Life | Special Issue : Revolutionizing Drug Delivery: Innovations in Targeted Therapeutic Nanocarriers

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17 pages, 5405 KiB

Open AccessArticle

Development, Analysis, and Determination of Pharmacokinetic Properties of a Solid SMEDDS of Voriconazole for Enhanced Antifungal Therapy

by Hitesh Kumar Dewangan, Rajiv Sharma, Kamal Shah and Perwez Alam

Life 2024, 14(11), 1417; https://doi.org/10.3390/life14111417 - 2 Nov 2024

Viewed by 488

Abstract

Background: Voriconazole is an antifungal drug, which is classified under Bio-Classification System-II and has low water solubility (0.71 mg/mL) and high permeability. Hardly any endeavors have been made to increase the bioavailability of voriconazole. Objective: To develop and evaluate a solid SMEDDS (self-microemulsifying [...] Read more.

Background: Voriconazole is an antifungal drug, which is classified under Bio-Classification System-II and has low water solubility (0.71 mg/mL) and high permeability. Hardly any endeavors have been made to increase the bioavailability of voriconazole. Objective: To develop and evaluate a solid SMEDDS (self-microemulsifying drug delivery system) for antifungal activity. Methods: Based on solubility studies of Labrafil-M 1994 CS (oil), Cremophor-RH 40 (a surfactant) and Transcutol-HP (a co-surfactant) were selected as components of the SMEDDS and a pseudo-ternary phase diagram was prepared. Thereafter, the oil, surfactant, and co-surfactant were mixed with altered weight ratios (1:1/1:2/2:1) and evaluated through various in vitro, in vivo analyses. Results: The particle size of the optimized formulation was observed to be 19.04 nm and the polydispersity index (PDI) value was found to be 0.162 with steady-state zeta potential. The optimized liquid SMEDDS was converted into a solid SMEDDS. Various adsorbents, such as Aerosil-200, Avicel-PH101, Neusilin-US2, and Neusilin UFL2 were screened to better detect the oil-absorbing capacity and flow properties of the powder. Neusilin UFL2 was selected as an adsorbent due to its better oil-absorbing capacity. DSC, X-ray diffraction, and dissolution studies were carried out to characterize the formulation. Further, the Pharmacokinetic profile was also studied in Wistar rats and the Cmax, tmax, and AUC0→t were calculated. The Cmax and AUC0→t plasma concentration is considerably better for the SMEDDS than for the pure drug and marketed formulation. Conclusions: This investigation clearly reveals the potential of developing a solid SMEDDS for candidiasis and invasive aspergillosis treatment, with better efficacy as compared to the commercially available marketed formulation. Full article

(This article belongs to the Special Issue Revolutionizing Drug Delivery: Innovations in Targeted Therapeutic Nanocarriers)

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19 pages, 2868 KiB

Open AccessArticle

Retinol and Oligopeptide-Loaded Lipid Nanocarriers as Effective Raw Material in Anti-Acne and Anti-Aging Therapies

by Małgorzata Pawłowska, Marta Marzec, Waldemar Jankowiak and Izabela Nowak

Life 2024, 14(10), 1212; https://doi.org/10.3390/life14101212 - 24 Sep 2024

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Abstract

The use of lipid nanocarriers as components of cosmetic formulations may provide an opportunity to fully exploit the beneficial properties of pentapeptide-18 and retinol while reducing the undesirable effects that occur during retinoid therapy. This study aimed to evaluate the effectiveness of semi-solid [...] Read more.

The use of lipid nanocarriers as components of cosmetic formulations may provide an opportunity to fully exploit the beneficial properties of pentapeptide-18 and retinol while reducing the undesirable effects that occur during retinoid therapy. This study aimed to evaluate the effectiveness of semi-solid formulations enriched with retinol and oligopeptide-loaded lipid nanocarriers. Solid lipid nanoparticles were produced using a high-shear homogenization method. The work included physicochemical characterization of the cosmetic products, and evaluation of their stability as well as their efficacy. The resulting semi-solid preparations were determined to be stable regardless of their storage temperature. No effect of the presence of lipid nanoparticles on the shelf-life stability of the cosmetic products was observed. A temperature of 25 °C was considered the recommended storage temperature for the tested semi-solid formulations. Beneficial effects of the cosmetic products were proven (in vivo study on volunteers), i.e., a significant reduction in the level of sebum secretion (anti-acne therapy) and a decrease in the number of facial wrinkles (anti-aging therapy). In addition, the protective properties of the lipid nanoparticles themselves against the skin were confirmed, reducing the irritating effect of retinol that is usually the case with classic retinoid therapies. Full article

(This article belongs to the Special Issue Revolutionizing Drug Delivery: Innovations in Targeted Therapeutic Nanocarriers)

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32 pages, 4170 KiB

Open AccessArticle

Role of Natural Binding Proteins in Therapy and Diagnostics

by Marco Eigenfeld, Kilian F. M. Lupp and Sebastian P. Schwaminger

Life 2024, 14(5), 630; https://doi.org/10.3390/life14050630 - 15 May 2024

Viewed by 1536

Abstract

This review systematically investigates the critical role of natural binding proteins (NBPs), encompassing DNA-, RNA-, carbohydrate-, fatty acid-, and chitin-binding proteins, in the realms of oncology and diagnostics. In an era where cancer continues to pose significant challenges to healthcare systems worldwide, the [...] Read more.

This review systematically investigates the critical role of natural binding proteins (NBPs), encompassing DNA-, RNA-, carbohydrate-, fatty acid-, and chitin-binding proteins, in the realms of oncology and diagnostics. In an era where cancer continues to pose significant challenges to healthcare systems worldwide, the innovative exploration of NBPs offers a promising frontier for advancing both the diagnostic accuracy and therapeutic efficacy of cancer management strategies. This manuscript provides an in-depth examination of the unique mechanisms by which NBPs interact with specific molecular targets, highlighting their potential to revolutionize cancer diagnostics and therapy. Furthermore, it discusses the burgeoning research on aptamers, demonstrating their utility as ‘nucleic acid antibodies’ for targeted therapy and precision diagnostics. Despite the promising applications of NBPs and aptamers in enhancing early cancer detection and developing personalized treatment protocols, this review identifies a critical knowledge gap: the need for comprehensive studies to understand the diverse functionalities and therapeutic potentials of NBPs across different cancer types and diagnostic scenarios. By bridging this gap, this manuscript underscores the importance of NBPs and aptamers in paving the way for next-generation diagnostics and targeted cancer treatments. Full article

(This article belongs to the Special Issue Revolutionizing Drug Delivery: Innovations in Targeted Therapeutic Nanocarriers)

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17 pages, 3917 KiB

Open AccessArticle

The Synthesis and Characterization of a Delivery System Based on Polymersomes and a Xanthone with Inhibitory Activity in Glioblastoma

by Ana Alves, Ana Margarida Silva, Claúdia Nunes, Sara Cravo, Salette Reis, Madalena Pinto, Emília Sousa, Francisca Rodrigues, Domingos Ferreira, Paulo C. Costa and Marta Correia-da-Silva

Life 2024, 14(1), 132; https://doi.org/10.3390/life14010132 - 17 Jan 2024

Cited by 2 | Viewed by 1910

Abstract

Glioblastoma (GBM) is the most common and deadly primary malignant brain tumor. Current therapies are insufficient, and survival for individuals diagnosed with GBM is limited to a few months. New GBM treatments are urgent. Polymeric nanoparticles (PNs) can increase the circulation time of [...] Read more.

Glioblastoma (GBM) is the most common and deadly primary malignant brain tumor. Current therapies are insufficient, and survival for individuals diagnosed with GBM is limited to a few months. New GBM treatments are urgent. Polymeric nanoparticles (PNs) can increase the circulation time of a drug in the brain capillaries. Polymersomes (PMs) are PNs that have been described as having attractive characteristics, mainly due to their stability, prolonged circulation period, biodegradability, their ability to sustain the release of drugs, and the possibility of surface functionalization. In this work, a poly(ethylene glycol)-ε-caprolactone (PEG-PCL) copolymer was synthesized and PMs were prepared and loaded with an hydrolytic instable compound, previously synthesized by our research team, the 3,6-bis(2,3,4,6-tetra-O-acetyl-β-glucopyranosyl)xanthone (XGAc), with promising cytotoxicity on glioblastoma cells (U-373 MG) but also on healthy cerebral endothelial cells (hCMEC/D3). The prepared PMs were spherical particles with uniform morphology and similar sizes (mean diameter of 200 nm) and were stable in aqueous suspension. The encapsulation of XGAc in PMs (80% encapsulation efficacy) protected the healthy endothelial cells from the cytotoxic effects of this compound, while maintaining cytotoxicity for the glioblastoma cell line U-373 MG. Our studies also showed that the prepared PMs can efficiently release XGAc at intratumoral pHs. Full article

(This article belongs to the Special Issue Revolutionizing Drug Delivery: Innovations in Targeted Therapeutic Nanocarriers)

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Review

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22 pages, 1948 KiB

Open AccessReview

Targeted Liposomal Drug Delivery: Overview of the Current Applications and Challenges

by Matthew S. Gatto, McNeely P. Johnson and Wided Najahi-Missaoui

Life 2024, 14(6), 672; https://doi.org/10.3390/life14060672 - 24 May 2024

Cited by 5 | Viewed by 3769

Abstract

In drug development, it is not uncommon that an active substance exhibits efficacy in vitro but lacks the ability to specifically reach its target in vivo. As a result, targeted drug delivery has become a primary focus in the pharmaceutical sciences. Since the [...] Read more.

In drug development, it is not uncommon that an active substance exhibits efficacy in vitro but lacks the ability to specifically reach its target in vivo. As a result, targeted drug delivery has become a primary focus in the pharmaceutical sciences. Since the approval of Doxil^® in 1995, liposomes have emerged as a leading nanoparticle in targeted drug delivery. Their low immunogenicity, high versatility, and well-documented efficacy have led to their clinical use against a wide variety of diseases. That being said, every disease is accompanied by a unique set of physiological conditions, and each liposomal product must be formulated with this consideration. There are a multitude of different targeting techniques for liposomes that can be employed depending on the application. Passive techniques such as PEGylation or the enhanced permeation and retention effect can improve general pharmacokinetics, while active techniques such as conjugating targeting molecules to the liposome surface may bring even further specificity. This review aims to summarize the current strategies for targeted liposomes in the treatment of diseases. Full article

(This article belongs to the Special Issue Revolutionizing Drug Delivery: Innovations in Targeted Therapeutic Nanocarriers)

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18 pages, 1513 KiB

Open AccessReview

Approaches to Characterize and Quantify Extracellular Vesicle Surface Conjugation Efficiency

by Leora Goldbloom-Helzner, Harjn Bains and Aijun Wang

Life 2024, 14(4), 511; https://doi.org/10.3390/life14040511 - 15 Apr 2024

Cited by 1 | Viewed by 2346

Abstract

Extracellular vesicles (EVs) are cell-secreted nanovesicles that play an important role in long-range cell–cell communication. Although EVs pose a promising alternative to cell-based therapy, targeted in vivo delivery still falls short. Many studies have explored the surface modification of EVs to enhance their [...] Read more.

Extracellular vesicles (EVs) are cell-secreted nanovesicles that play an important role in long-range cell–cell communication. Although EVs pose a promising alternative to cell-based therapy, targeted in vivo delivery still falls short. Many studies have explored the surface modification of EVs to enhance their targeting capabilities. However, to our knowledge, there are no standardized practices to confirm the successful surface modification of EVs or calculate the degree of conjugation on EV surfaces (conjugation efficiency). These pieces of information are essential in the reproducibility of targeted EV therapeutics and the determination of optimized conjugation conditions for EVs to see significant therapeutic effects in vitro and in vivo. This review will discuss the vast array of techniques adopted, technologies developed, and efficiency definitions made by studies that have calculated EV/nanoparticle surface conjugation efficiency and how differences between studies may contribute to differently reported conjugation efficiencies. Full article

(This article belongs to the Special Issue Revolutionizing Drug Delivery: Innovations in Targeted Therapeutic Nanocarriers)

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21 pages, 3217 KiB

Open AccessReview

Analytical Techniques for Characterizing Tumor-Targeted Antibody-Functionalized Nanoparticles

by Ana Camila Marques, Paulo C. Costa, Sérgia Velho and Maria Helena Amaral

Life 2024, 14(4), 489; https://doi.org/10.3390/life14040489 - 10 Apr 2024

Viewed by 1773

Abstract

The specific interaction between cell surface receptors and corresponding antibodies has driven opportunities for developing targeted cancer therapies using nanoparticle systems. It is challenging to design and develop such targeted nanomedicines using antibody ligands, as the final nanoconjugate’s specificity hinges on the cohesive [...] Read more.

The specific interaction between cell surface receptors and corresponding antibodies has driven opportunities for developing targeted cancer therapies using nanoparticle systems. It is challenging to design and develop such targeted nanomedicines using antibody ligands, as the final nanoconjugate’s specificity hinges on the cohesive functioning of its components. The multicomponent nature of antibody-conjugated nanoparticles also complicates the characterization process. Regardless of the type of nanoparticle, it is essential to perform physicochemical characterization to establish a solid foundation of knowledge and develop suitable preclinical studies. A meaningful physicochemical evaluation of antibody-conjugated nanoparticles should include determining the quantity and orientation of the antibodies, confirming the antibodies’ integrity following attachment, and assessing the immunoreactivity of the obtained nanoconjugates. In this review, the authors describe the various techniques (electrophoresis, spectroscopy, colorimetric assays, immunoassays, etc.) used to analyze the physicochemical properties of nanoparticles functionalized with antibodies and discuss the main results. Full article

(This article belongs to the Special Issue Revolutionizing Drug Delivery: Innovations in Targeted Therapeutic Nanocarriers)

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37 pages, 2103 KiB

Open AccessEditor’s ChoiceReview

Integrating Artificial Intelligence for Drug Discovery in the Context of Revolutionizing Drug Delivery

by Anita Ioana Visan and Irina Negut

Life 2024, 14(2), 233; https://doi.org/10.3390/life14020233 - 7 Feb 2024

Cited by 31 | Viewed by 13762

Abstract

Drug development is expensive, time-consuming, and has a high failure rate. In recent years, artificial intelligence (AI) has emerged as a transformative tool in drug discovery, offering innovative solutions to complex challenges in the pharmaceutical industry. This manuscript covers the multifaceted role of [...] Read more.

Drug development is expensive, time-consuming, and has a high failure rate. In recent years, artificial intelligence (AI) has emerged as a transformative tool in drug discovery, offering innovative solutions to complex challenges in the pharmaceutical industry. This manuscript covers the multifaceted role of AI in drug discovery, encompassing AI-assisted drug delivery design, the discovery of new drugs, and the development of novel AI techniques. We explore various AI methodologies, including machine learning and deep learning, and their applications in target identification, virtual screening, and drug design. This paper also discusses the historical development of AI in medicine, emphasizing its profound impact on healthcare. Furthermore, it addresses AI’s role in the repositioning of existing drugs and the identification of drug combinations, underscoring its potential in revolutionizing drug delivery systems. The manuscript provides a comprehensive overview of the AI programs and platforms currently used in drug discovery, illustrating the technological advancements and future directions of this field. This study not only presents the current state of AI in drug discovery but also anticipates its future trajectory, highlighting the challenges and opportunities that lie ahead. Full article

(This article belongs to the Special Issue Revolutionizing Drug Delivery: Innovations in Targeted Therapeutic Nanocarriers)

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