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Nanotechnology for Drug Delivery
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Nanotechnology for Drug Delivery

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Nanoscience".

Deadline for manuscript submissions: closed (31 August 2022) | Viewed by 11029

Special Issue Editor

Dr. Sung Giu Jin

E-Mail Website
Guest Editor
Department of Pharmaceutical Engineering, Dankook University, Cheonan 31116, Republic of Korea
Interests: drug delivery; nanotechnology; lipid-based emulsions; electrospinning/electrospray techniques; microneedle platforms
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Nanotechnology is an exciting scientific field with many applications in drug delivery. Nanoparticle-based systems are emerging as powerful tools to treat diseases by increasing the bioavailability of drugs or being used for targeting. For example, solubility is an important property of a drug, which must be dissolved and absorbed in a biological fluid to act in the desired tissue. Many new chemicals under development are characterized by low water solubility. Low solubility often results in limited or irregular bioavailability, which can impose higher doses to achieve pharmacological effects, increasing the risk of toxicity and material wastage. Moreover, several drug delivery systems are currently being studied to address the limitations of existing dosage forms and improve the potential of each drug. Among the innovative drug delivery systems based on nanotechnology, nanoparticles, liposomes, solid dispersion, supercritical fluid technology, cyclodextrin complexes, and lipid-based formulations can be mentioned. Nanotechnology has provided us with the potential to increase drug solubility and improve bioavailability over the past few decades. Nanotechnology is also widely used to successfully deliver to target tissues and ensure optimal drug delivery for a desired period of time.

The purpose of this Special Issue is to cover cutting-edge research activities and recent research advances in the field of nanotechnology in drug delivery.

Dr. Sung Giu Jin
Guest Editor

Manuscript Submission Information

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Keywords

  • drug delivery
  • nanomaterials
  • pharmaceutical engineering
  • targeting
  • solubilization technology
  • controlled release
  • microneedle
  • formulation of various routes of administration
  • lipid-based system

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Published Papers (3 papers)

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Research

19 pages, 5978 KiB  
Article
Aryl-Capped Lysine-Dehydroamino Acid Dipeptide Supergelators as Potential Drug Release Systems
by Carlos B. P. Oliveira, Renato B. Pereira, David M. Pereira, Loic Hilliou, Tarsila G. Castro, José A. Martins, Peter J. Jervis and Paula M. T. Ferreira
Int. J. Mol. Sci. 2022, 23(19), 11811; https://doi.org/10.3390/ijms231911811 - 5 Oct 2022
Cited by 4 | Viewed by 2178
Abstract
Employing amino acids and peptides as molecular building blocks provides unique opportunities for generating supramolecular hydrogels, owing to their inherent biological origin, bioactivity, biocompatibility, and biodegradability. However, they can suffer from proteolytic degradation. Short peptides (<8 amino acids) attached to an aromatic capping [...] Read more.
Employing amino acids and peptides as molecular building blocks provides unique opportunities for generating supramolecular hydrogels, owing to their inherent biological origin, bioactivity, biocompatibility, and biodegradability. However, they can suffer from proteolytic degradation. Short peptides (<8 amino acids) attached to an aromatic capping group are particularly attractive alternatives for minimalistic low molecular weight hydrogelators. Peptides with low critical gelation concentrations (CGCs) are especially desirable, as the low weight percentage required for gelation makes them more cost-effective and reduces toxicity. In this work, three dehydrodipeptides were studied for their self-assembly properties. The results showed that all three dehydrodipeptides can form self-standing hydrogels with very low critical gelation concentrations (0.05–0.20 wt%) using a pH trigger. Hydrogels of all three dehydrodipeptides were characterised by scanning tunnelling emission microscopy (STEM), rheology, fluorescence spectroscopy, and circular dichroism (CD) spectroscopy. Molecular modelling was performed to probe the structural patterns and interactions. The cytotoxicity of the new compounds was tested using human keratinocytes (HaCaT cell line). In general, the results suggest that all three compounds are non-cytotoxic, although one of the peptides shows a small impact on cell viability. In sustained release assays, the effect of the charge of the model drug compounds on the rate of cargo release from the hydrogel network was evaluated. The hydrogels provide a sustained release of methyl orange (anionic) and ciprofloxacin (neutral), while methylene blue (cationic) was retained by the network. Full article
(This article belongs to the Special Issue Nanotechnology for Drug Delivery)
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13 pages, 4403 KiB  
Article
Effects of Polymers on the Drug Solubility and Dissolution Enhancement of Poorly Water-Soluble Rivaroxaban
by Min-Jong Choi, Mi Ran Woo, Han-Gon Choi and Sung Giu Jin
Int. J. Mol. Sci. 2022, 23(16), 9491; https://doi.org/10.3390/ijms23169491 - 22 Aug 2022
Cited by 36 | Viewed by 4721
Abstract
The purpose of this study was to investigate the efficacy of hydrophilic polymers in a solid dispersion formulation in improving the solubility and dissolution rate of rivaroxaban (RXB), a poorly soluble drug. The developed solid dispersion consisted of two components, a drug and [...] Read more.
The purpose of this study was to investigate the efficacy of hydrophilic polymers in a solid dispersion formulation in improving the solubility and dissolution rate of rivaroxaban (RXB), a poorly soluble drug. The developed solid dispersion consisted of two components, a drug and a polymer, and the drug was dispersed as amorphous particles in a polymer matrix using the spray drying method. Polymeric solid dispersions were evaluated using solubility tests, in vitro dissolution tests, powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and particle size distribution analysis. To maximize physical stability against crystallization and improve the solubility and dissolution of RXB, it is important to select the appropriate polymer type and the optimal ratio of the polymer to the drug. The optimized polyvinyl alcohol (PVA)-based (1/0.5, w/w) and gelatin-based (1/5, w/w) solid dispersion formulations showed 6.3 and 3.6 times higher drug solubilities than pure RXB powder, respectively, and the final dissolution rate was improved by approximately 1.5 times. Scanning electron microscopy and particle size distribution analyses confirmed that the gelatin-based solid dispersion was smaller and more spherical than the PVA-based solid dispersion, suggesting that the gelatin-based solid dispersion had a faster initial dissolution rate. Differential scanning calorimetry and powder X-ray diffraction analyses confirmed that RXB had successfully changed from a crystalline form to an amorphous form, contributing to the improvement in its solubility and dissolution rate. This study provides a strategy for selecting suitable polymers for the development of amorphous polymer solid dispersions that can overcome precipitation during dissolution and stabilization of the amorphous state. In addition, the selected polymer solid dispersion improved the drug solubility and dissolution rate of RXB, a poorly soluble drug, and may be used as a promising drug delivery system. Full article
(This article belongs to the Special Issue Nanotechnology for Drug Delivery)
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40 pages, 11296 KiB  
Article
A Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound
by Emilia Jakubowska, Bartłomiej Milanowski and Janina Lulek
Int. J. Mol. Sci. 2021, 22(22), 12406; https://doi.org/10.3390/ijms222212406 - 17 Nov 2021
Cited by 13 | Viewed by 3380
Abstract
Nanosizing is an approach to improve the dissolution rate of poorly soluble drugs. The first aim of this work was to develop nanosuspension of cilostazol with liquid antisolvent precipitation (LASP) and its combination with ultrasound. Second, to systematically study the effect of bottom-up [...] Read more.
Nanosizing is an approach to improve the dissolution rate of poorly soluble drugs. The first aim of this work was to develop nanosuspension of cilostazol with liquid antisolvent precipitation (LASP) and its combination with ultrasound. Second, to systematically study the effect of bottom-up processing factors on precipitated particles’ size and identify the optimal settings for the best reduction. After solvent and stabilizer screening, in-depth process characterization and optimization was performed using Design of Experiments. The work discusses the influence of critical factors found with statistical analysis: feed concentration, stabilizer amount, stirring speed and ultrasound energy governed by time and amplitude. LASP alone only generated particle size of a few microns, but combination with ultrasound was successful in nanosizing (d10 = 0.06, d50 = 0.33, d90 = 1.45 µm). Micro- and nanosuspension’s stability, particle morphology and solid state were studied. Nanosuspension displayed higher apparent solubility than equilibrium and superior dissolution rate over coarse cilostazol and microsuspension. A bottom-up method of precipitation-sonication was demonstrated to be a successful approach to improve the dissolution characteristics of poorly soluble, BCS class II drug cilostazol by reducing its particle size below micron scale, while retaining nanosuspension stability and unchanged crystalline form. Full article
(This article belongs to the Special Issue Nanotechnology for Drug Delivery)
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