Effects of Different Formulation Methods on Drug Crystallinity, Drug-Carrier Interaction, and Ex Vivo Permeation of a Ternary Solid Dispersion Containing Nisoldipine

Oo, May Kyaw; Mahmood, Syed; Wui, Wong Tin; Mandal, Uttam Kumar; Chatterjee, Bappaditya

doi:10.1007/s12247-019-09415-2

Cited by 6 publications

(5 citation statements)

References 43 publications

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“…The shape and surface morphology of RXB powder and selected RXB-loaded microspheres (formulations IV and VIII) were investigated and are shown in Figure A–F . RXB appeared as irregular crystals with a smooth surface, whereas the RXB-loaded microspheres had spherical particles with a smooth surface . This suggests that crystalline RXB was converted to an amorphous form .…”

Section: Resultsmentioning

confidence: 99%

Enhanced Oral Bioavailability of Rivaroxaban-Loaded Microspheres by Optimizing the Polymer and Surfactant Based on Molecular Interaction Mechanisms

et al. 2023

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This study aimed to develop microspheres using water-soluble carriers and surfactants to improve the solubility, dissolution, and oral bioavailability of rivaroxaban (RXB). RXB-loaded microspheres with optimal carrier (poly(vinylpyrrolidone) K30, PVP) and surfactant (sodium lauryl sulfate (SLS)) ratios were prepared. 1H NMR and Fourier transform infrared (FTIR) analyses showed that drug–excipient and excipient–excipient interactions affected RXB solubility, dissolution, and oral absorption. Therefore, molecular interactions between RXB, PVP, and SLS played an important role in improving RXB solubility, dissolution, and oral bioavailability. Formulations IV and VIII, containing optimized RXB/PVP/SLS ratios (1:0.25:2 and 1:1:2, w/w/w), had significantly improved solubility by approximately 160- and 86-fold, respectively, compared to RXB powder, with the final dissolution rates improved by approximately 4.5- and 3.4-fold, respectively, compared to those of RXB powder at 120 min. Moreover, the oral bioavailability of RXB was improved by 2.4- and 1.7-fold, respectively, compared to that of RXB powder. Formulation IV showed the highest improvement in oral bioavailability compared to RXB powder (AUC, 2400.8 ± 237.1 vs 1002.0 ± 82.3 h·ng/mL). Finally, the microspheres developed in this study successfully improved the solubility, dissolution rate, and bioavailability of RXB, suggesting that formulation optimization with the optimal drug-to-excipient ratio can lead to successful formulation development.

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Section: Resultsmentioning

confidence: 99%

Enhanced Oral Bioavailability of Rivaroxaban-Loaded Microspheres by Optimizing the Polymer and Surfactant Based on Molecular Interaction Mechanisms

et al. 2023

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“…A summary of the low, high, or unclear risk for bias assessment of the analyzed articles is presented in Figure 5. [49,50,43,30,29,48,47,40,36,39,38,32,34,33,35,26,37].…”

Section: Risk Of Biasmentioning

confidence: 99%

“…Another explanation for better solubility is the "spring and parachute" effect, commonly seen in crystal engineering [62,63]. Oo et al discovered that better solubility is associated with an increase in the permeability of lyophilizate [48]. The passage through the cell membrane of raw and lyophilized nisoldipine was 31.26% and 51.55%, respectively [48].…”

Section: Influence Of Lyophilization On Morphology and Physicochemica...mentioning

confidence: 99%

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Modification of the Physicochemical Properties of Active Pharmaceutical Ingredients via Lyophilization

Taldaev,

Pankov,

Terekhov

et al. 2023

Pharmaceutics

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Bioavailability is an important biopharmaceutical characteristic of active pharmaceutical ingredients (APIs) that is often correlated with their solubility in water. One of the methods of increasing solubility is freeze drying (lyophilization). The article provides a systematic review of studies published from 2012 to 2022 aimed at optimizing the properties of active pharmaceutical ingredients by freeze drying. This review was carried out in accordance with the recommendations of Preferred Reporting Items for Systematic Reviews and Meta-Analysis (PRISMA). In general, 141 modifications of 36 APIs attributed to 12 pharmacological groups were reported in selected publications. To characterize the products of phase modification after lyophilization, a complex of analytical methods was used, including microscopic, thermal, X-ray, and spectral approaches. Solubility and pharmacokinetic parameters were assessed. There is a tendency to increase solubility due to the amorphization of APIs during lyophilization. Thus, the alcohol lyophilizate of dihydroquercetin is “soluble” in water compared to the initial substance belonging to the category “very poorly soluble”. Based on the analysis of the literature, it can be argued that lyophilization is a promising method for optimizing the properties of APIs.

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“…Recently, vinylpyrrolidone-vinyl acetate copolymers (Kollidon) 16 and HPMCAS (HPMC acetyl succinate) 17 have become popular solid dispersion carriers. A binary mixture of polymers is often used, such as PVP K30-PEG 6000, 18 PVP K30-poloxamer, 19 etc.…”

Section: Introductionmentioning

confidence: 99%

Comparison of Two Grafted Copolymers, Soluplus and Kollicoat IR, as Solid Dispersion Carriers of Arteether for Oral Delivery Prepared by Different Solvent-Based Methods

Desai,

Chatterjee

2023

ACS Omega

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Effects of Different Formulation Methods on Drug Crystallinity, Drug-Carrier Interaction, and Ex Vivo Permeation of a Ternary Solid Dispersion Containing Nisoldipine

Cited by 6 publications

References 43 publications

Enhanced Oral Bioavailability of Rivaroxaban-Loaded Microspheres by Optimizing the Polymer and Surfactant Based on Molecular Interaction Mechanisms

Enhanced Oral Bioavailability of Rivaroxaban-Loaded Microspheres by Optimizing the Polymer and Surfactant Based on Molecular Interaction Mechanisms

Modification of the Physicochemical Properties of Active Pharmaceutical Ingredients via Lyophilization

Comparison of Two Grafted Copolymers, Soluplus and Kollicoat IR, as Solid Dispersion Carriers of Arteether for Oral Delivery Prepared by Different Solvent-Based Methods

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