Enhancing the physical stability and supersaturation generation of amorphous drug-polyelectrolyte nanoparticle complex via incorporation of crystallization inhibitor at the nanoparticle formation step: A case of HPMC versus PVP

Dong, Bingxue; Lim, Li Ming; Hadinoto, Kunn

doi:10.1016/j.ejps.2019.105035

Cited by 12 publications

(9 citation statements)

References 36 publications

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“…Dong et al prepared amorphous drug-polyelectrolyte nanoplex (nanoparticle complex) for the enhancement of solubility of poorly soluble drugs [ 126 ]. The existing nanoplexes suffer from long term storage instability due to the crystallization propensity of certain drugs.…”

Section: Pharmaceutical and Other Applicationsmentioning

confidence: 99%

Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition

Kurakula

Rao

2020

Journal of Drug Delivery Science and Technology

262

172

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Polyvinylpyrrolidone (PVP) is a water-soluble polymer obtained by polymerization of monomer N -vinylpyrrolidone. PVP is an inert, non-toxic, temperature-resistant, pH-stable, biocompatible, biodegradable polymer that helps to encapsulate and cater both hydrophilic and lipophilic drugs. These advantages enable PVP a versatile excipient in the formulation development of broad conventional to novel controlled delivery systems. PVP has tunable properties and can be used as a brace component for gene delivery, orthopedic implants, and tissue engineering applications. Based on different molecular weights and modified forms, PVP can lead to exceptional beneficial features with varying chemical properties. Graft copolymerization and other techniques assist PVP to conjugate with poorly soluble drugs that can inflate bioavailability and even introduces the desired swelling tract for their control or sustained release. The present review provides chemistry, mechanical, physicochemical properties, evaluation parameters, dewy preparation methods of PVP derivatives intended for designing conventional to controlled systems for drug, gene, and cosmetic delivery. The past and growing interest in PVP establishes it as a promising polymer to enhance the trait and performance of current generation pharmaceutical dosage forms. Furthermore, the scrutiny explores existing patents, marketed products, new and futuristic approaches of PVP that have been identified and scope for future development, characterization, and its use. The exploration spotlights the importance and role of PVP in the design of Povidone-iodine (PVP–I) and clinical trials to assess therapeutic efficacy against the COVID-19 in the current pandemic scenario.

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Section: Pharmaceutical and Other Applicationsmentioning

confidence: 99%

Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition

Kurakula

Rao

2020

Journal of Drug Delivery Science and Technology

262

172

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“…The peak kinetic solubility, however, was short-lived as the kinetic solubility immediately decreased to (3.5 ± 0.5) × C Sat 10 min after reaching the peak due to precipitation of the supersaturated QUE solution. While the kinetic solubility continued to decrease with time, it remained at least twice higher than C Sat over 4 h. In this regard, polymeric crystallization inhibitors, such as hydroxypropylmethylcellulose, could be incorporated into the nanoplex dosage formulation to prolong the kinetic solubility of QUE [37].…”

Section: Dissolution Characteristicsmentioning

confidence: 99%

A Potential Quorum-Sensing Inhibitor for Bronchiectasis Therapy: Quercetin–Chitosan Nanoparticle Complex Exhibiting Superior Inhibition of Biofilm Formation and Swimming Motility of Pseudomonas aeruginosa to the Native Quercetin

Tran

Hadinoto

2021

IJMS

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Quercetin (QUE)—a plant-derived flavonoid, is recently established as an effective quorum sensing (QS) inhibiting agent in Pseudomonas aeruginosa—the main bacterial pathogen in bronchiectasis lungs. Successful clinical application of QUE, however, is hindered by its low solubility in physiological fluids. Herein we developed a solubility enhancement strategy of QUE in the form of a stable amorphous nanoparticle complex (nanoplex) of QUE and chitosan (CHI), which was prepared by electrostatically driven complexation between ionized QUE molecules and oppositely charged CHI. At its optimal preparation condition, the QUE–CHI nanoplex exhibited a size of roughly 150 nm with a 25% QUE payload and 60% complexation efficiency. The complexation with CHI had no adverse effect on the antibacterial and anticancer activities of QUE, signifying the preservation of QUE’s bioactivities in the nanoplex. Compared to the native QUE, the QUE–CHI nanoplex exhibited superior QS inhibition in suppressing the QS-regulated swimming motility and biofilm formation of P. aeruginosa, but not in suppressing the virulence factor production. The superior inhibitions of the biofilm formation and swimming motility afforded by the nanoplex were attributed to (1) its higher kinetic solubility (5-times higher) that led to higher QUE exposures, and (2) the synergistic QS inhibition attributed to its CHI fraction.

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“…The resultant nanoplex suspension is then spray-dried or freeze-dried if the nanoplex is intended for oral solid dosage form. A wide range of drugs and PE have been successfully formulated into an amorphous nanoplex [ 16 , 17 , 18 , 19 , 20 , 21 , 22 ] and in vivo bioavailability enhancements have been demonstrated in several studies [ 23 , 24 , 25 , 26 ]. Importantly, the amorphous nanoplex fares well in benchmarking studies against ASD [ 27 , 28 ].…”

Section: Introductionmentioning

confidence: 99%

“…The CUR and CIP nanoplexes were prepared using chitosan (CHI) and sodium dextran sulfate (DXT) as the oppositely charged PEs, respectively. Polymer HPMC was incorporated into the nanoplexes to enhance their storage stability [ 17 , 18 ].…”

Section: Introductionmentioning

confidence: 99%

Benchmarking the Solubility Enhancement and Storage Stability of Amorphous Drug–Polyelectrolyte Nanoplex against Co-Amorphous Formulation of the Same Drug

2022

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Amorphization, typically in the form of amorphous solid dispersion (ASD), represents a well-established solubility enhancement strategy for poorly soluble drugs. Recently, two amorphous drug formulations, i.e., the amorphous drug–polyelectrolyte nanoparticle complex (nanoplex) and co-amorphous system, have emerged as promising alternatives to circumvent the issues faced by ASD (i.e., large dosage requirement, high hygroscopicity). In the present work, the nanoplex was benchmarked against the co-amorphous system in terms of the preparation efficiency, drug payload, thermal stability, dissolution rate, supersaturation generation, and accelerated storage stability. Weakly acidic curcumin (CUR) and weakly basic ciprofloxacin (CIP) were used as the model poorly soluble drugs. The CUR and CIP nanoplexes were prepared using chitosan and sodium dextran sulfate as the polyelectrolytes, respectively. The co-amorphous CUR and CIP were prepared using tannic acid and tryptophan as the co-formers, respectively. The benchmarking results showed that the amorphous drug nanoplex performed as well as, if not better than, the co-amorphous system depending on the drug in question and the aspects being compared. The present work successfully established the nanoplex as an equally viable amorphous drug formulation as the more widely studied co-amorphous system to potentially serve as an alternative to ASD.

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Enhancing the physical stability and supersaturation generation of amorphous drug-polyelectrolyte nanoparticle complex via incorporation of crystallization inhibitor at the nanoparticle formation step: A case of HPMC versus PVP

Cited by 12 publications

References 36 publications

Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition

Pharmaceutical assessment of polyvinylpyrrolidone (PVP): As excipient from conventional to controlled delivery systems with a spotlight on COVID-19 inhibition

A Potential Quorum-Sensing Inhibitor for Bronchiectasis Therapy: Quercetin–Chitosan Nanoparticle Complex Exhibiting Superior Inhibition of Biofilm Formation and Swimming Motility of Pseudomonas aeruginosa to the Native Quercetin

Benchmarking the Solubility Enhancement and Storage Stability of Amorphous Drug–Polyelectrolyte Nanoplex against Co-Amorphous Formulation of the Same Drug

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