Vicissitudes of liquid crystals for solubility enhancement of poorly soluble drugs

Shoaib, Ambreen; Mangla, Bharti; Javed, Shamama; Sultan, Muhammad H.; Alqahtani, Saad S.; Shakeel, Faiyaz

doi:10.1016/j.molliq.2020.114924

Cited by 17 publications

(4 citation statements)

References 62 publications

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“…Therefore, the greater the RSV concentration, the larger the particle size. The higher drug loading promoted a greater supersaturation degree during solvent evaporation, and thus the tendency towards crystal growth was induced [32]. This phenomenon was confirmed by the main effects' coefficient of drug loading.…”

Section: The Effect On Particle Sizementioning

confidence: 66%

Resveratrol Nanocrystal Incorporated into Mesoporous Material: Rational Design and Screening through Quality-by-Design Approach

et al. 2022

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Bioflavonoids from grape seeds feature powerful antioxidant and immunostimulant activities, but they present problems related to solubility and bioavailability. Nanocrystal (NC) incorporated into a mesoporous carrier is a promising strategy to address these issues. However, the preparation of this formulation involves the selection of factors affecting its critical quality attributes. Hence, this study aimed to develop an NC formulation incorporating resveratrol into a soluble mesoporous carrier based on rational screening design using a systematic and continuous development process, the quality-by-design paradigm. A mesoporous soluble carrier was prepared by spray-drying mannitol and ammonium carbonate. The NC was obtained by introducing the evaporated solvent containing a drug/polymer/surfactant and mesoporous carrier to the medium. A 26−2 fractional factorial design (FFD) approach was carried out in the screening process to understand the main effect factors. The type and concentration of polymer and surfactant, resveratrol loading, and solvent were determined on the NC characteristics. The results indicated that drug loading, particle size, and solubility were mainly affected by RSV loading, PEG concentration, and Kolliphor EL concentration. The polymer contributed dominantly to reducing the particle size and enhancing solubility in this screening design. The presence of surfactants in this system made it possible to prolong the supersaturation process. According to the 26−2 FFD, the factors selected to be further developed using a statistical technique according to the quality-by design-approach, Box Behnken Design, were Kolliphor EL, PEG400, and RSV loading.

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Section: The Effect On Particle Sizementioning

confidence: 66%

Resveratrol Nanocrystal Incorporated into Mesoporous Material: Rational Design and Screening through Quality-by-Design Approach

et al. 2022

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“…The percentage of water present in the system is the determining factor for the transition from the lamellar phase to the cubic phase, attributing to each phase the ability to exhibit liquid or crystalline solid properties. These distinctive physicochemical properties make LLCs suitable for solubilizing and delivering both oil- and water-soluble compounds [ 17 ].…”

Section: Resultsmentioning

confidence: 99%

In Situ Swelling Formulation of Glycerol-Monooleate-Derived Lyotropic Liquid Crystals Proposed for Local Vaginal Application

et al. 2022

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Hydrogels have been extensively investigated to identify innovative formulations that can fulfill all the necessary purposes to improve local vaginal therapy through the mucosa. Herein, we propose in situ-forming lyotropic liquid crystals (LLCs) derived from a cheap and GRAS (generally recognized as safe) ingredient as an intravaginal delivery system. The system consists of a precursor solution loaded with sertaconazole nitrate as a model drug, which is able to easily swell in a stable three-dimensional structure by absorbing simulated vaginal fluid. Under polarized light microscopy the precursor solution and the formed phase of LLCs showed the typical textures belonging to anisotropic and an isotropic mesophases, respectively. A deep rheological investigation by Kinexus® Pro proved the stability and strength of the cubic phase, as well as its potential in mucoadhesion. In vitro degradation studies showed a slow matrix erosion, consistent with data obtained from lipophilic drug release studies in simulated vaginal fluid. Therefore, the suggested cubic phase based on lyotropic liquid crystals could represent a valid proposal as a vaginal drug delivery system due to its characteristics of resistance, adhesion and the possibility of providing a slow and controlled release of drugs directly at the administration site.

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“…As a result, absorption is inadequate. The pharmaceutical business and researchers are therefore faced with difficulty as a result of the high demand for better products [1][2][3][4][5][6]. The bioavailability and, therefore, the effectiveness of medicinal drugs are directly influenced by their physicochemical qualities.…”

Section: Introductionmentioning

confidence: 99%

“…The bioavailability and, therefore, the effectiveness of medicinal drugs are directly influenced by their physicochemical qualities. Therefore, raising the dissolution profile is a difficult issue for researchers [1][2][3][4][5][6]. For improving oral bioavailability, several dissolution enhancement techniques for rifampicin and quercetin have been reported in the literature.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Optimization of Rifampicin and Quercetin Laden Liquisolid Compact: In-Vitro and In-Vivo Study

Tandel¹,

Patel²,

Thakkar³

et al. 2022

Int J Pharm Res Allied Sci

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The major objective of this study is to create rifampicin and quercetin-containing liquisolid compacts with improved gastrointestinal absorption and dissolving properties. Propylene glycol, PEG 200, and Tween 20 were chosen as ideal non-volatile liquid carriers to create the required formulations because of their increased drug solubility. In an attempt to create a free-flowing, compressible powder, the liquisolid formulations were then combined with a carrier and coating material. In order to create liquisolid powders with good flow qualities, Avicel pH-102, Aeroperl 200, and Aerosil 200 demonstrated good liquid retention potential values, demonstrating their efficiency as solid carrier and coating materials in the creation of liquisolid compacts. The medication and carrier had no discernible interaction, according to FT-IR spectra. The DSC and PXRD experiments proved that the crystalline form of the medication was absent from the liquisolid powders. Furthermore, the improved drug dissolving performance in liquisolid systems revealed that the drug had changed into a molecular or amorphous state. In-vivo rat pharmacokinetic investigations revealed the ability of non-volatile liquid carriers of liquisolid systems to enhance drug absorption from formulation and enhance the gastrointestinal absorption and dissolving rate of rifampicin and quercetin.

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Vicissitudes of liquid crystals for solubility enhancement of poorly soluble drugs

Cited by 17 publications

References 62 publications

Resveratrol Nanocrystal Incorporated into Mesoporous Material: Rational Design and Screening through Quality-by-Design Approach

Resveratrol Nanocrystal Incorporated into Mesoporous Material: Rational Design and Screening through Quality-by-Design Approach

In Situ Swelling Formulation of Glycerol-Monooleate-Derived Lyotropic Liquid Crystals Proposed for Local Vaginal Application

Formulation and Optimization of Rifampicin and Quercetin Laden Liquisolid Compact: In-Vitro and In-Vivo Study

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