Supercritical fluid coating of flavonoids on excipients enhances drug release and antioxidant activity

He, Hongling; Huang, Yating; Zhang, Xiubing; Ouyang, Yanting; Pan, Piaopiao; Lan, Yanling; Zhong, Zicheng; Lu, Peixiang; Lu, Tiejun; Chen, Zhenqiu; Lü, Xing; Writing-, Qingguo Li; Qiu, Zhenwen

doi:10.1016/j.ijpharm.2023.122593

Cited by 3 publications

(9 citation statements)

References 54 publications

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“…Screening experiments confirmed that operating at 45 °C and 80 bar represented the optimal conditions for the SAS-FB process within this study system. Consistent trends were observed for PTX coating efficiency compared to previous findings with sirolimus and three flavonoids [ 26 , 27 ]. These findings established that the optimal conditions for the SAS-FB process corresponded to the low-density region of SC-CO 2 at high temperature and low pressure, facilitating drug precipitation.…”

Section: Resultssupporting

confidence: 87%

“…Different solvents possess unique physical and chemical characteristics, such as surface tension, viscosity, density, and dielectric constant. Hence, the selection of the solvent plays a critical role when conducting investigations employing the SAS-FB process [ 27 ].…”

Section: Resultsmentioning

confidence: 99%

“…SEM images revealed that PTX particles in the SAS-FB sample were smaller and evenly dispersed on lactose surface, preventing crystal growth and aggregation. This result suggests that the SAS-FB process holds promise in resolving challenges posed by insoluble BCS class II and IV drugs, offering valuable support for handling such compounds [ 26 , 27 , 28 , 30 ]. Additionally, considering that excipients can exert their inhibitory effect on P-gp below the critical micelle concentration (CMC) [ 32 ], the SAS-FB and SAS-FB (TPGS) samples, which demonstrated high drug loading capacity and superior in vitro dissolution, were selected for further studies.…”

Section: Resultsmentioning

confidence: 99%

“…However, these particles tend to agglomerate due to their high surface energy, leading to poor flowability and difficulties in subsequent processing, limiting the application of SAS technology. To address this issue, SAS-precipitated drugs were combined with a coating process inside a dynamic fluidized bed (FB) to develop highly dispersed drug-loaded particles [ 26 , 27 , 28 ]. This approach, termed the supercritical anti-solvent fluidized bed (SAS-FB) procedure, achieves one-step simultaneous precipitation and coating, significantly enhancing drug dissolution and bioavailability.…”

Section: Introductionmentioning

confidence: 99%

“…SAS-FB-processed Sirolimus demonstrated enhanced solubility and oral bioavailability [ 26 ], with additional improvements achieved by incorporating excipients into the SAS-FB process for co-precipitation with the drug [ 30 ]. In addition, flavonoids such as luteolin, naringenin, and dihydromyricetin achieved particle size reduction, solubility enhancement, and antioxidant activity increase through the SAS-FB process [ 27 ]. Naringin, coated onto micronized matrix particles using SAS-FB for dry powder inhaler delivery of nanomedicines, exhibited an amorphous structure at an average size of approximately 130 nm, demonstrating superior in vivo plasmatic and pulmonary bioavailability [ 28 ].…”

Section: Introductionmentioning

confidence: 99%

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Optimizing Paclitaxel Oral Absorption and Bioavailability: TPGS Co-Coating via Supercritical Anti-Solvent Fluidized Bed Technology

Zhong,

Lan,

Chen

et al. 2024

Pharmaceuticals

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Supercritical anti-solvent fluidized bed (SAS-FB) coating technology has the advantages of reducing particle size, preventing high surface energy particle aggregation, improving the dissolution performance and bioavailability of insoluble drugs. The poor solubility of Biopharmaceutics Classification System (BCS) class IV drugs poses challenges in achieving optimal bioavailability. Numerous anti-cancer drugs including paclitaxel (PTX) belong to the BCS class IV, hindering their therapeutic efficacy. To address this concern, our study explored SAS-FB technology to coat PTX with D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) onto lactose. Under our optimized conditions, we achieved a PTX coating efficiency of 96.8%. Further characterization confirmed the crystalline state of PTX in the lactose surface coating by scanning electron microscopy and X-ray powder diffraction. Dissolution studies indicated that SAS-FB processed samples release over 95% of the drug within 1 min. Moreover, cell transmembrane transport assays demonstrated that SAS-FB processed PTX samples co-coated with TPGS had an enhanced PTX internalization into cells and a higher permeability coefficient compared to those without TPGS. Finally, compared to unprocessed PTX, SAS-FB (TPGS) and SAS-FB processed samples showed a 2.66- and 1.49-fold increase in oral bioavailability in vivo, respectively. Our study highlights the efficacy of SAS-FB co-coating for PTX and TPGS as a promising strategy to overcome bioavailability challenges inherent in BCS class IV drugs. Our approach holds broader implications for enhancing the performance of similarly classified medications.

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Section: Resultssupporting

confidence: 87%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Optimizing Paclitaxel Oral Absorption and Bioavailability: TPGS Co-Coating via Supercritical Anti-Solvent Fluidized Bed Technology

Zhong,

Lan,

Chen

et al. 2024

Pharmaceuticals

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Supercritical Fluids: An Innovative Strategy for Drug Development

Liu,

Liang,

Peng

et al. 2024

Bioengineering

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Nanotechnology plays a pivotal role in the biomedical field, especially in the synthesis and regulation of drug particle size. Reducing drug particles to the micron or nanometer scale can enhance bioavailability. Supercritical fluid technology, as a green drug development strategy, is expected to resolve the challenges of thermal degradation, uneven particle size, and organic solvent residue faced by traditional methods such as milling and crystallization. This paper provides an insight into the application of super-stable homogeneous intermix formulating technology (SHIFT) and super-table pure-nanomedicine formulation technology (SPFT) developed based on supercritical fluids for drug dispersion and micronization. These technologies significantly enhance the solubility and permeability of hydrophobic drugs by controlling the particle size and morphology, and the modified drugs show excellent therapeutic efficacy in the treatment of hepatocellular carcinoma, pathological scarring, and corneal neovascularization, and their performance and efficacy are highlighted when administered through multiple routes of administration. Overall, supercritical fluids have opened a green and efficient pathway for clinical drug development, which is expected to reduce side effects and enhance therapeutic efficacy.

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Zein-Based Nanoparticles as Active Platforms for Sustainable Applications: Recent Advances and Perspectives

Oleandro,

Stanzione,

Buonocore

et al. 2024

Nanomaterials

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Nanomaterials, due to their unique structural and functional features, are widely investigated for potential applications in a wide range of industrial sectors. In this context, protein-based nanoparticles, given proteins’ abundance, non-toxicity, and stability, offer a promising and sustainable methodology for encapsulation and protection, and can be used in engineered nanocarriers that are capable of releasing active compounds on demand. Zein is a plant-based protein extracted from corn, and it is biocompatible, biodegradable, and amphiphilic. Several approaches and technologies are currently involved in zein-based nanoparticle preparation, such as antisolvent precipitation, spray drying, supercritical processes, coacervation, and emulsion procedures. Thanks to their peculiar characteristics, zein-based nanoparticles are widely used as nanocarriers of active compounds in targeted application fields such as drug delivery, bioimaging, or soft tissue engineering, as reported by others. The main goal of this review is to investigate the use of zein-based nanocarriers for different advanced applications including food/food packaging, cosmetics, and agriculture, which are attracting researchers’ efforts, and to exploit the future potential development of zein NPs in the field of cultural heritage, which is still relatively unexplored. Moreover, the presented overview focuses on several preparation methods (i.e., antisolvent processes, spry drying), correlating the different analyzed methodologies to NPs’ structural and functional properties and their capability to act as carriers of bioactive compounds, both to preserve their activity and to tune their release in specific working conditions.

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Supercritical fluid coating of flavonoids on excipients enhances drug release and antioxidant activity

Cited by 3 publications

References 54 publications

Optimizing Paclitaxel Oral Absorption and Bioavailability: TPGS Co-Coating via Supercritical Anti-Solvent Fluidized Bed Technology

Optimizing Paclitaxel Oral Absorption and Bioavailability: TPGS Co-Coating via Supercritical Anti-Solvent Fluidized Bed Technology

Supercritical Fluids: An Innovative Strategy for Drug Development

Zein-Based Nanoparticles as Active Platforms for Sustainable Applications: Recent Advances and Perspectives

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