IMPROVED CHARACTERISTICS OF GLIBENCLAMIDE AS TRANSETHOSOME VESICULAR SYSTEM: PHYSICOCHEMICAL, SOLUBILITY AND IN VITRO PERMEATION STUDY

NURUL ARFIYANTI YUSUF; MARLINE ABDASSAH; IYAN SOPYAN; RACHMAT MAULUDIN; I. MADE JONI; ANIS YOHANA CHAERUNISAA

doi:10.22159/ijap.2024v16i1.49245

Authors

NURUL ARFIYANTI YUSUF Doctoral Program, Faculty of Pharmacy, Padjadjaran University, Jalan Raya Bandung-Sumedang Km 21, Jatinangor-45363, West Java, Indonesia. Sekolah Tinggi Ilmu Farmasi Makassar, Jalan Perintis Kemerdekaan Km. 13,7, Makassar-90242, South Sulawesi, Indonesia https://orcid.org/0000-0002-4417-9263
MARLINE ABDASSAH Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Padjadjaran University, Jalan Raya Bandung-Sumedang Km 21, Jatinangor-45363, West Java, Indonesia
IYAN SOPYAN Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Padjadjaran University, Jalan Raya Bandung-Sumedang Km 21, Jatinangor-45363, West Java, Indonesia https://orcid.org/0000-0001-7616-5176
RACHMAT MAULUDIN School of Pharmacy, Institut Teknologi Bandung, Jalan Ganesha No. 10, Bandung-40132, West Java, Indonesia
I. MADE JONI Department of Physics, Faculty of Mathematics and Natural Sciences, Universitas Padjadjaran, Jalan Raya Bandung-Sumedang Km 21, Jatinangor-45363, West Java, Indonesia. Functional Nano Powder University Center of Excellence (FiNder U CoE), Universitas Padjadjaran, Jalan Raya Bandung-Sumedang Km 21, Jatinangor-45363, West Java, Indonesia https://orcid.org/0000-0001-5949-3418
ANIS YOHANA CHAERUNISAA Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Padjadjaran University, Jalan Raya Bandung-Sumedang Km 21, Jatinangor-45363, West Java, Indonesia https://orcid.org/0000-0002-4985-8206

DOI:

https://doi.org/10.22159/ijap.2024v16i1.49245

Keywords:

Glibenclamide, Transethosome, Box-behnken, Transdermal

Abstract

Objective: Transethosome as a vesicular system offers high skin permeation; therefore, it is expected to improve the solubility and permeability of the poorly soluble drug glibenclamide. The study aimed to optimize the effect of lipid and surfactant concentration as well as sonication time on the physical characteristics of glibenclamide-loaded transethosomes.

Methods: The transethosomes were prepared by solvent evaporation method. An experimental Box-Behnken design optimized the formula by assessing particle size, polydispersity index, zeta potential, and entrapment efficiency as response parameters. Further characterizations were conducted by determining the morphology by TEM, chemical interaction by FTIR, thermal behavior by DSC, as well as solubility improvement by using in vitro drug release and permeation study.

Results: The result showed that the optimal formula was that with the lipid composition of 75 mg of soya lecithin, 5 mg of tween 80 as surfactant at a sonication time of 18.79 min. The responses were particle size of 166.8±5.3 nm, polydispersity index of 0.463±0.1, zeta potential of-44.7±2.2 mV, and entrapment efficiency as much as 87.18±3.8%. Glibenclamide-loaded transethosomes exhibited a spherical morphology with no visible aggregation. FTIR study revealed no chemical interactions between Glibenclamide and the excipients. Solubility and in vitro drug release tests showed a significant increase of Glibenclamide from transethosome (p<0.05) compared with that as a bulk powder.

Conclusion: Overall, the optimized glibenclamide-loaded transethosomes designed with Box Behnken resulted in improved physicochemical characteristics and increased solubility and drug release compared with that from ethosomes and bulk powder comparison, which will be promising for Glibenclamide to be formulated as transdermal drug delivery.

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