Transfersome: a vesicular drug delivery with enhanced permeation

Yusuf, Nurul Arfiyanti; Abdassah, Marline; Mauludin, Rachmat; Joni, I Made; Chaerunisaa, Anis Yohana

doi:10.51847/vrynt7vhhp

Cited by 4 publications

(1 citation statement)

References 49 publications

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“…Transdermal drug delivery has various benefits, including fewer side effects, more patient compliance, avoidance of first-pass effects, slower drug delivery, and the ability to quit therapy [1][2][3][4][5][6]. The semipermeable characteristic of the skin barrier must be reduced without creating negative side effects, especially local irritation, which is a major difficulty in developing transdermal delivery systems [7][8][9][10].…”

Section: Introductionmentioning

confidence: 99%

Glibenclamide Transethosome Patch for Transdermal Delivery: Formulation and Evaluations

YUSUF,

ABDASSAH,

MAULUDIN

et al. 2023

Int J App Pharm

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Objective: The glibenclamide transethosome patch is a patch containing glibenclamide encapsulated in nanoparticle-based vesicles that can improve the penetration of the compound into the skin. The research work aims to evaluate glibenclamide transethosome patches using HPMC and PVP as matrix polymers and glibenclamide as a drug model. Methods: Glibenclamide transethosome patches were prepared using a solvent evaporation technique. Evaluations that have been carried out to assess the stability of the patch include weight variation, folding endurance, thickness, moisture absorption, moisture content, drug content, and drug release in vitro glibenclamide transethosome was carried out using Franz diffusion cell. Results: The results of the evaluation of the glibenclamide transethosome patch showed a patch weight uniformity between 0.051-0.063 g and a CV (Coefficient of Variation) value of less than 5%. The resulting folding resistance of the patch can withstand without tearing over 200 folds. The thickness of the glibenclamide transethosome patch is between 0.14-0.24 cm. The moisture absorption capacity of the patch is between 2.1-23.5%. The moisture content of the patch is between 4.7-7.4%. The drug content of the patch is between 6.7–12.7 g/cm2. Drug release from the patch was between 45.9-82.1% after 480 min. Overall, in the moisture absorption test (F3; F4; F5), moisture content, drug content, and drug release (F1) gave significantly different results (p<0.05). Conclusion: The glibenclamide transethosome patch showed evaluation results that met the requirements and were stable during the stability test. The polymer combinations also significantly influence drug release during stability tests.

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Section: Introductionmentioning

confidence: 99%

Glibenclamide Transethosome Patch for Transdermal Delivery: Formulation and Evaluations

YUSUF,

ABDASSAH,

MAULUDIN

et al. 2023

Int J App Pharm

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Improved Characteristics of Glibenclamide as Transethosome Vesicular System: Physicochemical, Solubility and in Vitro Permeation Study

YUSUF,

ABDASSAH,

SOPYAN

et al. 2024

Int J App Pharm

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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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