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Advances of Colloidal Systems in Drug Delivery and Therapeutic Application,...
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Advances of Colloidal Systems in Drug Delivery and Therapeutic Application, 2nd Edition

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

Deadline for manuscript submissions: closed (20 December 2023) | Viewed by 9054

Special Issue Editors

Prof. Dr. Ana Fernandez-Carballido

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Guest Editor
Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid, 28040 Madrid, Spain
Interests: nanomedicine; nanoparticles; microparticles; targeted treatment; breast cancer; chemotherapy
Special Issues, Collections and Topics in MDPI journals
Dr. Cristina Martín-Sabroso

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Guest Editor
Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid, 28040 Madrid, Spain
Interests: chorioallantoic membrane model; cannabinoids; cannabidiol; gynaecological cancer; nanomedicines
Special Issues, Collections and Topics in MDPI journals
Dr. Juan Aparicio-Blanco

E-Mail Website
Guest Editor
Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid, 28040 Madrid, Spain
Interests: nanomedicine; brain drug delivery; brain diseases; lipid nanocapsules; glioma; cannabinoids; tailored carriers
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The number of formulations of colloidal systems approved by the FDA and the EMA in recent years has been increasing, in applications as varied as in the treatment of cancer, vaccines, dry eye or fungal infections. However, it is an area undergoing continuous expansion thanks to the research of new biomaterials or polymers that improve the kinetics of drug release as well as the functionalization of these systems with the aim of achieving active targeting of the therapeutic target. In addition, in the context of challenges still lying ahead with the increasing number of marketed colloids for biomedical purposes, their characterization techniques remain to be fully established, as in the case of “macro” dosage forms.

In the present Special Issue, studies reporting original data or updated literature reviews aimed at characterization, development or therapeutic application of colloidal systems are welcome. Our aim is to compile the latest developments in the area of characterization, development or therapeutic application of colloidal systems, contributions reporting original data or updated literature reviews on this topic are welcome in this Special Issue.

Prof. Dr. Ana Fernandez-Carballido
Dr. Cristina Martín-Sabroso
Dr. Juan Aparicio-Blanco
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • novel production methods
  • smart colloids
  • colloidal systems
  • biomaterials
  • novel characterization techniques
  • quality by design

Published Papers (7 papers)

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Research

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19 pages, 2656 KiB  
Article
Effect of Molecules’ Physicochemical Properties on Whey Protein/Alginate Hydrogel Rheology, Microstructure and Release Profile
by A. Delanne-Cuménal, E. Lainé, V. Hoffart, V. Verney, G. Garrait and E. Beyssac
Pharmaceutics 2024, 16(2), 258; https://doi.org/10.3390/pharmaceutics16020258 - 09 Feb 2024
Viewed by 829
Abstract
The encapsulation of molecules with different physicochemical properties (theophylline, blue dextran, salicylic acid and insulin) in whey protein (WP) and alginate (ALG) microparticles (MP) for oral administration was studied. MP based on WP/ALG were prepared by a cold gelation technique and coated with [...] Read more.
The encapsulation of molecules with different physicochemical properties (theophylline, blue dextran, salicylic acid and insulin) in whey protein (WP) and alginate (ALG) microparticles (MP) for oral administration was studied. MP based on WP/ALG were prepared by a cold gelation technique and coated with WP solution after reticulation. Molecules influenced polymer solution viscosity and elasticity, resulting in differences regarding encapsulation efficiency (from 23 to 100%), MP structure and swelling (>10%) and in terms of pH tested. Molecule release was due to diffusion and/or erosion of MP and was very dependent on the substance encapsulated. All the loaded MP were successfully coated, but variation in coating thickness (from 68 to 146 µm) and function of the molecules encapsulated resulted in differences in molecule release (5 to 80% in 1 h). Gel rheology modification, due to interactions between WP, ALG, calcium and other substances, was responsible for the highlighted differences. Measuring rheologic parameters before extrusion and reticulation appeared to be one of the most important aspects to study in order to successfully develop a vector with optimal biopharmaceutical properties. Our vector seems to be more appropriate for anionic high-molecular-weight substances, leading to high viscosity and elasticity and to MP enabling gastroresistance and controlled release of molecules at intestinal pH. Full article
(This article belongs to the Special Issue Advances of Colloidal Systems in Drug Delivery and Therapeutic Application, 2nd Edition)
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19 pages, 1821 KiB  
Article
Design of High-Payload Ascorbyl Palmitate Nanosuspensions for Enhanced Skin Delivery
by Jun-Soo Park, Jun-Hyuk Choi, Min-Yeong Joung, In-Gyu Yang, Yong-Seok Choi, Myung-Joo Kang and Myoung-Jin Ho
Pharmaceutics 2024, 16(2), 171; https://doi.org/10.3390/pharmaceutics16020171 - 25 Jan 2024
Viewed by 803
Abstract
A high-payload ascorbyl palmitate (AP) nanosuspension (NS) was designed to improve skin delivery following topical application. The AP-loaded NS systems were prepared using the bead-milling technique, and softly thickened into NS-loaded gel (NS-G) using hydrophilic polymers. The optimized NS-G system consisted of up [...] Read more.
A high-payload ascorbyl palmitate (AP) nanosuspension (NS) was designed to improve skin delivery following topical application. The AP-loaded NS systems were prepared using the bead-milling technique, and softly thickened into NS-loaded gel (NS-G) using hydrophilic polymers. The optimized NS-G system consisted of up to 75 mg/mL of AP, 0.5% w/v of polyoxyl-40 hydrogenated castor oil (Kolliphor® RH40) as the suspending agent, and 1.0% w/v of sodium carboxymethyl cellulose (Na.CMC 700 K) as the thickening agent, in citrate buffer (pH 4.5). The NS-G system was embodied as follows: long and flaky nanocrystals, 493.2 nm in size, −48.7 mV in zeta potential, and 2.3 cP of viscosity with a shear rate of 100 s−1. Both NS and NS-G provided rapid dissolution of the poorly water-soluble antioxidant, which was comparable to that of the microemulsion gel (ME-G) containing AP in solubilized form. In an ex vivo skin absorption study using the Franz diffusion cell mounted on porcine skin, NS-G exhibited faster absorption in skin, providing approximately 4, 3, and 1.4 times larger accumulation than that of ME-G at 3, 6, and 12 h, respectively. Therefore, the high-payload NS makes it a promising platform for skin delivery of the lipid derivative of ascorbic acid. Full article
(This article belongs to the Special Issue Advances of Colloidal Systems in Drug Delivery and Therapeutic Application, 2nd Edition)
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15 pages, 2658 KiB  
Article
Cell Staining Microgels Derived from a Natural Phenolic Dye: Hematoxylin Has Intriguing Biomedical Potential
by Mehtap Sahiner, Aydin K. Sunol and Nurettin Sahiner
Pharmaceutics 2024, 16(1), 147; https://doi.org/10.3390/pharmaceutics16010147 - 22 Jan 2024
Viewed by 742
Abstract
Hematoxylin (HT) as a natural phenolic dye compound is generally used together with eosin (E) dye as H&E in the histological staining of tissues. Here, we report for the first time the polymeric particle preparation from HT as poly(Hematoxylin) ((p(HT)) microgels via microemulsion [...] Read more.
Hematoxylin (HT) as a natural phenolic dye compound is generally used together with eosin (E) dye as H&E in the histological staining of tissues. Here, we report for the first time the polymeric particle preparation from HT as poly(Hematoxylin) ((p(HT)) microgels via microemulsion method in a one-step using a benign crosslinker, glycerol diglycidyl ether (GDE). P(HT) microgels are about 10 µm and spherical in shape with a zeta potential value of −34.6 ± 2.8 mV and an isoelectric point (IEP) of pH 1.79. Interestingly, fluorescence properties of HT molecules were retained upon microgel formation, e.g., the fluorescence emission intensity of p(HT) at 343 nm was about 2.8 times less than that of the HT molecule at λex: 300 nm. P(HT) microgels are hydrolytically degradable and can be controlled by using an amount of crosslinker, GDE, e.g., about 40%, 20%, and 10% of p(HT) microgels was degraded in 15 days in aqueous environments for the microgels prepared at 100, 200, and 300% mole ratios of GDE to HT, respectively. Interestingly, HT molecules at 1000 mg/mL showed 22.7 + 0.4% cell viability whereas the p(HT) microgels exhibited a cell viability of 94.3 + 7.2% against fibroblast cells. Furthermore, even at 2000 mg/mL concentrations of HT and p(HT), the inhibition% of α-glucosidase enzyme were measured as 93.2 ± 0.3 and 81.3 ± 6.3%, respectively at a 0.03 unit/mL enzyme concentration, establishing some potential application of p(HT) microgels for neurogenerative diseases. Moreover, p(HT) microgels showed two times higher MBC values than HT molecules, e.g., 5.0 versus 2.5 mg/mL MIC values against Gram-negative E. coli and Gram-positive S. aureus, respectively. Full article
(This article belongs to the Special Issue Advances of Colloidal Systems in Drug Delivery and Therapeutic Application, 2nd Edition)
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37 pages, 5311 KiB  
Article
Gemcitabine-Vitamin E Prodrug-Loaded Micelles for Pancreatic Cancer Therapy
by Miguel Pereira-Silva, Darío Miranda-Pastoriza, Luis Diaz-Gomez, Eddy Sotelo, Ana Cláudia Paiva-Santos, Francisco Veiga, Angel Concheiro and Carmen Alvarez-Lorenzo
Pharmaceutics 2024, 16(1), 95; https://doi.org/10.3390/pharmaceutics16010095 - 10 Jan 2024
Viewed by 1553
Abstract
Pancreatic cancer (PC) is an aggressive cancer subtype presenting unmet clinical challenges. Conventional chemotherapy, which includes antimetabolite gemcitabine (GEM), is seriously undermined by a short half-life, its lack of targeting ability, and systemic toxicity. GEM incorporation in self-assembled nanosystems is still underexplored due [...] Read more.
Pancreatic cancer (PC) is an aggressive cancer subtype presenting unmet clinical challenges. Conventional chemotherapy, which includes antimetabolite gemcitabine (GEM), is seriously undermined by a short half-life, its lack of targeting ability, and systemic toxicity. GEM incorporation in self-assembled nanosystems is still underexplored due to GEM’s hydrophilicity which hinders efficient encapsulation. We hypothesized that vitamin E succinate–GEM prodrug (VES-GEM conjugate) combines hydrophobicity and multifunctionalities that can facilitate the development of Pluronic® F68 and Pluronic® F127 micelle-based nanocarriers, improving the therapeutic potential of GEM. Pluronic® F68/VES-GEM and Pluronic® F127/VES-GEM micelles covering a wide range of molar ratios were prepared by solvent evaporation applying different purification methods, and characterized regarding size, charge, polydispersity index, morphology, and encapsulation. Moreover, the effect of sonication and ultrasonication and the influence of a co-surfactant were explored together with drug release, stability, blood compatibility, efficacy against tumour cells, and cell uptake. The VES-GEM conjugate-loaded micelles showed acceptable size and high encapsulation efficiency (>95%) following an excipient reduction rationale. Pluronic® F127/VES-GEM micelles evidenced a superior VES-GEM release profile (cumulative release > 50%, pH = 7.4), stability, cell growth inhibition (<50% cell viability for 100 µM VES-GEM), blood compatibility, and extensive cell internalization, and therefore represent a promising approach to leveraging the efficacy and safety of GEM for PC-targeted therapies. Full article
(This article belongs to the Special Issue Advances of Colloidal Systems in Drug Delivery and Therapeutic Application, 2nd Edition)
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17 pages, 3942 KiB  
Article
Preparation of Dihydromyricetin-Loaded Self-Emulsifying Drug Delivery System and Its Anti-Alcoholism Effect
by Jianxia Dong, Shu Wang, Jiamin Mao, Zhidan Wang, Shiying Zhao, Qiao Ren, Jialing Kang, Jing Ye, Xiaohong Xu, Yujin Zhu and Quan Zhang
Pharmaceutics 2023, 15(9), 2296; https://doi.org/10.3390/pharmaceutics15092296 - 08 Sep 2023
Cited by 1 | Viewed by 998
Abstract
Intraperitoneal injection of dihydromyricetin (DMY) has shown promising potential in the treatment of alcoholism. However, its therapeutic effect is limited due to its low solubility, poor stability, and high gut-liver first-pass metabolism, resulting in very low oral bioavailability. In this study, we developed [...] Read more.
Intraperitoneal injection of dihydromyricetin (DMY) has shown promising potential in the treatment of alcoholism. However, its therapeutic effect is limited due to its low solubility, poor stability, and high gut-liver first-pass metabolism, resulting in very low oral bioavailability. In this study, we developed a DMY-loaded self-emulsifying drug delivery system (DMY-SEDDS) to enhance the oral bioavailability and anti-alcoholism effect of DMY. DMY-SEDDS improved the oral absorption of DMY by facilitating lymphatic transport. The area under the concentration-time curve (AUC) of DMY in the DMY-SEDDS group was 4.13-fold higher than in the DMY suspension group. Furthermore, treatment with DMY-SEDDS significantly enhanced the activities of alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH) in the liver of mice (p < 0.05). Interestingly, DMY-SEDDS also increased ADH activity in the stomach of mice with alcoholism (p < 0.01), thereby enhancing ethanol metabolism in the gastrointestinal tract and reducing ethanol absorption into the bloodstream. As a result, the blood alcohol concentration of mice with alcoholism was significantly decreased after DMY-SEDDS treatment (p < 0.01). In the acute alcoholism mice model, compared to saline treatment, DMY-SEDDS prolonged the onset of LORR (loss of righting reflex) (p < 0.05) and significantly shortened the duration of LORR (p < 0.01). Additionally, DMY-SEDDS treatment significantly reduced gastric injury in acute alcoholism mice. Collectively, these findings demonstrate the potential of DMY-SEDDS as a treatment in the treatment of alcoholism. Full article
(This article belongs to the Special Issue Advances of Colloidal Systems in Drug Delivery and Therapeutic Application, 2nd Edition)
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Review

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32 pages, 2419 KiB  
Review
Assessment of In Vitro Release Testing Methods for Colloidal Drug Carriers: The Lack of Standardized Protocols
by Laura Gómez-Lázaro, Cristina Martín-Sabroso, Juan Aparicio-Blanco and Ana Isabel Torres-Suárez
Pharmaceutics 2024, 16(1), 103; https://doi.org/10.3390/pharmaceutics16010103 - 12 Jan 2024
Viewed by 1213
Abstract
Although colloidal carriers have been in the pipeline for nearly four decades, standardized methods for testing their drug-release properties remain to be established in pharmacopeias. The in vitro assessment of drug release from these colloidal carriers is one of the most important parameters [...] Read more.
Although colloidal carriers have been in the pipeline for nearly four decades, standardized methods for testing their drug-release properties remain to be established in pharmacopeias. The in vitro assessment of drug release from these colloidal carriers is one of the most important parameters in the development and quality control of drug-loaded nano- and microcarriers. This lack of standardized protocols occurs due to the difficulties encountered in separating the released drug from the encapsulated one. This review aims to compare the most frequent types of release testing methods (i.e., membrane diffusion techniques, sample and separate methods and in situ detection techniques) in terms of the advantages and disadvantages of each one and of the key parameters that influence drug release in each case. Full article
(This article belongs to the Special Issue Advances of Colloidal Systems in Drug Delivery and Therapeutic Application, 2nd Edition)
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39 pages, 5389 KiB  
Review
Nano- and Microemulsions in Biomedicine: From Theory to Practice
by Boris Nikolaev, Ludmila Yakovleva, Viacheslav Fedorov, Hanmei Li, Huile Gao and Maxim Shevtsov
Pharmaceutics 2023, 15(7), 1989; https://doi.org/10.3390/pharmaceutics15071989 - 20 Jul 2023
Cited by 7 | Viewed by 2440
Abstract
Nano- and microemulsions are colloidal systems that are widely used in various fields of biomedicine, including wound and burn healing, cosmetology, the development of antibacterial and antiviral drugs, oncology, etc. The stability of these systems is governed by the balance of molecular interactions [...] Read more.
Nano- and microemulsions are colloidal systems that are widely used in various fields of biomedicine, including wound and burn healing, cosmetology, the development of antibacterial and antiviral drugs, oncology, etc. The stability of these systems is governed by the balance of molecular interactions between nanodomains. Microemulsions as a colloidal form play a special important role in stability. The microemulsion is the thermodynamically stable phase from oil, water, surfactant and co-surfactant which forms the surface of drops with very small surface energy. The last phenomena determines the shortage time of all fluid dispersions including nanoemulsions and emulgels. This review examines the theory and main methods of obtaining nano- and microemulsions, particularly focusing on the structure of microemulsions and methods for emulsion analysis. Additionally, we have analyzed the main preclinical and clinical studies in the field of wound healing and the use of emulsions in cancer therapy, emphasizing the prospects for further developments in this area. Full article
(This article belongs to the Special Issue Advances of Colloidal Systems in Drug Delivery and Therapeutic Application, 2nd Edition)
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