Lipospheres for Simultaneous Controlled Release and Improved Pharmacokinetic Profiles of Saxagliptin-Enalapril: Formulation, Optimization, and Comparative In Vitro-In Vivo Evaluation

Maheen, Safirah; Rasul, Akhtar; Hanif, Muhammad; Khan, Hafeez Ullah

doi:10.1208/s12249-020-01733-w

Cited by 4 publications

(2 citation statements)

References 34 publications

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“…The release data were studied using different kinetic models which include zero-order, first-order, Higuchi diffusion, and Korsmeyer–Peppas models (Maheen et al., 2020 ). The highest coefficient of determination (R2) model was considered to represent the drug release mechanism.…”

Section: Characterization Of the Prepared Nano Ganciclovir Solid Disp...mentioning

confidence: 99%

Design and optimization of ganciclovir solid dispersion for improving its bioavailability

Gaber¹,

Alnwiser²,

Alotaibi³

et al. 2022

Drug Delivery

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Development of new approaches for oral delivery of an existing antiviral drug aimed to enhance its permeability and hence bioavailability. Ganciclovir (GC) is an antiviral drug that belongs to class III in biopharmaceutical classification. The encapsulation of poorly absorbed drugs within nanosized particles offers several characteristics to drug due to their acquired surface properties. In the following study, the solvent evaporation technique was used to incorporate GC, within elegant nanosize particles using cyclodextrin and shellac polymers for enhancing its permeability and release pattern. Formulation variables were optimized using 2 3 full factorial design. The prepared formulations were assessed for yield, particle size, content, and micromeritics behavior. The optimized formula (F6) was identified through differential scanning calorimetry and Fourier transform infrared. In vitro release and stability were also assessed. Pharmacokinetic parameters of optimized nano GC solid dispersion particles (NGCSD-F6) were finally evaluated. The optimized formula (F6) showed a mean particle size of 288.5 ± 20.7 nm, a zeta potential of about 23.87 ± 2.27, and drug content 95.77 ± 2.1%. The in vitro drug release pattern of F6 showed an initial burst release followed by a sustained release over the next 12 h. The optimized formula showed accepted stability upon storage at room and refrigerator temperatures for 6 months with good flowing properties (Carr’s index = 18.28 ± 0.44). In vivo pharmacokinetic study in rabbits revealed 2.2 fold increases in the bioavailability of GC compared with commercial convention tablets. The study affords evidence for the success of the solid dispersion technique under specified conditions in improvement of bioavailability of GC.

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Section: Characterization Of the Prepared Nano Ganciclovir Solid Disp...mentioning

confidence: 99%

Design and optimization of ganciclovir solid dispersion for improving its bioavailability

Gaber¹,

Alnwiser²,

Alotaibi³

et al. 2022

Drug Delivery

View full text Add to dashboard Cite

show abstract

“…In vitro release data were analyzed using linear regression equations of zero-order, first-order diffusion-controlled release mechanism, 34 Higuchi's model, 35 and Korsmeyer-Peppas kinetic model to determine the kinetics and the mechanism of the drug release. 36 The highest coefficient of determination (R 2 ) model was deemed to depict the drug release mechanism.…”

Section: Kinetic Analysis Of the Drug Release Datamentioning

confidence: 99%

Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments

Maghrabia¹,

Boughdady²,

Meshali³

2021

IJN

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Purpose: Development of new strategies for oral delivery of existing antibiotics administered exclusively through intravenous route is one of the global priorities of pharmaceutical research. The encapsulation of these active pharmaceutical agents within nanosized natural products offers several traits due to their tunable surface properties. Ceftriaxone (CTX) is an injectable, third-generation cephalosporin that suffers poor oral bioavailability. Methods: In the present study, ionic gelation of two biopolymers, namely chitosan (CH) and shellac (SH), was implemented to consolidate CTX, within elegant nanoparticles (NPs) for oral administration that would increase its bioavailability and sustainability. Quality by design approach (2 3 full factorial design) was adopted to optimize CTX-loaded nanoparticles. The optimized formula (F2) was characterized through transmission electron microscopy (TEM), Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC). In vitro release behavior and stability study were also evaluated. Pharmacokinetic studies of enteric-coated hard gelatin capsules (HGCs) loaded with F2-NPs were finally assessed. Results: The optimized spherical F2-NPs had a mean particle size of 258 nm, zeta potential of about +30.1 and appreciable drug entrapment efficiency of 83%. The in vitro drug release profile of F2-NPs in pH 7.4 experienced biphasic configuration with an initial burst release for an hour, followed by a sustained release over 15 h with Higuchi model and non-Fickian diffusion mechanism (R 2 =0.9852). High stability upon storage at refrigerated and room temperature for 3 months and good flow properties (θ= 32.2 and HR= 1.13) of the optimized formula were also conferred. In vivo pharmacokinetic assessment in rabbits fruitfully displayed 92% absolute bioavailability of CTX. Conclusion:The obtained results provide evidence for the potential combination of CH and SH in NPs preparation to enhance the oral bioavailability of CTX.

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An apprise on novel drug delivery systems for management of diabetes mellitus

Pardhi,

Bhor,

Singh

et al. 2024

Journal of Drug Delivery Science and Technology

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Lipospheres for Simultaneous Controlled Release and Improved Pharmacokinetic Profiles of Saxagliptin-Enalapril: Formulation, Optimization, and Comparative In Vitro-In Vivo Evaluation

Cited by 4 publications

References 34 publications

Design and optimization of ganciclovir solid dispersion for improving its bioavailability

Design and optimization of ganciclovir solid dispersion for improving its bioavailability

Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments

An apprise on novel drug delivery systems for management of diabetes mellitus

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