Modelling of controlled drug release in gastrointestinal tract simulation

Permanadewi, Indrasukma; Kumoro, Andri Cahyo; Wardhani, Dyah Hesti; Aryanti, Nita

doi:10.1088/1742-6596/1295/1/012063

Cited by 83 publications

(39 citation statements)

References 8 publications

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“…As the second phase of the two-stage study, at 30 min, FaSSIF Concentrate was added to the FaSSGF dissolution medium to create a 1:1 volume ratio mixture (FaSSIF medium). With this step, the emptying of the stomach into the small intestine is modeled easily [ 54 , 55 ]. Due to the change of pH, the solubility of CIP decreased.…”

Section: Resultsmentioning

confidence: 99%

In Vitro Drug Release, Permeability, and Structural Test of Ciprofloxacin-Loaded Nanofibers

et al. 2021

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Nanofibers of the poorly water-soluble antibiotic ciprofloxacin (CIP) were fabricated in the form of an amorphous solid dispersion by using poly(vinyl pyrrolidone) as a polymer matrix, by the low-cost electrospinning method. The solubility of the nanofibers as well as their in vitro diffusion were remarkably higher than those of the CIP powder or the physical mixture of the two components. The fiber size and morphology were optimized, and it was found that the addition of the CIP to the electrospinning solution decreased the nanofiber diameter, leading to an increased specific surface area. Structural characterization confirmed the interactions between the drug and the polymer and the amorphous state of CIP inside the nanofibers. Since the solubility of CIP is pH-dependent, the in vitro solubility and dissolution studies were executed at different pH levels. The nanofiber sample with the finest morphology demonstrated a significant increase in solubility both in water and pH 7.4 buffer. Single medium and two-stage biorelevant dissolution studies were performed, and the release mechanism was described by mathematical models. Besides, in vitro diffusion from pH 6.8 to pH 7.4 notably increased when compared with the pure drug and physical mixture. Ciprofloxacin-loaded poly(vinyl pyrrolidone) (PVP) nanofibers can be considered as fast-dissolving formulations with improved physicochemical properties.

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Section: Resultsmentioning

confidence: 99%

In Vitro Drug Release, Permeability, and Structural Test of Ciprofloxacin-Loaded Nanofibers

et al. 2021

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“…The maximum R 2 (0.9506) value was found to be for Korsmeyer-Peppas, so this model was selected as the best kinetic release model. The n value was found to be 0.48 (<0.5), indicating the release of the drug by diffusion (Fickain type) [ 42 ].…”

Section: Resultsmentioning

confidence: 99%

Formulation and Optimization of Butenafine-Loaded Topical Nano Lipid Carrier-Based Gel: Characterization, Irritation Study, and Anti-Fungal Activity

et al. 2021

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The present study aims to prepare and optimize butenafine hydrochloride NLCs formulation using solid and liquid lipid. The optimized selected BF-NLCopt was further converted into Carbopol-based gel for topical application for the treatment of fungal infection. Box Behnken design was employed to optimize the nanostructure lipids carriers (NLCs) using the lipid content (A), Tween 80 (B), and homogenization cycle (C) as formulation factors at three levels. Their effects were observed on the particle size (Y1) and entrapment efficiency (Y2). The selected formulation was converted into gel and further assessed for gel characterization, drug release, anti-fungal study, irritation study, and stability study. The solid lipid (Compritol 888 ATO), liquid lipid (Labrasol), and surfactant (tween 80) were selected based on maximum solubility. The optimization result showed a particle size of 111 nm with high entrapment efficiency of 86.35% for BF-NLCopt. The optimized BF-NLCopt converted to gel (1% w/v, Carbopol 934) and showed ideal gel evaluation results (drug content 99.45 ± 2.11, pH 6.5 ± 0.2, viscosity 519 ± 1.43 CPs). The drug release study result depicted a prolonged drug release (65.09 ± 4.37%) with high drug permeation 641.37 ± 46.59 µg (32.07 ± 2.32%) than BF conventional gel. The low value of irritation score (0.17) exhibited negligible irritation on the skin after application. The anti-fungal result showed greater efficacy than the BF gel at both time points. The overall conclusion of the results revealed NLCs-based gel of BF as an ideal delivery system to treat the fungal infection.

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“…In the Korsmeyer-Peppas equation, the n value indicates the mechanism/s that describe/s release of an active compound from the carrier matrix [ 43 ]. Values of 0.45 ≤ n propose Fickian diffusion mechanism, 0.45 < n < 0.89—non-Fickian transport, n = 0.89—case II transport, and n > 0.89—super case II transport.…”

Section: Resultsmentioning

confidence: 99%

Clinoptilolite Microparticles as Carriers of Catechin-Rich Acacia catechu Extracts: Microencapsulation and In Vitro Release Study

Yaneva

Ivanova

Popov³

2021

Molecules

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The main goal of the present study was to investigate the microencapsulation, in vitro release capacity and efficiency of catechin-rich Acacia catechu extract by Clinosorbent-5 (CLS-5) microparticles by in-depth detailed analyses and mathematical modelling of the encapsulation and in vitro release kinetics behaviour of the polyphenol-mineral composite system. The bioflavanol encapsulation and release efficiency on/from the mineral matrix were assessed by sorption experiments and interpretative modelling of the experimental data. The surface and spectral characteristics of the natural bioactive substance and the inorganic microcarrier were determined by Fourier Transform Infrared Spectroscopy (FTIR) and Ultraviolet/Visible (UV/Vis) spectrophotometric analyses. The maximum extent of catechin microencapsulation in acidic medium was 32%. The in vitro release kinetics study in simulated enzyme-free gastric medium (pH = 1.2) approved 88% maximum release efficiency achieved after 24 h. The in vitro release profile displayed that the developed bioflavanol/clinoptilolite microcarrier system provided sustained catechin in vitro release behaviour without an initial burst effect. Thus, the results from the present study are essential for the design and development of innovative catechin-CLS-5 microcarrier systems for application in human and veterinary medicine.

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Modelling of controlled drug release in gastrointestinal tract simulation

Cited by 83 publications

References 8 publications

In Vitro Drug Release, Permeability, and Structural Test of Ciprofloxacin-Loaded Nanofibers

In Vitro Drug Release, Permeability, and Structural Test of Ciprofloxacin-Loaded Nanofibers

Formulation and Optimization of Butenafine-Loaded Topical Nano Lipid Carrier-Based Gel: Characterization, Irritation Study, and Anti-Fungal Activity

Clinoptilolite Microparticles as Carriers of Catechin-Rich Acacia catechu Extracts: Microencapsulation and In Vitro Release Study

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