Advancements in Ocular Therapy: A Review of Emerging Drug Delivery Approaches and Pharmaceutical Technologies
Serum Albumin in Nasal Drug Delivery Systems: Exploring the Role and Application
Development of Targeted Drug Delivery System for the Treatment of SARS-CoV-2 Using Aptamer-Conjugated Gold Nanoparticles

Journal Description

Pharmaceutics

Pharmaceutics is a peer-reviewed, open access journal on the science and technology of pharmaceutics and biopharmaceutics, and is published monthly online by MDPI. The Spanish Society of Pharmaceutics and Pharmaceutical Technology (SEFIG), Pharmaceutical Solid State Research Cluster (PSSRC), Academy of Pharmaceutical Sciences (APS) and Korean Society of Pharmaceutical Sciences and Technology (KSPST) are affiliated with Pharmaceutics and their members receive a discount on the article processing charges.

Open Access— free for readers, with article processing charges (APC) paid by authors or their institutions.
High Visibility: indexed within Scopus, SCIE (Web of Science), PubMed, PMC, Embase, CAPlus / SciFinder, and other databases.
Journal Rank: JCR - Q1 (Pharmacology and Pharmacy) / CiteScore - Q1 (Pharmaceutical Science)
Rapid Publication: manuscripts are peer-reviewed and a first decision is provided to authors approximately 14.9 days after submission; acceptance to publication is undertaken in 3.4 days (median values for papers published in this journal in the first half of 2024).
Recognition of Reviewers: reviewers who provide timely, thorough peer-review reports receive vouchers entitling them to a discount on the APC of their next publication in any MDPI journal, in appreciation of the work done.
Companion journals for Pharmaceutics include: Future Pharmacology and Journal of Pharmaceutical and BioTech Industry.

Impact Factor: 4.9 (2023); 5-Year Impact Factor: 5.5 (2023)

Imprint Information Journal Flyer Open Access ISSN: 1999-4923

Latest Articles

19 pages, 981 KiB

Open AccessArticle

Pharmacokinetic Interaction Between Olaparib and Regorafenib in an Animal Model

by Danuta Szkutnik-Fiedler, Agnieszka Karbownik, Filip Otto, Julia Maciejewska, Alicja Kuźnik, Tomasz Grabowski, Anna Wolc, Edmund Grześkowiak, Joanna Stanisławiak-Rudowicz and Edyta Szałek

Pharmaceutics 2024, 16(12), 1575; https://doi.org/10.3390/pharmaceutics16121575 - 9 Dec 2024

Abstract

Abstract: Background: Olaparib (OLA) and regorafenib (REG) are metabolized by the CYP3A4 isoenzyme of cytochrome P450. Both drugs are also substrates and inhibitors of the membrane transporters P-glycoprotein and BCRP. Therefore, the potential concomitant use of OLA and REG may result in clinically relevant drug–drug interactions. Knowledge of the influence of membrane transporters and cytochrome P450 enzymes on the pharmacokinetics of drugs makes it possible to assess their impact on the efficacy and safety of therapy. Purpose: The study aimed to evaluate the bilateral pharmacokinetic interactions of OLA and REG and its active metabolites after a single administration in healthy rats. Methods: The study was performed in male Wistar rats (n = 24) randomly divided into three groups: one study group, I_REG+OLA (n = 8), received REG with OLA, and two control groups, II_REG (n = 8) and III_OLA (n = 8), received REG and OLA, respectively. The concentrations of OLA, REG, REG-N-oxide (M-2), and N-desmethyl-REG-N-oxide (M-5) were determined by ultra-performance liquid chromatography–tandem mass spectrometry (UPLC-MS/MS). The values of the pharmacokinetic parameters of OLA, REG, M-2, and M-5 were determined by non-compartmental analysis with linear interpolation. Results: After OLA administration, the pharmacokinetic parameters of REG (AUC_0–∞, t_max, and t_0.5) increased significantly by 3.38-, 2.66-, and 1.82-fold, respectively. On the other hand, REG elimination parameters, i.e., k_el and Cl/F, were significantly reduced in the study group by 1.77- and 1.70-fold, respectively. In the study group, C_max and AUC_0-t values were also 7.22- and 8.86-fold higher for M-2 and 16.32- and 17.83-fold higher for M-5, respectively. The Metabolite M-2/Parent and Metabolite M-5/Parent ratios for C_max and AUC_0-t increased by 6.52-, 10.74-, 28-, and 13-fold, respectively. After administration of OLA with REG, the C_max, AUC_0-t, and AUC_0-∞ of OLA increased by 2.0-, 3.4-, and 3.4-fold, respectively, compared to the control group. Meanwhile, Cl/F and Vd/F of OLA were significantly decreased in the presence of REG. Conclusions: OLA was shown to significantly affect the pharmacokinetics of REG and its active metabolites M-2 and M-5 in rats after co-administration of both drugs. There was also a significant effect of REG on the pharmacokinetics of OLA, which may have clinical relevance. The AUC ratios (study group/control group) were 3.41 and 3.39 for REG and OLA, respectively, indicating that REG and OLA were moderate inhibitors in this preclinical study. The results obtained need to be confirmed in clinical studies. This study may provide guidance on the safety of using both drugs in clinical practice. Full article

(This article belongs to the Special Issue Kinase Inhibitors: Innovative Delivery Strategies and Anticancer Potential)

19 pages, 2029 KiB

Open AccessArticle

Enhanced Stability and In Vitro Biocompatibility of Chitosan-Coated Lipid Vesicles for Indomethacin Delivery

by Angy Abu Koush, Eliza Gratiela Popa, Daniela Angelica Pricop, Loredana Nita, Cezar-Ilie Foia, Ana-Maria Raluca Pauna, Beatrice Rozalina Buca, Liliana Lacramioara Pavel and Liliana Mititelu-Tartau

Pharmaceutics 2024, 16(12), 1574; https://doi.org/10.3390/pharmaceutics16121574 - 9 Dec 2024

Abstract

Background: Lipid vesicles, especially those utilizing biocompatible materials like chitosan (CHIT), hold significant promise for enhancing the stability and release characteristics of drugs such as indomethacin (IND), effectively overcoming the drawbacks associated with conventional drug formulations. Objectives: This study seeks to develop and characterize novel lipid vesicles composed of phosphatidylcholine and CHIT that encapsulate indomethacin (IND-ves), as well as to evaluate their in vitro hemocompatibility. Methods: The systems encapsulating IND were prepared using a molecular droplet self-assembly technique, involving the dissolution of lipids, cholesterol, and indomethacin in ethanol, followed by sonication and the gradual incorporation of a CHIT solution to form stable vesicular structures. The vesicles were characterized in terms of size, morphology, Zeta potential, and encapsulation efficiency and the profile release of drug was assessd. In vitro hemocompatibility was evaluated by measuring erythrocyte lysis and quantifying hemolysis rates. Results: The IND-ves exhibited an entrapment efficiency of 85%, with vesicles averaging 317.6 nm in size, and a Zeta potential of 24 mV, indicating good stability in suspension. In vitro release kinetics demonstrated an extended release profile of IND from the vesicles over 8 h, contrasting with the immediate release observed from plain drug solutions. The hemocompatibility assessment revealed that IND-ves exhibited minimal hemolysis, comparable to control groups, indicating good compatibility with erythrocytes. Conclusions: IND-ves provide a promising approach for modified indomethacin delivery, enhancing stability and hemocompatibility. These findings suggest their potential for effective NSAID delivery, with further in vivo studies required to explore clinical applications. Full article

(This article belongs to the Special Issue Recent Advances in Chitosan-Based Nanoparticles for Drug Delivery)

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22 pages, 4498 KiB

Open AccessArticle

Oral Delivery of miR146a Conjugated to Cerium Oxide Nanoparticles Improves an Established T Cell-Mediated Experimental Colitis in Mice

by Anisha Apte, Pujarini Dutta Dey, Srisaianirudh Reddy Julakanti, Monica Midura-Kiela, Stacy M. Skopp, Jimena Canchis, Tobias Fauser, James Bardill, Sudipta Seal, David M. Jackson, Fayez K. Ghishan, Pawel R. Kiela, Carlos Zgheib and Kenneth W. Liechty

Pharmaceutics 2024, 16(12), 1573; https://doi.org/10.3390/pharmaceutics16121573 - 9 Dec 2024

Abstract

Background: Dysregulated inflammation and oxidative stress are strongly implicated in the pathogenesis of inflammatory bowel disease. We have developed a novel therapeutic that targets inflammation and oxidative stress. It is comprised of microRNA-146a (miR146a)-loaded cerium oxide nanoparticles (CNPs) (CNP-miR146a). We hypothesized that oral delivery of CNP-miR146a would reduce colonic inflammation in a mouse model of established, chronic, T cell-mediated colitis. Methods: The stability of CNP-miR146a and mucosal delivery was assessed in vitro with simulated gastrointestinal fluid and in vivo after oral gavage by quantitative real-time RT-PCR. The efficacy of orally administered CNP-miR146a was tested in mice with established colitis using the model of adoptive naïve T-cell transfer in recombinant activating gene 2 knockout (Rag2^−/−) mice. Measured outcomes included histopathology; CD45⁺ immune cell infiltration; oxidative DNA damage (tissue 8-hydroxy-2′-deoxyguanosine; 8-OHdG); expression of IL-6 and TNF mRNA and protein, and flow cytometry analysis of lamina propria Th1 and Th17 cell populations. Results: miR146a expression remained stable in simulated gastric and intestinal conditions. miR146a expression increased in the intestines of mice six hours following oral gavage of CNP-miR146a. Oral delivery of CNP-miR146a in mice with colitis was associated with reduced inflammation and oxidative stress in the proximal and distal colons as evidenced by histopathology scoring, reduced immune cell infiltration, reduced IL-6 and TNF expression, and decreased populations of CD4⁺Tbet⁺IFNg+ Th1, CD4⁺RorgT⁺IL17⁺ Th17, as well as pathogenic double positive IFNg⁺IL17⁺ T cells. Conclusions: CNP-miR146a represents a novel orally available therapeutic with high potential to advance into clinical trials. Full article

(This article belongs to the Section Nanomedicine and Nanotechnology)

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28 pages, 2888 KiB

Open AccessReview

Nanotechnology-Based Approaches for the Management of Diabetes Mellitus: An Innovative Solution to Long-Lasting Challenges in Antidiabetic Drug Delivery

by Shounak Sarkhel, Saikat Mollick Shuvo, Md Ahesan Ansari, Sourav Mondal, Pritam Kapat, Arindam Ghosh, Tanima Sarkar, Ranu Biswas, Leonard Ionut Atanase and Alexandru Carauleanu

Pharmaceutics 2024, 16(12), 1572; https://doi.org/10.3390/pharmaceutics16121572 - 9 Dec 2024

Abstract

Diabetes is a widespread metabolic illness. Mismanagement of diabetes can lead to severe complications that tremendously impact patients’ quality of life. The assimilation of nanotechnology in diabetes care holds the potential to revolutionize treatment paradigms, improve patient outcomes, and reduce the economic burden associated with this pervasive disease. This manuscript explores the multifaceted utilization of nanomaterials in diabetes care, emphasizing the unique features of nano-based medication delivery methods and smart drug delivery mechanisms. Additionally, this paper talks about research on nanocarrier-integrated oral, transdermal, and inhalable insulin delivery; dendrimer- and nanocarrier-coupled antisense oligonucleotide-driven gene therapy; the implementation of gold nanoparticles and quantum dots for glucose surveillance; and nucleic acid therapies. There are certain restrictions when using medication delivery methods that are commonly available to handle diabetes. In order to increase efficacy and safety, the rapidly developing science of nanotechnology is also being explored and employed in medical biology. Nanomaterials like liposomes, dendrimers, niosomes, polymeric and metallic nanocarriers, and solid lipid nanoparticles are among the nanocarriers that have been developed for better delivery of various oral hypoglycemic agents in comparison to conventional therapies. These nanocarriers provide great control over elevated blood glucose levels, making them one of the most intriguing and promising technologies available today. Furthermore, adding additional ligands to nanocarriers allows for more focused distribution while protecting the encapsulated hypoglycemic drugs. Full article

(This article belongs to the Special Issue Biofunctional Pharmaceutical Additives for Targeted, Improved Bioavailability and Safety of Medicine)

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20 pages, 3731 KiB

Open AccessReview

Advances in Research of Hydrogel Microneedle-Based Delivery Systems for Disease Treatment

by Juan Cao, Bo Wu, Ping Yuan, Yeqi Liu and Cheng Hu

Pharmaceutics 2024, 16(12), 1571; https://doi.org/10.3390/pharmaceutics16121571 - 9 Dec 2024

Abstract

Microneedles (MNs), composed of multiple micron-scale needle-like structures attached to a base, offer a minimally invasive approach for transdermal drug delivery by penetrating the stratum corneum and delivering therapeutic agents directly to the epidermis or dermis. Hydrogel microneedles (HMNs) stand out among various MN types due to their excellent biocompatibility, high drug-loading capacity, and tunable drug-release properties. This review systematically examines the matrix materials and fabrication methods of HMN systems, highlighting advancements in natural and synthetic polymers, and explores their applications in treating conditions such as wound healing, hair loss, cardiovascular diseases, and cancer. Furthermore, the potential of HMNs for disease diagnostics is discussed. The review identifies key challenges, including limited mechanical strength, drug-loading efficiency, and lack of standardization, while proposing strategies to overcome these issues. With the integration of intelligent design and enhanced control over drug dosage and safety, HMNs are poised to revolutionize transdermal drug delivery and expand their applications in personalized medicine. Full article

(This article belongs to the Special Issue Multifunctional Hydrogels for Controlled Drug Delivery)

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23 pages, 6285 KiB

Open AccessArticle

Concomitant Inhibition and Collaring of Dual-Species Biofilms Formed by Candida auris and Staphylococcus aureus by Triazole Based Small Molecule Inhibitors

by Humaira Parveen, Sayeed Mukhtar, Mona O. Albalawi, Syed Khasim, Aijaz Ahmad and Mohmmad Younus Wani

Pharmaceutics 2024, 16(12), 1570; https://doi.org/10.3390/pharmaceutics16121570 - 8 Dec 2024

Abstract

Background/Objectives: Biofilm-associated infections, particularly those involving Candida auris and Staphylococcus aureus, pose significant challenges in clinical settings due to their resilience and resistance to conventional treatments. This study aimed to synthesize novel triazole derivatives containing a piperazine ring via click chemistry and evaluate their efficacy in disrupting biofilms formed by these pathogens. Methods: Triazole derivatives were synthesized using click chemistry techniques. The antimicrobial activity of the compounds was tested against planktonic cells of C. auris and S. aureus in single and dual-species culture conditions. Biofilm disruption efficacy was assessed, alongside the evaluation of physicochemical properties, oral bioavailability potential, and toxicity profiles. Results: The compound T3 demonstrated potent antimicrobial activity against planktonic cells of C. auris and S. aureus in both single and dual-species cultures. T3 exhibited significant efficacy in reducing microbial viability within biofilms formed by these pathogens. Physicochemical analyses revealed favorable solubility and permeability profiles, supporting its potential for oral bioavailability. Toxicity assessments showed a non-toxic profile, highlighting a promising safety margin for further development. Conclusions: This study underscores the anti-biofilm properties of novel triazole-piperazine derivatives, particularly T3, against single and dual-species biofilms of C. auris and S. aureus. These findings position T3 as a promising candidate for developing therapies targeting polymicrobial infections and provide a foundation for future research into alternative strategies for combating biofilm-associated infections. Full article

(This article belongs to the Topic Design, Synthesis and Biological Evaluation of Novel Small Molecules as Multi-target Enzyme Inhibitors)

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23 pages, 13418 KiB

Open AccessArticle

Newly Designed PCL-Wrapped Cryogel-Based Conduit Activated with IKVAV Peptide Derivative for Peripheral Nerve Repair

by Abdulla Yergeshov, Mohamed Zoughaib, Kenana Dayob, Marat Kamalov, Duong Luong, Albina Zakirova, Ruslan Mullin, Diana Salakhieva and Timur I. Abdullin

Pharmaceutics 2024, 16(12), 1569; https://doi.org/10.3390/pharmaceutics16121569 - 8 Dec 2024

Abstract

Background: The combination of macroporous cryogels with synthetic peptide factors represents a promising but poorly explored strategy for the development of extracellular matrix (ECM)-mimicking scaffolds for peripheral nerve (PN) repair. Methods: In this study, IKVAV peptide was functionalized with terminal lysine residues to allow its in situ cross-linking with gelatin macromer, resulting in the formation of IKVAV-containing proteinaceous cryogels. The controllable inclusion and distribution of the peptide molecules within the scaffold was verified using a fluorescently labelled peptide counterpart. The optimized cryogel scaffold was combined with polycaprolactone (PCL)-based shell tube to form a suturable nerve conduit (NC) to be implanted into sciatic nerve diastasis in rats. Results: The NC constituents did not impair the viability of primary skin fibroblasts. Concentration-dependent effects of the peptide component on interrelated viscoelastic and swelling properties of the cryogels as well as on proliferation and morphological differentiation of neurogenic PC-12 cells were established, also indicating the existence of an optimal-density range of the introduced peptide. The in vivo implanted NC sustained the connection of the nerve stumps with partial degradation of the PCL tube over eight weeks, whereas the core-filling cryogel profoundly improved local electromyographic recovery and morphological repair of the nerve tissues, confirming the regenerative activity of the developed scaffold. Conclusions: These results provide proof-of-concept for the development of a newly designed PN conduit prototype based on IKVAV-activated cryogel, and they can be exploited to create other ECM-mimicking scaffolds. Full article

(This article belongs to the Special Issue New Advances and Applications of Cryogels in Drug Delivery and Regenerative Medicine)

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5 pages, 165 KiB

Open AccessEditorial

Editorial 15th Anniversary of Pharmaceutics—Improvement of Drug Bioavailability

by Thierry F. Vandamme

Pharmaceutics 2024, 16(12), 1568; https://doi.org/10.3390/pharmaceutics16121568 - 8 Dec 2024

Abstract

Improving the health of humans and animals depends on the discovery of new active molecules as well as improving the bioavailability of molecules already marketed [...] Full article

(This article belongs to the Special Issue 15th Anniversary of Pharmaceutics—Improvement of Drug Bioavailability)

17 pages, 2110 KiB

Open AccessArticle

5-Aminosalicylic Acid Distribution into the Intestinal Membrane Along the Gastrointestinal Tract After Oral Administration in Rats

by Yorinobu Maeda, Yuta Goto, Fumiya Ohnishi, Syoutarou Koga, Satoshi Kawano, Yuhzo Hieda, Takeshi Goromaru and Teruo Murakami

Pharmaceutics 2024, 16(12), 1567; https://doi.org/10.3390/pharmaceutics16121567 - 7 Dec 2024

Abstract

Background: 5-Aminosalicylic acid (5-ASA), the first-line therapy for ulcerative colitis, is a poorly soluble zwitterionic drug. Unformulated 5-ASA is thought to be extensively absorbed in the small intestine. Methods: The pH-dependent solubility of 5-ASA in vitro and the intestinal membrane distribution of 5-ASA and its N-acetyl metabolite (AC-5-ASA) after the oral administration of 5-ASA were examined in fed rats. 5-ASA was administered as a suspension in water, 0.1 M HCl, or 0.1 M NaOH to untreated rats or as a solution in 5% NaHCO₃ to lansoprazole-pretreated rats. Results: 5-ASA solubility in vitro was higher at pH < 2 and pH > 7. In rats, the 5-ASA and AC-5-ASA were detected mostly in the small intestine at 3 h and in the colonic region at 8 h after administration. The dosing vehicle (suspension or solution) and lansoprazole pretreatment did not significantly affect the pH of the luminal fluid in rats or the 5-ASA distribution in membranes. Conclusions: The 5-ASA distribution in membranes in the proximal intestine was found to be restricted by the intrinsic regional luminal pH, low solubility, and saturable membrane permeability. Unabsorbed 5-ASA in the proximal intestine was delivered to the distal intestine. The higher the oral dose of 5-ASA, the more 5-ASA may be delivered to the distal intestine due to the restricted absorption in the small intestine. Full article

(This article belongs to the Topic Complementary Strategies in Drug Delivery: From Particle Engineering to System Optimization)

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20 pages, 3992 KiB

Open AccessArticle

Liposomal Formulation of an Organogold Complex Enhancing Its Activity as Antimelanoma Agent—In Vitro and In Vivo Studies

by Jacinta O. Pinho, Mariana Coelho, Catarina Pimpão, Jahnobi Konwar, Ana Godinho-Santos, Rute M. Noiva, Sophie R. Thomas, Angela Casini, Graça Soveral and Maria Manuela Gaspar

Pharmaceutics 2024, 16(12), 1566; https://doi.org/10.3390/pharmaceutics16121566 - 6 Dec 2024

Abstract

Background/Objectives: The therapeutic management of melanoma, the most aggressive form of skin cancer, remains challenging. In the search for more effective therapeutic options, metal-based complexes are being investigated for their anticancer properties. Cisplatin was the first clinically approved platinum-based drug and, based on its success, other metals (e.g., gold) are being used to design novel compounds. Methods: the antimelanoma potential of a new organometallic cyclometalated Au(III) complex [[Au(C^NOxN)Cl₂] (C^NOxN = 2-(phenyl-(2-pyridinylmethylene)aminoxy acetic acid))] (ST004) was evaluated in vitro and in vivo. Furthermore, the gold-based complex was incorporated in liposomes to overcome solubility and stability problems, to promote accumulation at melanoma sites and to maximize the therapeutic effect while controlling its reactivity. The antiproliferative activity of ST004 formulations was assessed in murine (B16F10) and human (A375 and MNT-1) melanoma cell lines after 24 and 48 h incubation periods. The proof-of-concept of the antimelanoma properties of ST004 formulations was carried out in subcutaneous and metastatic murine melanoma models. Results: the developed liposomal formulations showed a low mean size (around 100 nm), high homogeneity (with a low polydispersity index) and high incorporation efficiency (51 ± 15%). ST004 formulations exhibited antiproliferative activity with EC₅₀ values in the μmolar range being cell-line- and incubation-period-dependent. On the opposite side, the benchmark antimelanoma compound, dacarbazine (DTIC), presented an EC₅₀ > 100 μM. Cell cycle analysis revealed an arrest in G0/G1 phase for Free-ST004 in all cell lines. In turn, LIP-ST004 led to a G0/G1 halt in B16F10, and to an arrest in S phase in A375 and MNT-1 cells. Preliminary mechanistic studies in human red blood cells suggest that gold-based inhibition of glycerol permeation acts through aquaglyceroporin 3 (AQP3). In a metastatic murine melanoma, a significant reduction in lung metastases in animals receiving LIP-ST004, compared to free gold complex and DTIC, was observed. Conclusion: This study highlights the antimelanoma potential of a new gold-based complex. Additional studies, namely in vivo biodistribution profile and therapeutic validation of this organogold complex in other melanoma models, are expected to be performed in further investigations. Full article

(This article belongs to the Special Issue Research on the Design and Development of Infectious, Inflammatory and Cancer Therapeutics)

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19 pages, 10301 KiB

Open AccessArticle

Biocompatible Carbon Dots/Polyurethane Composites as Potential Agents for Combating Bacterial Biofilms: N-Doped Carbon Quantum Dots/Polyurethane and Gamma Ray-Modified Graphene Quantum Dots/Polyurethane Composites

by Zoran Marković, Sladjana Dorontić, Svetlana Jovanović, Janez Kovač, Dušan Milivojević, Dragana Marinković, Marija Mojsin and Biljana Todorović Marković

Pharmaceutics 2024, 16(12), 1565; https://doi.org/10.3390/pharmaceutics16121565 - 6 Dec 2024

Abstract

Background: Pathogen bacteria appear and survive on various surfaces made of steel or glass. The existence of these bacteria in different forms causes significant problems in healthcare facilities and society. Therefore, the surface engineering of highly potent antimicrobial coatings is highly important in the 21st century, a period that began with a series of epidemics. Methods: In this study, we prepared two types of photodynamic polyurethane-based composite films encapsulated by N-doped carbon quantum dots and graphene quantum dots irradiated by gamma rays at a dose of 50 kGy, respectively. Further, we investigated their structural, optical, antibacterial, antibiofouling and biocompatibility properties. Results: Nanoelectrical and nanomechanical microscopy measurements revealed deviations in the structure of these quantum dots and polyurethane films. The Young’s modulus of elasticity of the carbon and graphene quantum dots was several times lower than that for single-walled carbon nanotubes (SWCNTs) with chirality (6,5). The electrical properties of the carbon and graphene quantum dots were quite similar to those of the SWCNTs (6,5). The polyurethane films with carbon quantum dots were much more elastic and smoother than the films with graphene quantum dots. Antibacterial tests indicated excellent antibacterial activities of these films against a wide range of tested bacteria, whereas the antibiofouling activities of both composite films showed the best results against the Staphylococcus aureus and Escherichia coli biofilms. Biocompatibility studies showed that neither composite film exhibited any cytotoxicity or hemolysis. Conclusions: Obtained results indicate that these composite films could be used as antibacterial surfaces in the healthcare facilities. Full article

(This article belongs to the Special Issue Carbon Nanomaterials in Pharmaceutical Sciences: Exploring Antibacterial, Antiviral, and Anticancer Properties)

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5 pages, 179 KiB

Open AccessEditorial

Photodynamic Therapy in Cancer: Principles, State of the Art, and Future Directions

by Dmitri V. Krysko, Irina V. Balalaeva and Tatiana A. Mishchenko

Pharmaceutics 2024, 16(12), 1564; https://doi.org/10.3390/pharmaceutics16121564 - 6 Dec 2024

Abstract

Since its discovery more than 100 years ago, photodynamic therapy (PDT) has become a potent strategy for the treatment of many types of cancer [...] Full article

(This article belongs to the Special Issue Photodynamic Therapy in Cancer: Principles, State of the Art, and Future Directions)

15 pages, 980 KiB

Open AccessReview

Buccal Absorption of Biopharmaceutics Classification System III Drugs: Formulation Approaches and Mechanistic Insights

by Rayan Sabra, Daniel Kirby, Vikram Chouk, Kleta Malgorzata and Afzal R. Mohammed

Pharmaceutics 2024, 16(12), 1563; https://doi.org/10.3390/pharmaceutics16121563 - 6 Dec 2024

Abstract

Buccal drug delivery emerges as a promising strategy to enhance the absorption of drugs classified under the Biopharmaceutics Classification System (BCS) Class III, characterized by high solubility and low permeability. However, addressing the absorption challenges of BCS Class III drugs necessitates innovative formulation strategies. This review delves into optimizing buccal drug delivery for BCS III drugs, focusing on various formulation approaches to improve absorption. Strategies such as permeation enhancers, mucoadhesive polymers, pH modifiers, ion pairing, and prodrugs are systematically explored for their potential to overcome challenges associated with BCS Class III drugs. The mechanistic insight into how these strategies influence drug absorption is discussed, providing a detailed understanding of their applicability. Furthermore, the review advocates for integrating conventional buccal dosage forms with these formulation approaches as a potential strategy to enhance absorption. By emphasizing bioavailability enhancement, this review contributes to a holistic understanding of optimizing buccal absorption for BCS Class III drugs, presenting a unified approach to overcome inherent limitations in their delivery. Full article

(This article belongs to the Section Physical Pharmacy and Formulation)

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15 pages, 7467 KiB

Open AccessArticle

Engineered Lubricative Lecithin-Based Electrospun Nanofibers for the Prevention of Postoperative Abdominal Adhesion

by Junhan Li, Hao Lin, Jinghua Li and Yi Wang

Pharmaceutics 2024, 16(12), 1562; https://doi.org/10.3390/pharmaceutics16121562 - 6 Dec 2024

Abstract

Background: Postoperative abdominal adhesion is a prevalent complication following abdominal surgery, with the incidence of adhesion reaching up to 90%, which may precipitate a range of adverse outcomes. Although fibrous membranes loaded with various anti-inflammatory or other drugs have been proposed for anti-adhesion, most of them suffer from drug-induced adverse effects. Methods: In this study, a lecithin-based electrospun polylactic acid (PLA) nanofibrous membrane (L/P-NM) was developed for the prevention of postoperative abdominal adhesion, utilizing the hydration lubrication theory. The loaded zwitterionic lecithin allows the nanofiber surface to strongly bind water molecules to create a hydration lubrication interface. Results: As the TGA results show, the content of bound water in the nanofibers increased significantly with the increase in the lecithin content. Tribological test results show that L/P-NM reached a minimum coefficient of friction (COF) of about 0.112. Additionally, the developed nanofibrous membranes possess favorable tensile property and biocompatibility. Rat postoperative abdominal adhesion model evaluation results demonstrated that L/P-NM possesses significant anti-adhesive performance, with an adhesion score of only 1. Conclusions: Therefore, this study offers a promising strategy for efficiently preventing abdominal adhesion. Full article

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23 pages, 1919 KiB

Open AccessReview

Nanocrystals in Dermal Drug Delivery: A Breakthrough for Enhanced Skin Penetration and Targeted Skin Disorder Treatments

by Ahmed S. Alnaim

Pharmaceutics 2024, 16(12), 1561; https://doi.org/10.3390/pharmaceutics16121561 - 6 Dec 2024

Abstract

One of the major challenges in dermal drug delivery is the adequate penetration of the active compound into the skin without causing any skin irritation and inflammation. Nanocrystals (NCs) are nanoscale particles, and their sizes are below 1000 nm. NCs are made up of drug particles only, which are used to improve the aqueous solubility and bioavailability of poorly water-soluble drugs. NCs are typically prepared either by bottom-up or top-down techniques. The advantages of using NC-based formulations in enhancing dermal drug delivery include increased drug loading capacity, easier and deeper penetration into the skin tissue, and increased passive diffusion. NC-based formulations with the capacity of enhanced dermal drug delivery can be effectively used to treat a wide range of skin disorders, including melanoma, inflammation, psoriasis, acne vulgaris, bacterial infections, fungal infections, eczema, skin aging, herpes simplex virus infections, skin manifestations of tick bites, frostbite-related infections, hyperpigmentation, and diabetic foot ulcer. In this review, major challenges in dermal drug delivery across the skin barrier, mechanism of action of dermal NCs, advantages of using NCs in enhancing dermal drug delivery, NC preparation methods, and applications of NCs in the treatment of various skin disorders have been discussed. Full article

(This article belongs to the Section Nanomedicine and Nanotechnology)

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18 pages, 3891 KiB

Open AccessArticle

Nanoencapsulation of Achyrocline satureioides (Lam) DC—Essential Oil and Controlled Release: Experiments and Modeling

by Caroline G. F. da Silva, Rafaela R. Petró, Jéssica H. de Castro, Rafael N. Almeida, Eduardo Cassel and Rubem M. F. Vargas

Pharmaceutics 2024, 16(12), 1560; https://doi.org/10.3390/pharmaceutics16121560 - 5 Dec 2024

Abstract

Background/Objectives: Degradation by physical and chemical agents affects the properties of essential oils; therefore, this study aimed to protect the volatile compounds present in essential oils through biopolymer encapsulation. Methods: The Achyrocline satureioides (Lam) DC. essential oil was obtained by steam distillation at 2.5 bar. The nano-sized physical coating of the active oil core resulted in an optimal polymer/oil ratio of 1:3 and particle diameter of 178 nm. The particle morphology was evaluated using scanning electron microscopy and transmission electron microscopy. The inclusion of the essential oil in the polymer was confirmed using thermogravimetric analysis. Results: The pH of the formulation remained stable for 90 days, and controlled release and encapsulation efficiencies were evaluated. Formulations were evaluated using the perfumery radar technique, which indicated a predominantly woody profile. The diffusion of fragrant compounds in the air was assessed over time and mathematically modeled. Conclusions: The produced nanostructures were efficient for the controlled release of volatile compounds from the essential oil of Achyrocline satureioides. Full article

(This article belongs to the Special Issue Biopolymer-Based Nanosystem for Drug Delivery, 2nd Edition)

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54 pages, 991 KiB

Open AccessReview

The Role of Pharmacometrics in Advancing the Therapies for Autoimmune Diseases

by Artur Świerczek, Dominika Batko and Elżbieta Wyska

Pharmaceutics 2024, 16(12), 1559; https://doi.org/10.3390/pharmaceutics16121559 - 5 Dec 2024

Abstract

Autoimmune diseases (AIDs) are a group of disorders in which the immune system attacks the body’s own tissues, leading to chronic inflammation and organ damage. These diseases are difficult to treat due to variability in drug PK among individuals, patient responses to treatment, and the side effects of long-term immunosuppressive therapies. In recent years, pharmacometrics has emerged as a critical tool in drug discovery and development (DDD) and precision medicine. The aim of this review is to explore the diverse roles that pharmacometrics has played in addressing the challenges associated with DDD and personalized therapies in the treatment of AIDs. Methods: This review synthesizes research from the past two decades on pharmacometric methodologies, including Physiologically Based Pharmacokinetic (PBPK) modeling, Pharmacokinetic/Pharmacodynamic (PK/PD) modeling, disease progression (DisP) modeling, population modeling, model-based meta-analysis (MBMA), and Quantitative Systems Pharmacology (QSP). The incorporation of artificial intelligence (AI) and machine learning (ML) into pharmacometrics is also discussed. Results: Pharmacometrics has demonstrated significant potential in optimizing dosing regimens, improving drug safety, and predicting patient-specific responses in AIDs. PBPK and PK/PD models have been instrumental in personalizing treatments, while DisP and QSP models provide insights into disease evolution and pathophysiological mechanisms in AIDs. AI/ML implementation has further enhanced the precision of these models. Conclusions: Pharmacometrics plays a crucial role in bridging pre-clinical findings and clinical applications, driving more personalized and effective treatments for AIDs. Its integration into DDD and translational science, in combination with AI and ML algorithms, holds promise for advancing therapeutic strategies and improving autoimmune patients’ outcomes. Full article

(This article belongs to the Special Issue Mechanism-Based Pharmacokinetic and Pharmacodynamic Modeling)

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15 pages, 6353 KiB

Open AccessArticle

Tissue Engineering Construct for Articular Cartilage Restoration with Stromal Cells from Synovium vs. Dental Pulp—A Pre-Clinical Study

by Tiago Lazzaretti Fernandes, João Paulo Cortez Santanna, Rafaella Rogatto de Faria, Enzo Radaic Pastore, Daniela Franco Bueno and Arnaldo José Hernandez

Pharmaceutics 2024, 16(12), 1558; https://doi.org/10.3390/pharmaceutics16121558 - 5 Dec 2024

Abstract

Background/Objectives: Cartilage injuries and osteoarthritis are prevalent public health problems, due to their disabling nature and economic impact. Mesenchymal stromal cells (MSCs) isolated from different tissues have the immunomodulatory capacity to regulate local joint environment. This translational study aims to compare cartilage restoration from MSCs from the synovial membrane (SM) and dental pulp (DP) by a tissue-engineered construct with Good Manufacturing Practices. Methods: A controlled experimental study was conducted on fourteen miniature pigs, using scaffold-free Tissue Engineering Constructs (TECs) from DP and SM MSCs, with a 6-month follow-up. Total thickness cartilage defects were created in both hind knees; one side was left untreated and the other received a TEC from either DP (n = 7) or SM (n = 7). An MRI assessed the morphology using the MOCART scoring system, T2 mapping evaluated water, and collagen fiber composition, and histological analysis was performed using the ICRS-2 score. Results: The untreated group had a mean MOCART value of 46.2 ± 13.4, while the SM-treated group was 65.7 ± 15.5 (p < 0.05) and the DP-treated group was 59.0 ± 7.9 (n.s.). The T2 mapping indicated a mean value of T2 of 54.9 ± 1.9 for native cartilage, with the untreated group at 50.9 ± 2.4 (p < 0.05). No difference was found between the T2 value of native cartilage and the treated groups. The ICRS-2 mean values were 42.1 ± 14.8 for the untreated group, 64.3 ± 19.0 for SM (p < 0.05), and 54.3 ± 12.2 for DP (n.s.). Conclusion: MRI and histological analysis indicated that TEC treatment led to superior cartilage coverage and quality compared to the defect group. TECs from SM demonstrated better results than the defect group in the histological assessment. Full article

(This article belongs to the Special Issue Osteoarthritis and Cartilage Biologics)

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20 pages, 6644 KiB

Open AccessArticle

Host–Guest Complexation of Olmesartan Medoxomil by Heptakis(2,6-di-O-methyl)-β-cyclodextrin: Compatibility Study with Excipients

by Dana Emilia Man, Ema-Teodora Nițu, Claudia Temereancă, Laura Sbârcea, Adriana Ledeți, Denisa Ivan, Amalia Ridichie, Minodora Andor, Alex-Robert Jîjie, Paul Barvinschi, Gerlinde Rusu, Renata-Maria Văruţ and Ionuț Ledeți

Pharmaceutics 2024, 16(12), 1557; https://doi.org/10.3390/pharmaceutics16121557 - 4 Dec 2024

Abstract

Background: Olmesartan medoxomil (OLM) is the prodrug of olmesartan, an angiotensin II type 1 receptor blocker that has antihypertensive and antioxidant activities and renal protective properties. It exhibits low water solubility, which leads to poor bioavailability and limits its clinical potential. To improve the solubility of OLM, a host–guest inclusion complex (IC) between heptakis(2,6-di-O-methyl)-β-cyclodextrin (DMβCD) and the drug substance was obtained. Along with active substances, excipients play a crucial role in the quality, safety, and efficacy of pharmaceutical formulations. Therefore, the compatibility of OLM/DMβCD IC with several pharmaceutical excipients was evaluated. Methods: IC was characterized in both solid and liquid states, employing thermoanalytical techniques, universal-attenuated total reflectance Fourier-transform infrared spectroscopy, powder X-ray diffractometry, UV spectroscopy, and saturation solubility studies. Compatibility studies were carried out using thermal and spectroscopic methods to assess potential physical and chemical interactions. Results: The 1:1 OLM:DMβCD stoichiometry ratio and the value of the apparent stability constant were determined by means of the phase solubility method that revealed an A_L-type diagram. The binary system showed different physicochemical characteristics from those of the parent entities, supporting IC formation. The geometry of the IC was thoroughly investigated using molecular modeling. Compatibility studies revealed a lack of interaction between the IC and all studied excipients at ambient conditions and the thermally induced incompatibility of IC with magnesium stearate and α-lactose monohydrate. Conclusions: The results of this study emphasize that OLM/DMβCD IC stands out as a valuable candidate for future research in the development of new pharmaceutical formulations, in which precautions should be considered in choosing magnesium stearate and α-lactose monohydrate as excipients if the manufacture stage requires temperatures above 100 °C. Full article

(This article belongs to the Special Issue Biofunctional Pharmaceutical Additives for Targeted, Improved Bioavailability and Safety of Medicine)

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19 pages, 932 KiB

Open AccessReview

Polycystic Ovary Syndrome and the Potential for Nanomaterial-Based Drug Delivery in Therapy of This Disease

by Mingqin Shi, Xinyao Li, Liwei Xing, Zhenmin Li, Sitong Zhou, Zihui Wang, Xuelian Zou, Yuqing She, Rong Zhao and Dongdong Qin

Pharmaceutics 2024, 16(12), 1556; https://doi.org/10.3390/pharmaceutics16121556 - 4 Dec 2024

Abstract

Polycystic ovary syndrome (PCOS) is the predominant endocrine disorder among women of reproductive age and represents the leading cause of anovulatory infertility, which imposes a considerable health and economic burden. Currently, medications used to treat PCOS can lead to certain adverse reactions, such as affecting fertility and increasing the risk of venous thrombosis. Drug delivery systems utilizing nanomaterials, characterized by prolonged half-life, precision-targeted delivery, enhanced bioavailability, and reduced toxicity, are currently being employed in the management of PCOS. This innovative approach is gaining traction as a favored strategy for augmenting the therapeutic efficacy of medications. Consequently, this paper discusses the roles of nanoparticles, nanocarriers, and targeted ligands within nanomaterial-based drug delivery systems, aiming to identify optimal methodologies for treating PCOS using nanomaterials. Additionally, prospective research avenues concerning nanomaterial-based delivery systems in the context of PCOS, as well as the implications of existing insights on the advancement of novel therapies for PCOS, are highlighted. Full article

(This article belongs to the Special Issue New Technology for Prolonged Drug Release, 2nd Edition)

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