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<p>Hyperlipidemia, defined as abnormally elevated lipid levels, is a significant risk factor for the development of cardiovascular diseases. Atorvastatin, a statin drug, inhibits HMG-CoA reductase and reduces cholesterol synthesis. However, its oral bioavailability is limited because of extensive first-pass metabolism. This study aimed to improve atorvastatin bioavailability by formulating atorvastatin-loaded transferosomes for transdermal administration. Transferosomes were prepared using the thin-film hydration technique with a constant drug concentration and varying lipid surfactant ratios. The prepared transferosomes were characterized in terms of morphology, particle size, zeta potential, and entrapment efficiency. The extracts were then incorporated into a Carbopol gel to form a transferosomal gel. The preformulation studies included physicochemical characterization, solubility profile, log <i>P</i> value, melting point determination, calibration curve, and compatibility studies using FT-IR analysis. <i>In vitro</i> characterization revealed that the transferosomes had optimal particle size (78.6 to 240.6&#xa0;nm with a size of 206.3&#xa0;nm for the optimized batch), high entrapment efficiency (70.322 to 92.7812%), and moderate stability (zeta potential of − 21.2&#xa0;mV). The transferosomal gel exhibited excellent homogeneity, appropriate pH (6.87 to 6.99), good spreadability, pseudoplastic flow behavior, and sustained drug release over 9&#xa0;h, with AT-TG3 showing the highest drug release (93.25%). <i>In vivo</i> experiments were conducted on hyperlipidemic rats to assess the therapeutic effectiveness of the transferosome gel. The findings showed a significant decrease in serum cholesterol levels in comparison to the control group, validating the promise of this transdermal system. Atorvastatin-loaded transferosomes offer a promising approach for transdermal drug delivery, with improved bioavailability and sustained release. Further investigations, including clinical trials, are necessary to corroborate these observations and fully elucidate the therapeutic potential of this novel drug-delivery system.</p>

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Atorvastatin-Loaded Transferosomal Gel for Hyperlipidaemia: In Vitro and In Vivo Evaluation in Rodents

  • 期刊论文

  • 发表日期：

    2025年10月15日

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  • Deepika Kumari,
  • Shoaeb Mohammad Syed

摘要

Hyperlipidemia, defined as abnormally elevated lipid levels, is a significant risk factor for the development of cardiovascular diseases. Atorvastatin, a statin drug, inhibits HMG-CoA reductase and reduces cholesterol synthesis. However, its oral bioavailability is limited because of extensive first-pass metabolism. This study aimed to improve atorvastatin bioavailability by formulating atorvastatin-loaded transferosomes for transdermal administration. Transferosomes were prepared using the thin-film hydration technique with a constant drug concentration and varying lipid surfactant ratios. The prepared transferosomes were characterized in terms of morphology, particle size, zeta potential, and entrapment efficiency. The extracts were then incorporated into a Carbopol gel to form a transferosomal gel. The preformulation studies included physicochemical characterization, solubility profile, log P value, melting point determination, calibration curve, and compatibility studies using FT-IR analysis. In vitro characterization revealed that the transferosomes had optimal particle size (78.6 to 240.6 nm with a size of 206.3 nm for the optimized batch), high entrapment efficiency (70.322 to 92.7812%), and moderate stability (zeta potential of − 21.2 mV). The transferosomal gel exhibited excellent homogeneity, appropriate pH (6.87 to 6.99), good spreadability, pseudoplastic flow behavior, and sustained drug release over 9 h, with AT-TG3 showing the highest drug release (93.25%). In vivo experiments were conducted on hyperlipidemic rats to assess the therapeutic effectiveness of the transferosome gel. The findings showed a significant decrease in serum cholesterol levels in comparison to the control group, validating the promise of this transdermal system. Atorvastatin-loaded transferosomes offer a promising approach for transdermal drug delivery, with improved bioavailability and sustained release. Further investigations, including clinical trials, are necessary to corroborate these observations and fully elucidate the therapeutic potential of this novel drug-delivery system.