Fabrication, solid state characterization and bioavailability assessment of stable binary amorphous phases of Ritonavir with Quercetin

Dengale, Swapnil J.; Hussen, Syed Sajjad; Krishna, Bandarupalli; Musmade, Prashant B; Shenoy, Gautham G.; Bhat, Krishnamurthy

doi:10.1016/j.ejpb.2014.12.025

Cited by 70 publications

(30 citation statements)

References 34 publications

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“…GFA and fragility may be considered as an indicator of life expectancy of an ASD. 91 It has been suggested that crystallization is inversely related to the GFA of amorphous drugs, and GFA is defined as the ease with which materials can undergo vitrification on cooling. 92 Different methods are reported in the literature to measure the GFA of a drug compound such as reduced glass transition temperature (T rg ), cooling rate dependence, and the crossover point of the heating/cooling rate dependencies of the crystallization temperature.…”

Section: Crystallization Inhibitionmentioning

confidence: 99%

Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

Baghel

Cathcart

O’Reilly

2016

Journal of Pharmaceutical Sciences

786

452

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Poor water solubility of many drugs has emerged as one of the major challenges in the pharmaceutical world. Polymer-based amorphous solid dispersions have been considered as the major advancement in overcoming limited aqueous solubility and oral absorption issues. The principle drawback of this approach is that they can lack necessary stability and revert to the crystalline form on storage. Significant upfront development is, therefore, required to generate stable amorphous formulations. A thorough understanding of the processes occurring at a molecular level is imperative for the rational design of amorphous solid dispersion products. This review attempts to address the critical molecular and thermodynamic aspects governing the physicochemical properties of such systems. A brief introduction to Biopharmaceutical Classification System, solid dispersions, glass transition, and solubility advantage of amorphous drugs is provided. The objective of this review is to weigh the current understanding of solid dispersion chemistry and to critically review the theoretical, technical, and molecular aspects of solid dispersions (amorphization and crystallization) and potential advantage of polymers (stabilization and solubilization) as inert, hydrophilic, pharmaceutical carrier matrices. In addition, different preformulation tools for the rational selection of polymers, state-of-the-art techniques for preparation and characterization of polymeric amorphous solid dispersions, and drug supersaturation in gastric media are also discussed.

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Section: Crystallization Inhibitionmentioning

confidence: 99%

Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

Baghel

Cathcart

O’Reilly

2016

Journal of Pharmaceutical Sciences

786

452

View full text Add to dashboard Cite

show abstract

“…Third, the temperature stability of BG phases can be attributed to the intermolecular mainly hydrogen bonding interactions between TLN and NRG (as proved in the earlier section 3.2). Intermolecular interactions have previously been reported as contributing factor for stability of BG systems [9, 11,13]. The molecular mobility can be restricted by such intermolecular interactions due to which BG systems become endurable physically.…”

Section: Physical Stabilitymentioning

confidence: 99%

“…There is an increased interest in the binary glassy materials containing two small molecules, due to the disadvantages of solid dispersion technology which includes system tackiness, phase separation, reduced glass transition temperature due to hygroscopicity [9][10][11][12][13][14][15][16]. It uses small molecules as a stabilizing agent instead of using polymers, which is devoid of problems faced by solid dispersion technology.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous improvement of solubility and permeability by fabricating binary glassy materials of Talinolol with Naringin: Solid state characterization, in-vivo in-situ evaluation

Teja

Musmade

Khade

et al. 2015

European Journal of Pharmaceutical Sciences

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“…The oral bioavailability of QUT is <17% in rats and ~1% in humans [ 5 , 6 ]; this low bioavailability would be a consequence of QUT's lipophilic character. QUT which exhibited poor water solubility, low permeation, and short biological half-life was classified as a class IV compound according to the Biopharmaceutical Classification System [ 7 , 8 ]. Therefore, there is a need to improve the oral bioavailability of QUT in the further study and application of QUT.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of Quercetin-Loaded Methoxy Poly(ethylene glycol)-b-poly(L-lactic acid) Micelle after Oral Administration in Rats

Liu

et al. 2017

BioMed Research International

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The purpose of this study was to evaluate the potential of micelle to change the pharmacokinetics of quercetin (QUT), with a primary goal of enhancing its oral bioavailability. QUT-loaded methoxy poly(ethylene glycol)-b-poly(L-lactic acid) micelle (QUT-loaded MPEG-b-PLLA micelle) was prepared by a thin-film hydration method, resulting in a particle size of 88.5 nm. A liquid chromatography tandem-mass spectrometry (LC-MS/MS) method was developed and validated for determination of QUT in rat plasma. The chromatographic separation was performed on an Agilent Eclipse-C18 (4.6 mm × 50 mm, 3.5 μm) with an isocratic mobile phase system consisting of water and methanol (30 : 70, v/v) at a flow rate of 0.4 mL/min. Calibration curves were linear over the concentration ranges of 2.5–2000 ng/mL for QUT. The micelle was orally administered at a single does in rats, and the pharmacokinetic parameters were evaluated and compared with that administered with the QUT aqueous suspension. The results show that the micelle was able to increase the QUT's oral bioavailability 9-fold compared to the QUT aqueous suspension. These results suggest that methoxy poly(ethylene glycol)-b-poly(L-lactic acid) is a potential carrier for the oral delivery of QUT.

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Fabrication, solid state characterization and bioavailability assessment of stable binary amorphous phases of Ritonavir with Quercetin

Cited by 70 publications

References 34 publications

Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

Simultaneous improvement of solubility and permeability by fabricating binary glassy materials of Talinolol with Naringin: Solid state characterization, in-vivo in-situ evaluation

Pharmacokinetics of Quercetin-Loaded Methoxy Poly(ethylene glycol)-b-poly(L-lactic acid) Micelle after Oral Administration in Rats

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