Innovative Oral and Topical Drug Delivery Systems for Enhanced Bioavailability

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: 31 October 2026 | Viewed by 878

Special Issue Editors


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1. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica, Consejo Nacional de Investigaciones Científicas y Tecnológicas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Av. Haya de la Torre y Medina Allende, Córdoba 5000, Argentina
2. Pill.AR Apotheke Revolution S.A, Córdoba 5000, Argentina
Interests: materials chemistry; nanotechnology; nanoparticles; vaccines; nanomaterials; gels; surfactants; solid dispersion; formulations; rheology
Special Issues, Collections and Topics in MDPI journals

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1. Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba (UNC), Córdoba X5000HUA, Argentina
2. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA), Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET-UNC), Haya de la Torre y Medina Allende, Ciudad Universitaria, Córdoba X5000HUA, Argentina
Interests: drug delivery; nanomedicine; pediatric formulation

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Facultad de Ingeniería de la UNSa, INIQUI (Instituto de Investigaciones para la Industria Química), UNSa (Universidad Nacional de Salta), CONICET (Consejo Nacional de Investigaciones Científicas y Técnicas), Salta 4400, Argentina
Interests: pharmaceutical technology; controlled release; drug delivery systems; drug release; neglected infectious diseases; mathematical modeling

Special Issue Information

Dear Colleagues,

This Special Issue focuses on the development and characterization of oral and topical pharmaceutical formulations designed to enhance the bioavailability of active pharmaceutical ingredients (APIs), particularly those with limited solubility or permeability. The scope encompasses both conventional and advanced drug delivery strategies, designed to enhance absorption, prolong retention at the site of action, and overcome physiological barriers. Emphasis is placed on formulation approaches, including lipid-based systems, polymeric hydrogels, solid dispersions, mucoadhesive platforms, and micro/nanoparticulate carriers. Additionally, contributions addressing the physicochemical optimization, in vitro–in vivo correlation, and innovative techniques for formulation design (e.g., 3D printing or hot-melt extrusion) are welcome. The issue aims to highlight the latest research efforts that contribute to improving the therapeutic performance of oral and topical drug products, with relevance in both pharmaceutical development and clinical practice. 

Prof. Dr. Santiago Daniel Palma
Prof. Dr. Alvaro Jimenez-Kairuz
Dr. José Bermudez
Guest Editors

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Keywords

  • oral drug delivery
  • topical formulations
  • bioavailability enhancement
  • polymeric drug delivery systems
  • mucoadhesive systems
  • solubility and permeability improvement
  • in situ forming systems
  • 3D printing in pharmaceutics

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Published Papers (1 paper)

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Research

26 pages, 10683 KB  
Article
Advanced Optimization of Clonazepam-Loaded Solid Self-Emulsifying Drug Delivery Systems: Comparison of Weighted Goal Programming and Desirability Function in a Quality by Design Framework
by María Luisa González-Rodríguez, Sonia Valverde-Cabeza, Enrique Pérez-Terrón, Antonio María Rabasco and Pedro Luis González-Rodriguez
Pharmaceutics 2026, 18(3), 305; https://doi.org/10.3390/pharmaceutics18030305 - 28 Feb 2026
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Abstract
Background/Objectives: Clonazepam (CLZ), a BCS Class II drug, presents significant oral delivery challenges due to its low aqueous solubility. This study explores the systematic development of solid self-emulsifying drug delivery systems (S-SEDDS) using Quality by Design (QbD). The primary objective was to evaluate [...] Read more.
Background/Objectives: Clonazepam (CLZ), a BCS Class II drug, presents significant oral delivery challenges due to its low aqueous solubility. This study explores the systematic development of solid self-emulsifying drug delivery systems (S-SEDDS) using Quality by Design (QbD). The primary objective was to evaluate and compare advanced mathematical optimization frameworks, specifically Derringer’s Desirability Function (D) and Weighted Goal Programming (WGP), to identify a robust formulation that enhances drug solubilization while ensuring superior processability and flowability. Methods: Liquid SEDDS were solidified by adsorption onto a porous matrix (Aerosil® 200/Lactose). A multi-objective optimization was conducted to define a robust Design Space (DS), comparing D against WGP. The trade-offs between competing Critical Quality Attributes (CQAs), specifically powder flowability (angle of repose, AR), blending efficiency (BE), and CLZ recovery (CR), were evaluated. Characterization included morphology from Environmental Scanning Electron Microscopy (ESEM), droplet size analysis, and pH-dependent dissolution studies. Results: D provided a highly robust baseline, yielding constant optimal coordinates (F2, F3 = +1; F4 = 0) across all sensitivity levels, with a predicted AR of 40.46°, BE of 0.12 and CR of 90.0%. However, WGP successfully refined this solution by allowing a more flexible weighting of goals, achieving a more favorable compromise with an AR of 38.96°, a BE of 0.11, and a CR of 90.23%. The optimized system maintained nanometric droplet sizes (<200 nm) and showed a controlled, pH-independent release profile, reaching 80% drug solubilization at 6 h. Conclusions: Integrating WGP into the QbD framework offers a more versatile and precise optimization than the traditional D for complex pharmaceutical systems. This approach ensures the production of high-quality S-SEDDS, bridging the gap between mathematical modeling and the stringent requirements of industrial solid dosage manufacturing. Full article
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