Systematic Development of Solid Lipid Nanoparticles of Abiraterone Acetate with Improved Oral Bioavailability and Anticancer Activity for Prostate Carcinoma Treatment

In the present work, an attempt was undertaken to improve the oral bioavailability and anticancer activity of abiraterone acetate. Solid lipid nanoparticles (SLNs) were developed using the quality by design (QbD) principles and evaluated through in vitro, ex vivo, and in vivo studies. Solid lipid suitability was evaluated by equilibrium solubility study, while surfactant and cosurfactant were screened based on the ability to form microemulsion with the selected lipid. SLNs were prepared by emulsion/solvent evaporation method using glyceryl monostearate, Tween 80, and Poloxamer 407 as the solid lipid, surfactant, and cosurfactant, respectively. Box-Behnken design was applied for optimization of material attributes and evaluating their impact on particle size, polydispersity index, zeta potential, and entrapment efficiency of the SLNs. In vitro drug release study was evaluated in simulated gastric and intestinal fluids. Cell culture studies on PC-3 cells were performed to evaluate the cytotoxicity of the drug-loaded SLNs in comparison to the free drug suspension. Qualitative uptake was evaluated for Rhodamine B-loaded SLNs and compared with free dye solution. Ex vivo permeability was evaluated on Wistar rat intestine and in vivo pharmacokinetic evaluation on Wistar rats for SLNs and free drug suspension. Concisely, the SLNs showed potential for significant improvement in the biopharmaceutical performance of the selected drug candidate over the existing formulations of abiraterone acetate.

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Lipids viewed in the study besides others:Compritol ATO 888, Precirol ATO 5, Gelucire 50/13

Surfactants and Co-Surfactants viewed in the study besides others: Poloxamer 407, Tween 80, Tween 20

Sarwar Beg, Ankit K. Malik, Mohammad Javed Ansari, Asrar A. Malik, Ahmed Mahmoud Abdelhaleem Ali, Abdulrahman Theyab, Mohammad Algahtani, Waleed H. Almalki, Khalid S. Alharbi, Sattam K. Alenezi, Md. Abul Barkat, Mahfoozur Rahman, and Hani Choudhry
ACS Omega 2022, 7, 20, 16968–16979
Publication Date:May 9, 2022
https://doi.org/10.1021/acsomega.1c07254