An effective polyvinyl alcohol for the solubilization of poorly water-soluble drugs in solid dispersion formulations

Umemoto, Yoshiaki; Uchida, Shinya; Yoshida, Tsuneya; Shimada, Ken; Kojima, Hiroyuki; Takagi, Akira; Tanaka, Shimako; Kashiwagura, Yasuharu; Namiki, Noriyuki

doi:10.1016/j.jddst.2019.101401

Cited by 14 publications

(14 citation statements)

References 29 publications

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“…Consequently, the dissolution rate was markedly higher compared to the HPMCAS ASDs. It has been shown that ASD formulations using PVA as carrier exhibited relatively higher dissolution rates compared to other common carriers [41,42]. In order to benefit from both, a rapid dissolution and a sufficiently stabilized supersaturation, it was decided to combine the PVA ASD with predissolved or physically added HPMCAS and additionally, a ternary ASD was formulated.…”

Section: Discussionmentioning

confidence: 99%

Impact of HPMCAS on the Dissolution Performance of Polyvinyl Alcohol Celecoxib Amorphous Solid Dispersions

Monschke

Wagner

2020

Pharmaceutics

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Amorphous solid dispersions (ASDs) have been proven to increase the bioavailability of poorly soluble drugs. It is desirable that the ASD provide a rapid dissolution rate and a sufficient stabilization of the generated supersaturation. In many cases, one polymer alone is not able to provide both features, which raises a need for reasonable polymer combinations. In this study we aimed to generate a rapidly dissolving ASD using the hydrophilic polymer polyvinyl alcohol (PVA) combined with a suitable precipitation inhibitor. Initially, PVA and hydroxypropylmethylcellulose acetate succinate (HPMCAS) were screened for their precipitation inhibitory potential for celecoxib in solution. The generated supersaturation in presence of PVA or HPMCAS was further characterized using dynamic light scattering. Binary ASDs of either PVA or HPMCAS (at 10% and 20% drug load) were prepared by hot-melt extrusion and solid-state analytics were conducted using differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and fourier-transformed infrared spectroscopy (FT-IR). The non-sink dissolution studies of the binary ASDs revealed a high dissolution rate for the PVA ASDs with subsequent precipitation and for the HPMCAS ASDs a suppressed dissolution. In order to utilize the unexploited potential of the binary ASDs, the PVA ASDs were combined with HPMCAS either predissolved or added as powder and also formulated as ternary ASD. We successfully generated a solid formulation consisting of the powdered PVA ASD and HPMCAS powder, which was superior in monophasic non-sink dissolution and biorelevant biphasic dissolution studies compared to the binary and ternary ASDs.

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Section: Discussionmentioning

confidence: 99%

Impact of HPMCAS on the Dissolution Performance of Polyvinyl Alcohol Celecoxib Amorphous Solid Dispersions

Monschke

Wagner

2020

Pharmaceutics

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“…Previous studies reported that the low molecular weight PVA showed a higher reduction of surface tension and faster dissolution in water. In addition, the lower degree of hydrolysis PVA polymer solubilized poor soluble drugs to a greater extent in water (Umemoto et al 2020 ). In this study, we used low molecular weight PVA (78 kDa) with 87–89% degree of hydrolysis.…”

Section: Resultsmentioning

confidence: 99%

Enhanced curcumin loaded nanocellulose: a possible inhalable nanotherapeutic to treat COVID-19

et al. 2022

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Graphical abstract Nanocellulose/polyvinyl alcohol/curcumin (CNC/PVA/curcumin) nanoparticles with enhanced drug loading properties were developed by the dispersion of nanocellulose in curcumin/polyvinyl alcohol aqueous medium. Due to the physical and chemical nature of sulphuric acid hydrolyzed nanocellulose and the antiviral properties of curcumin, the possibility of using these nanoparticles as an inhalable nanotherapeutic for the treatment of coronavirus disease 2019 (COVID-19) is discussed. The adsorption of curcumin and PVA into nanocellulose, and the presence of anionic sulphate groups, which is important for the interaction with viral glycoproteins were confirmed by Fourier transform infrared (FTIR) spectroscopy. FESEM images showed that the diameter of nanocellulose ranged from 50 to 100 nm, which is closer to the diameter (60–140 nm) of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The solubility of poorly water-soluble curcumin was increased from 40.58 ± 1.42 to 313.61 ± 1.05 mg/L with increasing the PVA concentration from 0.05 to 0.8% (w/v) in aqueous medium. This is a significant increase in the solubility compared to curcumin’s solubility in carboxymethyl cellulose medium in our previous study. The drug loading capacity increased by 22-fold with the addition of 0.8% PVA to the nanocellulose dispersed curcumin solution. The highest drug release increased from 1.25 ± 0.15 mg/L to 17.11 ± 0.22 mg/L with increasing the PVA concentration from 0 to 0.8% in the drug-loaded medium. Future studies of this material will be based on the antiviral efficacy against SARS-CoV-2 and cell cytotoxicity studies. Due to the particulate nature, morphology and size of SARS-CoV-2, nanoparticle-based strategies offer a strong approach to tackling this virus. Hence, we believe that the enhanced loading of curcumin in nanocellulose will provide a promising nano-based solution for the treatment of COVID-19.

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“…96 There are approaches, such as prodrugs, cyclodextrin complexation, nanosizing, cocrystals, self-emulsifying drug delivery systems, and solid dispersions to increase the bioavailability and effectiveness of orally administered drugs. 97 Polymeric micelles, dendrimers, inorganic NPs, metallic NPs, Qdots, protein, and polysaccharide NPs are promising systems for oral administration in applications. 3 Table 2 presents a list of studies published in 2019 and 2020, including drug delivery formulations of cyclodextrin complexes, liposome, nanoemulsion, NP, NLC, nanosuspension, niosome, proliposome, proliposome powder, and SLN for oral administration and the treatment of different diseases, such as angiocardiopathy, GI infections, intestinal bowel disease, psychiatric disorders, and trichinellosis.…”

Section: Formulation Strategies Of Drugs For Oral Administrationmentioning

confidence: 99%

Nano Spray-Dried Drugs for Oral Administration: A Review

Öztürk

Arpagaus

2021

ASSAY and Drug Development Technologies

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Spray drying is an important technology that is fast, simple, reproducible, and scalable. It has a wide application range, that is, in food, chemicals, and encapsulation of pharmaceuticals. The technology can be divided into conventional spray drying and nano spray drying. The key advantage of nano spray drying is the production of drug-loaded nanosized particles for various drug delivery applications. The recent developments in nano spray dryer technology and the market launch of the Nano Spray Dryer B-90 by Bu ¨chi Labortechnik AG in 2009 enabled the production of submicron spray-dried particles. This review focuses on nanosized drug delivery systems intended for oral administration produced by nano spray drying. First, the nano spray drying concept, the basic technologies implemented in the equipment, and the effects of the various process parameters on the final dry submicron powder properties are presented. Then, the topics of new formulation strategies of oral drugs are highlighted with examples that have entered the research literature in recent years. Next, the subjects of direct conversion of poorly watersoluble drugs, encapsulation of drugs, and drying of preformed nanoparticles are considered. Finally, topics such as morphology, particle size, size distribution, surface analysis, bioavailability, drug release, release kinetics, and solid-state characterization (by differential scanning calorimetry, X-ray diffraction, Fourier transform infrared spectroscopy, nuclear magnetic resonance) of oral drug delivery systems produced by nano spray drying are discussed. The review attempts to provide a comprehensive knowledge base with current literature and foresight to researchers working in the field of pharmaceutical technology and nanotechnology and especially in the field of nano spray drying.

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An effective polyvinyl alcohol for the solubilization of poorly water-soluble drugs in solid dispersion formulations

Cited by 14 publications

References 29 publications

Impact of HPMCAS on the Dissolution Performance of Polyvinyl Alcohol Celecoxib Amorphous Solid Dispersions

Impact of HPMCAS on the Dissolution Performance of Polyvinyl Alcohol Celecoxib Amorphous Solid Dispersions

Enhanced curcumin loaded nanocellulose: a possible inhalable nanotherapeutic to treat COVID-19

Nano Spray-Dried Drugs for Oral Administration: A Review

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