Strategic application of self-micellizing solid dispersion technology to respirable powder formulation of tranilast for improved therapeutic potential

Suzuki, Haruo; Kojo, Yoshiki; Yakushiji, Keisuke; Yuminoki, Kayo; Hashimoto, Naofumi; Onoue, Satomi

doi:10.1016/j.ijpharm.2015.12.065

Cited by 9 publications

(3 citation statements)

References 34 publications

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“…Soluplus ® has a critical micelle concentration value of ca. 1 μg/mL in aqueous mediums (pH 6.5–7.0) (Shi et al., 2018), and formation of fine micelle can lead to improvement in the dissolution behavior of coexisting poorly water‐soluble drugs (Kojo et al., 2018; Suzuki et al., 2016). In the present study, self‐micellizing potency was evaluated with TEM observation (Figure 4A) and dynamic light scattering (DLS) analysis (Figure 4B).…”

Section: Resultsmentioning

confidence: 99%

Self‐micellizing solid dispersion of tacrolimus: Physicochemical and pharmacokinetic characterization

Makino

Tsukada

Kambayashi

et al. 2023

Biopharm & Drug Disp

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The present study was undertaken to develop a self‐micellizing solid dispersion (SMSD) of tacrolimus (TAC) to improve the biopharmaceutical properties of TAC. An SMSD formulation of TAC (SMSD/TAC) and amorphous solid dispersion formulation of TAC (ASD/TAC) were prepared with Soluplus®, an amphiphilic copolymer, and hydroxypropyl cellulose, respectively. Physicochemical properties were characterized in terms of morphology, crystallinity, storage stability, interaction of TAC with Soluplus®, and micelle‐forming potency; pharmacokinetic behavior was also evaluated in rats. Tacrolimus in both formulations was in an amorphous state. After storage at 40°C/75% relativity humidity for 4 weeks, there were no significant changes in the crystallinity of TAC between nonaged and aged SMSD/TAC, whereas slight recrystallization was observed in aged ASD/TAC. The results of circular dichroism (CD) and infrared spectroscopic analyses were indicative of the potent drug–polymer interaction in SMSD/TAC, possibly leading to the prevention of recrystallization. Compared with other TAC samples, SMSD/TAC exhibited significant improvement in the dissolution behavior of TAC through the immediate formation of fine micelles. After the oral administration of TAC samples (10 mg TAC/kg) to rats, there was marked enhancement in systemic exposure to TAC with both formulations; in particular, SMSD/TAC achieved an increase in bioavailability ca. 20‐fold higher than crystalline TAC. The SMSD approach might provide an effective dosage form for TAC with enhanced physicochemical stability and oral absorption.

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Section: Resultsmentioning

confidence: 99%

Self‐micellizing solid dispersion of tacrolimus: Physicochemical and pharmacokinetic characterization

Makino

Tsukada

Kambayashi

et al. 2023

Biopharm & Drug Disp

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“…Self-micellizing solid dispersion (SMSD), a recent promising formulation strategy has attracted considerable attention since it can increase the bioavailability of drugs while reducing the inconsistency of oral absorption under various pathophysiological situations (Onoue et al., 2014 ). By using an amphiphilic block copolymer, SMSD technology is a solid dispersion system that can achieve high dissolution characteristics of poorly water-soluble drugs (Onoue et al., 2014 ; Suzuki et al., 2016 ; Halder et al., 2019 ). In brief, SMSD’s usually consist of an amphiphilic carrier and the drug mixed in a suitable solvent.…”

Section: Introductionmentioning

confidence: 99%

Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects

Halder,

Afrose,

Shill

et al. 2024

Drug Delivery

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The present study was designed to develop a self-micellizing solid dispersion (SMSD) containing Thymoquinone (TQM), a phytonutrient obtained from Nigella sativa seeds, aiming to improve its biopharmaceutical and nephroprotective functions. The apparent solubility of TQM in polymer solutions was used to choose an appropriate amphiphilic polymer that could be used to make an SMSD system. Based on the apparent solubility, Soluplus® was selected as an appropriate carrier, and mixing with TQM, SMSD-TQM with different loadings of TQM (5–15%) was made by solvent evaporation and freeze-drying techniques, respectively, and the formulations were optimized. The optimized SMSD-TQM was evaluated in terms of particle size distribution, morphology, release characteristics, pharmacokinetic behavior, and nephroprotective effects in a rat model of acute kidney injury. SMSD-TQM significantly improved the dissolution characteristics (97.8%) of TQM in water within 60 min. Oral administration of SMSD-TQM in rats exhibited a 4.9-fold higher systemic exposure than crystalline TQM. In a cisplatin-induced (6 mg/kg, i.p. ) acute kidney-damaged rat model, oral SMSD-TQM (10 mg/kg) improved the nephroprotective effects of TQM based on the results of kidney biomarkers and histological abnormalities. These findings suggest that SMSD-TQM might be efficacious in enhancing the nephroprotective effect of TQM by overcoming biopharmaceutical limitations.

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“…Self-micellizing solid dispersion (SMSD), a recent promising formulation strategy, has attracted considerable attention since it can increase the bioavailability of drugs while reducing the inconsistency of oral absorption under various patho-physiological situations [16]. By using an amphiphilic block co-polymer, SMSD technology is a solid dispersion system that can achieve high dissolution characteristics of poorly water soluble drugs [17][18][19]. In brief, SMSD's usually consist of an amphiphilic carrier and the drug mixed in a suitable solvent.…”

Section: Introductionmentioning

confidence: 99%

Self-Micellizing Solid Dispersion of Thymoquinone with Enhanced Biopharmaceutical and Nephroprotective Effects

Halder¹,

Afrose²,

Shill³

et al. 2023

Preprint

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The present study was designed to develop a self-micellizing solid dispersion (SMSD) containing Thymoquinone (TQM), a phytonutrient obtained from Nigella sativa seeds, aiming to improve its biopharmaceutical and nephroprotective functions. The apparent solubility of TQM in polymer solutions was used to choose an appropriate amphiphilic polymer that could be used to make an SMSD system. Based on the apparent solubility, Soluplus® was chosen as an appropriate carrier, and mixing with TQM, SMSD-TQM with different loadings of TQM (5–15%) was made by solvent evaporation and freeze-drying techniques, respectively, and the formulations were optimized. The optimized SMSD-TQM was evaluated in terms of particle size distribution, morphology, release characteristics, pharmacokinetic behavior, and nephroprotective effects in a rat model of acute kidney injury. SMSD-TQM significantly improved the dissolution characteristics (97.8%) of TQM in water within 60 min. Oral administration of SMSD-TQM in rats exhibited a 4.9-fold higher systemic exposure than crystalline TQM. In a cisplatin-induced (6 mg/kg, i.p.) acute kidney-damaged rat model, oral SMSD-TQM (10 mg/kg) improved the nephroprotective effects of TQM based on the results of kidney biomarkers and histological abnormalities. These findings suggest that SMSD-TQM might be efficacious in enhancing the nephroprotective effect of TQM by overcoming biopharmaceutical limitations.

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Strategic application of self-micellizing solid dispersion technology to respirable powder formulation of tranilast for improved therapeutic potential

Cited by 9 publications

References 34 publications

Self‐micellizing solid dispersion of tacrolimus: Physicochemical and pharmacokinetic characterization

Self‐micellizing solid dispersion of tacrolimus: Physicochemical and pharmacokinetic characterization

Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects

Self-Micellizing Solid Dispersion of Thymoquinone with Enhanced Biopharmaceutical and Nephroprotective Effects

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