Linseed hydrogel based floating drug delivery system for fluoroquinolone antibiotics: Design, in vitro drug release and in vivo real-time floating detection

Sheikh, Fatima Akbar; Hussain, Muhammad Ajaz; Ashraf, Muhammad; Haseeb, Muhammad Tahir; Farid-ul-Haq, Muhammad

doi:10.1016/j.jsps.2020.03.005

Cited by 26 publications

(10 citation statements)

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“…Nevertheless, for other hydrogel drug delivery systems destined to be implanted and/or used to release a drug locally; often, the drug quantity per sample is in the sub-milligram range [94,125]. This could explain why the dissolution apparatus setup, however useful, may not be suitable to study the release of such smaller-scale systems [64,65].…”

Section: Release Media Volumementioning

confidence: 99%

“…The release studies were comprehensive in terms of pH, but the release media could have been elaborated more, i.e., containing gastrointestinal enzymes for the pH 1.2 and 6.8 or using plasma for the release at pH 7.4 [102]. The dissolution apparatus (Figure 3) is the best manner to precisely control the experimental parameters, and the usage of USP-defined release media to thoroughly mimic the release in the gastrointestinal tract (GIT) ensures the best possible predictions of in vivo release [65]. For hydrogel drug delivery systems that are to be implanted in areas other than the intestinal or gastric environment, the physiological pH of the study in most healthy areas is 7.4.…”

Section: Phmentioning

confidence: 99%

“…Consequently, it is not well-suited to model the drug release for hydrogel drug delivery systems [114]. When the Peppas model indicates that the release is the result of an "anomalous transport" (0.43 < n < 0.89), diffusion exponent n values closer to 0.43 indicate that the release is closer to a diffusionbased release, whereas n values closer to 0.89 suggest that the swelling mechanism dominates [64,65,102]. On the other hand, values around 1 corresponded to a case II characteristic of a zero-order kinetic, and release is usually swelling or erosion controlled [64].…”

Section: Release Kinetics and Mathematical Modelingmentioning

confidence: 99%

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Hydrogels as Drug Delivery Systems: A Review of Current Characterization and Evaluation Techniques

et al. 2020

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Owing to their tunable properties, controllable degradation, and ability to protect labile drugs, hydrogels are increasingly investigated as local drug delivery systems. However, a lack of standardized methodologies used to characterize and evaluate drug release poses significant difficulties when comparing findings from different investigations, preventing an accurate assessment of systems. Here, we review the commonly used analytical techniques for drug detection and quantification from hydrogel delivery systems. The experimental conditions of drug release in saline solutions and their impact are discussed, along with the main mathematical and statistical approaches to characterize drug release profiles. We also review methods to determine drug diffusion coefficients and in vitro and in vivo models used to assess drug release and efficacy with the goal to provide guidelines and harmonized practices when investigating novel hydrogel drug delivery systems.

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Section: Release Media Volumementioning

confidence: 99%

Section: Phmentioning

confidence: 99%

Section: Release Kinetics and Mathematical Modelingmentioning

confidence: 99%

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Hydrogels as Drug Delivery Systems: A Review of Current Characterization and Evaluation Techniques

et al. 2020

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“…At pH 6.8, due to substantially reduced swelling of the floating tablets, the observed drug release was unpredictable. This might be due to the fact that metronidazole, being weakly basic drug, remained unionized at higher pH value, leading to obvious reduced solubility, thus resulting into unpredictable drug release [ 54 ]. To note the effect of osmotic pressure on release studies, optimized formulations were exposed to media having different osmotic pressures.…”

Section: Discussionmentioning

confidence: 99%

Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of H. pylori: Preparation and In Vitro Characterization

et al. 2022

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Metronidazole has the potential to produce local stomach specific action in order to treat Helicobacter pylori induced peptic ulcer disease. The current project executes the development of osmotically controlled bioadhesive metronidazole loaded effervescent floating tablets with optimized floating and swelling behavior. Direct compression technique was used to prepare the tablets. The designed formulations exhibited physico-chemical properties within acceptable optimum limits as per pharmacopeial requirements. The results of tablet floating studies revealed that all formulations, except F1 and F5, had good buoyancy characteristics (TFT > 12 h except F2 and F8 with TFT of 6 h). Formulation F2 containing guar gum in higher concentration with carbopol and formulation F8 containing guar gum in 50% decreased concentration in combination with HPMC and carbopol had enhanced FLT appreciably, with least TFT as compared to formulations F3, F4, and F6 (ANOVA; p ≤ 0.05). Formulation batches of F3, F4, and F6 exhibited appreciable FLT as well as TFT and were optimized formulations. Out of the above mentioned optimized batches, F4 and F6 formulations showed low FLT (4 and 5 s respectively). The results of the swelling study indicated a proportionate increase in the swelling index with increase in time. A significantly higher swelling ratio was found with formulation F6 and F4 compared with that of F7 and F8 (ANOVA; p ≤ 0.05). Additionally, the impact of pH change, agitational intensity, as well as increasing concentration of NaCl was investigated on drug release. It was observed that agitational intensity had no effect on drug release rate while increasing concentration of NaCl produced an increased drug release from the dosage form as compared to the drug release exhibited by the formulations in the absence of NaCl. Overall, this project could have valuable contribution in the fabrication of metronidazole loaded effervescent floating tablets. Gastro-retentive systems are expected to enhance local stomach specific action of anti H. pylori agents based on their buoyancy and swelling behavior.

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“…In the past decade or so, its initial utilization was reported as a gelling adhesive agent in combination with other polymers for buccal delivery [ 15 , 16 ] and colon targeting [ 17 ]. The swelling properties of the mucilage led to an investigation of their hydro-gelling potential; however, because of the lower mechanical strength, they were being used as an admixture with other polymers [ 18 , 19 ]. In our opinion, the graft copolymerization technique can help in fabricating harder and denser networks with enhanced mechanical strength of hydrogel with linseed mucilage.…”

Section: Introductionmentioning

confidence: 99%

Preliminary Investigation of Linum usitatissimum Mucilage-Based Hydrogel as Possible Substitute to Synthetic Polymer-Based Hydrogels for Sustained Release Oral Drug Delivery

Mahmood

Erum

Mumtaz

et al. 2022

Gels

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The aim of this study was to investigate the potential of Linum usitatissimum mucilage, a natural polymer, in developing a sustained release hydrogel for orally delivered drugs that require frequent dosing. For this purpose, nicorandil (a model drug)-loaded hydrogels with various feed ratios of Linum usitatissimum mucilage, acrylamide (monomer) and methylene bis-acrylamide (crosslinker) were prepared. The newly synthesized hydrogel formulations were probed fundamentally with respect to swelling behaviour, solvent penetration, and the release of the drug from the hydrogels. Later, the selected formulations were further characterized by Fourier-transform infrared spectroscopy, thermal analysis, X-ray diffraction analysis, and scanning electron microscopy. The swelling coefficient demonstrated a linear relation with the polymer ratio; however, an inverse behaviour in the case of monomer and crosslinker was observed. The drug release studies, performed at pH 1.2 and 4.5 and considering the dynamic environment of GIT, demonstrated that all formulations followed the Korsmeyer–Peppas model, displaying a slow drug release via diffusion and polymer erosion. FTIR analysis confirmed the successful grafting of acrylamide on linseed mucilage. Furthermore, scanning electron microscopy revealed a clear surface morphology with folds and pinholes in the hydrogel. Therefore, based upon the in-vitro outcomes, it can be concluded that a promising sustained release hydrogel can be prepared from natural polymer, Linum usitatissimum mucilage, offering many-fold benefits over the conventional synthetic polymers for oral delivery of drugs.

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Linseed hydrogel based floating drug delivery system for fluoroquinolone antibiotics: Design, in vitro drug release and in vivo real-time floating detection

Cited by 26 publications

References 50 publications

Hydrogels as Drug Delivery Systems: A Review of Current Characterization and Evaluation Techniques

Hydrogels as Drug Delivery Systems: A Review of Current Characterization and Evaluation Techniques

Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of H. pylori: Preparation and In Vitro Characterization

Preliminary Investigation of Linum usitatissimum Mucilage-Based Hydrogel as Possible Substitute to Synthetic Polymer-Based Hydrogels for Sustained Release Oral Drug Delivery

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