Formulation, Characterization, and Taguchi Design Study of Eplerenone Lipid-Based Solid Dispersions Integrated with Gelucire

Eplerenone is a potassium-sparing diuretic of aldosterone antagonist employed to treat chronic heart failure and high blood pressure. Eplerenone is classified as a BSC class II drug since it has poor oral absorption and is difficult to absorb in the body. The solid dispersions approach is the most practical and least expensive method to increase the solubility and dissolution rate of poorly water-soluble eplerenone. Formulating lipid-based solid dispersions employing a mix of hydrophilic lipid carriers has shown to be quite common. Gelucire 50/13 and Gelucire 44/14 were both in there. These compositions included a range of different concentrations and ratios, including 1:1, 1:3, and 1:5, and their phase solubility properties were tested. A comparison was made between in vitro dissolving results of our product and those of the market using 7.4 pH phosphate buffer.

FTIR, DSC, and XRD characterized the lipid-based solid dispersions. The crystalline structure of eplerenone was ameliorated. The commercial medicine was 85% dissolved after 2 h, while F3 dissolved at 99% in the same timeframe. It was discovered that 4 h after starting the ex vivo permeation study, the permeability of eplerenone was 51%, the penetration of the commercial medication was 76%, and the permeation of formulation F3 was 81%. Taguchi design explored significant factors contributed responses. Eplerenone is better absorbed and transported with the help of formulation F3. To investigate permeability further, ex vivo tests were undertaken with impressive results compared to what was available on the market.

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Vasam, M., Maddiboyina, B., Talluri, C. et al. Formulation, Characterization, and Taguchi Design Study of Eplerenone Lipid-Based Solid Dispersions Integrated with Gelucire. BioNanoSci. (2023). https://doi.org/10.1007/s12668-023-01102-4

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