Background <p>Oral delivery remains the predominant route of drug administration due to its convenience and patient acceptability; however, many new chemical entities exhibit poor aqueous solubility and limited permeability, resulting in sub-optimal bioavailability. These challenges are particularly relevant for BCS class II–IV compounds.</p> Area covered <p>This review examines the multifunctional roles of lipid-based excipients in oral dosage forms, with emphasis on their pharmaceutical contributions as described within Gattefossé’s lipid portfolio. Lipid excipients are discussed as functional materials that enhance oral bioavailability through mechanisms including self-emulsification, sustained release, enhanced intestinal permeability, P-glycoprotein inhibition, and promotion of lymphatic transport. Additional roles such as taste masking, protection of labile actives, and lubrication during tableting are addressed. Representative nonionic surfactant systems including Gelucire<sup>®</sup>, Labrasol<sup>®</sup>, Compritol<sup>®</sup>, and Precirol<sup>®</sup> are highlighted in the context of formulation considerations.</p> Expert opinion <p>The multifunctionality of lipid excipients positions them as key enabling components for addressing solubility and permeability limitations in oral drug delivery. Their ability to improve both biopharmaceutical performance and manufacturing characteristics supports their continued integration into formulation design strategies.</p>

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Multifunctional roles and innovative applications of lipid excipients in oral dosage forms: pharmaceutical considerations from Gattefossé’s lipid portfolio

  • Kyoungho Yoon,
  • Philippe Caisse,
  • Hongyi Ouyang,
  • Sangkil Lee

摘要

Background

Oral delivery remains the predominant route of drug administration due to its convenience and patient acceptability; however, many new chemical entities exhibit poor aqueous solubility and limited permeability, resulting in sub-optimal bioavailability. These challenges are particularly relevant for BCS class II–IV compounds.

Area covered

This review examines the multifunctional roles of lipid-based excipients in oral dosage forms, with emphasis on their pharmaceutical contributions as described within Gattefossé’s lipid portfolio. Lipid excipients are discussed as functional materials that enhance oral bioavailability through mechanisms including self-emulsification, sustained release, enhanced intestinal permeability, P-glycoprotein inhibition, and promotion of lymphatic transport. Additional roles such as taste masking, protection of labile actives, and lubrication during tableting are addressed. Representative nonionic surfactant systems including Gelucire®, Labrasol®, Compritol®, and Precirol® are highlighted in the context of formulation considerations.

Expert opinion

The multifunctionality of lipid excipients positions them as key enabling components for addressing solubility and permeability limitations in oral drug delivery. Their ability to improve both biopharmaceutical performance and manufacturing characteristics supports their continued integration into formulation design strategies.