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13 pages, 1988 KiB

Open AccessArticle

The Biosynthesized Zinc Oxide Nanoparticles’ Antiviral Activity in Combination with Pelargonium zonale Extract against the Human Corona 229E Virus

by Abdulsalam A. Alqahtani, Mohamed A. El Raey, Eman Abdelsalam, Ammar M. Ibrahim, Omaish Alqahtani, Zenab Aly Torky and Hany G. Attia

Molecules 2022, 27(23), 8362; https://doi.org/10.3390/molecules27238362 - 30 Nov 2022

Cited by 6 | Viewed by 1280

Abstract

Almost one-third of all infectious diseases are caused by viruses, and these diseases account for nearly 20% of all deaths globally. It is becoming increasingly clear that highly contagious viral infections pose a significant threat to global health and economy around the world. [...] Read more.

Almost one-third of all infectious diseases are caused by viruses, and these diseases account for nearly 20% of all deaths globally. It is becoming increasingly clear that highly contagious viral infections pose a significant threat to global health and economy around the world. The need for innovative, affordable, and safe antiviral therapies is a must. Zinc oxide nanoparticles are novel materials of low toxicity and low cost and are known for their antiviral activity. The genus Pelargonium was previously reported for its antiviral and antimicrobial activity. In this work, Pelargonium zonale leaf extract chemical profile was studied via high-performance liquid chromatography (HPLC) and was used for the biosynthesis of zinc oxide nanoparticles. Furthermore, the antiviral activity of the combination of P. zonale extract and the biosynthesized nanoparticles of ZnO against the human corona 229E virus was investigated. Results revealed that ZnONPs had been biosynthesized with an average particle size of about 5.5 nm and characterized with UV, FTIR, TEM, XRD, and SEM. The antiviral activity showed significant activity and differences among the tested samples in favor of the combination of P. zonale extract and ZnONPs (ZnONPs/Ex). The lowest IC_50, 2.028 µg/mL, and the highest SI, 68.4 of ZnONPs/Ex, assert the highest antiviral activity of the combination against human coronavirus (229E). Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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17 pages, 4923 KiB

Open AccessArticle

Green Synthesis of Titanium Dioxide Nanoparticles Using Ocimum sanctum Leaf Extract: In Vitro Characterization and Its Healing Efficacy in Diabetic Wounds

by Mohammad Zaki Ahmad, Ali S. Alasiri, Javed Ahmad, Abdulsalam A. Alqahtani, Md Margub Abdullah, Basel A. Abdel-Wahab, Kalyani Pathak, Riya Saikia, Aparoop Das, Himangshu Sarma and Seham Abdullah Alzahrani

Molecules 2022, 27(22), 7712; https://doi.org/10.3390/molecules27227712 - 09 Nov 2022

Cited by 14 | Viewed by 3531

Abstract

Diabetes mellitus is one of the most prevalent metabolic disorders characterized by hyperglycemia due to impaired glucose metabolism. Overproduction of free radicals due to chronic hyperglycemia may cause oxidative stress, which delays wound healing in diabetic conditions. For people with diabetes, this impeded [...] Read more.

Diabetes mellitus is one of the most prevalent metabolic disorders characterized by hyperglycemia due to impaired glucose metabolism. Overproduction of free radicals due to chronic hyperglycemia may cause oxidative stress, which delays wound healing in diabetic conditions. For people with diabetes, this impeded wound healing is one of the predominant reasons for mortality and morbidity. The study aimed to develop an Ocimum sanctum leaf extract-mediated green synthesis of titanium dioxide (TiO₂) nanoparticles (NPs) and further incorporate them into 2% chitosan (CS) gel for diabetic wound healing. UV-visible spectrum analysis recorded the sharp peak at 235 and 320 nm, and this was the preliminary sign for the biosynthesis of TiO₂ NPs. The FTIR analysis was used to perform a qualitative validation of the biosynthesized TiO₂ nanoparticles. XRD analysis indicated the crystallinity of TiO₂ NPs in anatase form. Microscopic investigation revealed that TiO₂ NPs were spherical and polygonal in shape, with sizes ranging from 75 to 123 nm. The EDX analysis of green synthesized NPs showed the presence of TiO₂ NPs, demonstrating the peak of titanium ion and oxygen. The hydrodynamic diameter and polydispersity index (PDI) of the TiO₂ NPs were found to be 130.3 nm and 0.237, respectively. The developed TiO₂ NPs containing CS gel exhibited the desired thixotropic properties with pseudoplastic behavior. In vivo wound healing studies and histopathological investigations of healed wounds demonstrated the excellent wound-healing efficacy of TiO₂ NPs containing CS gel in diabetic rats. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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16 pages, 4465 KiB

Open AccessArticle

In Vitro Evaluation of NLS-DTX Activity in Triple-Negative Breast Cancer

by Karen L. R. Paiva, Marina A. Radicchi and Sônia N. Báo

Molecules 2022, 27(15), 4920; https://doi.org/10.3390/molecules27154920 - 02 Aug 2022

Cited by 3 | Viewed by 1641

Abstract

Cancer is one of the most lethal diseases in the world, and the development and improvement of treatments used in cancer therapies are extremely important for a better quality of life for patients. In view of the current problems in drug administration such [...] Read more.

Cancer is one of the most lethal diseases in the world, and the development and improvement of treatments used in cancer therapies are extremely important for a better quality of life for patients. In view of the current problems in drug administration such as low solubility and adverse effects, the activity of a solid lipid nanoparticle containing docetaxel (SLN-DTX), a drug already used in conventional therapies, was evaluated in a cell line (MDA-MB-231) of one of the most aggressive types of breast cancer with the worst prognosis, triple-negative breast cancer. Viability tests indicated that SLN-DTX has a greater dependence on the treatment dose when compared to the free drug, which indicates a more controlled release of the drug, and both reduced viability by around 50% at a concentration of 1 µg/mL after 72 h. Transmission electron microscopy (TEM) and confocal and light microscopy analyses indicated that after treatment the cells enter a mitotic catastrophe, characteristic of antimitotic drugs that usually make cells progress to death or senescence. Cells treated with both DTX and SLN-DTX showed significant inhibition of mobility, 73.6% and 66.5% when treated with SLN-DTX and DTX, respectively, compared to the 11.4% of the control after 72 h, characteristics that are very relevant in tumor development and progression. SLN-DTX demonstrated its great potential as a nanocarrier by maintaining and improving the drug’s action in the MDA-MB-231 cell line. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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22 pages, 5924 KiB

Open AccessArticle

Development of Self-Emulsifying Drug Delivery Systems (SEDDSs) Displaying Enhanced Permeation of the Intestinal Mucus Following Sustained Release of Prototype Thiol-Based Mucolytic Agent Load

by Ahmad Malkawi, Nasr Alrabadi, Razan Haddad, Azhar Malkawi, Khaled Khaled and Airemwen Collins Ovenseri

Molecules 2022, 27(14), 4611; https://doi.org/10.3390/molecules27144611 - 19 Jul 2022

Viewed by 1690

Abstract

In this study, mucoactive self-emulsifying drug delivery systems (SEDDSs) based on sustained release of N-acetylcysteine (NAC) were developed for providing effective intestinal mucopermeation. Polymeric ionic complexes of NAC were formed with polyethyleneimine (PEI), Eudragit E 100, and Eudragit RS 100 and loaded [...] Read more.

In this study, mucoactive self-emulsifying drug delivery systems (SEDDSs) based on sustained release of N-acetylcysteine (NAC) were developed for providing effective intestinal mucopermeation. Polymeric ionic complexes of NAC were formed with polyethyleneimine (PEI), Eudragit E 100, and Eudragit RS 100 and loaded into a novel SEDDS. The SEDDSs exhibited a stable average size of 75 ± 12 nm (polydispersity index (PDI) < 0.3) and showed a rise in the zeta potential from −17.31 mV to −7.72 mV. On Caco-2 cells, SEDDSs at 1–3% were non-cytotoxic. An average of 91.8 ± 5.4% NAC was released from SEDDSs containing Eudragit E 100 (p ≤ 0.05) and Eudragit RS 100 (p ≤ 0.001) complexes at a significantly slower rate within 80 min, whereas the SEDDS containing PEI released NAC in a matter of seconds. Similarly, the SEDDS complexes revealed a time-dependent reduction in mucus dynamic viscosity of 52.6 ± 19.9%. Consequently, as compared with a blank SEDDS, mucodiffusion revealed about 2- and 1.8-fold significantly greater mucopermeation of SEDDSs anchoring Eudragit E 100–NAC and RS 100–NAC complexes (p ≤ 0.05), respectively. The mucoactive SEDDSs, which steadily released NAC while permeating the mucus, were linked to a significantly increased mucopermeation in vitro as a result of optimal mucolytic targeting. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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12 pages, 1745 KiB

Open AccessArticle

Synergistic Effect between Amoxicillin and Zinc Oxide Nanoparticles Reduced by Oak Gall Extract against Helicobacter pylori

by Hany G. Attia, Hassan A. Albarqi, Ismail G. Said, Omaish Alqahtani and Mohamed A. EI Raey

Molecules 2022, 27(14), 4559; https://doi.org/10.3390/molecules27144559 - 17 Jul 2022

Cited by 10 | Viewed by 1843

Abstract

Helicobacter pylori (H. pylori) is a global health threat, and the World Health Organization has included H. pylori among 12 bacterial species that require high priority future strategies for the development of new antibiotics due mainly to its high rates of [...] Read more.

Helicobacter pylori (H. pylori) is a global health threat, and the World Health Organization has included H. pylori among 12 bacterial species that require high priority future strategies for the development of new antibiotics due mainly to its high rates of resistance. Metallic nanoparticles are known for their antimicrobial properties. The FDA (Food and Drug Administration) has approved zinc oxide nanoparticles (ZnONPs) as biocompatible antimicrobials. Green synthesis of ZnONPs was performed based on Oak galls extract (OGE) and was characterized by UV, IR, DLS, TEM, and SEM measurements. In addition, LC-MS/MS was used for the identification of OGE constituents. A checkerboard assay was used to evaluate the activity of synthesized Qi-ZnONPs and OGE against H. pylori, and their synergistic effects with amoxicillin were evaluated. LC-MS/MS analyses identified 20 compounds as major gallic acid conjugates. The ZnONPs had average particle sizes of 5.5 nm (DLS) and 7.99 nm (TEM). Both OGE and Qi-ZnONPs exhibited moderate activity against H. pylori. Amoxicillin and Qi-ZnONPs combinations (1:2 and 1:4 amoxicillin:/Qi-ZnONPs) significantly decreased the MIC₉₀ by two-fold and four-fold, respectively, and FIC values for the combinations were more significant than with OGE alone. OGE is rich in phenolics. The synergism between Qi-ZnONPs and amoxicillin can provide an alternative safe agent of low cost to combat H. Pylori infections. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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17 pages, 2735 KiB

Open AccessArticle

Fabrication and Evaluation of Voriconazole Loaded Transethosomal Gel for Enhanced Antifungal and Antileishmanial Activity

by Mudassir Farooq, Faisal Usman, Sumera Zaib, Hamid Saeed Shah, Qazi Adnan Jamil, Fatima Akbar Sheikh, Ajmal Khan, Sameh Rabea, Soheir A. A. Hagras, Gaber El-Saber Batiha and Imtiaz Khan

Molecules 2022, 27(10), 3347; https://doi.org/10.3390/molecules27103347 - 23 May 2022

Cited by 11 | Viewed by 3236

Abstract

Voriconazole (VRC) is a broad-spectrum antifungal agent belonging to BCS class II (biopharmaceutical classification system). Despite many efforts to enhance its solubility, this primary issue still remains challenging for formulation scientists. Transethosomes (TELs) are one of the potential innovative nano-carriers for improving the [...] Read more.

Voriconazole (VRC) is a broad-spectrum antifungal agent belonging to BCS class II (biopharmaceutical classification system). Despite many efforts to enhance its solubility, this primary issue still remains challenging for formulation scientists. Transethosomes (TELs) are one of the potential innovative nano-carriers for improving the solubility and permeation of poorly soluble and permeable drugs. We herein report voriconazole-loaded transethosomes (VRCT) fabricated by the cold method and followed by their incorporation into carbopol 940 as a gel. The prepared VRCT were evaluated for % yield, % entrapment efficiency (EE), surface morphology, possible chemical interaction, particle size, zeta potential, and polydispersity index (PDI). The optimized formulation had a particle size of 228.2 nm, a zeta potential of −26.5 mV, and a PDI of 0.45 with enhanced % EE. Rheology, spreadability, extrudability, in vitro release, skin permeation, molecular docking, antifungal, and antileishmanial activity were also assessed for VRCT and VRC loaded transethosomal gel (VTEG). Ex-vivo permeation using rat skin depicted a transdermal flux of 22.8 µg/cm²/h with enhanced efficiency up to 4-fold. A two-fold reduction in inhibitory as well as fungicidal concentration was observed against various fungal strains by VRCT and VTEG besides similar results against L-donovani. The development of transethosomal formulation can serve as an efficient drug delivery system through a topical route with enhanced efficacy and better patient compliance. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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14 pages, 2216 KiB

Open AccessArticle

Novasomes as Nano-Vesicular Carriers to Enhance Topical Delivery of Fluconazole: A New Approach to Treat Fungal Infections

by Iman Fatima, Akhtar Rasul, Shahid Shah, Malik Saadullah, Nayyer Islam, Ahmed Khames, Ahmad Salawi, Muhammad Masood Ahmed, Yosif Almoshari, Ghulam Abbas, Mohammed A. S. Abourehab, Sajid Mehmood Khan, Zunera Chauhdary, Meshal Alshamrani, Nader Ibrahim Namazi and Demiana M. Naguib

Molecules 2022, 27(9), 2936; https://doi.org/10.3390/molecules27092936 - 04 May 2022

Cited by 9 | Viewed by 2682

Abstract

The occurrence of fungal infections has increased over the past two decades. It is observed that superficial fungal infections are treated by conventional dosage forms, which are incapable of treating deep infections due to the barrier activity possessed by the stratum corneum of [...] Read more.

The occurrence of fungal infections has increased over the past two decades. It is observed that superficial fungal infections are treated by conventional dosage forms, which are incapable of treating deep infections due to the barrier activity possessed by the stratum corneum of the skin. This is why the need for a topical preparation with advanced penetration techniques has arisen. This research aimed to encapsulate fluconazole (FLZ) in a novasome in order to improve the topical delivery. The novasomes were prepared using the ethanol injection technique and characterized for percent entrapment efficiency (EE), particle size (PS), zeta potential (ZP), drug release, Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), scanning electron microscopy (SEM) and antifungal activity. The FN7 formulation with 94.45% EE, 110 nm PS and −24 ZP proved to be the best formulation. The FN7 formulation showed a 96% release of FLZ in 8 h. FTIR showed the compatibility of FLZ with excipients and DSC studies confirmed the thermal stability of FLZ in the developed formulation. The FN7 formulation showed superior inhibition of the growth of Candida albicans compared to the FLZ suspension using a resazurin reduction assay, suggesting high efficacy in inhibiting fungal growth. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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17 pages, 4209 KiB

Open AccessArticle

Bovine Serum Albumin-Based Nanoparticles: Preparation, Characterization, and Antioxidant Activity Enhancement of Three Main Curcuminoids from Curcuma longa

by Andrea Mariela Araya-Sibaja, Krissia Wilhelm-Romero, María Isabel Quirós-Fallas, Luis Felipe Vargas Huertas, José Roberto Vega-Baudrit and Mirtha Navarro-Hoyos

Molecules 2022, 27(9), 2758; https://doi.org/10.3390/molecules27092758 - 25 Apr 2022

Cited by 7 | Viewed by 3206

Abstract

Bovine Serum Albumin (BSA) lipid hybrid nanoparticles are part of the new solutions to overcome low bioavailability of poor solubility drugs such as curcuminoids, which possess multiple biological advantages; however, they are counterbalanced by its short biological half-life. In this line, we prepared [...] Read more.

Bovine Serum Albumin (BSA) lipid hybrid nanoparticles are part of the new solutions to overcome low bioavailability of poor solubility drugs such as curcuminoids, which possess multiple biological advantages; however, they are counterbalanced by its short biological half-life. In this line, we prepared the three main curcuminoids: curcumin (CUR), desmethoxycurcumin (DMC), and bisdemethoxycurcumin (BDM)-loaded BSA nanoparticles. The three formulations were characterized by the average size, size distribution, crystallinity, weight loss, drug release, kinetic mechanism, and antioxidant activity. The developed method produced CUR-, DMC-, and BDM-loaded BSA nanoparticles with a size average of 15.83 ± 0.18, 17.29 ± 3.34, and 15.14 ± 0.14 nm for CUR, DMC, and BDM loaded BSA, respectively. FT-IR analysis confirmed the encapsulation, and TEM images showed their spherical shape. The three formulations achieved encapsulation efficiency upper to 96% and an exhibited significantly increased release from the nanoparticle compared to free compounds in water. The antioxidant activity was enhanced as well, in agreement with the improvement in water release, obtaining IC₅₀ values of 9.28, 11.70, and 15.19 µg/mL for CUR, DMC, and BDM loaded BSA nanoparticles, respectively, while free curcuminoids exhibited considerably lower antioxidant values in aqueous solution. Hence, this study shows promises for such hybrid systems, which have been ignored so far, regarding proper encapsulation, protection, and delivery of curcuminoids for the development of functional foods and pharmaceuticals. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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15 pages, 2585 KiB

Open AccessArticle

Characterization of Bioactive Compounds from Acacia concinna and Citrus limon, Silver Nanoparticles’ Production by A. concinna Extract, and Their Biological Properties

by Ibrahim Ahmed Shaikh, Uday M. Muddapur, Zabin K. Bagewadi, Sneha Chiniwal, Mohammed M. Ghoneim, Mater H. Mahnashi, Fahad Alsaikhan, Deepak Yaraguppi, Francois N. Niyonzima, Sunil S. More, Basheerahmed Abdulaziz Mannasaheb, Amer Al Ali, Abdulaziz Asiri, Aejaz Abdullatif Khan and S. M. Shakeel Iqubal

Molecules 2022, 27(9), 2715; https://doi.org/10.3390/molecules27092715 - 22 Apr 2022

Cited by 18 | Viewed by 3023

Abstract

The applications of bioactive compounds from medicinal plants as therapeutic drugs are largely increasing. The present study selected the bioactive compounds from Acacia concinna (A. concinna) and Citrus limon (C. limon) to assess their phytochemicals, proteins, and biological activity. [...] Read more.

The applications of bioactive compounds from medicinal plants as therapeutic drugs are largely increasing. The present study selected the bioactive compounds from Acacia concinna (A. concinna) and Citrus limon (C. limon) to assess their phytochemicals, proteins, and biological activity. The plant material was collected, and extraction performed as per the standard procedure. Qualitative analysis was undertaken, and identification of functional organic groups was performed by FTIR and HPLC. Antibacterial, anticancer, antioxidant, antihyperglycemic, antihyperlipidemic, and inhibition kinetics studies for enzymes were performed to assess the different biological activities. Flavonoids and phenols were present in a significant amount in both the selected plants. A. concinna showed significant antimicrobial activity against Z. mobilis, E. coli, and S. aureus, with minimum inhibition zones (MIZ) of 24, 22, and 20 mm, respectively. C. limon strongly inhibited all the tested pathogenic bacteria with maximum and minimum MIZ of 32 and 17 mm. A. concinna silver nanoparticles also exhibited potent antimicrobial activity. Both extracts showed substantial antioxidant, antihyperlipidemic, antidiabetic, anticancer (MCF-7), and anti-urease (antiulcer) properties. To conclude, these plants can be used to treat hyperlipidemia, diabetes, cancer, and gastrointestinal ulcers. They can also serve as antimicrobial and antioxidant agents. Thus, the studied plants must be exploited cost-effectively to generate therapeutic drugs for various diseases. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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12 pages, 1448 KiB

Open AccessArticle

In Silico Molecular Docking and Simulation Studies of Protein HBx Involved in the Pathogenesis of Hepatitis B Virus-HBV

by Ibrahim Ahmed Shaikh, Uday M. Muddapur, Krithika C, Shrikanth Badiger, Madhura Kulkarni, Mater H. Mahnashi, Saleh A. Alshamrani, Mohammed A. Huneif, Sunil S. More, Aejaz Abdullatif Khan and S. M. Shakeel Iqubal

Molecules 2022, 27(5), 1513; https://doi.org/10.3390/molecules27051513 - 23 Feb 2022

Cited by 5 | Viewed by 4164

Abstract

Current drug discovery involves finding leading drug candidates for further development. New scientific approaches include molecular docking, ADMET studies, and molecular dynamic simulation to determine targets and lead compounds. Hepatitis B is a disease of concern that is a life-threatening liver infection. The [...] Read more.

Current drug discovery involves finding leading drug candidates for further development. New scientific approaches include molecular docking, ADMET studies, and molecular dynamic simulation to determine targets and lead compounds. Hepatitis B is a disease of concern that is a life-threatening liver infection. The protein considered for the study was HBx. The hepatitis B X-interacting protein crystal structure was obtained from the PDB database (PDB ID-3MSH). Twenty ligands were chosen from the PubChem database for further in silico studies. The present study focused on in silico molecular docking studies using iGEMDOCK. The triethylene glycol monoethyl ether derivative showed an optimum binding affinity with the molecular target HBx, with a high negative affinity binding energy of −59.02 kcal/mol. Lipinski’s rule of five, Veber, and Ghose were followed in subsequent ADMET studies. Molecular dynamic simulation was performed to confirm the docking studies and to analyze the stability of the structure. In these respects, the triethylene glycol monoethyl ether derivative may be a promising molecule to prepare future hepatitis B drug candidates. Substantial research effort to find a promising drug for hepatitis B is warranted in the future. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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13 pages, 2812 KiB

Open AccessArticle

Phytochemicals Mediated Synthesis of AuNPs from Citrullus colocynthis and Their Characterization

by Bismillah Mubeen, Mahvish Ghulam Rasool, Inam Ullah, Rabia Rasool, Syed Sarim Imam, Sultan Alshehri, Mohammed M. Ghoneim, Sami I. Alzarea, Muhammad Shahid Nadeem and Imran Kazmi

Molecules 2022, 27(4), 1300; https://doi.org/10.3390/molecules27041300 - 15 Feb 2022

Cited by 10 | Viewed by 2468

Abstract

Engineered nanoparticles that have distinctive targeted characteristics with high potency are modernistic technological innovations. In the modern era of research, nanotechnology has assumed critical importance due to its vast applications in all fields of science. Biologically synthesized nanoparticles using plants are an alternative [...] Read more.

Engineered nanoparticles that have distinctive targeted characteristics with high potency are modernistic technological innovations. In the modern era of research, nanotechnology has assumed critical importance due to its vast applications in all fields of science. Biologically synthesized nanoparticles using plants are an alternative to conventional methods. In the present study, Citrullus colocynthis (bitter apple) was used for the synthesis of gold nanoparticles (AuNPs). UV-Vis’s spectroscopy, XRD, SEM and FTIR were performed to confirm the formation of AuNPs. UV-Vis’s spectra showed a characteristic peak at the range of 531.5–541.5 nm. XRD peaks at 2 θ = 38°, 44°, 64° and 77°, corresponding to 111, 200, 220 and 311 planes, confirmed the crystalline nature of AuNPs. Spherical AuNPs ranged mostly between 7 and 33 nm, and were measured using SEM. The FTIR analysis confirmed the presence of phytochemicals on the surface of AuNPs. Successful synthesis of AuNPs by seed extract of Citrullus colocynthis (bitter apple) as a capping and reducing agent represents the novelty of the present study. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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17 pages, 5028 KiB

Open AccessArticle

Stealth Liposomes (PEGylated) Containing an Anticancer Drug Camptothecin: In Vitro Characterization and In Vivo Pharmacokinetic and Tissue Distribution Study

by Durgaramani Sivadasan, Muhammad H. Sultan, Osama Ali Madkhali, Shahd Hassan Alsabei and Asia Abdullah Alessa

Molecules 2022, 27(3), 1086; https://doi.org/10.3390/molecules27031086 - 06 Feb 2022

Cited by 20 | Viewed by 3440

Abstract

Numerous attempts to overcome the poor water solubility of cam ptothecin (CPT) by various nano drug delivery systems are described in various sources in the literature. However, the results of these approaches may be hampered by the incomplete separation of free CPT from [...] Read more.

Numerous attempts to overcome the poor water solubility of cam ptothecin (CPT) by various nano drug delivery systems are described in various sources in the literature. However, the results of these approaches may be hampered by the incomplete separation of free CPT from the formulations, and this issue has not been investigated in detail. This study aimed to promote the solubility and continuous delivery of CPT by developing long-lasting liposomes using various weights (M.W. 2000 and 5000 Daltons) of the hydrophilic polymer polyethylene glycol (PEG). Conventional and PEGylated liposomes containing CPT were formulated via the lipid film hydration method (solvent evaporation) using a rotary flash evaporator after optimising various formulation parameters. The following physicochemical characteristics were investigated: surface morphology, particle size, encapsulation efficiency, in vitro release, and formulation stability. Different molecular weights of PEG were used to improve the encapsulation efficiency and particle size. The stealth liposomes prepared with PEG₅₀₀₀ were discrete in shape and with a higher encapsulation efficiency (83 ± 0.4%) and a prolonged rate of drug release (32.2% in 9 h) compared with conventional liposomes (64.8 ± 0.8% and 52.4%, respectively) and stealth liposomes containing PEG₂₀₀₀ (79.00 ± 0.4% and 45.3%, respectively). Furthermore, the stealth liposomes prepared with PEG₅₀₀₀ were highly stable at refrigeration temperature. Significant changes were observed using various pharmacokinetic parameters (mean residence time (MRT), half-life, elimination rate, volume of distribution, clearance, and area under the curve) of stealth liposomes containing PEG₂₀₀₀ and PEG₅₀₀₀ compared with conventional liposomes. The stealth liposomes prepared with PEG₅₀₀₀ showed promising results with a slow rate of release over a long period compared with conventional liposomes and liposomes prepared with PEG₂₀₀₀, with altered tissue distribution and pharmacokinetic parameters. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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12 pages, 1512 KiB

Open AccessArticle

Liposome-Mediated Delivery of MERS Antigen Induces Potent Humoral and Cell-Mediated Immune Response in Mice

by Masood Alam Khan, Ajamaluddin Malik, Mohammad A. Alzohairy, Abdulmohsen M. Alruwetei, Bader Y. Alhatlani, Osamah Al Rugaie and Arif Khan

Molecules 2022, 27(2), 403; https://doi.org/10.3390/molecules27020403 - 09 Jan 2022

Cited by 5 | Viewed by 2079

Abstract

The advancements in the field of nanotechnology have provided a great platform for the development of effective antiviral vaccines. Liposome-mediated delivery of antigens has been shown to induce the antigen-specific stimulation of the humoral and cell-mediated immune responses. Here, we prepared dried, reconstituted [...] Read more.

The advancements in the field of nanotechnology have provided a great platform for the development of effective antiviral vaccines. Liposome-mediated delivery of antigens has been shown to induce the antigen-specific stimulation of the humoral and cell-mediated immune responses. Here, we prepared dried, reconstituted vesicles (DRVs) from DPPC liposomes and used them as the vaccine carrier system for the Middle East respiratory syndrome coronavirus papain-like protease (DRVs-MERS-CoV PLpro). MERS-CoV PLpro emulsified in the Incomplete Freund’s Adjuvant (IFA-MERS-CoV PLpro) was used as a control. Immunization of mice with DRVs-MERS-CoV PLpro did not induce any notable toxicity, as revealed by the levels of the serum alanine transaminase (ALT), aspartate transaminase (AST), blood urea nitrogen (BUN) and lactate dehydrogenase (LDH) in the blood of immunized mice. Immunization with DRVs-MERS-CoV PLpro induced greater antigen-specific antibody titer and switching of IgG1 isotyping to IgG2a as compared to immunization with IFA-MERS-CoV PLpro. Moreover, splenocytes from mice immunized with DRVs-MERS-CoV PLpro exhibited greater proliferation in response to antigen stimulation. Moreover, splenocytes from DRVs-MERS-CoV PLpro-immunized mice secreted significantly higher IFN-γ as compared to splenocytes from IFA-MERS-CoV PLpro mice. In summary, DRVs-MERS-CoV PLpro may prove to be an effective prophylactic formulation to prevent MERS-CoV infection. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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20 pages, 19867 KiB

Open AccessArticle

Superfast Synthesis of Stabilized Silver Nanoparticles Using Aqueous Allium sativum (Garlic) Extract and Isoniazid Hydrazide Conjugates: Molecular Docking and In-Vitro Characterizations

by Jamal Moideen Muthu Mohamed, Ali Alqahtani, Thankakan Vimala Ajay Kumar, Adel Al Fatease, Taha Alqahtani, Venkatesan Krishnaraju, Fazil Ahmad, Farid Menaa, Ali Alamri, Ranjini Muthumani and Rajendran Vijaya

Molecules 2022, 27(1), 110; https://doi.org/10.3390/molecules27010110 - 24 Dec 2021

Cited by 36 | Viewed by 3844

Abstract

Green synthesis of silver nanoparticles (AgNPs) was synthesized from fresh garlic extract coupled with isoniazid hydrazide (INH), a commonly used antibiotic to treat tuberculosis. A molecular docking study conducted with the selected compounds compared with anthranilate phosphoribosyltransferase (trpD) from Mycobacterium tuberculosis. The [...] Read more.

Green synthesis of silver nanoparticles (AgNPs) was synthesized from fresh garlic extract coupled with isoniazid hydrazide (INH), a commonly used antibiotic to treat tuberculosis. A molecular docking study conducted with the selected compounds compared with anthranilate phosphoribosyltransferase (trpD) from Mycobacterium tuberculosis. The aqueous extract of garlic was prepared and mixed with silver nitrate (AgNO3) solution for the superfast synthesis of stable AgNPs. INH was then conjugated with AgNPs at different ratios (v/v) to obtain stable INH-AgNPs conjugates (AgNCs). The resulting AgNCs characterized by FTIR spectra revealed the ultrafast formation of AgNPs (<5 s) and perfectly conjugated with INH. The shifting of λmax to longer wavelength, as found from UV spectral analysis, confirmed the formation of AgNCs, among which ideal formulations (F7, F10, and F13) have been pre-selected. The zeta particle size (PS) and the zeta potential (ZP) of AgNPs were found to be 145.3 ± 2.1 nm and −33.1 mV, respectively. These data were significantly different compared to that of AgNCs (160 ± 2.7 nm and −14.4 mV for F7; 208.9 ± 2.9 nm and −19.8 mV for F10; and 281.3 ± 3.6 nm and −19.5 mV for F13), most probably due to INH conjugation. The results of XRD, SEM and EDX confirmed the formation of AgNCs. From UV spectral analysis, EE of INH as 51.6 ± 5.21, 53.6 ± 6.88, and 70.01 ± 7.11 %, for F7, F10, and F13, respectively. The stability of the three formulations was confirmed in various physiological conditions. Drug was released in a sustainable fashion. Besides, from the preferred 23 compounds, five compounds namely Sativoside R2, Degalactotigonin, Proto-desgalactotigonin, Eruboside B and Sativoside R1 showed a better docking score than trpD, and therefore may help in promoting anti-tubercular activity. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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Review

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32 pages, 2620 KiB

Open AccessReview

Recent Advances in Well-Designed Therapeutic Nanosystems for the Pancreatic Ductal Adenocarcinoma Treatment Dilemma

by Xiao-Yan Yang, Yuan-Fei Lu, Jian-Xia Xu, Yong-Zhong Du and Ri-Sheng Yu

Molecules 2023, 28(3), 1506; https://doi.org/10.3390/molecules28031506 - 03 Feb 2023

Cited by 2 | Viewed by 2169

Abstract

Pancreatic ductal adenocarcinoma (PDAC) is a highly malignant tumor with an extremely poor prognosis and low survival rate. Due to its inconspicuous symptoms, PDAC is difficult to diagnose early. Most patients are diagnosed in the middle and late stages, losing the opportunity for [...] Read more.

Pancreatic ductal adenocarcinoma (PDAC) is a highly malignant tumor with an extremely poor prognosis and low survival rate. Due to its inconspicuous symptoms, PDAC is difficult to diagnose early. Most patients are diagnosed in the middle and late stages, losing the opportunity for surgery. Chemotherapy is the main treatment in clinical practice and improves the survival of patients to some extent. However, the improved prognosis is associated with higher side effects, and the overall prognosis is far from satisfactory. In addition to resistance to chemotherapy, PDAC is significantly resistant to targeted therapy and immunotherapy. The failure of multiple treatment modalities indicates great dilemmas in treating PDAC, including high molecular heterogeneity, high drug resistance, an immunosuppressive microenvironment, and a dense matrix. Nanomedicine shows great potential to overcome the therapeutic barriers of PDAC. Through the careful design and rational modification of nanomaterials, multifunctional intelligent nanosystems can be obtained. These nanosystems can adapt to the environment’s needs and compensate for conventional treatments’ shortcomings. This review is focused on recent advances in the use of well-designed nanosystems in different therapeutic modalities to overcome the PDAC treatment dilemma, including a variety of novel therapeutic modalities. Finally, these nanosystems’ bottlenecks in treating PDAC and the prospect of future clinical translation are briefly discussed. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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15 pages, 1923 KiB

Open AccessReview

Drug Delivery Applications of Coaxial Electrospun Nanofibres in Cancer Therapy

by Jiayao Li, Yinan Liu and Hend E. Abdelhakim

Molecules 2022, 27(6), 1803; https://doi.org/10.3390/molecules27061803 - 10 Mar 2022

Cited by 33 | Viewed by 4135

Abstract

Cancer is one of the most serious health problems and the second leading cause of death worldwide, and with an ageing and growing population, problems related to cancer will continue. In the battle against cancer, many therapies and anticancer drugs have been developed. [...] Read more.

Cancer is one of the most serious health problems and the second leading cause of death worldwide, and with an ageing and growing population, problems related to cancer will continue. In the battle against cancer, many therapies and anticancer drugs have been developed. Chemotherapy and relevant drugs are widely used in clinical practice; however, their applications are always accompanied by severe side effects. In recent years, the drug delivery system has been improved by nanotechnology to reduce the adverse effects of the delivered drugs. Among the different candidates, core–sheath nanofibres prepared by coaxial electrospinning are outstanding due to their unique properties, including their large surface area, high encapsulation efficiency, good mechanical property, multidrug loading capacity, and ability to govern drug release kinetics. Therefore, encapsulating drugs in coaxial electrospun nanofibres is a desirable method for controlled and sustained drug release. This review summarises the drug delivery applications of coaxial electrospun nanofibres with different structures and drugs for various cancer treatments. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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12 pages, 2225 KiB

Open AccessReview

Perspectives and Prospective on Solid Lipid Nanoparticles as Drug Delivery Systems

by Osama A. Madkhali

Molecules 2022, 27(5), 1543; https://doi.org/10.3390/molecules27051543 - 24 Feb 2022

Cited by 32 | Viewed by 5483

Abstract

Combating multiple drug resistance necessitates the delivery of drug molecules at the cellular level. Novel drug delivery formulations have made it possible to improve the therapeutic effects of drugs and have opened up new possibilities for research. Solid lipid nanoparticles (SLNs), a class [...] Read more.

Combating multiple drug resistance necessitates the delivery of drug molecules at the cellular level. Novel drug delivery formulations have made it possible to improve the therapeutic effects of drugs and have opened up new possibilities for research. Solid lipid nanoparticles (SLNs), a class of colloidal drug carriers made of lipids, have emerged as potentially effective drug delivery systems. The use of SLNs is associated with numerous advantages such as low toxicity, high bioavailability of drugs, versatility in the incorporation of hydrophilic and lipophilic drugs, and the potential for production of large quantities of the carrier systems. The SLNs and nanostructured lipid carriers (NLCs) are the two most frequently used types of nanoparticles. These types of nanoparticles can be adjusted to deliver medications in specific dosages to specific tissues, while minimizing leakage and binding to non-target tissues. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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22 pages, 3879 KiB

Open AccessReview

Plant-Based Synthesis of Gold Nanoparticles and Theranostic Applications: A Review

by Uday M. Muddapur, Sultan Alshehri, Mohammed M. Ghoneim, Mater H. Mahnashi, Mohammed Abdulrahman Alshahrani, Aejaz Abdullatif Khan, S. M. Shakeel Iqubal, Amal Bahafi, Sunil S. More, Ibrahim Ahmed Shaikh, Basheerahmed Abdulaziz Mannasaheb, Noordin Othman, Muazzam Sheriff Maqbul and Mohammad Zaki Ahmad

Molecules 2022, 27(4), 1391; https://doi.org/10.3390/molecules27041391 - 18 Feb 2022

Cited by 46 | Viewed by 7732

Abstract

Bionanotechnology is a branch of science that has revolutionized modern science and technology. Nanomaterials, especially noble metals, have attracted researchers due to their size and application in different branches of sciences that benefit humanity. Metal nanoparticles can be synthesized using green methods, which [...] Read more.

Bionanotechnology is a branch of science that has revolutionized modern science and technology. Nanomaterials, especially noble metals, have attracted researchers due to their size and application in different branches of sciences that benefit humanity. Metal nanoparticles can be synthesized using green methods, which are good for the environment, economically viable, and facilitate synthesis. Due to their size and form, gold nanoparticles have become significant. Plant materials are of particular interest in the synthesis and manufacture of theranostic gold nanoparticles (NPs), which have been generated using various materials. On the other hand, chemically produced nanoparticles have several drawbacks in terms of cost, toxicity, and effectiveness. A plant-mediated integration of metallic nanoparticles has been developed in the field of nanotechnology to overcome the drawbacks of traditional synthesis, such as physical and synthetic strategies. Nanomaterials′ tunable features make them sophisticated tools in the biomedical platform, especially for developing new diagnostics and therapeutics for malignancy, neurodegenerative, and other chronic disorders. Therefore, this review outlines the theranostic approach, the different plant materials utilized in theranostic applications, and future directions based on current breakthroughs in these fields. Full article

(This article belongs to the Special Issue Recent Advances in Nano-Based Drug Delivery System)

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