Stabilizing excipients for engineered clopidogrel bisulfate procubosome derived in situ cubosomes for enhanced intestinal dissolution: Stability and bioavailability considerations

El-Laithy, Hanan M.; Badawi, Alia; Abdelmalak, Nevine Shawky; Elsayyad, Nihal Mohamed Elmahdy

doi:10.1016/j.ejps.2019.06.008

Cited by 22 publications

(18 citation statements)

References 55 publications

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“…Our present study indicated that 734THIF, which belongs to BCS class II or IV, has poor water solubility, which might influence its pharmaceutical effect. Many drug delivery systems are used to improve the water solubility of lipophilic compounds, including microemulsions [37], cyclodextrin inclusion [18], nanoparticle formulations [38] and so on. HPBCD, a cyclodextrin with lipophilic inner cavities and hydrophilic outer surfaces, can interact with poorly soluble drugs to enhance drug solubility and stability [18].…”

Section: Discussionmentioning

confidence: 99%

Improvement of Skin Penetration, Antipollutant Activity and Skin Hydration of 7,3′,4′-Trihydroxyisoflavone Cyclodextrin Inclusion Complex

Huang

Yen

et al. 2019

Pharmaceutics

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As is known, many antioxidants from plant extracts have been used as additives in skincare products to prevent skin damage following overexposure to environmental pollutants. 7,3′,4′-trihydroxyisoflavone (734THIF), an isoflavone compound, possesses various biological activities, including antioxidant, antityrosinase, photodamage protection, and anticancer effects. Unfortunately, 734THIF has poor water solubility, which limits its skin penetration and absorption, and subsequently influences its biological activity. The aim of the present study was to investigate the mechanisms for the improvement in water solubility and skin penetration of 2-hydroxypropyl-β-cyclodextrin (HPBCD) inclusion complex with 734THIF (5-7HP). We also determined its photostability, antipollutant activity in HaCaT keratinocytes, and moisturizing effect in human subjects. Our results showed that 734THIF was embedded into the lipophilic inner cavity of HPBCD and its water solubility and skin penetration were thereby improved through amorphous transformation, surface area enhancement, and hydrogen bonding formation between 734THIF and HPBCD. In addition, 5-7HP inhibited PM-induced ROS generation and then downregulated ROS-mediated COX-2 and MMP9 production and AQP-3 consumption by inhibiting the phosphorylation of MAPKs. Consequently, we suggest that 5-7HP is a safe and photostable topical ingredient to enhance the skin penetration of 734THIF and skin hydration, and therefore 5-7HP may be used as an antipollutant additive in skin care products.

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Section: Discussionmentioning

confidence: 99%

Improvement of Skin Penetration, Antipollutant Activity and Skin Hydration of 7,3′,4′-Trihydroxyisoflavone Cyclodextrin Inclusion Complex

Huang

Yen

et al. 2019

Pharmaceutics

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“…A potential strategy that may possible to resolve the stability problem is pro-form formulations (proliposomes and procubosomes). Proliposomes and procubosomes are dry and free-flowing powders that could form liposomes and cubosomes by hydration with water, either through contact with physiological fluid or reconstitution right before administration, and thus can be stored for long time [72][73][74].…”

Section: Limitations Of Developed Formulations and Future Challengesmentioning

confidence: 99%

“…Proliposomes has proven able to improve drug compounds with poor solubility and bioavailability significantly in several studies [73][74][75][76]. However, there has been only one study on procubosome formulation to date [72]. Procubosome compressed into tablet form successfully improved the solubility of BCS class II drug clopidogrel and even obtained superior Cmax, Tmax, bioavailability, and antiplatelet activity, compared to commercial Plavix ®…”

Section: Limitations Of Developed Formulations and Future Challengesmentioning

confidence: 99%

Recent Strategies for Improving Solubility and Oral Bioavailability of Piperine

2021

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Piperine, the main bioactive compound found in black pepper (Piper nigrum L.), has long been used in Ayurveda and traditional Chinese medicine (TCM). This compound has remarkable potential pharmacological properties, including being anti-inflammatory, antimicrobial, anticancer, anticonvulsant, antidepressant, neuroprotective, and hepatoprotective. Recent studies have reported piperine activity as an antiviral against SARS-CoV-2, which caused COVID-19. Nevertheless, the clinical use of piperine is still limited, due to its poor water solubility and bioavailability; therefore, various approaches have been developed in order to solve these limitations. This review summarises recent studies (i.e. uploaded to electronic databases in the last 10 y) regarding strategies that have been investigated to improve piperine’s solubility and pharmacokinetic properties, using ‘piperine’, ‘solubility’, ‘bioavailability’, and ‘formulation’ as keywords. Articles that have focused on piperine as the main compound were selected and sorted based on their modification and formulation types. Studies reported various approaches: from derivatives and analogue synthesis, crystal engineering, complexation, particle size reduction (micro-and nanonisation), and lipid-and polymer-based drug delivery systems, to inorganic and hybrid nanoparticles. This review also highlights limitations and challenges for these approaches and encourages further studies to optimise piperine’s potential benefits.

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“…The release profiles of IND from CUB dispersions were evaluated by means of the dialysis method using cellulose acetate dialysis tubing (Spectra/Por with molecular cutoff 12,000-14,000 by Spectrum Laboratories Inc., Eindhoven, The Netherlands) sealed at both ends with clips [7,[14][15][16][17][18]. A phosphate buffer solution pH 6.8 containing 1% SLS to maintain sink conditions constantly shaken at 100 rpm and warmed to 37 ± 0.1•C was used as the release medium.…”

Section: In Vitro Drug Release Studiesmentioning

confidence: 99%

“…To date, drug delivery systems based on lipid carriers remain apparently one of the most important delivery systems to improve the oral absorption of poor-water soluble drugs. Recently, among these carriers is the cubosome (CUB) which have attracted much attention as promising versatile delivery system to encapsulate both hydrophilic and hydrophobic drugs, improve drug absorption and offer protection for drugs against degradation [7]. CUB is nanostructured liquid-crystalline particles, in a liquid-crystalline phase with cubic crystallographic symmetry formed by amphiphilic lipids which self-assemble into the complex three-dimensional cubic phase structure through the self-organization into bilayers around bicontinuous non-intersecting water channels.…”

Section: Introductionmentioning

confidence: 99%

Cubosomes Dispersions as Enhanced Indomethacin Oral Delivery Systems: In vitro and Stability Evaluation

Alfagih

AlQuadeib

Aldosari

et al. 2021

JPRI

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Aims: To improve the dissolution of indomethacin through developing liquid indomethacin loaded cubosomes dispersion for oral delivery. Methodology: Glyceryl monooleate based indomethacin loaded cubosomes dispersion were prepared using Taguchi design to study the effect of indomethacin to the disperse phase ratio and poloxamer 407 (PLX%) concentrations on the particle size and entrapment efficiency (%EE). Furthermore, in vitro release in phosphate buffer (pH 6.8), and morphology were investigated. Also, the stability of indomethacin loaded cubosomes dispersions was examined after 6 months storage at 25°C in the dark. Results: The prepared indomethacin cubosomes dispersions were in the nanoscale (184.53±0.7 to 261.33±0.8 nm) with reasonable %EE (49.30±2.6 to 95.55±3.4 %). Moreover, a biphasic release profile was predominant for all formulations, up to 50% of payload released after 2h followed by a second continuous sustained release phase over 24h. The kinetics of indomethacin release was best explained by Higuchi model and the mechanism of drug release from these cubosomes dispersions was by fickian diffusion mechanism. In general, the indomethacin loaded cubosomes dispersions were stable after 6 months storage at 25°C in the dark. Conclusion: Indomethacin loaded cubosomes dispersions proved to be a successful platform to encapsulate and enhance the release of indomethacin with a good stability profile over 6 months.

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Stabilizing excipients for engineered clopidogrel bisulfate procubosome derived in situ cubosomes for enhanced intestinal dissolution: Stability and bioavailability considerations

Cited by 22 publications

References 55 publications

Improvement of Skin Penetration, Antipollutant Activity and Skin Hydration of 7,3′,4′-Trihydroxyisoflavone Cyclodextrin Inclusion Complex

Improvement of Skin Penetration, Antipollutant Activity and Skin Hydration of 7,3′,4′-Trihydroxyisoflavone Cyclodextrin Inclusion Complex

Recent Strategies for Improving Solubility and Oral Bioavailability of Piperine

Cubosomes Dispersions as Enhanced Indomethacin Oral Delivery Systems: In vitro and Stability Evaluation

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