Polymorphism of Risperidone in Supercritical Fluid Processes of Micronization and Encapsulation into Aliphatic Polyesters

Баграташвили, В. Н.; Bogorodskiy, S. E.; Egorov, A. M.; Кротова, Л. И.; Миронов, А. Н.; Паренаго, О. О.; Pokrovskiy, O. I.; Ustinovich, K. B.; Chizhov, Pavel S.; Прокопчук, Д. И.; Попов, В. К.; Tsypina, S. I.

doi:10.1134/s199079311707003x

Cited by 5 publications

(2 citation statements)

References 16 publications

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“…The diffractograms of PLGA, the pure drug risperidone, the commercial product, and the developed microcapsules and microgels are shown in Figure 8. It is known that the drug can exist in different polymorphs [32][33][34]. As expected, the polymer PLGA does not show sharp peaks, but only broad lines, indicating an amorphous state.…”

Section: Scanning Electron Microscopy and Focused Ion Beam Investigatsupporting

confidence: 66%

“…From the measurements, it can be concluded that risperidone exists in all formulations at least partially in the crystalline state. The crystalline state in the formulation is different from the crystal structure of the parent drug, but very similar to the crystal form of risperidone, which has been observed after micronization with supercritical fluids [33].…”

Section: Scanning Electron Microscopy and Focused Ion Beam Investigatmentioning

confidence: 76%

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Risperidone-Loaded PLGA–Lipid Particles with Improved Release Kinetics: Manufacturing and Detailed Characterization by Electron Microscopy and Nano-CT

et al. 2019

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For parenteral controlled drug release, the desired zero order release profile with no lag time is often difficult to achieve. To overcome the undesired lag time of the current commercial risperidone controlled release formulation, we developed PLGA–lipid microcapsules (MCs) and PLGA–lipid microgels (MGs). The lipid phase was composed of middle chain triglycerides (MCT) or isopropylmyristate (IPM). Hydroxystearic acid was used as an oleogelator. The three-dimensional inner structure of Risperidone-loaded MCs and MGs was assessed by using the invasive method of electron microscopy with focused ion beam cutting (FIB-SEM) and the noninvasive method of high-resolution nanoscale X-ray computed tomography (nano-CT). FIB-SEM and nano-CT measurements revealed the presence of highly dispersed spherical structures around two micrometres in size. Drug release kinetics did strongly depend on the used lipid phase and the presence or absence of hydroxystearic acid. We achieved a nearly zero order release without a lag time over 60 days with the MC-MCT formulation. In conclusion, the developed lipid-PLGA microparticles are attractive alternatives to pure PLGA-based particles. The advantages include improved release profiles, which can be easily tuned by the lipid composition.

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Section: Scanning Electron Microscopy and Focused Ion Beam Investigatsupporting

confidence: 66%

Section: Scanning Electron Microscopy and Focused Ion Beam Investigatmentioning

confidence: 76%

Risperidone-Loaded PLGA–Lipid Particles with Improved Release Kinetics: Manufacturing and Detailed Characterization by Electron Microscopy and Nano-CT

et al. 2019

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A critical review on the particle generation and other applications of rapid expansion of supercritical solution

Kumar

Thakur

Banerjee

et al. 2021

International Journal of Pharmaceutics

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Reverse engineering of Perseris and development of compositionally equivalent formulations

Wang

Bao

Wang

et al. 2023

International Journal of Pharmaceutics

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Polymorphism of Risperidone in Supercritical Fluid Processes of Micronization and Encapsulation into Aliphatic Polyesters

Cited by 5 publications

References 16 publications

Risperidone-Loaded PLGA–Lipid Particles with Improved Release Kinetics: Manufacturing and Detailed Characterization by Electron Microscopy and Nano-CT

Risperidone-Loaded PLGA–Lipid Particles with Improved Release Kinetics: Manufacturing and Detailed Characterization by Electron Microscopy and Nano-CT

A critical review on the particle generation and other applications of rapid expansion of supercritical solution

Reverse engineering of Perseris and development of compositionally equivalent formulations

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