Development of mucoadhesive microbeads using thiolated sodium alginate for intrapocket delivery of resveratrol

Abeer Ahmed Kassem, Ragwa Mohamed Farid, Doaa Ahmed Elsayed Issa, Doaa Said Khalil, Mona Yehia Abd-El-Razzak, Hussein Ibrahim Saudi, Heba Mohamed Eltokhey, Enas Arafa El-Zamarany

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

Abstract

Resveratrol (Res), a polyphenolic phytoalexin, had shown a promising therapeutic efficacy towards treatment of periodontal disease in vitro. This work aims to develop Res microbeads with strong mucoadhesion using thiolated alginate (TA) for local treatment of periodontal pockets. TA was synthesized by conjugating sodium alginate (A) with thioglycolic acid. Product was evaluated by IR and DSC. Both A and A:TA Res microbeads with different ratios were prepared by ionotropic gelation method. Formulations were evaluated regarding their entrapment efficiency (%EE), swelling index (SI), in vitro drug release and kinetics. Selected formula was examined for its mucoadhesion by ex vivo wash-off method, surface morphology using scanning electron microscope (SEM) and stability against light. Clinical evaluation is running.Formation of TA was confirmed. %EE for all formulations ranged from 83.72 to 104.54%. Results revealed a significant lower SI for TA rich formulation (A/TA 1:1) along with slower release rate and zero-order kinetics, in addition to powerful mucoadhesion; 26% remaining of microbeads after 1 h, compared to 2% for A microbeads. SEM micrographs showed a rough surface with drug precipitation. The formula maintained its %EE after 5 h exposure to direct sunlight. A/TA 1:1 mucoadhesive Res microbeads could be exploited as a prolonged drug release devices for intrapocket application.

Original languageEnglish
Pages (from-to)305-313
Number of pages9
JournalInternational Journal of Pharmaceutics
Volume487
Issue number1-2
DOIs
Publication statusPublished - 20 Jun 2015

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Microspheres
Electrons
Periodontal Pocket
resveratrol
alginic acid
Sunlight
Periodontal Diseases
Pharmacokinetics
Light
Equipment and Supplies
Pharmaceutical Preparations

Keywords

  • Alginate - thioglycolic acid conjugate
  • Ionotropic gelation
  • Periodontal
  • Polyphenol

Cite this

Kassem, Abeer Ahmed ; Farid, Ragwa Mohamed ; Issa, Doaa Ahmed Elsayed ; Khalil, Doaa Said ; Abd-El-Razzak, Mona Yehia ; Saudi, Hussein Ibrahim ; Eltokhey, Heba Mohamed ; El-Zamarany, Enas Arafa. / Development of mucoadhesive microbeads using thiolated sodium alginate for intrapocket delivery of resveratrol. In: International Journal of Pharmaceutics. 2015 ; Vol. 487, No. 1-2. pp. 305-313.
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title = "Development of mucoadhesive microbeads using thiolated sodium alginate for intrapocket delivery of resveratrol",
abstract = "Resveratrol (Res), a polyphenolic phytoalexin, had shown a promising therapeutic efficacy towards treatment of periodontal disease in vitro. This work aims to develop Res microbeads with strong mucoadhesion using thiolated alginate (TA) for local treatment of periodontal pockets. TA was synthesized by conjugating sodium alginate (A) with thioglycolic acid. Product was evaluated by IR and DSC. Both A and A:TA Res microbeads with different ratios were prepared by ionotropic gelation method. Formulations were evaluated regarding their entrapment efficiency ({\%}EE), swelling index (SI), in vitro drug release and kinetics. Selected formula was examined for its mucoadhesion by ex vivo wash-off method, surface morphology using scanning electron microscope (SEM) and stability against light. Clinical evaluation is running.Formation of TA was confirmed. {\%}EE for all formulations ranged from 83.72 to 104.54{\%}. Results revealed a significant lower SI for TA rich formulation (A/TA 1:1) along with slower release rate and zero-order kinetics, in addition to powerful mucoadhesion; 26{\%} remaining of microbeads after 1 h, compared to 2{\%} for A microbeads. SEM micrographs showed a rough surface with drug precipitation. The formula maintained its {\%}EE after 5 h exposure to direct sunlight. A/TA 1:1 mucoadhesive Res microbeads could be exploited as a prolonged drug release devices for intrapocket application.",
keywords = "Alginate - thioglycolic acid conjugate, Ionotropic gelation, Periodontal, Polyphenol",
author = "Kassem, {Abeer Ahmed} and Farid, {Ragwa Mohamed} and Issa, {Doaa Ahmed Elsayed} and Khalil, {Doaa Said} and Abd-El-Razzak, {Mona Yehia} and Saudi, {Hussein Ibrahim} and Eltokhey, {Heba Mohamed} and El-Zamarany, {Enas Arafa}",
year = "2015",
month = "6",
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doi = "10.1016/j.ijpharm.2015.04.010",
language = "English",
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Kassem, AA, Farid, RM, Issa, DAE, Khalil, DS, Abd-El-Razzak, MY, Saudi, HI, Eltokhey, HM & El-Zamarany, EA 2015, 'Development of mucoadhesive microbeads using thiolated sodium alginate for intrapocket delivery of resveratrol', International Journal of Pharmaceutics, vol. 487, no. 1-2, pp. 305-313. https://doi.org/10.1016/j.ijpharm.2015.04.010

Development of mucoadhesive microbeads using thiolated sodium alginate for intrapocket delivery of resveratrol. / Kassem, Abeer Ahmed; Farid, Ragwa Mohamed; Issa, Doaa Ahmed Elsayed; Khalil, Doaa Said; Abd-El-Razzak, Mona Yehia; Saudi, Hussein Ibrahim; Eltokhey, Heba Mohamed; El-Zamarany, Enas Arafa.

In: International Journal of Pharmaceutics, Vol. 487, No. 1-2, 20.06.2015, p. 305-313.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

T1 - Development of mucoadhesive microbeads using thiolated sodium alginate for intrapocket delivery of resveratrol

AU - Kassem, Abeer Ahmed

AU - Farid, Ragwa Mohamed

AU - Issa, Doaa Ahmed Elsayed

AU - Khalil, Doaa Said

AU - Abd-El-Razzak, Mona Yehia

AU - Saudi, Hussein Ibrahim

AU - Eltokhey, Heba Mohamed

AU - El-Zamarany, Enas Arafa

PY - 2015/6/20

Y1 - 2015/6/20

N2 - Resveratrol (Res), a polyphenolic phytoalexin, had shown a promising therapeutic efficacy towards treatment of periodontal disease in vitro. This work aims to develop Res microbeads with strong mucoadhesion using thiolated alginate (TA) for local treatment of periodontal pockets. TA was synthesized by conjugating sodium alginate (A) with thioglycolic acid. Product was evaluated by IR and DSC. Both A and A:TA Res microbeads with different ratios were prepared by ionotropic gelation method. Formulations were evaluated regarding their entrapment efficiency (%EE), swelling index (SI), in vitro drug release and kinetics. Selected formula was examined for its mucoadhesion by ex vivo wash-off method, surface morphology using scanning electron microscope (SEM) and stability against light. Clinical evaluation is running.Formation of TA was confirmed. %EE for all formulations ranged from 83.72 to 104.54%. Results revealed a significant lower SI for TA rich formulation (A/TA 1:1) along with slower release rate and zero-order kinetics, in addition to powerful mucoadhesion; 26% remaining of microbeads after 1 h, compared to 2% for A microbeads. SEM micrographs showed a rough surface with drug precipitation. The formula maintained its %EE after 5 h exposure to direct sunlight. A/TA 1:1 mucoadhesive Res microbeads could be exploited as a prolonged drug release devices for intrapocket application.

AB - Resveratrol (Res), a polyphenolic phytoalexin, had shown a promising therapeutic efficacy towards treatment of periodontal disease in vitro. This work aims to develop Res microbeads with strong mucoadhesion using thiolated alginate (TA) for local treatment of periodontal pockets. TA was synthesized by conjugating sodium alginate (A) with thioglycolic acid. Product was evaluated by IR and DSC. Both A and A:TA Res microbeads with different ratios were prepared by ionotropic gelation method. Formulations were evaluated regarding their entrapment efficiency (%EE), swelling index (SI), in vitro drug release and kinetics. Selected formula was examined for its mucoadhesion by ex vivo wash-off method, surface morphology using scanning electron microscope (SEM) and stability against light. Clinical evaluation is running.Formation of TA was confirmed. %EE for all formulations ranged from 83.72 to 104.54%. Results revealed a significant lower SI for TA rich formulation (A/TA 1:1) along with slower release rate and zero-order kinetics, in addition to powerful mucoadhesion; 26% remaining of microbeads after 1 h, compared to 2% for A microbeads. SEM micrographs showed a rough surface with drug precipitation. The formula maintained its %EE after 5 h exposure to direct sunlight. A/TA 1:1 mucoadhesive Res microbeads could be exploited as a prolonged drug release devices for intrapocket application.

KW - Alginate - thioglycolic acid conjugate

KW - Ionotropic gelation

KW - Periodontal

KW - Polyphenol

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