Comparison of the physicochemical properties, aqueous solubility, and oral bioavailability of rivaroxaban-loaded high-pressure homogenised and Shirasu porous glass membrane emulsified solid self-nanoemulsifying drug delivery systems

Woo

et al. 2022

IJMS

Self Cite

The purpose of this study was to investigate the efficacy of hydrophilic polymers in a solid dispersion formulation in improving the solubility and dissolution rate of rivaroxaban (RXB), a poorly soluble drug. The developed solid dispersion consisted of two components, a drug and a polymer, and the drug was dispersed as amorphous particles in a polymer matrix using the spray drying method. Polymeric solid dispersions were evaluated using solubility tests, in vitro dissolution tests, powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and particle size distribution analysis. To maximize physical stability against crystallization and improve the solubility and dissolution of RXB, it is important to select the appropriate polymer type and the optimal ratio of the polymer to the drug. The optimized polyvinyl alcohol (PVA)-based (1/0.5, w/w) and gelatin-based (1/5, w/w) solid dispersion formulations showed 6.3 and 3.6 times higher drug solubilities than pure RXB powder, respectively, and the final dissolution rate was improved by approximately 1.5 times. Scanning electron microscopy and particle size distribution analyses confirmed that the gelatin-based solid dispersion was smaller and more spherical than the PVA-based solid dispersion, suggesting that the gelatin-based solid dispersion had a faster initial dissolution rate. Differential scanning calorimetry and powder X-ray diffraction analyses confirmed that RXB had successfully changed from a crystalline form to an amorphous form, contributing to the improvement in its solubility and dissolution rate. This study provides a strategy for selecting suitable polymers for the development of amorphous polymer solid dispersions that can overcome precipitation during dissolution and stabilization of the amorphous state. In addition, the selected polymer solid dispersion improved the drug solubility and dissolution rate of RXB, a poorly soluble drug, and may be used as a promising drug delivery system.

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Effects of Polymers on the Drug Solubility and Dissolution Enhancement of Poorly Water-Soluble Rivaroxaban

Woo

et al. 2022

IJMS

Self Cite

“…To compare the impact of various solidifying agents on drug bioavailability, SNEDDS was suspended with two mesoporous carriers, calcium silicate and colloidal silica. The results demonstrated that SNEDDS with calcium silicate showed a higher released rate than SNEDDS with colloidal silica, with oral bioavailability exhibiting a 3.2-fold increase in the AUC value (p<0.05) of rivaroxaban-loaded solid SNEDDS being significantly higher than that of pure drug powder [25]. The biopharmaceutics classification system (BCS) classifies abiraterone acetate (AbA) as a Class IV chemical because of its extremely low water solubility (0.5 g/ml), low permeability, and high lipophilicity.…”

Section: Silica Nanoparticlesmentioning

confidence: 94%

Nano-Delivery Systems for Enhancing Oral Bioavailability of Drugs

Abdellatif

AHMED²,

El-Nabarawi³

et al. 2023

Int J App Pharm

The two main issues impacting oral delivery are drug solubility and permeability. The FDA adopted the Biopharmaceutics Classification System (BCS) in 2000. The BCS categorizes drugs into four classes based on their solubility and permeability. For permeability improvement and bioavailability, many experimental systems are utilized. Numerous nanocarrier technologies have recently been utilized to increase drug permeability by employing nanocarrier systems such as lipid vesicles, polymeric and lipid nanoparticles, polymeric micelles, and submicron lipid emulsions. This review proposes innovative nano-delivery systems for permeability augmentation. It focuses on some illustrations of drugs with various nanosystems, how these systems were developed, and how they successfully boost intestinal drug permeability and bioavailability.

“…Selected oil and Smix ratio was taken for further preparation of S-SEDDS. Preparation of S-SEDDS [22][23][24] : Ciprofloxacin drug was solubilized in oil phase and then added in that Tween 20 and Span 80 mixtures (Smix) and methanol as co-solvent with titration method. That mixture was mixed properly to get emulsion formed by the cyclo mixer.…”

Section: Methodmentioning

confidence: 99%

Untitled

2022

IJPSR

The purpose is to formulate the solid self emulsifying drug delivery system (S-SEDDS) to improve poor aqueous solubility and dissolution of ciprofloxacin. A solubility study was carried out, and then Soyabean oil (as oil phase), Tween 20 (as surfactant), and Span 80 (as co-surfactant) were selected for preparation of emulsion by titration method. Adsorption to solid carrier technique was used for solid SEDDS, areosil (Colloidal silica) used as adsorbent. In that formulation, I was having carbopol 934 and another formulation II HPMC K 4 M. The flow properties of all formulation were within the acceptable range; therefore, they can be easily filled into capsule. IR spectral and DSC thermograph analysis showed that there was chemical interaction between drug and polymer. In-vitro release studies were carried out in phosphate buffer pH 7.4. Release profile of pure drug formulation showed 38%, formulation I showed highest 54% cumulative drug release and formulation II showed lowest i.e. 14% drug release. Student's t-test was determined for In-vitro drug release data for different polymeric formulations and showed a p-value of 0.001891 (<0.01) 99.99% significant.