Biomaterial-Based Nanoencapsulation Systems for Drug Protection and Controlled Release

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: 20 July 2026 | Viewed by 1711

Special Issue Editor


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Guest Editor
Instituto de Química Biológica de la Facultad de Ciencias Exactas y Naturales (IQUIBICEN), UBA-CONICET, Buenos Aires 1428, Argentina
Interests: nanotechnology; biomaterial; nanoencapsulation; controlled release; bioavailability

Special Issue Information

Dear Colleagues,

The concept of nanoencapsulation falls within the area of nanotechnology, which is defined as any technology related to materials, systems, and processes that operate at a scale of ≤100 nm, although, in practice, a maximum limit of 500 nm is accepted. Nanoencapsulation encompasses processes that have the advantage of providing protection to the component of interest, drugs, and bioactive compounds. Nanoencapsulation techniques and processes have emerged as promising tools in the pharmaceutical and nutraceutical sectors. An encapsulated bioactive would be trapped by a system that can preserve it from degradation, increasing its solubility and its bioavailability with the possibility of exerting a controlled release.

Biopolymers, i.e., polysaccharides, lipids, and proteins, are promising materials for constructing encapsulation matrices due to their characteristics such as abundance, biocompatibility, and non-toxicity. Furthermore, nanostructures could act as a versatile tool to enhance the therapeutic index of drugs, the bioavailability of which depends on the stability of the drug or bioactive in the oral, gastric, and intestinal environment, its solubility and mode of absorption, and, subsequently, its reach to the target organ.

Dr. Oscar E. Pérez
Guest Editor

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Keywords

  • nanostructures
  • nanoencapsulation
  • drugs/bioactive compounds
  • biopolymer materials
  • controlled release
  • bioavailability
  • nanoproducts

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Published Papers (4 papers)

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Research

17 pages, 1741 KB  
Article
Fabrication and Characterization of Curcumin-Complexed Nanoparticles Using Coconut Protein Nanoparticles
by Leila Ziaeifar, Maryam Salami, Gholamreza Askari, Zahra Emam-Djomeh, Raimar Loebenberg, Michael J Serpe and Neal M. Davies
Pharmaceutics 2025, 17(10), 1247; https://doi.org/10.3390/pharmaceutics17101247 - 24 Sep 2025
Abstract
Background/Objectives: Curcumin (Cur) has various biological properties, including anti-microbial, antioxidant, anticancer, anti-diabetic, anticarcinogenic, antitumor, and anti-inflammatory activities. However, using Cur in functional food products is challenging because of its low solubility in an aqueous environment, rapid degradation, and low bioavailability. Nanostructure delivery [...] Read more.
Background/Objectives: Curcumin (Cur) has various biological properties, including anti-microbial, antioxidant, anticancer, anti-diabetic, anticarcinogenic, antitumor, and anti-inflammatory activities. However, using Cur in functional food products is challenging because of its low solubility in an aqueous environment, rapid degradation, and low bioavailability. Nanostructure delivery systems provide a high surface area to volume ratio and sustainable release properties. Methods: Coconut protein nanoparticles (CPNPs) have been fabricated through heat treatment at 85 °C and pH 2 for 5 h. The formation of CPNP-Cur was used to improve Cur solubility, followed by antioxidant activity at neutral pH in an aqueous solution. Results: The maximum efficiency and loading capacity of Cur in CPNP were 96.6% and 19.32 µg/mg protein, respectively. Scanning electron microscopy indicated the spherical and organized shape of CPNP with a small size of 80 nm. The fluorescence quenching of CPNP-Cur confirmed the potential of Cur to bind to the tryptophane and tyrosine residues in CPNP. The structural properties of CPNP and CPNP-Cur were investigated using FTIR and X-ray diffraction. The antioxidant activity of samples, measured with the ABTS radical scavenging method, demonstrated that the antioxidant capacity of the aqueous solution of Cur was significantly enhanced through the encapsulation into CPNP. The steady release of Cur was observed in the simulated gastrointestinal tract, and the percentage of the cumulative release increased up to 29.2% after 4 h. Conclusions: Our findings suggest that CPNP was a suitable nanocarrier for Cur due to improved antioxidant activity and controlled release behavior. These results are valuable for the development of coconut protein nanoparticles to use as a novel nano-delivery system of bioactive components. Full article
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17 pages, 2295 KB  
Article
Solid Tranilast Nanocrystal-Loaded Cationic Contact Lenses for Sustained Ocular Drug Delivery
by Shinichiro Kobayakawa, Toru Matsunaga, Hiroko Otake, Shiori Hino, Fumihiko Ogata, Manju Misra, Kazutaka Kanai, Naohito Kawasaki and Noriaki Nagai
Pharmaceutics 2025, 17(10), 1240; https://doi.org/10.3390/pharmaceutics17101240 - 23 Sep 2025
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Abstract
Background/Objectives Conventional eye drops are the primary therapeutic option for ocular diseases; however, their clinical utility is hindered by several drawbacks, including limited bioavailability and suboptimal patient compliance. To overcome these challenges, we designed a sustained-release contact lens (CL) device loaded with tranilast [...] Read more.
Background/Objectives Conventional eye drops are the primary therapeutic option for ocular diseases; however, their clinical utility is hindered by several drawbacks, including limited bioavailability and suboptimal patient compliance. To overcome these challenges, we designed a sustained-release contact lens (CL) device loaded with tranilast (TRA) and determined whether the TRA-laden CL could provide sustained drug delivery to the lacrimal fluid and aqueous humor. Methods TRA nanocrystals were prepared using the bead-milling approach. Using three types of CLs (nonionic, anionic, and cationic), we prepared TRA-laden CLs by employing a combination of solid TRA nanocrystals and soaking methods under high-temperature and high-pressure conditions in an autoclave (the hThP method). Male Japanese albino rabbits (2–3 kg) were used to evaluate the CLs. Results Bead milling reduced the size of the solid TRA nanoparticles (STNs) to approximately 35–180 nm. The TRA-laden cationic CLs prepared using STNs and the hThP method contained a higher amount of TRA than those prepared using the corresponding conventional soaking method. The CLs prepared using the hThP method remained transparent after drug loading. Compared with nonionic and anionic CLs, cationic CLs had the highest drug-loading capacity and allowed for sustained drug release. Moreover, STNs were observed in the released TRA, with no corneal damage or light scattering detected in the rabbits’ eyes. TRA-laden cationic CLs prepared using the hThP method achieved sustained and higher drug delivery into the lacrimal fluid and aqueous humor than those prepared using the conventional soaking method. Conclusions Our findings suggest that TRA-laden cationic CLs prepared using STNs and the hThP method can overcome the challenges associated with the conventional soaking method, including low drug uptake and high burst release. Full article
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19 pages, 4026 KB  
Article
Synthesis of Terminal-Alkylated PEGs with Imine Spacer to Form Iminium Mono-Ion Complexes for pDNA Delivery into Skeletal Muscle
by Riku Oba, Yoko Endo-Takahashi, Yoichi Negishi and Shoichiro Asayama
Pharmaceutics 2025, 17(8), 1054; https://doi.org/10.3390/pharmaceutics17081054 - 13 Aug 2025
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Abstract
Background/Objectives: To design the pDNA delivery carrier for delivery into skeletal muscle, a total of twelve terminal-alkylated PEGs (Cx-I-PEGy) with four alkyl groups of different carbon numbers (Cx: x = 4, 8, 12, 16) modified via an imine spacer at the ends of [...] Read more.
Background/Objectives: To design the pDNA delivery carrier for delivery into skeletal muscle, a total of twelve terminal-alkylated PEGs (Cx-I-PEGy) with four alkyl groups of different carbon numbers (Cx: x = 4, 8, 12, 16) modified via an imine spacer at the ends of three methoxy PEGs of different molecular weights (PEGy: y = 500, 2k, 5k) have been synthesized. Methods: Among them, four Cx-I-PEG5k formed an imine-mediated complex formation with pDNA, as assessed by agarose gel electrophoresis, defined as an iminium mono-ion complex (I-MIC) without multivalent electrostatic interaction by minimizing potential toxic cations. Results: Most resulting I-MICs maintained the flexible structure of pDNA and promoted the binding to pDNA. The expression of pDNA by intramuscular injection with the resulting I-MICs was the highest by using I-MICs with C4-I-PEG5k and was observed extensively by the in vivo imaging system (IVIS). Conclusions: These results suggest that the I-MICs with C4-I-PEG5k are promising for pDNA transfection into skeletal muscle, offering the alkyl iminium for the pDNA binding group to demonstrate the factor of pDNA’s flexible structure as one of the key parameters for in vivo local pDNA transfection. Full article
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26 pages, 11210 KB  
Article
Perspectives on the pH-Influenced Design of Chitosan–Genipin Nanogels for Cell-Targeted Delivery
by Julieta D. Glasman, Agustina Alaimo, Cecilia Samaniego López, María Edith Farías, Romina B. Currá, Diego G. Lamas and Oscar E. Pérez
Pharmaceutics 2025, 17(7), 876; https://doi.org/10.3390/pharmaceutics17070876 - 3 Jul 2025
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Abstract
Background: Chitosan (CS) crosslinked with genipin (GNP) provides a mild, non-toxic route to generate nanogels (NGs) with enhanced integrity and colloidal stability. Objectives: To develop and characterise CS-GNP NG as a novel platform for targeted cellular delivery, optimising design through physicochemical [...] Read more.
Background: Chitosan (CS) crosslinked with genipin (GNP) provides a mild, non-toxic route to generate nanogels (NGs) with enhanced integrity and colloidal stability. Objectives: To develop and characterise CS-GNP NG as a novel platform for targeted cellular delivery, optimising design through physicochemical characterisation and biocompatibility evaluation. Methods: NGs were synthesised under optimised conditions by adjusting the pH of the CS solution, followed by high-intensity ultrasound (HIUS) to achieve disaggregation. Physicochemical characterisation was carried out using UV-Vis spectroscopy, FTIR, dynamic light scattering (DLS), and scanning electron microscopy (SEM). Rheological studies and SAXS analysis assessed structural properties. Biocompatibility was evaluated via MTT assay, and internalisation was monitored by fluorescence microscopy on mammalian cell lines. Results: NG formation was highly pH-dependent, with optimal configuration at pH 4.5, yielding stable, uniformly sized particles (~200 nm, ζ-potential +29 mV). Kinetic modelling showed a sigmoidal formation pattern, suggesting nucleation, growth, and stabilisation. FTIR confirmed covalent bonding between CS and GNP via primary amide bonds and Schiff bases. Rheology indicated pseudoplastic behaviour, and SAXS revealed a compact network formation. Biocompatibility assays confirmed non-cytotoxicity below 100 µg/mL and efficient cellular uptake. Conclusions: This study presents a rapid, reproducible protocol for generating colloidally stable, biocompatible NGs suitable for drug delivery. Full article
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