DEVELOPMENT OF TRANSDERMAL DOSAGE FORM USING COPROCESSED EXCIPIENTS OF XANTHAN GUM AND CROSS-LINKED AMYLOSE: IN VITRO AND IN VIVO STUDIES

  • SILVIA SURINI Laboratory of Pharmaceutics and Pharmaceutical Technology Development, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia.
  • ASTINA SICILIA Laboratory of Pharmaceutics and Pharmaceutical Technology Development, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia.
  • RIKA SOFIANI Laboratory of Pharmaceutics and Pharmaceutical Technology Development, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia.
  • SITI KHOIRIAH Laboratory of Pharmaceutics and Pharmaceutical Technology Development, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia.
  • UFAIRAH H. INDRIATIN Laboratory of Pharmaceutics and Pharmaceutical Technology Development, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia.
  • SANTI PURNA SARI Laboratory of Pharmacology, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia.
  • YAHDIANA HARAHAP Laboratory of Bioavailability and Bioequivalence, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia.

Abstract

Objective: A transdermal hydrogel dosage form consists of a three-dimensional polymer network that binds water in large quantities and is used
for drug delivery. The study’s aim was to prepare coprocessed excipients as a matrix for a transdermal hydrogel containing diclofenac sodium and
examine in vitro and in vivo drug penetrations.
Methods: Four types of coprocessed excipients were produced using two methods that combined crosslinking and coprocessing steps. The produced
excipients were formulated as transdermal gels containing sodium diclofenac. An in vitro penetration test was then performed using a Franz diffusion
cell to pass the drug through a rat skin membrane. An in vivo penetration test was performed by applying the hydrogel to the abdominal skin of male
Sprague-Dawley rats and then measuring the plasma drug concentration.
Results: In vitro penetration results showed that the flux from Co-CLA6-XG 1:2, Co-CLA12-XG 1:2, CL6-Co-A-XG 1:2, and CL12-Co-A-XG 1:2 transdermal
hydrogels was 655.23±116.43 μg∙cm−2/h, 569.08±26.58 μg∙cm−2/h, 867.42±101.27 μg∙cm−2/h−1, and 736.99±15.39 μg∙cm−2/h−1. The in vivo study
resulted in area under the curve for the Co−CLA6−XG 1:2, Co−CLA12−XG 1:2, CL6−Co−A−XG 1:2, and CL12−Co−A−XG 1:2 transdermal hydrogels was
32.08±5.40 μg∙ml−1∙h, 34.27±8.34 μg/ml∙h, 6.20±2.90 μg/ml∙h, and 14.38±2.38 μg/mL∙h, respectively.
Conclusion: The study results showed that the excipients could be processed to form a matrix within a transdermal hydrogel formulation and deliver
sodium diclofenac into systemic circulation in a controlled release manner.

Keywords: Amylose, Xanthan gum, Coprocessed excipient, Transdermal hydrogel, In vitro penetration, In vivo penetration

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SURINI, S., SICILIA, A., SOFIANI, R., KHOIRIAH, S., INDRIATIN, U. H., SARI, S. P., & HARAHAP, Y. (2020). DEVELOPMENT OF TRANSDERMAL DOSAGE FORM USING COPROCESSED EXCIPIENTS OF XANTHAN GUM AND CROSS-LINKED AMYLOSE: IN VITRO AND IN VIVO STUDIES. International Journal of Applied Pharmaceutics, 12(1), 207-211. https://doi.org/10.22159/ijap.2020.v12s1.FF047
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