Voriconazole Cyclodextrin Based Polymeric Nanobeads for Enhanced Solubility and Activity: In Vitro/In Vivo and Molecular Simulation Approach

Farooq, Mudassir; Usman, Faisal; Naseem, Mahrukh; Aati, Hanan Y.; Ahmad, Hafiz Badaruddin; Manee, Sirikhwan; Khalil, Ruqaiya; Khan, Kashif-ur-Rehman; Qureshi, Muhammad Imran; Umair, Muhammad

doi:10.3390/pharmaceutics15020389

Cited by 9 publications

(3 citation statements)

References 44 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The thermal properties of MA and HP-β-CD/MA microcapsules were determined using TAQ2000 (Waters, Framingham, MA, USA) differential scanning calorimeter [ 28 ]. A total of 4 mg of sample was placed onto the sample tray and heated from 30 °C to 300 °C at a rate of 10/min in the nitrogen environment.…”

Section: Methodsmentioning

confidence: 99%

Preparation and Embedding Characterization of Hydroxypropyl-β-cyclodextrin/Menthyl Acetate Microcapsules with Enhanced Stability

et al. 2023

View full text Add to dashboard Cite

Objective: Hydroxypropyl-β-cyclodextrin (HP-β-CD)/menthyl acetate (MA) microcapsules were developed to overcome the volatile and unstable defects of MA and improve the ease of use and storage. Methods: MA microcapsules were prepared via spray drying using HP-β-CD as the wall material. The embedding rate of MA microcapsules was determined through gas chromatography. The embedding characteristics were studied using phase solubility and nuclear magnetic resonance (NMR). The stability was characterized via differential scanning calorimetry (DSC) and the release and retention rates of MA microcapsules at different temperatures. Results: The embedding rate of HP-β-CD /MA microcapsules was 96.3%. The Gibbs free energy change, enthalpy change and entropy change of the embedding reaction between HP-β-CD and MA were all less than zero, indicating that the embedding process was a spontaneous exothermic reaction. NMR spectra showed that MA entered the cavity of HP-β-CD through the large opening end and interacted with the inner wall of the small opening end. DSC and the release and retention rates of MA microcapsules at different temperatures showed that the stability of MA was significantly enhanced after being embedded in HP-β-CD. Conclusion: The HP-β-CD/MA microcapsules are able to significantly improve the stability of MA and reduce the volatilization of MA.

show abstract

Section: Methodsmentioning

confidence: 99%

Preparation and Embedding Characterization of Hydroxypropyl-β-cyclodextrin/Menthyl Acetate Microcapsules with Enhanced Stability

et al. 2023

View full text Add to dashboard Cite

show abstract

“…Farooq M. et al demonstrated that by complexing voriconazole with HP-β-CD, no acute toxicity phenomena were observed after oral administration in experimental animals [ 43 ]. Another study investigated the clinical effects of voriconazole complexed with SBE-β-CD administered intravenously in 25 human patients with invasive aspergillosis.…”

Section: Benefits Of Inclusion Complexes (Cd–antifungal) In Antifunga...mentioning

confidence: 99%

Short Review on the Biological Activity of Cyclodextrin-Drug Inclusion Complexes Applicable in Veterinary Therapy

et al. 2023

View full text Add to dashboard Cite

Cyclodextrins (CDs) are a family of carrier molecules used to improve the pharmacokinetic parameters of therapeutic molecules. These cyclic oligosaccharides have medical and pharmaceutical applications by being able to form inclusion complexes with molecules that are poorly soluble in water. The benefits of these complexes are directed towards improving the chemical and biological properties—i.e., solubility, bioavailability, stability, non-toxicity and shelf life of drug molecules. Since the 1960s, the first inclusion complexes used in therapeutics were those with α-, β- and γ-CD, which proved their usefulness, but had certain degrees of particularly renal toxicity. Currently, to correct these deficiencies, β-CD derivatives are most frequently used, such as sulfobutylether-β-CD, hydroxypropyl-β-CD, etc. Therefore, it is of interest to bring to the attention of those interested the diversity of current and potential future clinical applications of inclusion complexes in veterinary medicine and to present the contribution of these inclusion complexes in improving drug efficacy. The most important biological activities of β-CD complexed molecules in the veterinary field are summarized in this short review.

show abstract

“…At predefined intervals (0.5 to 12 h), the sample solution was removed from the receptor compartment and replaced with PBS. Finally, the absorption of samples was measured by uv/vis spectrophotometer (PerkinElmer Lambda 35, Riegelsville, PA, USA) at 229 nm, and different parameters such as permeation flux and enhancement ratio were calculated using Equations ( 4)-( 6) [37].…”

Section: Ex Vivo Skin Permeationmentioning

confidence: 99%

Sulconazole-Loaded Solid Lipid Nanoparticles for Enhanced Antifungal Activity: In Vitro and In Vivo Approach

Samee,

Usman,

Wani

et al. 2023

Molecules

Self Cite

View full text Add to dashboard Cite

Solid lipid nanoparticles (SLNs) have the advantages of a cell-specific delivery and sustained release of hydrophobic drugs that can be exploited against infectious diseases. The topical delivery of hydrophobic drugs needs pharmaceutical strategies to enhance drug permeation, which is a challenge faced by conventional formulations containing a drug suspended in gel, creams or ointments. We report the fabrication and optimization of SLNs with sulconazole (SCZ) as a model hydrophobic drug and then a formulation of an SLN-based topical gel against fungal infections. The SLNs were optimized through excipients of glyceryl monostearate and Phospholipon® 90 H as lipids and tween 20 as a surfactant for its size, drug entrapment and sustained release and resistance against aggregation. The SCZ-SLNs were physically characterized for their particle size (89.81 ± 2.64), polydispersity index (0.311 ± 0.07), zeta potential (−26.98 ± 1.19) and encapsulation efficiency (86.52 ± 0.53). The SCZ-SLNs showed sustained release of 85.29% drug at the 12 h timepoint. The TEM results demonstrated spherical morphology, while DSC, XRD and FTIR showed the compatibility of the drug inside SLNs. SCZ-SLNs were incorporated into a gel using carbopol and were further optimized for their rheological behavior, pH, homogeneity and spreadability on the skin. The antifungal activity against Candida albicans and Trichophyton rubrum was increased in comparison to a SCZ carbopol-based gel. In vivo antifungal activity in rabbits presented faster healing of skin fungal infections. The histopathological examination of the treated skin from rabbits presented restoration of the dermal architecture. In summary, the approach of formulating SLNs into a topical gel presented an advantageous drug delivery system against mycosis.

show abstract

Voriconazole Cyclodextrin Based Polymeric Nanobeads for Enhanced Solubility and Activity: In Vitro/In Vivo and Molecular Simulation Approach

Cited by 9 publications

References 44 publications

Preparation and Embedding Characterization of Hydroxypropyl-β-cyclodextrin/Menthyl Acetate Microcapsules with Enhanced Stability

Preparation and Embedding Characterization of Hydroxypropyl-β-cyclodextrin/Menthyl Acetate Microcapsules with Enhanced Stability

Short Review on the Biological Activity of Cyclodextrin-Drug Inclusion Complexes Applicable in Veterinary Therapy

Sulconazole-Loaded Solid Lipid Nanoparticles for Enhanced Antifungal Activity: In Vitro and In Vivo Approach

Contact Info

Product

Resources

About