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Objectives <p>This review critically examines the integration of nanocarriers into oral tablet formulations, focusing on compaction strategies, excipient selection, and the impact of nanosystem properties on manufacturability, drug release, and biopharmaceutical performance.</p> Literature search <p>A comprehensive literature search was conducted in PubMed and Web of Science to identify peer-reviewed publications reporting oral tablet formulations based on nanocarriers, including polymeric nanoparticles, liposomes, mesoporous silica nanoparticles (MSNs), dendrimers, and hybrid or lipid-based nanosystems. Relevant data on formulation strategies, compression methods, excipients, in vitro and in vivo performance, and critical quality attributes were extracted and analyzed.</p> Results <p>After removing duplicates and assessing relevance, 40 studies were selected for in-depth review. Polymeric nanoparticles consistently enhanced controlled release, with chitosan, polylactide acid, and casein-based systems enabling mucoadhesion or delayed dissolution. Silica-based nanocarriers, particularly MSNs, enhanced powder flow and tablet hardness when used within an optimal concentration range, whereas higher loadings negatively affected compressibility. Lipid nanoparticles and self-emulsifying systems facilitated immediate or sustained release while improving drug solubility. Freeze-drying, spray drying, and 3D printing were pivotal for stabilizing sensitive carriers. Hybrid systems, including metal–organic frameworks and chitosomes, provided tailored release and pharmacokinetic enhancement. Challenges included aggregation, poor flow, mechanical fragility, and regulatory limitations, though advances in excipient engineering, smart coatings, and manufacturing technologies are mitigating these barriers.</p> Conclusions <p>Nanocarrier-based tablets are a promising frontier for improving oral drug delivery, offering controlled release, enhanced bioavailability, and potential for multifunctionality. While nanocrystal-based products dominate the market, newer nanosystems show increasing promise. Future directions include personalized therapies, oral delivery of biologics, and integration of multifunctional nanocarriers enabled by emerging technologies such as 3D printing and stimuli-responsive coatings.</p>

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Tableting of nanoparticle-based formulations for oral delivery: Enhancing biopharmaceutical performance

  • 期刊论文

  • 发表日期：

    2026年5月6日

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  • Sofía Peñaloza,
  • Rodrigo Rozas,
  • Andrés Núñez-Salinas,
  • Rodrigo Pérez,
  • Andrea Ortiz,
  • Javier Morales,
  • Francisco Arriagada

摘要

Objectives

This review critically examines the integration of nanocarriers into oral tablet formulations, focusing on compaction strategies, excipient selection, and the impact of nanosystem properties on manufacturability, drug release, and biopharmaceutical performance.

Literature search

A comprehensive literature search was conducted in PubMed and Web of Science to identify peer-reviewed publications reporting oral tablet formulations based on nanocarriers, including polymeric nanoparticles, liposomes, mesoporous silica nanoparticles (MSNs), dendrimers, and hybrid or lipid-based nanosystems. Relevant data on formulation strategies, compression methods, excipients, in vitro and in vivo performance, and critical quality attributes were extracted and analyzed.

Results

After removing duplicates and assessing relevance, 40 studies were selected for in-depth review. Polymeric nanoparticles consistently enhanced controlled release, with chitosan, polylactide acid, and casein-based systems enabling mucoadhesion or delayed dissolution. Silica-based nanocarriers, particularly MSNs, enhanced powder flow and tablet hardness when used within an optimal concentration range, whereas higher loadings negatively affected compressibility. Lipid nanoparticles and self-emulsifying systems facilitated immediate or sustained release while improving drug solubility. Freeze-drying, spray drying, and 3D printing were pivotal for stabilizing sensitive carriers. Hybrid systems, including metal–organic frameworks and chitosomes, provided tailored release and pharmacokinetic enhancement. Challenges included aggregation, poor flow, mechanical fragility, and regulatory limitations, though advances in excipient engineering, smart coatings, and manufacturing technologies are mitigating these barriers.

Conclusions

Nanocarrier-based tablets are a promising frontier for improving oral drug delivery, offering controlled release, enhanced bioavailability, and potential for multifunctionality. While nanocrystal-based products dominate the market, newer nanosystems show increasing promise. Future directions include personalized therapies, oral delivery of biologics, and integration of multifunctional nanocarriers enabled by emerging technologies such as 3D printing and stimuli-responsive coatings.