Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation

Objective: To formulate and assess bucco-adhesive films of propranolol hydrochloride for pediatric use. Methods: Different films were formulated adopting mucin, polyvinyl alcohol, chitosan and carbopol. A drug/polymer compatibility study was conducted adopting differential scanning calorimetry and F...

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Veröffentlicht in:Drug design, development and therapy development and therapy, 2020-01, Vol.14, p.4277-4289
Hauptverfasser: Mohamad, Soad A., Salem, Hesham, Yassin, Heba A., Mansour, Heba F.
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creator Mohamad, Soad A.
Salem, Hesham
Yassin, Heba A.
Mansour, Heba F.
description Objective: To formulate and assess bucco-adhesive films of propranolol hydrochloride for pediatric use. Methods: Different films were formulated adopting mucin, polyvinyl alcohol, chitosan and carbopol. A drug/polymer compatibility study was conducted adopting differential scanning calorimetry and Fourier transform infrared spectroscopy. The prepared films were physically investigated for variation of weight, propranolol content, thickness, surface pH, proportion of moisture, folding endurance and mucoadhesion. In vitro drug release study and kinetic analysis of the corresponding data have been conducted. The optimized formulation was selected for a bioavailability study using albino rabbits and adopting a developed HPLC method. The pharmacokinetic parameters of the drug were calculated following administration of the optimized film and the corresponding marketed oral tablets to albino rabbits. Key Finding: The compatibility study revealed the absence of drug/polymer interaction. The film formulations had suitable mucoadhesive and mechanical properties. The optimized formulation exhibited reasonable drug release that followed Higuchi diffusion pattern. The calculated AUC0-8h presented an enhancement in the bioavailability of propranolol hydrochloride from the selected film formulation by 1.9 times relative to the marketed propranolol oral tablets. Conclusion: These findings support that propranolol hydrochloride bucco-adhesive film can be considered as a proper effective dosage form for pediatric delivery.
doi_str_mv 10.2147/DDDT.S267317
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Methods: Different films were formulated adopting mucin, polyvinyl alcohol, chitosan and carbopol. A drug/polymer compatibility study was conducted adopting differential scanning calorimetry and Fourier transform infrared spectroscopy. The prepared films were physically investigated for variation of weight, propranolol content, thickness, surface pH, proportion of moisture, folding endurance and mucoadhesion. In vitro drug release study and kinetic analysis of the corresponding data have been conducted. The optimized formulation was selected for a bioavailability study using albino rabbits and adopting a developed HPLC method. The pharmacokinetic parameters of the drug were calculated following administration of the optimized film and the corresponding marketed oral tablets to albino rabbits. Key Finding: The compatibility study revealed the absence of drug/polymer interaction. The film formulations had suitable mucoadhesive and mechanical properties. The optimized formulation exhibited reasonable drug release that followed Higuchi diffusion pattern. The calculated AUC0-8h presented an enhancement in the bioavailability of propranolol hydrochloride from the selected film formulation by 1.9 times relative to the marketed propranolol oral tablets. Conclusion: These findings support that propranolol hydrochloride bucco-adhesive film can be considered as a proper effective dosage form for pediatric delivery.</abstract><cop>ALBANY</cop><pub>Dove Medical Press Ltd</pub><pmid>33116415</pmid><doi>10.2147/DDDT.S267317</doi><tpages>13</tpages><orcidid>https://orcid.org/0000-0002-6467-849X</orcidid><orcidid>https://orcid.org/0000-0002-2948-1691</orcidid><oa>free_for_read</oa></addata></record>
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subjects Adhesion tests
Adhesiveness
Adhesives
Administration, Buccal
Adrenergic beta-Antagonists - administration & dosage
Adrenergic beta-Antagonists - chemistry
Adrenergic beta-Antagonists - pharmacology
Animals
Area Under Curve
Bioavailability
Biocompatibility
Biological Availability
buccoadhesive
Calorimetry
Cheek
Chemistry, Medicinal
Child
Chitosan
Chromatography, High Pressure Liquid
Differential scanning calorimetry
Dosage
Dosage Forms
Drug Compounding
Drug delivery systems
Drug dosages
Excipients
Fourier analysis
Fourier transforms
High-performance liquid chromatography
hplc
Humans
Hydrogen-Ion Concentration
Infant
Infrared spectroscopy
Investigations
Life Sciences & Biomedicine
Liquid chromatography
Mathematical analysis
Mechanical properties
Moisture content
Mucin
Oral administration
Original Research
paediatric
Patient compliance
Pediatric pharmacology
Pediatrics
Pharmacokinetics
Pharmacology & Pharmacy
Polymer blends
Polymer films
Polymers
Polyvinyl alcohol
Potassium
Propanolol hydrochloride
Propranolol
Propranolol - administration & dosage
Propranolol - pharmacokinetics
Propranolol - pharmacology
Rabbits
Science & Technology
Spectrum analysis
Tablets
title Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation
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