Host-guest complex of β-cyclodextrin and pluronic F127 with Luteolin: Physicochemical characterization, anti-oxidant activity and molecular modeling studies

Alshehri, Sultan; Imam, Syed Sarim; Altamimi, Mohammad A.; Jafar, Mohammed; Hassan, Mohd. Zaheen; Hussain, Afzal; Ahad, Abdul; Mahdi, Wael A.

doi:10.1016/j.jddst.2019.101356

Cited by 28 publications

(25 citation statements)

References 35 publications

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“…used PIP TIC (MI) showed greater release than PIP TIC (SE). The application of microwave gives the production of uniform heat to the sample at the same rate and gives better intimate contact between PIP, TPGS, and HP- β CD [ 6 , 29 ].…”

Section: Resultsmentioning

confidence: 99%

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Formulation and Evaluation of Supramolecular Food-Grade Piperine HP β CD and TPGS Complex: Dissolution, Physicochemical Characterization, Molecular Docking, In Vitro Antioxidant Activity, and Antimicrobial Assessment

et al. 2020

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The purpose of the present study was to improve the aqueous solubility, dissolution, and antioxidant activity of the water-insoluble drug piperine (PIP). The study was performed by preparing PIP binary inclusion complex (PIP BIC) and piperine ternary inclusion complex (PIP TIC) by different methods. The effect of a hydrophilic auxiliary substance (TPGS) was assessed with addition to PIP and hydroxypropyl beta cyclodextrin (HP β CD) complex. The phase solubility study was performed to evaluate the complexation efficiency and stability constant. The aqueous solubility, dissolution, physicochemical assessment, antioxidant activity, antimicrobial activity, and molecular docking were further evaluated to check the effect of the complexation of PIP. The stability constant (Ks) value was found to be 238 and 461 M−1 for the binary and ternary inclusion complex. The dissolution study results showed a marked enhancement of release in comparison to pure drug. XRD and SEM studies revealed the presence of more agglomerated and amorphous structures of PIP, which confirmed the formation of complexes. The results of DPPH radical scavenging and antimicrobial activity showed a significant (p < 0.05) enhancement in scavenging activity for PIP TIC (microwave irradiation (MI)). The docking studies have revealed that the binding affinity of TPGS at the PIP-HP β CD complex was −5.2 kcal/mol.

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Section: Resultsmentioning

confidence: 99%

“…CDs have an internal hydrophobic cavity and an outer hydrophilic surface. It forms the inclusion complex with different hydrophobic guest molecules by hydrophobic interaction in aqueous solution [ 6 ]. The formed inclusion complex enhances the solubility by several orders of magnitude in comparison to a pure drug.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Supramolecular Food-Grade Piperine HP β CD and TPGS Complex: Dissolution, Physicochemical Characterization, Molecular Docking, In Vitro Antioxidant Activity, and Antimicrobial Assessment

et al. 2020

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“…The complete chromatogram was obtained over a run time of 8 min. The drug was analyzed using a UV detector at an absorption wavelength of 350 nm [ 7 , 13 ]. A standard calibration curve was obtained over a range of 20.0–100 µg/mL with a regression coefficient correlation (r 2 ) of 0.99.…”

Section: Analysis Methodsmentioning

confidence: 99%

“…The drug has been reported to have low oral bioavailability (<30%) in a rat model [ 9 , 10 ]. Several reports have been published to improve the solubility, efficacy, and systemic availability of the drug by tailoring it as a nanoemulsion, liposome, self-nanoemulsifying drug delivery system (SNEDDS), solid dispersion, solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs) [ 8 , 11 , 12 , 13 , 14 , 15 ].…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluations of Transdermally Delivered Luteolin Loaded Cationic Nanoemulsion: In Vitro and Ex Vivo Evaluations

et al. 2021

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Introduction: Luteolin (LUT) is natural flavonoid with multiple therapeutic potentials and is explored for transdermal delivery using a nanocarrier system. LUT loaded cationic nanoemulsions (CNE1–CNE9) using bergamot oil (BO) were developed, optimized, and characterized in terms of in vitro and ex vivo parameters for improved permeation. Materials and methods: The solubility study of LUT was carried out in selected excipients, namely BO, cremophor EL (CEL as surfactant), labrasol (LAB), and oleylamine (OA as cationic charge inducer). Formulations were characterized with globular size, polydispersity index (PDI), zeta potential, pH, and thermodynamic stability studies. The optimized formulation (CNE4) was selected for comparative investigations (% transmittance as %T, morphology, chemical compatibility, drug content, in vitro % drug release, ex vivo skin permeation, and drug deposition, DD) against ANE4 (anionic nanoemulsion for comparison) and drug suspension (DS). Results: Formulations such as CNE1–CNE9 and ANE4 (except CNE6 and CNE8) were found to be stable. The optimized CNE4 based on the lowest value of globular size (112 nm), minimum PDI (0.15), and optimum zeta potential (+26 mV) was selected for comparative assessment against ANE4 and DS. The %T values of CNE1–CNE9 were found to be ˃95% and CEL content slightly improved the %T value. The spherical CNE4 was compatible with excipients and showed % total drug content in the range of 97.9–99.7%. In vitro drug release values from CNE4 and ANE4 were significantly higher than DS. Moreover, permeation flux (138.82 ± 8.4 µg/cm2·h), enhancement ratio (8.23), and DD (10.98%) were remarkably higher than DS. Thus, ex vivo parameters were relatively high as compared to DS which may be attributed to nanonization, surfactant-mediated reversible changes in skin lipid matrix, and electrostatic interaction of nanoglobules with the cellular surface. Conclusion: Transdermal delivery of LUT can be a suitable alternative to oral drug delivery for augmented skin permeation and drug deposition.

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“…The PS and PDI of a nanosuspension can be altered by adding different stabilizers in the crystallization milieu. 38,39 As suggested in Figure 2E, under identical preparation conditions, the use of charged stabilizers (SDS or sodium deoxycholate) can effectively reduce PS and PDI of ETO nanosuspension. However, the addition of polymers such as Pluronic 127, PVP K30, CMC-Na, PVA 217, TPGS, Pluronic F68 or PEG-2000 could not reduce PS and PDI of ETO nanosuspension.…”

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confidence: 93%

<p>Etoposide Amorphous Nanopowder for Improved Oral Bioavailability: Formulation Development, Optimization, in vitro and in vivo Evaluation</p>

Wang

et al. 2020

IJN

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Introduction: Etoposide refers to a derivative of podophyllotoxin, which plays an important role in the treatment of cancer due to its prominent anti-tumor effect. As a BCS IV drug, etoposide exhibits insufficient aqueous solubility and permeability, thereby limiting its oral absorption. To enhance the oral bioavailability of etoposide, this study developed an amorphous nanopowder. Methods: Based on preliminary screening and experimental design, the stabilizer and preparation process of etoposide nanosuspension were explored. Subsequently, using a Box-Behnken design, the effects of independent factors (ultrasonication time, ratio of two phases and stabilizer concentration) on response variables (particle size and polydispersity index) were studied, and then the formulation was optimized. Finally, nanosuspension was further freeze dried with 1% of mannitol resulting in the formation of etoposide amorphous nanopowder. Results: The optimized etoposide nanopowder showed as spherical particles with an average particle size and polydispersity index of 211.7 ± 10.4 nm and 0.125 ± 0.028. X-ray powder diffraction and differential scanning calorimetry confirmed the ETO in the nanopowder was amorphous. Compared with coarse powder and physical mixture, etoposide nanopowder achieved significantly enhanced saturated solubility and dissolution in various pH environments. The C max and AUC 0-t of etoposide nanopowder after oral administration in rats were respectively 2.21 and 2.13 times higher than the crude etoposide suspension. Additionally, the T max value of nanopowder was 0.25 h, compared with 0.5 h of reference group. Discussion: In the present study, the optimized amorphous nanopowder could significantly facilitate the dissolution and oral absorption of etoposide and might act as an effective delivery method to enhance its oral bioavailability.

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Host-guest complex of β-cyclodextrin and pluronic F127 with Luteolin: Physicochemical characterization, anti-oxidant activity and molecular modeling studies

Cited by 28 publications

References 35 publications

Formulation and Evaluation of Supramolecular Food-Grade Piperine HP β CD and TPGS Complex: Dissolution, Physicochemical Characterization, Molecular Docking, In Vitro Antioxidant Activity, and Antimicrobial Assessment

Formulation and Evaluation of Supramolecular Food-Grade Piperine HP β CD and TPGS Complex: Dissolution, Physicochemical Characterization, Molecular Docking, In Vitro Antioxidant Activity, and Antimicrobial Assessment

Development and Evaluations of Transdermally Delivered Luteolin Loaded Cationic Nanoemulsion: In Vitro and Ex Vivo Evaluations

<p>Etoposide Amorphous Nanopowder for Improved Oral Bioavailability: Formulation Development, Optimization, in vitro and in vivo Evaluation</p>

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