Isoniazid-loaded orodispersible strips: Methodical design, optimization and in vitro-in silico characterization

Adeleke, Oluwatoyin A.; Tsai, Pei Chin; Karry, Krizia M.; Monama, Nkwe O.; Michniak‐Kohn, Bozena

doi:10.1016/j.ijpharm.2018.06.004

Cited by 19 publications

(20 citation statements)

References 59 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The most common used polymers are cellulose derivates, such as hypromellose and hydroxypropylcellulose [2,39]. Furthermore, formulations with polyvinylalcohol are often mentioned in literature [9,[40][41][42][43][44][45].…”

Section: Local and Systemic Drug Deliverymentioning

confidence: 99%

Oromucosal films: from patient centricity to production by printing techniques

Tian

Orlu

Woerdenbag

et al. 2019

Expert Opinion on Drug Delivery

View full text Add to dashboard Cite

Introduction: Oromucosal films, comprising mucoadhesive buccal films (MBFs) and orodispersible films (ODFs), are considered patient-centric dosage forms. Target groups are patients with special needs. Various active pharmaceutical ingredients have been shown to be suitable for oromucosal film production. A shift is seen in the production techniques, from conventional solvent casting to printing techniques. Areas covered: In this review, the patient acceptability of oromucosal films is discussed. An overview is given of the small molecule drugs, biopharmaceuticals and herbal extracts that have been incorporated so far. Finally, the current state of 2D and 3D printing techniques for production purposes is discussed. Expert opinion: The patient-centric features are important for the further development and acceptance of this oral solid dosage form. Oromucosal films perfectly fit in the current attention for personalized medicine. Both MBFs and ODFs are intended for either a local or a systemic effect. For buccal absorption, sufficient mucoadhesion is one of the most important criteria an oromucosal film must comply with. For the preparation, the solvent casting technique is still predominately used. Some limitations of this production method can be tackled by printing techniques. However, these novel techniques introduce new requirements, yet to be set, for oromucosal film preparation.

show abstract

Section: Local and Systemic Drug Deliverymentioning

confidence: 99%

Oromucosal films: from patient centricity to production by printing techniques

Tian

Orlu

Woerdenbag

et al. 2019

Expert Opinion on Drug Delivery

View full text Add to dashboard Cite

show abstract

“…To get an indication of the release kinetics of the RDS formulation, the pH 7.4 release profile was selected for further mathematical model fitting over an extended period when 100% drug release was achieved. Resulting data were further analyzed using the KientDS version 3.0 open source software, which aided the selection of the model of best fit, which was based on mathematical computations, such as the zero, first, and second order kinetics, Higuchi, Korsmeyer-Peppas, Michaelis-Menten and Weibull approaches [19,24,27].…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

“…Although subject to considerable hepatic metabolism (or first-pass effect) after oral dosing, it reaches concentrations well above the minimum inhibitory levels of Mtb in most tissues and TB lesions when given in standard doses [17]. Isoniazid is considered a class III drug according to the Biopharmaceutics Classification System (BCS) [18], meaning that it is highly hydrophilic (aqueous solubility = 125 mg/mL at 25 • C) [18,19] but not very permeable (log P = −0.64 at 25 • C) [19]. It is weakly basic, crystalline in nature, and does not display polymorphism [20].…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of a Reconstitutable Dry Suspension Containing Isoniazid for Flexible Pediatric Dosing

2020

Self Cite

View full text Add to dashboard Cite

Tuberculosis (TB) is a major cause of childhood death. Despite the startling statistics, it is neglected globally as evidenced by treatment and clinical care schemes, mostly extrapolated from studies in adults. The objective of this study was to formulate and evaluate a reconstitutable dry suspension (RDS) containing isoniazid, a first-line anti-tubercular agent used in the treatment and prevention of TB infection in both children and adults. The RDS formulation was prepared by direct dispersion emulsification of an aqueous-lipid particulate interphase coupled with lyophilization and dry milling. The RDS appeared as a cream-white free-flowing powder with a semi-crystalline and microparticulate nature. Isoniazid release was characterized with an initial burst up to 5 minutes followed by a cumulative release of 67.88% ± 1.88% (pH 1.2), 60.18% ± 3.33% (pH 6.8), and 49.36% ± 2.83% (pH 7.4) over 2 h. An extended release at pH 7.4 and 100% drug liberation was achieved within 300 min. The generated release profile best fitted the zero order kinetics (R2 = 0.976). RDS was re-dispersible and remained stable in the dried and reconstituted states over 4 months and 11 days respectively, under common storage conditions.

show abstract

“…Pyrazinamide loaded orodispersible formulations were prepared using the solvent casting technique [27,40,41]. Each formulation consisted of different amounts of polyvinyl alcohol polyethylene glycol, sodium starch glycolate, citric acid and xylitol based on the design template detailed in Table 5.…”

Section: Preparation Of Orodispersible Formulationsmentioning

confidence: 99%

“…In vitro disintegration time was recorded at the point when the sample started breaking apart. Thereafter, test samples were allowed to dissolve completely to form a homogenous solution and dissolution pH recorded using a pH meter (GmbH 8603, Mettler Toledo, Sonnenbergstrasse, Schwerzenbach, Switzerland) [40,66]. All the measurements were done in three replicates.…”

Section: In Vitro Disintegration Time and Dissolution Ph Of The Matricesmentioning

confidence: 99%

Optimal Design, Characterization and Preliminary Safety Evaluation of an Edible Orodispersible Formulation for Pediatric Tuberculosis Pharmacotherapy

Matawo

Adeleke

Wesley-Smith

2020

IJMS

Self Cite

View full text Add to dashboard Cite

The severity of tuberculosis (TB) in children is considered a global crisis compounded by the scarcity of pharmaceutical formulations suitable for pediatric use. The purpose of this study was to optimally develop and evaluate a pyrazinamide containing edible orodispersible film formulation potentially suitable for use in pediatrics actively infected with TB. The formulation was prepared employing aqueous-particulate blending and solvent casting methods facilitated by a high performance Box Behnken experimental design template. The optimized orodispersible formulation was mechanically robust, flexible, easy to handle, exhibited rapid disintegration with initial matrix collapse occurring under 60 s (0.58 ± 0.05 min ≡ 34.98 ± 3.00 s) and pyrazinamide release was controlled by anomalous diffusion coupled with matrix disintegration and erosion mechanisms. It was microporous in nature, light weight (57.5 ± 0.5 mg) with an average diameter of 10.5 mm and uniformly distributed pyrazinamide load of 101.13 ± 2.03 %w/w. The formulation was physicochemically stable with no evidence of destructive drug–excipient interactions founded on outcomes of characterization and environmental stability investigations. Preliminary inquiries revealed that the orodispersible formulation was cytobiocompatible, palatable and remained intact under specific storage conditions. Summarily, an edible pyrazinamide containing orodispersible film formulation was optimally designed to potentially improve TB pharmacotherapy in children, particularly the under 5 year olds.

show abstract

Isoniazid-loaded orodispersible strips: Methodical design, optimization and in vitro-in silico characterization

Cited by 19 publications

References 59 publications

Oromucosal films: from patient centricity to production by printing techniques

Oromucosal films: from patient centricity to production by printing techniques

Development and Evaluation of a Reconstitutable Dry Suspension Containing Isoniazid for Flexible Pediatric Dosing

Optimal Design, Characterization and Preliminary Safety Evaluation of an Edible Orodispersible Formulation for Pediatric Tuberculosis Pharmacotherapy

Contact Info

Product

Resources

About