersed to the original nanoparticles. Significantly enhanced aqueous solubility (about 11-fold) and accelerated dissolution rate were observed for the optimized formulation. This could be attributed to the reduced particle size and partial amorphization of EZ during the preparation process, studied by X-ray diffraction. Accelerated studies confirmed the stability of the optimum freeze-dried formulation over the examined period of three months. Conclusions: Optimization of different variables led to the formation of EZ-NSs with desired properties through wet milling in a very short time compared to the previous study and therefore reduced production costs. This formulation seems to be a suitable approach for solubility and dissolution enhancement of EZ and may have great potential to improve the drug's oral bioavailability.

show abstract

Section: Discussionsupporting

confidence: 60%

The Impact of Process and Formulation Parameters on the Fabrication of Efavirenz Nanosuspension to Improve Drug Solubility and Dissolution

2022

View full text Add to dashboard Cite

show abstract

“…The intrinsic dissolution rate can be improved by identifying the solid-state of the compound in terms of salts formation, anhydrous form or polymorph or cocrystals, and or by improving the solubility using novel formulation strategies like solid dispersion or inclusion complexation, and or by optimizing the particle size 6 . Super saturable solid micelles using surfactant and solid carriers can also be used to improve the dissolution and oral bioavailability 7 .…”

Section: Introductionmentioning

confidence: 99%

A Brief Review on Pharmaceutical Dissolution Interlinking the Aspects of Science and Regulation

Rangarao¹,

Monica²,

Bhattacharyya³

2022

Bulletin of Pharmaceutical Sciences. Assiut

View full text Add to dashboard Cite

Dissolution is a multistep process describes the affinity of the solute and the solvent by which a solid substance interacts among the heterogeneous phases of solute -solute, solventsolvent, and the solute-solvent interface to yield a solution. In the pharmaceutical industry dissolution testing of solid dosage form gives a signal of the operability of the dosage form in the biological system. The rate of absorption is partially or completely controlled by the dissolution of the drug from its dosage forms in the gastrointestinal tract. Dissolution, the vital quality control aspects, also ensure batch-to-batch uniformity in drug release, bioavailability, and the development of efficacious therapeutic dosage forms. It also ensures the evaluation of their critical biopharmaceutical parameters. Hence the study of dissolution is an interplay between the science and the development of the regulatory profile of a dosage form for quality control aspects. The present review focuses on the science, factors relevant to in-vitro dissolution, and therefore the role of its in pharmaceutical regulation.

show abstract

Toward mechanical recyclability of high barrier food packaging films through filler incorporation on the EVOH layer

Barros,

Azevedo,

Cerqueira

et al. 2024

J of Applied Polymer Sci

View full text Add to dashboard Cite

To preserve food from moisture and oxygen, polymers, such as ethylene vinyl alcohol (EVOH) are used in multilayer structures to provide oxygen barrier, while low‐density polyethylene (LDPE) is used for a water vapor barrier. While this material combination is functionally ideal, it may not comply with the new packaging recycling guidelines. Some European markets have implemented rules that limit the weight percentage of EVOH in LDPE films. One way to increase recyclability is by reducing the amount of EVOH in the film structure while maintaining the packaging's oxygen barrier properties. To achieve this, it is necessary to improve the barrier properties of EVOH. With this objective in mind, this study evaluated the incorporation of nanoclays (NC), cellulose microcrystals (MCC), silicon dioxide nanoparticles (SiO2), and cellulose nanocrystals (CNC) into an EVOH matrix. The results indicate that NC and MCC facilitate a stable blown film extrusion process and have a better dispersion in the EVOH matrix. Based on this finding, three‐layer films (with an ABA configuration) consisting of LDPE (A) and EVOH (7 μm layer) with 0.5 or 1 wt.% MCC or NC (B) were produced to protect the EVOH from moisture and enable blown film processing. The oxygen transmission rate (OTR) values were lowest for 0.5 wt.% NC and 1 wt.% MCC incorporation. Although the films with micro and nanoparticles had increased haze, this did not affect the visibility of the packaged food.

show abstract

Development of a Solid Supersaturable Micelle of Revaprazan for Improved Dissolution and Oral Bioavailability Using Box-Behnken Design

Cited by 15 publications

References 54 publications

The Impact of Process and Formulation Parameters on the Fabrication of Efavirenz Nanosuspension to Improve Drug Solubility and Dissolution

The Impact of Process and Formulation Parameters on the Fabrication of Efavirenz Nanosuspension to Improve Drug Solubility and Dissolution

A Brief Review on Pharmaceutical Dissolution Interlinking the Aspects of Science and Regulation

Toward mechanical recyclability of high barrier food packaging films through filler incorporation on the EVOH layer

Contact Info

Product

Resources

About