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<p>Bioavailability is a critical determinant of the therapeutic efficacy of orally administered drugs. Poor aqueous solubility and limited intestinal permeability are major factors that restrict the bioavailability of many drugs. According to the Biopharmaceutics Classification System (BCS), drugs are categorized based on their solubility and permeability characteristics, with BCS class III and IV drugs facing significant absorption challenges. Various pharmaceutical strategies, including prodrugs, novel dosage forms, and absorption enhancers, have been developed to improve bioavailability. However, these approaches often come with limitations, such as non-specific effects, toxicity, and inconsistent outcomes. Recently, bioenhancers derived from natural sources have gained attention as a promising alternative for enhancing the bioavailability of poorly absorbed drugs. Unlike conventional absorption enhancers, bioenhancers improve drug absorption without causing independent pharmacological effects. This review provides an in-depth overview of the role of natural bioenhancers in improving oral drug bioavailability. It discusses the challenges associated with drug absorption, the advantages of bioenhancers over traditional absorption enhancers, and their ideal characteristics. The article also examines the mechanisms of action of several bioenhancers, such as Piperine, <i>Glycyrrhiza glabra</i>, <i>Carum carvi</i>, <i>Cuminum cyminum</i>, and Quercetin. Additionally, it explores drug delivery strategies for incorporating bioenhancers, offering a comparative analysis of their efficacy, safety, and limitations. The review addresses the discrepancies between <i>In vitro</i> and <i>In vivo</i> results, as well as the regulatory and translational challenges related to bioenhancers. In conclusion, natural bioenhancers present a promising approach to improving the oral bioavailability of poorly absorbed drugs, thus enhancing their therapeutic efficacy and clinical outcomes. However, further research is required to optimize their formulations, address their limitations, and enable their successful application in clinical practice.</p>

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Strategies to Enhance the Bioavailability of Hydrophilic Drugs Using Natural Bioenhancers

  • 期刊论文

  • 发表日期：

    2025年7月21日

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  • Mohan V. Kodli,
  • Prerana K. Raikar,
  • Pooja Kulkarni,
  • Upendra Kulkarni,
  • Khaja Anees Ahmed

摘要

Bioavailability is a critical determinant of the therapeutic efficacy of orally administered drugs. Poor aqueous solubility and limited intestinal permeability are major factors that restrict the bioavailability of many drugs. According to the Biopharmaceutics Classification System (BCS), drugs are categorized based on their solubility and permeability characteristics, with BCS class III and IV drugs facing significant absorption challenges. Various pharmaceutical strategies, including prodrugs, novel dosage forms, and absorption enhancers, have been developed to improve bioavailability. However, these approaches often come with limitations, such as non-specific effects, toxicity, and inconsistent outcomes. Recently, bioenhancers derived from natural sources have gained attention as a promising alternative for enhancing the bioavailability of poorly absorbed drugs. Unlike conventional absorption enhancers, bioenhancers improve drug absorption without causing independent pharmacological effects. This review provides an in-depth overview of the role of natural bioenhancers in improving oral drug bioavailability. It discusses the challenges associated with drug absorption, the advantages of bioenhancers over traditional absorption enhancers, and their ideal characteristics. The article also examines the mechanisms of action of several bioenhancers, such as Piperine, Glycyrrhiza glabra, Carum carvi, Cuminum cyminum, and Quercetin. Additionally, it explores drug delivery strategies for incorporating bioenhancers, offering a comparative analysis of their efficacy, safety, and limitations. The review addresses the discrepancies between In vitro and In vivo results, as well as the regulatory and translational challenges related to bioenhancers. In conclusion, natural bioenhancers present a promising approach to improving the oral bioavailability of poorly absorbed drugs, thus enhancing their therapeutic efficacy and clinical outcomes. However, further research is required to optimize their formulations, address their limitations, and enable their successful application in clinical practice.