In Vivo and Ex Vivo Evaluation of a Multi-Particulate Composite Construct for Sustained Transbuccal Delivery of Carbamazepine

Adeleke, Oluwatoyin A.; Choonara, Yahya E.; Toit, Lisa C. du; Pillay, Viness

doi:10.1002/jps.23884

Cited by 12 publications

(10 citation statements)

References 57 publications

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“…In cases where the volume is significantly reduced to only 10-25 mL, the agitation is performed by the use of shaking incubators. Using such apparatus, level A IVIVC with correlation coefficient of 0.909 was obtained for carbamazepine release from buccal multi-composite constructs [34]. The same level of IVIVC was obtained in the case of vaginal NuvaRing®, using similar approach [36].…”

Section: Paddle Apparatus and Modificationsmentioning

confidence: 72%

“…and FDA (Table 1), the paddle apparatus is used for a variety of mucosal drug delivery systems. However, the general intention of the researchers in the field is to reduce the volume of the dissolution medium applied [34,35]. In cases where the volume is significantly reduced to only 10-25 mL, the agitation is performed by the use of shaking incubators.…”

Section: Paddle Apparatus and Modificationsmentioning

confidence: 99%

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In vitro dissolution/release methods for mucosal delivery systems

et al. 2017

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Section: Paddle Apparatus and Modificationsmentioning

confidence: 72%

Section: Paddle Apparatus and Modificationsmentioning

confidence: 99%

In vitro dissolution/release methods for mucosal delivery systems

et al. 2017

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“…Multiparticulated systems provide several advantages over single-unit dosage forms such as tablets, because of their multiplicity and small sizes, including reduced risk of systemic toxicity, low risk of dose dumping, and more uniform and reliable gastrointestinal transit ( AlHusban et al, 2011;Auriemma et al, 2013;Dey et al, 2008;Pan et al, 2010;Severino et al, 2012). Indeed, the usefulness of multiparticles for controlled drug release has been reported (Adeleke et al, 2014;AlHusban et al, 2011;Auriemma et al, 2013;Severino et al, 2012), where the selected polymer can offer different drug delivery behaviors.…”

Section: Discussionmentioning

confidence: 99%

Preclinical pharmacokinetics of benznidazole-loaded interpolyelectrolyte complex-based delivery systems

García

Guzmán

Himelfarb

et al. 2018

European Journal of Pharmaceutical Sciences

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“…Collected samples were assayed for their PYZ content at 268 nm using the Cary 50 UV−vis spectrophotometer. PYZ flux (J ss ) through the excised porcine buccal mucosa was calculated at steady state per unit area 34,35 while the permeability coefficient (k p ) was obtained from the equation described by Yang et al 31 2.4.6. In Vitro and in Silico Determination of the Mechanical Properties.…”

Section: Molecular Pharmaceuticsmentioning

confidence: 99%

Combined Atomistic Molecular Calculations and Experimental Investigations for the Architecture, Screening, Optimization, and Characterization of Pyrazinamide Containing Oral Film Formulations for Tuberculosis Management

et al. 2015

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To date, effective treatment, prophylaxis, and control of tuberculosis (TB) infection is mainly dependent on the use of drugs. However, patient noncompliance with prescribed anti-TB treatment schemes remains a major problem confronting successful pharmacotherapeutic outcomes. Thus, the development of alternative delivery systems that can improve adherence for the existing anti-TB bioactives has been intensified in recent times. The aim of this investigation was to engineer an optimal, thermodynamically stable oral film (OF) formulation containing a key anti-TB agent, pyrazinamide (PYZ), employing molecular modeling and experimental tools. Four PYZ-loaded film variants (OF 1, OF 2, OF 3, OF 4) were constructed in silico and then prepared in vitro using the Accelrys Materials Studio software and solvent casting method, respectively. Screening and selection of the optimal OF was based on the computation of the total interaction energy (ET), kinetic energy (EK), solubility parameter (S), and cohesive energy density (CED) as well as determining mass, thickness, dissolution and disintegration times, dissolution pH, drug loading capacity, and surface morphology in vitro. OF 2 was selected as the optimal formulation as it displayed the lowest ET (-8006.28 kcal/mol), dissolution time (9.96 min), disintegration time (56.49 s), and weight (39.33 mg); moderate EK (1052.98 kcal/mol); highest S (44.55 (J/cm(3))(0.5)) and CED (1.99 × 10(9) J/m(3)), slim dimension (166 μm), good and unvarying drug loading capacity (98.04%), acceptable dissolution pH (6.70), and well-layered surface topography. The drug release behavior of the optimal OF 2 was best elucidated with the zero order (R(2) = 0.97) and Korsmeyer-Peppas (R(2) = 0.99) models. X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) analyses showed that OF 2 was made of physically mixed multiple component polymeric and nonpolymeric compounds. OF 2 was semicrystalline in nature and displayed a dual phased ex vivo mucosal permeation pattern. In silico and in vitro physicomechanical quantities revealed OF 2's flexibility, robustness, and compressibility. OF 2 was most stable under controlled environmental humidity, pressure, and temperature conditions in silico and in vitro. OF 2 was potentially non-cytotoxic and biocompatible. Succinctly, this work demonstrated the applicability of a combination of atomistic molecular mechanics and dynamics calculations as well as experimental analyses to the fabrication, screening, optimization, and characterization of drug formulations. Lastly, the fabricated OF 2 formulation can function as a potential alternative for the effective loading and delivery of PYZ.

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In Vivo and Ex Vivo Evaluation of a Multi-Particulate Composite Construct for Sustained Transbuccal Delivery of Carbamazepine

Cited by 12 publications

References 57 publications

In vitro dissolution/release methods for mucosal delivery systems

In vitro dissolution/release methods for mucosal delivery systems

Preclinical pharmacokinetics of benznidazole-loaded interpolyelectrolyte complex-based delivery systems

Combined Atomistic Molecular Calculations and Experimental Investigations for the Architecture, Screening, Optimization, and Characterization of Pyrazinamide Containing Oral Film Formulations for Tuberculosis Management

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