Assessing compatibility of excipients selected for a sustained release formulation of bilberry leaf extract

Kolisnyk, Tetiana; Vashchenko, O. V.; Рубан, О. А.; Fil, Nataliya; Сліпченко, Г. Д.

doi:10.1590/s2175-97902022e19753

Cited by 5 publications

(5 citation statements)

References 32 publications

(32 reference statements)

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“…On the other hand, they are toxic due to a high blood drug concentration after oral administration resulting from the initial burst release, which is particularly a negative case for numerous nano/micro drug delivery systems [ 5 , 6 , 7 , 8 ]. Thus, better drug dissolution and sustained release of these drugs after oral delivery is highly desired for a “safe, efficacious, and convenient” delivery to the patients [ 9 , 10 , 11 , 12 ].…”

Section: Introductionmentioning

confidence: 99%

Electrosprayed Stearic-Acid-Coated Ethylcellulose Microparticles for an Improved Sustained Release of Anticancer Drug

Ji,

Zhao,

Liu

et al. 2023

Gels

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Sustained release is highly desired for “efficacious, safe and convenient” drug delivery, particularly for those anticancer drug molecules with toxicity. In this study, a modified coaxial electrospraying process was developed to coat a hydrophobic lipid, i.e., stearic acid (SA), on composites composed of the anticancer drug tamoxifen citrate (TC) and insoluble polymeric matrix ethylcellulose (EC). Compared with the electrosprayed TC-EC composite microparticles M1, the electrosprayed SA-coated hybrid microparticles M2 were able to provide an improved TC sustained-release profile. The 30% and 90% loaded drug sustained-release time periods were extended to 3.21 h and 19.43 h for M2, respectively, which were significantly longer than those provided by M1 (0.88 h and 9.98 h, respectively). The morphology, inner structure, physical state, and compatibility of the components of the particles M1 and M2 were disclosed through SEM, TEM, XRD, and FTIR. Based on the analyses, the drug sustained-release mechanism of multiple factors co-acting for microparticles M2 is suggested, which include the reasonable selections and organizations of lipid and polymeric excipient, the blank SA shell drug loading, the regularly round shape, and also the high density. The reported protocols pioneered a brand-new manner for developing sustained drug delivery hybrids through a combination of insoluble cellulose gels and lipid using modified coaxial electrospraying.

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Section: Introductionmentioning

confidence: 99%

Electrosprayed Stearic-Acid-Coated Ethylcellulose Microparticles for an Improved Sustained Release of Anticancer Drug

Ji,

Zhao,

Liu

et al. 2023

Gels

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show abstract

“…These successful outcomes mainly rely on the continuous introduction of advanced materials processing techniques into the pharmaceutic field to implement effective material conversion [ 26 , 27 , 28 , 29 ]. Those DDSs have been demonstrated to be able to provide all kinds of desired drug-controlled release profiles able to deliver loaded drug molecules in a designed manner, such as via targeted release at different levels (at the molecular level and organic level and in terms of drug-controlled release place), delayed release (in terms of the initial time point of drug-controlled release), fast release, sustained release and multiple-phase release (in term of drug-controlled release speed) [ 30 , 31 , 32 , 33 , 34 ].…”

Section: Introductionmentioning

confidence: 99%

Electrosprayed Core (Cellulose Acetate)–Shell (Polyvinylpyrrolidone) Nanoparticles for Smart Acetaminophen Delivery

Xu,

He,

et al. 2023

Pharmaceutics

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Smart drug delivery, through which the drug molecules are delivered according to the requests of human biological rhythms or by maximizing drug therapeutic effects, is highly desired in pharmaceutics. Many biomacromolecules have been exploited for this application in the past few decades, both in industry and laboratories. Biphasic release, with an intentional pulsatile release and a following extended release stage, represents a typical smart drug delivery approach, which aims to provide fast therapeutic action and a long time period of effective blood drug concentration to the patients. In this study, based on the use of a well-known biomacromolecule, i.e., cellulose acetate (CA), as the drug (acetaminophen, ATP)-based sustained release carrier, a modified coaxial electrospraying process was developed to fabricate a new kind of core–shell nanoparticle. The nanoparticles were able to furnish a pulsatile release of ATP due to the shell polyvinylpyrrolidone (PVP). The time cost for a release of 30% was 0.32 h, whereas the core–shell particles were able to provide a 30.84-h sustained release of the 90% loaded ATP. The scanning electron microscope and transmission electron microscope results verified in terms of their round surface morphologies and the obvious core–shell double-chamber structures. ATP presented in both the core and shell sections in an amorphous state owing to its fine compatibility with CA and PVP. The controlled release mechanisms of ATP were suggested. The disclosed biomacromolecule-based process–structure–performance relationship can shed light on how to develop new sorts of advanced nano drug delivery systems.

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“…These methods have shown their usefulness in our previous studies for the identification of single- and dual-component preparations containing theophylline [ 18 ]. In addition, other authors have demonstrated their usefulness in the pharmaceutical industry for the identification of polymorphic substances [ 19 , 20 ], the influence of ambient relative humidity on vapor sorption [ 21 ], thermal stability [ 22 , 23 ], or compatibility of excipients with API [ 24 , 25 , 26 , 27 ] and API with API [ 28 ], as well as quality control in pharmacies [ 29 , 30 , 31 ].…”

Section: Introductionmentioning

confidence: 99%

Application of TGA/c-DTA for Distinguishing between Two Forms of Naproxen in Pharmaceutical Preparations

Ramos,

Raczak,

Silvestri

et al. 2023

Pharmaceutics

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Naproxen is one of the most used non-steroidal anti-inflammatory drugs (NSAIDs). It is used to treat pain of various origins, inflammation and fever. Pharmaceutical preparations containing naproxen are available with prescription and over-the-counter (OTC). Naproxen in pharmaceutical preparations is used in the form of acid and sodium salt. From the point of view of pharmaceutical analysis, it is crucial to distinguish between these two forms of drugs. There are many costly and laborious methods to do this. Therefore, new, faster, cheaper and, at the same time, simple-to-perform identification methods are sought. In the conducted studies, thermal methods such as thermogravimetry (TGA) supported by calculated differential thermal analysis (c-DTA) were proposed to identify the type of naproxen in commercially available pharmaceutical preparations. In addition, the thermal methods used were compared with pharmacopoeial methods for the identification of compounds, such as high-performance liquid chromatography (HPLC), Fourier-transform infrared spectroscopy (FTIR), UV-Vis spectrophotometry, and a simple colorimetric analyses. In addition, using nabumetone, a close structural analog of naproxen, the specificity of the TGA and c-DTA methods was assessed. Studies have shown that the thermal analyses used are effective and selective in distinguishing the form of naproxen in pharmaceutical preparations. This indicates the potential possibility of using TGA supported by c-DTA as an alternative method.

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Assessing compatibility of excipients selected for a sustained release formulation of bilberry leaf extract

Cited by 5 publications

References 32 publications

Electrosprayed Stearic-Acid-Coated Ethylcellulose Microparticles for an Improved Sustained Release of Anticancer Drug

Electrosprayed Stearic-Acid-Coated Ethylcellulose Microparticles for an Improved Sustained Release of Anticancer Drug

Electrosprayed Core (Cellulose Acetate)–Shell (Polyvinylpyrrolidone) Nanoparticles for Smart Acetaminophen Delivery

Application of TGA/c-DTA for Distinguishing between Two Forms of Naproxen in Pharmaceutical Preparations

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