Abstract:Sinapic acid (SA) is a poorly water-soluble substance which could result in poor bioavailability. The aim of this study was to determine the “hydroxypropyl β-cyclodextrin (HPβCD)” solubilization of SA in the presence of the auxiliary substance hydroxypropyl methylcellulose (HPMC) and to evaluate the ternary inclusion complex prepared by microwave technology. Phase-solubility profiles showed that HPβCD exhibited the greatest solubilizing effect on SA in the presence of HPMC. The enhanced rate of SA dissolution … Show more
“… 25 , 32 The slope value was smaller than 1, which denotes an inclusion complex with molecules in a 1:1 molar ratio (BRA: βCD). 26 The apparent stability constant, K1:1, was found to be 119.06 M −1 . Therefore, it can be said that BAR and βCD formed a stable inclusion complex at a 1:1 molar ratio.…”
Section: Resultsmentioning
confidence: 95%
“…These interaction with BAR were established by the cavity of βCD through intermolecular forces, confirming BAR’s incorporation inside the cavity of –CD. 26 Figure 1 Phase solubility plot of βCD and BAR. …”
Section: Resultsmentioning
confidence: 99%
“…The stability constant (K) and complexation efficiency (CE) of the combination including BAR/βCD were determined using a phase solubility analysis. Briefly, an excess quantity of BAR was dispersed into aqueous solution containing βCD (0–50 mM), and conical flasks were shaken at 25°C, 100 rpm for 72 h. 26 The supernatant of the samples were carefully collected and filtered (0.45 µm), and the filtrate was diluted and analysed by UV- spectrophotometer at 224 nm (Jasco V-630 Made in Japan). 27 The stability constant (Kc) was calculated from the phase solubility plot using following equations: 26 …”
Background:The aim of the present investigation is to prepare baricitinib (BAR)-loaded diphenyl carbonate (DPC) β-cyclodextrin (βCD) based nanosponges (NSs) to improve the oral bioavailability. Methods: BAR-loaded DPC-crosslinked βCD NSs (B-DCNs) were prepared prepared by varying the molar ratio of βCD: DPC (1:1.5 to 1:6). The developed B-DCNs loaded with BAR were characterized for particle size, polydispersity index (PDI), zeta potential (ZP), % yield and percent entrapment efficiency (%EE). Results: Based on the above evaluations, BAR-loaded DPC βCD NSs (B-CDN3) was optimized with mean size (345.8±4.7 nm), PDI (0.335±0.005), Yield (91.46±7.4%) and EE (79.1±1.6%). The optimized NSs (B-CDN3) was further confirmed by SEM, spectral analysis, BET analysis, in vitro release and pharmacokinetic studies. The optimized NSs (B-CDN3) showed 2.13 times enhancement in bioavailability in comparison to pure BAR suspension. Conclusion: It could be anticipated that NSs loaded with BAR as a promising tool for release and bioavailability for the treatment of rheumatic arthritis and Covid-19.
“… 25 , 32 The slope value was smaller than 1, which denotes an inclusion complex with molecules in a 1:1 molar ratio (BRA: βCD). 26 The apparent stability constant, K1:1, was found to be 119.06 M −1 . Therefore, it can be said that BAR and βCD formed a stable inclusion complex at a 1:1 molar ratio.…”
Section: Resultsmentioning
confidence: 95%
“…These interaction with BAR were established by the cavity of βCD through intermolecular forces, confirming BAR’s incorporation inside the cavity of –CD. 26 Figure 1 Phase solubility plot of βCD and BAR. …”
Section: Resultsmentioning
confidence: 99%
“…The stability constant (K) and complexation efficiency (CE) of the combination including BAR/βCD were determined using a phase solubility analysis. Briefly, an excess quantity of BAR was dispersed into aqueous solution containing βCD (0–50 mM), and conical flasks were shaken at 25°C, 100 rpm for 72 h. 26 The supernatant of the samples were carefully collected and filtered (0.45 µm), and the filtrate was diluted and analysed by UV- spectrophotometer at 224 nm (Jasco V-630 Made in Japan). 27 The stability constant (Kc) was calculated from the phase solubility plot using following equations: 26 …”
Background:The aim of the present investigation is to prepare baricitinib (BAR)-loaded diphenyl carbonate (DPC) β-cyclodextrin (βCD) based nanosponges (NSs) to improve the oral bioavailability. Methods: BAR-loaded DPC-crosslinked βCD NSs (B-DCNs) were prepared prepared by varying the molar ratio of βCD: DPC (1:1.5 to 1:6). The developed B-DCNs loaded with BAR were characterized for particle size, polydispersity index (PDI), zeta potential (ZP), % yield and percent entrapment efficiency (%EE). Results: Based on the above evaluations, BAR-loaded DPC βCD NSs (B-CDN3) was optimized with mean size (345.8±4.7 nm), PDI (0.335±0.005), Yield (91.46±7.4%) and EE (79.1±1.6%). The optimized NSs (B-CDN3) was further confirmed by SEM, spectral analysis, BET analysis, in vitro release and pharmacokinetic studies. The optimized NSs (B-CDN3) showed 2.13 times enhancement in bioavailability in comparison to pure BAR suspension. Conclusion: It could be anticipated that NSs loaded with BAR as a promising tool for release and bioavailability for the treatment of rheumatic arthritis and Covid-19.
“…Taupitz et al [94] confirmed enhancing of itraconazole solubility by forming ternary systems with polymer (Soluplus ® ) in a dry complex with cyclodextrin (HPβCD) or hydroxybutenyl-β-cyclodextrin (HBen-β-CD). Ahad et al [95] showed improved solubility of sinapic acid in water in the presence of HPβCD/HPMC. A similar observation was reported by El-Maradny et al [89] for the meloxicam-HPβCD-PVP complexes.…”
In this study, binary amorphous solid dispersions (ASDs, fisetin-Eudragit®) and ternary amorphous solid inclusions (ASIs, fisetin-Eudragit®-HP-β-cyclodextrin) of fisetin (FIS) were prepared by the mechanochemical method without solvent. The amorphous nature of FIS in ASDs and ASIs was confirmed using XRPD (X-ray powder diffraction). DSC (Differential scanning calorimetry) confirmed full miscibility of multicomponent delivery systems. FT-IR (Fourier-transform infrared analysis) confirmed interactions that stabilize FIS’s amorphous state and identified the functional groups involved. The study culminated in evaluating the impact of amorphization on water solubility and conducting in vitro antioxidant assays: 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)—ABTS, 2,2-diphenyl-1-picrylhydrazyl—DPPH, Cupric Reducing Antioxidant Capacity—CUPRAC, and Ferric Reducing Antioxidant Power—FRAP and in vitro neuroprotective assays: inhibition of acetylcholinesterase—AChE and butyrylcholinesterase—BChE. In addition, molecular docking allowed for the determination of possible bonds and interactions between FIS and the mentioned above enzymes. The best preparation turned out to be ASI_30_EPO (ASD fisetin-Eudragit® containing 30% FIS in combination with HP-β-cyclodextrin), which showed an improvement in apparent solubility (126.5 ± 0.1 µg∙mL−1) and antioxidant properties (ABTS: IC50 = 10.25 µg∙mL−1, DPPH: IC50 = 27.69 µg∙mL−1, CUPRAC: IC0.5 = 9.52 µg∙mL−1, FRAP: IC0.5 = 8.56 µg∙mL−1) and neuroprotective properties (inhibition AChE: 39.91%, and BChE: 42.62%).
“…However, more research is needed to determine the optimal dose and long-term safety of SA supplementation. Also, SA has poor solubility in water, which limits its therapeutic efficacy and bioavailability [13]. A self-nanoemulsifying drug delivery system (SNEDDS) has been used to solve these problems.…”
This study aimed to develop a self-nanoemulsifying drug delivery system (SNE) for sinapic acid (SA) to improve its solubility and antiviral activity. Optimal components for the SA-SNE formulation were selected, including Labrafil as the oil, Cremophor EL as the surfactant, and Transcutol as the co-surfactant. The formulation was optimized using surface response design, and the optimized SA-SNE formulation exhibited a small globule size of 83.6 nm, high solubility up to 127.1 ± 3.3, and a 100% transmittance. In vitro release studies demonstrated rapid and high SA release from the formulation. Pharmacokinetic analysis showed improved bioavailability by 2.43 times, and the optimized SA-SNE formulation exhibited potent antiviral activity against SARS-CoV-2. The developed SA-SNE formulation can enhance SA’s therapeutic efficacy by improving its solubility, bioavailability, and antiviral activity. Further in silico, modeling, and Gaussian accelerated molecular dynamics (GaMD)-based studies revealed that SA could interact with and inhibit the viral main protease (Mpro). This research contributes to developing effective drug delivery systems for poorly soluble drugs like SA, opening new possibilities for their application via nebulization in SARS-CoV-2 therapy.
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