article · Pharmaceutical Development and Technology
This research investigated hybrid nanoparticles made from sucrose acetate isobutyrate (SAIB) and glyceryl monooleate (GMO) to improve the bioavailability of the drug rivaroxaban. Formulations were created using a modified melt dispersion technique with varied ratios of GMO, SAIB, and rivaroxaban, alongside a fixed ratio of poloxamer 407. Particle size, polydispersity index, zeta potential, and encapsulation efficiency were measured to identify an optimal formulation. The chosen formulation, designated L4, was freeze-dried and assessed through structural characterisation, dissolution testing, and pharmacokinetic evaluation. In laboratory comparisons against commercial Xarelto tablets, L4 tablets demonstrated superior dissolution parameters. In pharmacokinetic testing, the L4 formulation achieved higher maximum drug concentration and nearly doubled the total drug exposure compared to the commercial tablet. The findings show that GMO and SAIB co-formers enhance rivaroxaban bioavailability.
Poor drug solubility and low bioavailability often restrict the effectiveness of oral medications. By using lipid and sucrose-based hybrid nanoparticles, this work demonstrates a method to increase the absorption and circulating levels of rivaroxaban. Improving drug uptake can potentially lead to more reliable oral formulations that deliver therapeutic benefits more effectively than existing commercial alternatives.
This work is relevant to pharmaceutical manufacturers seeking to reformulate poorly soluble oral therapies like rivaroxaban. The technology is applied and tested in laboratory dissolution and pharmacokinetic models, showing clear performance gains over commercial tablets. However, the abstract notes that further research is required to enhance formulation effectiveness, placing the technology at an intermediate developmental stage prior to formal clinical evaluation or scaled manufacturing.
AI-generated from the published abstract. Always read the original work before citing.
This study aims to improve the RXB bioavailability using hybrid nanoparticles. A modified melt dispersion technique created different formulas with varying GMO-SAIB: RXB and GMO: SAIB ratios, with fixed GMO-SAIB: poloxamer 407 ratios. The PS, PDI, ZP, and EE were measured to determine the optimal formula, which was selected using Design-Expert™ software. The optimized formula was lyophilized and tested for PS, PDI, ZP, and EE. The chosen lyophilized formula (L4) was characterized using FTIR, DSC, PXRD, dissolution studies, and pharmacokinetics studies. The study found correlations between variables and identified how GMO-SAIB concentration affects drug encapsulation. The dissolution parameters were calculated, including % Q5 and % DE). The % Q5 values were 68.4 ± 1.7% and 89.7 ± 3.6% for Xarelto and L4 tablets, respectively. The % DE values were 89.7 ± 0.4% and 97.5 ± 2.1% for Xarelto and L4 tablets, respectively. The AUC values were 2117.0 ng.h/mL (±77.3) and 3919.4 ng.h/mL (±134.8) for Xarelto and L4 tablets, respectively. The Cmax values were 241.3 ng/mL (±21.0) and 521.5 ng/mL (±91.5) for Xarelto and L4 tablets, respectively. In conclusion, the study found that using GMO-SAIB as co-formers effectively enhanced the bioavailability of RXB. The authors recommend using the hybrid nanoparticles technique and suggest further research to enhance its effectiveness for drug delivery.
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DOI: 10.1080/10837450.2023.2274944
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