Comparison of the Use of Kinetic Model Plots and DD Solver Software to Evaluate the Drug Release from Griseofulvin Tablets

Ekenna, Ifeoma Cynthia; Abali, Sunday Okorie

doi:10.22270/jddt.v12i2-s.5402

Cited by 20 publications

(15 citation statements)

References 20 publications

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“…When b = 1, the shape of the release profile is exponential, when b < 1 (such as in our case), a parabolic release behavior occurs, and b > 1 predicts a sigmoidal form for the release profile . For a parabolic release profile, such as for our data, the rate of drug release reduces as time increases …”

Section: Discussionsupporting

confidence: 52%

“…43 For a parabolic release profile, such as for our data, the rate of drug release reduces as time increases. 44 Our dual functioning platform was used along with a differentiated human leukemia-60 cell line model to study the variations in neutrophil infection-fighting capacities, including phagocytosis, bacterial elimination, ROS, and NET production in response to oxygen abundance and antibiotic delivery. To induce antibacterial functions, HL-60s need to differentiate into phagocytic neutrophils through a series of chemical cues.…”

Section: Discussionmentioning

confidence: 99%

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Modulatory Contribution of Oxygenating Hydrogels and Polyhexamethylene Biguanide on the Antimicrobial Potency of Neutrophil-like Cells

Abri

Attia

Pukale

et al. 2022

ACS Biomater. Sci. Eng.

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Neutrophils are a first line of host defense against infection and utilize a series of oxygen-dependent processes to eliminate pathogens. Research suggests that oxygen availability can improve anti-infective mechanisms by promoting the formation of reactive oxygen species. Also, oxygen can synergistically upregulate the antibacterial properties of certain antibiotics against bacteria by altering their metabolism and causing an increase in the antibiotic uptake of bacteria. Therefore, understanding the effects of oxygen availability, as provided via a biomaterial treatment alone or along with potent antibacterial agents, on neutrophil functions can lead us to the development of new anti-inflammatory and anti-infective approaches. However, the study of neutrophil functions in vitro is often limited by their short life span and nonreproducibility, which suggests the need for cell line-based models as a substitute for primary neutrophils. Here, we took advantage of the differentiated human leukemia-60 cell line (HL-60), as an in vitro neutrophil model, to test the effects of local oxygen and antibacterial delivery by fluorinated methacrylamide chitosan (MACF) hydrogels incorporated with polyhexamethylene biguanide (PHMB) antibacterial agent. Considering the natural modes of neutrophil actions to combat bacteria, we studied the impact of our dual functioning oxygenating-antibacterial platforms on neutrophil phagocytosis and antibacterial properties as well as the formation of neutrophil extracellular traps (NETs) and reactive oxygen species (ROS). Our results demonstrated that supplemental oxygen and antibacterial delivery from MACF–PHMB hydrogel platforms upregulated neutrophil antibacterial properties and ROS production. NET formation by neutrophils upon treatment with MACF and PHMB varied when chemical and biological stimuli were used. Overall, this study presents a model to study immune responses in vitro and lays the foundation for future studies to investigate if similar responses also occur in vivo.

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Section: Discussionsupporting

confidence: 52%

Section: Discussionmentioning

confidence: 99%

Modulatory Contribution of Oxygenating Hydrogels and Polyhexamethylene Biguanide on the Antimicrobial Potency of Neutrophil-like Cells

Abri

Attia

Pukale

et al. 2022

ACS Biomater. Sci. Eng.

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“…The second equation showed a diffusional release exponent parameter, indicated with n , which was 0.414. This suggests a quasi-Fickian diffusion profile (when n < 0.45) of MEL release [ 64 ]. Regarding the in vitro RSV release, this was best described by Korsmeyer–Peppas equation (R 2 = 0.9736) with n = 0.084, indicating again a quasi-Fickian diffusion profile [ 64 ].…”

Section: Resultsmentioning

confidence: 99%

Formulating Resveratrol and Melatonin Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Ocular Administration Using Design of Experiments

Zingale,

Bonaccorso,

D’Amico

et al. 2024

Pharmaceutics

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Recent studies have demonstrated that Sirtuin-1 (SIRT-1)-activating molecules exert a protective role in degenerative ocular diseases. However, these molecules hardly reach the back of the eye due to poor solubility in aqueous environments and low bioavailability after topical application on the eye’s surface. Such hindrances, combined with stability issues, call for the need for innovative delivery strategies. Within this context, the development of self-nanoemulsifying drug delivery systems (SNEDDS) for SIRT-1 delivery can represent a promising approach. The aim of the work was to design and optimize SNEDDS for the ocular delivery of two natural SIRT-1 agonists, resveratrol (RSV) and melatonin (MEL), with potential implications for treating diabetic retinopathy. Pre-formulation studies were performed by a Design of Experiment (DoE) approach to construct the ternary phase diagram. The optimization phase was carried out using Response Surface Methodology (RSM). Four types of SNEDDS consisting of different surfactants (Tween® 80, Tween® 20, Solutol® HS15, and Cremophor® EL) were optimized to achieve the best physico-chemical parameters for ocular application. Stability tests indicated that SNEDDS produced with Tween® 80 was the formulation that best preserved the stability of molecules, and so it was, therefore, selected for further technological studies. The optimized formulation was prepared with Capryol® PGMC, Tween® 80, and Transcutol® P and loaded with RSV or MEL. The SNEDDS were evaluated for other parameters, such as the mean size (found to be ˂50 nm), size homogeneity (PDI < 0.2), emulsion time (around 40 s), transparency, drug content (>90%), mucoadhesion strength, in vitro drug release, pH and osmolarity, stability to dilution, and cloud point. Finally, an in vitro evaluation was performed on a rabbit corneal epithelial cell line (SIRC) to assess their cytocompatibility. The overall results suggest that SNEDDS can be used as promising nanocarriers for the ocular drug delivery of RSV and MEL.

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“…Estimates for β ≤ 0.75 indicate Fickian diffusion, while anomalous and Case II transport are associated with β values in the range of 0.75 < β < 1. For values of β higher than 1, the drug transport follows a super Case II transport [ 44 ]. In the case of pH 1.2–6.8, besides OA, β values for all the formulations were higher than 1, which corresponded to super Case II transport.…”

Section: Resultsmentioning

confidence: 99%

Thymol-Modified Oleic and Linoleic Acids Encapsulated in Polymeric Nanoparticles: Enhanced Bioactivity, Stability, and Biomedical Potential

Sokol,

Sokhraneva,

Groza

et al. 2023

Polymers

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Unsaturated fatty acids, such as oleic acid (OA) and linoleic acid (LA), are promising antimicrobial and cytostatic agents. We modified OA and LA with thymol (TOA and TLA, respectively) to expand their bioavailability, stability, and possible applications, and encapsulated these derivatives in polymeric nanoparticles (TOA-NPs and TLA-NPs, respectively). Prior to synthesis, we performed mathematical simulations with PASS and ADMETlab 2.0 to predict the biological activity and pharmacokinetics of TOA and TLA. TOA and TLA were synthesized via esterification in the presence of catalysts. Next, we formulated nanoparticles using the single-emulsion solvent evaporation technique. We applied dynamic light scattering, Uv-vis spectroscopy, release studies under gastrointestinal (pH 1.2–6.8) and blood environment simulation conditions (pH 7.4), and in vitro biological activity testing to characterize the nanoparticles. PASS revealed that TOA and TLA have antimicrobial and anticancer therapeutic potential. ADMETlab 2.0 provided a rationale for TOA and TLA encapsulation. The nanoparticles had an average size of 212–227 nm, with a high encapsulation efficiency (71–93%), and released TOA and TLA in a gradual and prolonged mode. TLA-NPs possessed higher antibacterial activity against B. cereus and S. aureus and pronounced cytotoxic activity against MCF-7, K562, and A549 cell lines compared to TOA-NPs. Our findings expand the biomedical application of fatty acids and provide a basis for further in vivo evaluation of designed derivatives and formulations.

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Comparison of the Use of Kinetic Model Plots and DD Solver Software to Evaluate the Drug Release from Griseofulvin Tablets

Cited by 20 publications

References 20 publications

Modulatory Contribution of Oxygenating Hydrogels and Polyhexamethylene Biguanide on the Antimicrobial Potency of Neutrophil-like Cells

Modulatory Contribution of Oxygenating Hydrogels and Polyhexamethylene Biguanide on the Antimicrobial Potency of Neutrophil-like Cells

Formulating Resveratrol and Melatonin Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Ocular Administration Using Design of Experiments

Thymol-Modified Oleic and Linoleic Acids Encapsulated in Polymeric Nanoparticles: Enhanced Bioactivity, Stability, and Biomedical Potential

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