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

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

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Drug treatment remains the most effective global approach to managing and preventing tuberculosis. This work focuses on formulating and evaluating an optimized polyvinyl alcohol-polyethylene glycol based orodispersible strip containing isoniazid, a first-line anti-tubercular agent. A solvent casting method guided through a Taguchi experimental design was employed in the fabrication, optimization and characterization of the orodispersible strip. The optimized strip was physically amalgamated with a monolayer, uniformly distributed surface geometry. It was 159.2 ± 3.0 µm thick, weighed 36.9 ± 0.3 mg, had an isoniazid load of 99.5 ± 0.8%w/w, disintegration and dissolution times of 17.6 ± 0.9 s and 5.5 ± 0.1 min respectively. In vitro crystallinity, thermal measurements and in silico thermodynamic predictions confirmed the strip's intrinsic miscibility, thermodynamic stability and amorphous nature. A Korsmeyer-Peppas (r = 0.99; n > 1 = 1.07) fitted kinetics typified by an initial burst release of 49.4 ± 1.9% at 4 min and a total of 99.8 ± 3.3% at 30 min was noted. Ex vivo isoniazid permeation through porcine buccal mucosa was bi-phasic and characterized by a 50.4 ± 3.8% surge and 95.6 ± 2.9% at 5 and 120 min respectively. The strip was physicomechanically robust, environmentally stable and non-cytotoxic.

Original languageEnglish (US)
Pages (from-to)347-359
Number of pages13
JournalInternational Journal of Pharmaceutics
Volume547
Issue number1-2
DOIs
StatePublished - Aug 25 2018

Fingerprint

Isoniazid
Computer Simulation
Thermodynamics
Polyvinyl Alcohol
Mouth Mucosa
Tuberculosis
Research Design
Swine
Hot Temperature
Pharmaceutical Preparations
In Vitro Techniques

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Keywords

  • Buccal absorption
  • Experimental design
  • Isoniazid
  • Monolayer film
  • Orodispersible strip
  • Tuberculosis

Cite this

Adeleke, Oluwatoyin A. ; Tsai, Pei Chin ; Karry, Krizia M. ; Monama, Nkwe O. ; Michniak-Kohn, Bozena. / Isoniazid-loaded orodispersible strips : Methodical design, optimization and in vitro-in silico characterization. In: International Journal of Pharmaceutics. 2018 ; Vol. 547, No. 1-2. pp. 347-359.
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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.

In: International Journal of Pharmaceutics, Vol. 547, No. 1-2, 25.08.2018, p. 347-359.

Research output: Contribution to journalArticle

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T1 - Isoniazid-loaded orodispersible strips

T2 - Methodical design, optimization and in vitro-in silico characterization

AU - Adeleke, Oluwatoyin A.

AU - Tsai, Pei Chin

AU - Karry, Krizia M.

AU - Monama, Nkwe O.

AU - Michniak-Kohn, Bozena

PY - 2018/8/25

Y1 - 2018/8/25

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AB - Drug treatment remains the most effective global approach to managing and preventing tuberculosis. This work focuses on formulating and evaluating an optimized polyvinyl alcohol-polyethylene glycol based orodispersible strip containing isoniazid, a first-line anti-tubercular agent. A solvent casting method guided through a Taguchi experimental design was employed in the fabrication, optimization and characterization of the orodispersible strip. The optimized strip was physically amalgamated with a monolayer, uniformly distributed surface geometry. It was 159.2 ± 3.0 µm thick, weighed 36.9 ± 0.3 mg, had an isoniazid load of 99.5 ± 0.8%w/w, disintegration and dissolution times of 17.6 ± 0.9 s and 5.5 ± 0.1 min respectively. In vitro crystallinity, thermal measurements and in silico thermodynamic predictions confirmed the strip's intrinsic miscibility, thermodynamic stability and amorphous nature. A Korsmeyer-Peppas (r = 0.99; n > 1 = 1.07) fitted kinetics typified by an initial burst release of 49.4 ± 1.9% at 4 min and a total of 99.8 ± 3.3% at 30 min was noted. Ex vivo isoniazid permeation through porcine buccal mucosa was bi-phasic and characterized by a 50.4 ± 3.8% surge and 95.6 ± 2.9% at 5 and 120 min respectively. The strip was physicomechanically robust, environmentally stable and non-cytotoxic.

KW - Buccal absorption

KW - Experimental design

KW - Isoniazid

KW - Monolayer film

KW - Orodispersible strip

KW - Tuberculosis

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