Three months extended-release microspheres prepared by multi-microchannel microfluidics in beagle dog models

Kim, Ju Hee; Ryu, Choong Ho; Chon, Chan Hee; Kim, Seyeon; Lee, Sangno; Maharjan, Ravi; Kim, Nam Ah; Jeong, Seong Hoon

doi:10.1016/j.ijpharm.2021.121039

Cited by 12 publications

(6 citation statements)

References 64 publications

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“…However, the pain-relieving effect of the bufalin-PLGA MS was not obvious within 3 h after administration. It is important to mention that although it is not recommended to have a release rate exceeding certain amount as it will cause burst release ( Kim et al, 2021 ), the design of drug release for analgesic purpose should consider an initial burst to create the immediacy of drug efficacy, allowing the drug diffusion to trigger faster onset of action.…”

Section: Discussionmentioning

confidence: 99%

Effect of Bufalin-PLGA Microspheres in the Alleviation of Neuropathic Pain via the CCI Model

et al. 2022

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The treatment of neuropathic pain (NPP) is considered challenging, while the search for alternative medication is striving. NPP pathology is related with the expression of both the purinergic 2X7 (P2X7) receptor and the transient receptor potential vanilloid 1 receptor (TRPV1). Bufalin is a traditional Chinese medication derived from toad venom with pronounced antitumor, analgesic, and anti-inflammatory properties. However, poor solubility, rapid metabolism, and the knowledge gap on its pain alleviation mechanism have limited the clinical application of bufalin. Hence, the purpose of this study is to illustrate the NPP alleviation mechanism of bufalin via chronic constriction injury (CCI). To address the concern on fast metabolism, bufalin-PLGA microspheres (MS) were prepared via membrane emulsification to achieve prolonged pain-relieving effects. Western blot, real-time PCR, immunofluorescence, and molecular docking were employed to demonstrate the therapeutic action of bufalin on NPP. The results showed enhanced thermal withdrawal latency (TWL) and mechanical withdrawal threshold (MWT) after the administration of both bufalin and bufalin-PLGA MS in the CCI rats. Prolonged pain-relieving effects for up to 3 days with reduced dose frequency was achieved via bufalin-PLGA MS. In the CCI rats treated with bufalin-PLGA MS, the expression levels of protein and mRNA in TRPV1 and P2X7, both localized in the dorsal root ganglion (DRG), were reduced. Moreover, bufalin-PLGA MS effectively reduced the levels of IL-1β, IL-18, IL-6, and TNF-α in the CCI group. The results from molecular docking suggested a possible mechanism of NPP alleviation of bufalin through binding to P2X7 receptors directly. The administration of bufalin-PLGA MS prepared by membrane emulsification demonstrated promising applications for sustained effect on the alleviation of NPP.

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Section: Discussionmentioning

confidence: 99%

Effect of Bufalin-PLGA Microspheres in the Alleviation of Neuropathic Pain via the CCI Model

et al. 2022

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“…Some synthetic polymers have already been classified as food-grade, such as poly-lactic-co-glycolic acid (PLGA), polymethyl methacrylate (PMMA), polyethyleneimine (PEI), poly (vinyl alcohol) (PVA), and polyethylene glycol (PEG) [ 26 , 83 , 84 ]. PLGA is the most commonly used synthetic polymer for microfluidic assembly as a carrier material [ 27 , 28 , 85 ]. It is a copolymer comprising PGA (polyglycolic acid) and PLA (polylactic acid) that decomposes into nontoxic byproducts through the Krebs cycle.…”

Section: Microfluidic Assembly Of Food-grade Delivery Systems Based O...mentioning

confidence: 99%

“…PLGA 5050A (acid-terminated with a lactide/glycolide ratio of 50/50) or PLGA 7525A (acid-terminated with a lactide/glycolide ratio of 75/25) were dissolved in dichloromethane (DCM) followed by the addition of finasteride (28 mg) to compose the dispersed phase. At the same time, the aqueous solution of PVA (0.25% w / v ) was used as the continuous phase [ 27 , 28 ]. The dispersed and continuous phases were inserted into the microfluidic chip with a pressure of 1100 mbar and 2200 mbar, respectively.…”

Section: Microfluidic Assembly Of Food-grade Delivery Systems Based O...mentioning

confidence: 99%

“…Synthetic materials have been widely explored as carriers in microfluidic-assembled delivery systems, while few are food-grade [ 26 ]. However, the assembly of food-grade delivery systems using microfluidic approaches has been the subject of interest in many studies since several food-grade materials emerged as viable options for this proposal [ 27 , 28 , 29 , 30 ]. As shown in Figure 1 A, over the past 5 years, there has been an increase in the number of citations and publications on food-grade emulsion-based delivery systems obtained by microfluidic techniques (keywords: food-grade, emulsion, droplet microfluidics, and droplet-based microfluidics).…”

Section: Introductionmentioning

confidence: 99%

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Droplet-Based Microfluidics as a Platform to Design Food-Grade Delivery Systems Based on the Entrapped Compound Type

Bianchi,

de la Torre,

Costa

2023

Foods

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Microfluidic technology has emerged as a powerful tool for several applications, including chemistry, physics, biology, and engineering. Due to the laminar regime, droplet-based microfluidics enable the development of diverse delivery systems based on food-grade emulsions, such as multiple emulsions, microgels, microcapsules, solid lipid microparticles, and giant liposomes. Additionally, by precisely manipulating fluids on the low-energy-demand micrometer scale, it becomes possible to control the size, shape, and dispersity of generated droplets, which makes microfluidic emulsification an excellent approach for tailoring delivery system properties based on the nature of the entrapped compounds. Thus, this review points out the most current advances in droplet-based microfluidic processes, which successfully use food-grade emulsions to develop simple and complex delivery systems. In this context, we summarized the principles of droplet-based microfluidics, introducing the most common microdevice geometries, the materials used in the manufacture, and the forces involved in the different droplet-generation processes into the microchannels. Subsequently, the encapsulated compound type, classified as lipophilic or hydrophilic functional compounds, was used as a starting point to present current advances in delivery systems using food-grade emulsions and their assembly using microfluidic technologies. Finally, we discuss the limitations and perspectives of scale-up in droplet-based microfluidic approaches, including the challenges that have limited the transition of microfluidic processes from the lab-scale to the industrial-scale.

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“…Therefore, PLGA has good biocompatibility and biodegradability (Choi et al., 2021 ; Wen et al., 2022 ), and its safety has been recognized by FDA and the European Drug Agency, and has been officially included by FDA as pharmaceutical excipients. Moreover, PLGA also has the characteristics of easy processing and suitable biodegradation kinetics (Kim et al., 2021 ). The hydrophilic and hydrophobic properties and degradation kinetics of PLGA can be changed by adjusting the monomer composition ratio (LA/GA), molecular weight, and terminal groups of PLGA (Hua et al., 2021 ).…”

Section: Introductionmentioning

confidence: 99%

PLGA sustained-release microspheres loaded with an insoluble small-molecule drug: microfluidic-based preparation, optimization, characterization, and evaluation in vitro and in vivo

Liu

Tan

et al. 2022

Drug Delivery

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Microspheres play an important role in controlling drug delivery and release rate accurately. To realize the sustainable release of insoluble small-molecule drugs, a new three-phase flow-focusing microfluidic device was developed to produce the drug-loaded sustained-release microspheres which were prepared with bicalutamide (BCS class-II) as the model drug and poly(lactide-co-glycolide) (PLGA) as the carrier material. Under optimized prescription conditions, the microspheres showed a smooth surface and uniform size of 51.33 μm with a CV value of 4.43%. Sustained-release microspheres had a releasing duration of around 40 days in vitro without any initial burst release. The drug release mechanism of the microspheres was drug diffusion and polymer erosion. Meanwhile, the drug release of microspheres in vivo could be up to 30 days. Briefly, the microfluidic device in this study provides a new solution for the preparation of sustained-release microspheres for insoluble small-molecule drugs. PLGA sustained-release microspheres developed by the microfluidic device have good application prospects in precise delivery and sustainable release of insoluble small-molecule drugs.

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Three months extended-release microspheres prepared by multi-microchannel microfluidics in beagle dog models

Cited by 12 publications

References 64 publications

Effect of Bufalin-PLGA Microspheres in the Alleviation of Neuropathic Pain via the CCI Model

Effect of Bufalin-PLGA Microspheres in the Alleviation of Neuropathic Pain via the CCI Model

Droplet-Based Microfluidics as a Platform to Design Food-Grade Delivery Systems Based on the Entrapped Compound Type

PLGA sustained-release microspheres loaded with an insoluble small-molecule drug: microfluidic-based preparation, optimization, characterization, and evaluation in vitro and in vivo

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