Hydroxypropylcellulose as matrix carrier for novel cage-like microparticles prepared by spray-freeze-drying technology

Wei, Shaofeng; Ma, Ying; Luo, Jing; He, Xiao-Ru; Yue, Pengfei; Guan, Zhiwei; Yang, Ming

doi:10.1016/j.carbpol.2016.10.043

Cited by 11 publications

(5 citation statements)

References 31 publications

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“…Similar results were obtained by Wei et al, who showed enhanced dissolution of microparticles loaded with poorly soluble drug nanocrystals: the hydroxypropyl cellulose (HPC) polymer used as a matrix carrier had a low viscosity. This enhancement was due to the spray freeze-dried composite particles, which was attributed to the reduction in particle size of the drug [38]. Elgindy et al showed a similar result for a flutamide (FLT) formulation prepared by incorporating immediate-release lyophilized monophasic dispersions and prolonged-release chitosan microparticles.…”

Section: In Vitro Release Study Of the Ethylcellulose Microparticles Loaded With Etomentioning

confidence: 82%

Freeze-Drying Ethylcellulose Microparticles Loaded with Etoposide for In Vitro Fast Dissolution and In Vitro Cytotoxicity against Cancer Cell Types, MCF-7 and Caco-2

et al. 2021

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The aim of this study was to improve the solubility of etoposide–ethylcellulose (ET–ETO) microparticles using the freeze-drying technique. Ethylcellulose (EC) microparticles loaded with etoposide (ETO) were prepared with different drug–polymer molar ratios of 1:1, 1:3, 1:6, and 1:20 by the solvent evaporation method. The size of the prepared microparticles was 0.088 µm. The results showed that the amount of ETO encapsulated into the microparticles was 387.3, 365.0, 350.0, and 250 µg/50 mg microparticles for microparticles with drug–polymer ratios of 1:1, 1:3, 1:6, and 1:20, respectively. The FT-IR spectra showed no chemical interaction between ETO and the polymer in the solid state. The results obtained from the dissolution experiment showed that the freeze-dried microparticles were stable in 0.1 N HCl (gastric pH) for 2 h. At pH 7.4, the ETO release was 60 to 70% within the first 15 min and approximately 100% within 30 min. Results from the application of different dissolution models showed that the equations that best fit the dissolution data for the ET–ETO microparticles at pH 7.4 were the Higuchi and Peppas model equations. The in vitro cytotoxicity assay of free ETO and freeze-dried microspheres prepared in this study with a drug–polymer ratio of 1:1 was performed in two mammalian cancer cell lines, MCF-7 (for bone cancer of the mammary organ) and Caco-2 (for mammalian epithelial colorectal adenocarcinoma). The results showed that the half-maximal inhibitory concentrations (IC50 values) for ETO and freeze-dried ET–ETO microparticles were 18.6 µM and 27.1 µM, respectively. In conclusion, freeze-dried ET–ETO is a promising formulation for developing a fast-dissolving form of ETO with a significant antiproliferative activity against the tested cell lines used in this study. It is a promising formulation for local duodenal area targeting.

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Section: In Vitro Release Study Of the Ethylcellulose Microparticles Loaded With Etomentioning

confidence: 82%

Freeze-Drying Ethylcellulose Microparticles Loaded with Etoposide for In Vitro Fast Dissolution and In Vitro Cytotoxicity against Cancer Cell Types, MCF-7 and Caco-2

et al. 2021

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“…The method most employed for spray freezing (Figure 2-left) in pharmaceutical applications is defined as the atomization of a feed solution into a cryogenic vapor over liquid. In the process, the droplet sprayed from a nozzle positioned at a distance above the boiling cryogenic liquid that is stirred or not stirred begins to freeze slowly while falling down through the cold vapor phase before it comes into contact with the cryogen [82]. When they pass through the cold vapor phase, the droplets begin to freeze and become completely frozen as contact is made with the liquid cryogen.…”

Section: Spray Freezing Into Vapor Over Liquid (Sfv/l)mentioning

confidence: 99%

“…SFD can also be used for dissolution-enhanced formulation strategies. Wei et al [82] suggested a combination of homogenization and the spray freeze-drying technique to produce poorly soluble and temperature-sensitive diterpenoid lactone drug nanocrystals with improved dissolution using low viscosity hydroxypropyl cellulose (HPC) as a matrix carrier. They reported that higher ratios of HPC (1:2 and 1:1) possessed excellent dispersibility, and it can be an effective stabilizer for agglomeration during storage due to the immobilization of drug nanocrystals in its cage-like structure.…”

Section: Application Of Spray Freeze-drying To Pharmaceutical and Bio...mentioning

confidence: 99%

Spray Freeze-Drying as a Solution to Continuous Manufacturing of Pharmaceutical Products in Bulk

et al. 2020

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Pharmaceutical manufacturing is evolving from traditional batch processes to continuous ones. The new global competition focused on throughput and quality of drug products is certainly the driving force behind this transition which, thus, represents the new challenge of pharmaceutical manufacturing and hence of lyophilization as a downstream operation. In this direction, the present review deals with the most recent technologies, based on spray freeze-drying, that can achieve this objective. It provides a comprehensive overview of the physics behind this process and of the most recent equipment design.

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“…[15] Among previous approaches, ASD performed using spray freeze-drying (SFD) has conventional benefits with unique characteristics, including less thermal degradation, formation of stable spherical particles with high porosity, and molecular stability inhibiting recrystallization. [16] Interestingly, a special bioactive material, prebiotics (including inulin, oligofructose, glycan, and algae), was reported as a promising reagent for SFD preparation. [17] Prebiotics are no digestible food ingredients that promote the growth of beneficial microorganisms in the gut and improve the health of individuals.…”

Section: Introductionmentioning

confidence: 99%

Prebiotic‐Based Nanoamorphous Atorvastatin Attenuates Nonalcoholic Fatty Liver Disease by Retrieving Gut and Liver Health

Cui

et al. 2023

Small Structures

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The pathogenesis of nonalcoholic fatty liver disease (NAFLD) is multifactorial and composite, with the disorder of lipid metabolism‐induced lipotoxicity being one of the main risk factors. Atorvastatin (AT), the most widely prescribed lipid‐lowering drug, has pleiotropic actions benefiting NAFLD treatment. However, low absorption rate in the gut and potential disruption of AT on gut flora hindered its further applications. Notably, gut dysbiosis is involved in and is thus a promising management strategy for NAFLD. In this study, we constructed a prebiotic‐based AT nanoamorphous (PANA) to improve the efficacy of AT against NAFLD by retrieving liver and gut health. After oral administration, PANA showed superior drug accumulation in the liver tissue compared with pure AT. Moreover, PANA intervention effectively restored gut healthiness, indicated by reconstructed gut flora, and improved intestinal immunity, barrier integrity, and inflammation. Consequently, compared with AT, PANA treatment caused profound inhibition of weight gain and fat deposition, decreased plasma lipid levels, and alleviated hepatic steatosis and liver inflammation. The transcriptome analysis in the gut and liver tissues identified improved immunity and inflammation as potential mechanisms. This study suggests a promising strategy to treat NAFLD, assisted with nanotechnology in synergy with functional biomaterials.

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Hydroxypropylcellulose as matrix carrier for novel cage-like microparticles prepared by spray-freeze-drying technology

Cited by 11 publications

References 31 publications

Freeze-Drying Ethylcellulose Microparticles Loaded with Etoposide for In Vitro Fast Dissolution and In Vitro Cytotoxicity against Cancer Cell Types, MCF-7 and Caco-2

Freeze-Drying Ethylcellulose Microparticles Loaded with Etoposide for In Vitro Fast Dissolution and In Vitro Cytotoxicity against Cancer Cell Types, MCF-7 and Caco-2

Spray Freeze-Drying as a Solution to Continuous Manufacturing of Pharmaceutical Products in Bulk

Prebiotic‐Based Nanoamorphous Atorvastatin Attenuates Nonalcoholic Fatty Liver Disease by Retrieving Gut and Liver Health

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