Life | Special Issue : Pharmaceutical Biotechnology

Editorial

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3 pages, 210 KiB

Open AccessEditorial

Pharmaceutical Biotechnology

by Cesar Augusto Roque-Borda, Fernando Rogério Pavan and Andréía Bagliotti Meneguin

Life 2022, 12(8), 1240; https://doi.org/10.3390/life12081240 - 16 Aug 2022

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Abstract

Biotechnology and pharmacy have shown efficient results when combined to generate innovative technological products [...] Full article

(This article belongs to the Special Issue Pharmaceutical Biotechnology)

Research

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27 pages, 11476 KiB

Open AccessArticle

Discovery of Potential SARS-CoV-2 Papain-like Protease Natural Inhibitors Employing a Multi-Phase In Silico Approach

by Eslam B. Elkaeed, Ahmed M. Metwaly, Mohamed S. Alesawy, Abdulrahman M. Saleh, Aisha A. Alsfouk and Ibrahim H. Eissa

Life 2022, 12(9), 1407; https://doi.org/10.3390/life12091407 - 9 Sep 2022

Cited by 15 | Viewed by 1973

Abstract

As an extension of our research against COVID-19, a multiphase in silico approach was applied in the selection of the three most common inhibitors (Glycyrrhizoflavone (76), Arctigenin (94), and Thiangazole (298)) against papain-like protease, PLpro (PDB [...] Read more.

As an extension of our research against COVID-19, a multiphase in silico approach was applied in the selection of the three most common inhibitors (Glycyrrhizoflavone (76), Arctigenin (94), and Thiangazole (298)) against papain-like protease, PLpro (PDB ID: 4OW0), among 310 metabolites of natural origin. All compounds of the exam set were reported as antivirals. The structural similarity between the examined compound set and S88, the co-crystallized ligand of PLpro, was examined through structural similarity and fingerprint studies. The two experiments pointed to Brevicollin (28), Cryptopleurine (41), Columbamine (46), Palmatine (47), Glycyrrhizoflavone (76), Licochalcone A (87), Arctigenin (94), Termilignan (98), Anolignan B (99), 4,5-dihydroxy-6″-deoxybromotopsentin (192), Dercitin (193), Tryptanthrin (200), 6-Cyano-5-methoxy-12-methylindolo [2, 3A] carbazole (211), Thiangazole (298), and Phenoxan (300). The binding ability against PLpro was screened through molecular docking, disclosing the favorable binding modes of six metabolites. ADMET studies expected molecules 28, 76, 94, 200, and 298 as the most favorable metabolites. Then, molecules 76, 94, and 298 were chosen through in silico toxicity studies. Finally, DFT studies were carried out on glycyrrhizoflavone (76) and indicated a high level of similarity in the molecular orbital analysis. The obtained data can be used in further in vitro and in vivo studies to examine and confirm the inhibitory effect of the filtered metabolites against PLpro and SARS-CoV-2. Full article

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18 pages, 9030 KiB

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Self-Nanoemulsifying Drug Delivery System of 2-Methoxyestradiol Exhibits Enhanced Anti-Proliferative and Pro-Apoptotic Activities in MCF-7 Breast Cancer Cells

by Salwa D. Al-Qahtani, Hawazen H. Bin-Melaih, Eman M. Atiya, Usama A. Fahmy, Lenah S. Binmahfouz, Thikryat Neamatallah, Fahad A. Al-Abbasi and Ashraf B. Abdel-Naim

Life 2022, 12(9), 1369; https://doi.org/10.3390/life12091369 - 2 Sep 2022

Cited by 3 | Viewed by 2289 | Correction

Abstract

(1) Background: 2-Methoxyestradiol (2ME) is a metabolite of estrogens and possesses promising anti-proliferative and cytotoxic activities. However, it suffers unfavorable pharmacokinetic characteristics such as absorption after oral administration. The aim of this study was to prepare an optimized 2ME self-nanoemulsifying drug delivery system [...] Read more.

(1) Background: 2-Methoxyestradiol (2ME) is a metabolite of estrogens and possesses promising anti-proliferative and cytotoxic activities. However, it suffers unfavorable pharmacokinetic characteristics such as absorption after oral administration. The aim of this study was to prepare an optimized 2ME self-nanoemulsifying drug delivery system (2ME-SNEDDS) and evaluate its cytotoxicity and pro-apoptotic activities in MCF-7 breast cancer cells. (2) Methods: For optimization of the 2ME-SNEDDS, a three-component system was used in the D-optimal mixture experimental study. MCF-7 cells were incubated with the 2ME-SNEDDS and subjected to an assessment of growth inhibition, cell cycle progression, annexin V staining, caspase-3 concentration, Bax, Bcl-2, and cyclin D1 mRNA expression, and reactive oxygen species (ROS) generation. (3) Results: The optimized formula had a globule size of 94.97 ± 4.35 nm. Zeta potential was found to be −3.4 ± 1.2 mV with a polydispersity index (PDI) of 0.34. In addition, 96.3 ± 4.3% of 2ME was released from the 2ME-SNEDDS within 24 h using the activated analysis bag technique. Moreover, the prepared 2ME-SNEDDS exhibited a significant enhancement of the anti-proliferative activity against MCF-7 cells in comparison to raw 2ME. This was associated with cyclin D1 expression down-regulation and the accumulation of cells in the G0/G1 and G2/M phases. The pro-apoptotic activities of the 2ME-SNEDDS were confirmed by annexin V staining, which indicated enhanced early and late cell death. This accompanied modulation of the mRNA expression of Bax and Bcl-2 in favor of apoptosis. The 2ME-SNEDDS significantly enhanced cleaved caspase-3 concentration in comparison to raw 2ME. In addition, the 2ME-SNEDDS significantly increased the generation of ROS in MCF-7 cells. (4) Conclusions: The 2ME-SNEDDS exhibits enhanced cytotoxicity and pro-apoptotic activity in MCF-7 cells. This is mediated by, at least partially, ROS generation. Full article

(This article belongs to the Special Issue Pharmaceutical Biotechnology)

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21 pages, 6397 KiB

Open AccessArticle

Development of a Mucoadhesive Liquid Crystal System for the Administration of Rifampicin Applicable in Tuberculosis Therapy

by Kaio Pini Santos, Camila Fernanda Rodero, Camila Maríngolo Ribeiro, Maria P. D. Gremião, Rosângela Gonçalves Peccinini, Fernando Rogerio Pavan, Camron Pearce, Mercedes Gonzalez-Juarrero and Marlus Chorilli

Life 2022, 12(8), 1138; https://doi.org/10.3390/life12081138 - 28 Jul 2022

Cited by 3 | Viewed by 1818

Abstract

Since 1966, rifampicin (RIF) has been considered one of the most potent drugs in the treatment of tuberculosis (TB), which is caused by infection with M. tuberculosis (Mtb). New nanostructured formulations for RIF delivery and alternative routes of administration have been studied as [...] Read more.

Since 1966, rifampicin (RIF) has been considered one of the most potent drugs in the treatment of tuberculosis (TB), which is caused by infection with M. tuberculosis (Mtb). New nanostructured formulations for RIF delivery and alternative routes of administration have been studied as potential forms of treatment. This study evaluates a liquid crystal system for RIF delivery, using alternative drug delivery routes. The systems developed are composed of surfactant, oleylamine, and soy phosphatidylcholine. With the aid of polarized light microscopy, it was possible to determine that the developed systems had a hexagonal mesophase. All systems developed showed non-Newtonian pseudoplasticity and a high degree of thixotropy. Liquid crystal systems with RIF showed an increase in elastic potential, indicating greater mu-coadhesiveness. The evaluation of mucoadhesive forces revealed an increase in the mucoadhesive potential in the presence of mucus, indicating the presence of satisfactory mucoadhesive forces. The 9DR and 10DR liquid crystal systems, when submitted to Differential Scanning Calorimetry analysis, remained structured even at temperatures above 100 °C, showing excellent stability. The developed liquid crystal systems showed a tolerable degree of cytotoxicity and bactericidal potential, for example, the 9DR system demonstrated a reduction in bacterial load after the third day and reached zero CFU on the seventh day of the test. The developed systems were also evaluated in the preclinical model of Mtb-infected mice, using the nasal, sublingual, and cutaneous route for the delivery of RIF associated with a nanostructured liquid crystal system as a possible tool in the treatment of TB. Full article

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14 pages, 3342 KiB

Open AccessArticle

In Vitro Skin Co-Delivery and Antibacterial Properties of Chitosan-Based Microparticles Containing Ascorbic Acid and Nicotinamide

by Leonardo Delello Di Filippo, Jonatas Lobato Duarte, Cesar Augusto Roque-Borda, Fernando Rogério Pavan, Andreia Bagliotti Meneguin, Marlus Chorilli, Ana Melero, Antonio José Guillot, Caroline Magnani Spagnol and Marcos Antônio Correa

Life 2022, 12(7), 1049; https://doi.org/10.3390/life12071049 - 14 Jul 2022

Cited by 9 | Viewed by 3554

Abstract

Vitamins are widely found in nature, for example, in plants and fruits. Ascorbic acid and nicotinamide are examples of these compounds that have potent antioxidant properties, besides stimulating collagen production and depigmenting properties that protect the skin from premature aging. To overcome the [...] Read more.

Vitamins are widely found in nature, for example, in plants and fruits. Ascorbic acid and nicotinamide are examples of these compounds that have potent antioxidant properties, besides stimulating collagen production and depigmenting properties that protect the skin from premature aging. To overcome the skin barrier and reduce the instability of antioxidant compounds, alternative systems have been developed to facilitate the delivery of antioxidants, making them efficiently available to the tissue for an extended time without causing damage or toxicity. The objective of this study was to obtain chitosan biodegradable microparticles containing ascorbic acid and nicotinamide for topical delivery. The microparticles were obtained by spray drying and characterized chemically by means of scanning electron microscopy, infrared spectroscopy, X-ray diffraction, and differential exploratory calorimetry. The drugs were successfully encapsulated and the microparticles showed positive zeta potential. In vitro release assays showed a sustained release profile. The evaluation of ex vivo skin permeation and retention demonstrated low permeation and adequate retention of the compounds in the epidermis/dermis, suggesting the efficient delivery from the obtained microparticles. Antibacterial assays have shown that microparticles can inhibit the growth of microorganisms in a time- and dose-dependent manner, corroborating their use in cosmetic products for application on the skin. Full article

(This article belongs to the Special Issue Pharmaceutical Biotechnology)

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18 pages, 3287 KiB

Open AccessArticle

Tea Tree Oil Nanoemulsion-Based Hydrogel Vehicle for Enhancing Topical Delivery of Neomycin

by Heba S. Elsewedy, Tamer M. Shehata and Wafaa E. Soliman

Life 2022, 12(7), 1011; https://doi.org/10.3390/life12071011 - 7 Jul 2022

Cited by 15 | Viewed by 3071

Abstract

The present investigation aims to improve the antimicrobial influence of certain antibacterial drugs, namely, neomycin (NEO), exploiting the benefits of natural oils such as tea tree oil (TTO). Therefore, a distinctive nanolipid formulation, namely, a nanoemulsion (NE), was developed using a Central Composite [...] Read more.

The present investigation aims to improve the antimicrobial influence of certain antibacterial drugs, namely, neomycin (NEO), exploiting the benefits of natural oils such as tea tree oil (TTO). Therefore, a distinctive nanolipid formulation, namely, a nanoemulsion (NE), was developed using a Central Composite Factorial Design (CCD) approach depending on the amount of TTO and tween 80 as surfactant. The optimized NEO-NE formula exhibiting minimum globular size and maximum in vitro release was selected. For efficient topical delivery, NEO-NE was incorporated into a pre-formulated hydrogel. The developed NEO-NE-hydrogel was characterized by its physical characteristics such as pH, viscosity, and spreadability. Next, it was tested for stability under different conditions for 3 months. Ultimately, an irritation test was conducted followed by an antibacterial examination. The preparation demonstrated acceptable properties to be successfully applied topically. It showed non-significant changes in stability in both conditions up to 3 months storage when compared to a fresh preparation. It exhibited no irritation when applied on hairless animal skin. Finally, TTO revealed a good inhibition for the bacterial growth that could improve the influence of NEO antibacterial activity, indicating the efficiency of NE containing NEO prepared with TTO to be a promising antibacterial nanocarrier. Full article

(This article belongs to the Special Issue Pharmaceutical Biotechnology)

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12 pages, 2306 KiB

Open AccessArticle

Green Biosynthesis of Selenium Nanoparticles Using Orange Peel Waste: Characterization, Antibacterial and Antibiofilm Activities against Multidrug-Resistant Bacteria

by Salem S. Salem, Mona Shaban E. M. Badawy, Abdulaziz A. Al-Askar, Amr Abker Arishi, Fathy M. Elkady and Amr H. Hashem

Life 2022, 12(6), 893; https://doi.org/10.3390/life12060893 - 15 Jun 2022

Cited by 85 | Viewed by 5597

Abstract

There is an increase of pathogenic multidrug-resistant bacteria globally due to the misuse of antibiotics. Recently, more scientists used metal nanoparticles to counteract antibacterial resistance. In this study, orange peel waste (OPW) was used for selenium nanoparticles’ (Se-NPs) biosynthesis through the green and [...] Read more.

There is an increase of pathogenic multidrug-resistant bacteria globally due to the misuse of antibiotics. Recently, more scientists used metal nanoparticles to counteract antibacterial resistance. In this study, orange peel waste (OPW) was used for selenium nanoparticles’ (Se-NPs) biosynthesis through the green and ecofriendly method, and their applications as antibacterial and antibiofilm agents. Green biosynthesized Se-NPs were characterized using FTIR, XRD, SEM, EDAX, and TEM. Characterization results revealed that biosynthesized Se-NPs were highly crystalline, spherical, and polydisperse, and had sizes in the range of 16–95 nm. The biosynthesized Se-NPs were evaluated as antibacterial and antibiofilm activities against multidrug-resistant bacteria. Results illustrated that Se-NPs exhibited potential antibacterial activity against Gram-positive bacteria (S. aureus ATCC 29213 and biofilm-producing clinical isolates of S. aureus) and Gram-negative bacteria (Pseudomonas aeruginosa PAO1, MDR, biofilm, and quorum-sensing and producing clinical isolates of MDR P. aeruginosa, MDR E. coli, and K. pneumonia). Moreover, results illustrated that S. aureus ATCC 29213 was the most sensitive bacteria to Se-NPs at 1000 µg/mL, where the inhibition zone was 35 mm and MIC was 25 µg/mL. Furthermore, Se-NPs at 0.25 and 0.5 MIC decreased the biofilm significantly. The largest inhibition of biofilm was noticed in MDR K. pneumonia, which was 62% and 92% at 0.25 and 0.5 MIC, respectively. In conclusion, Se-NPs were successfully biosynthesized using OPW through the green method and had promising antibacterial and antibiofilm activity against multidrug-resistant bacteria, which can be used later in fighting resistant bacteria. Full article

(This article belongs to the Special Issue Pharmaceutical Biotechnology)

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11 pages, 1620 KiB

Open AccessArticle

Intestinal Disorder in Zebrafish Larvae (Danio rerio): The Protective Action of N-Palmitoylethanolamide-oxazoline

by Davide Di Paola, Sabrina Natale, Carmelo Iaria, Marika Cordaro, Rosalia Crupi, Rosalba Siracusa, Ramona D’Amico, Roberta Fusco, Daniela Impellizzeri, Salvatore Cuzzocrea, Nunziacarla Spanò, Enrico Gugliandolo and Alessio Filippo Peritore

Life 2022, 12(1), 125; https://doi.org/10.3390/life12010125 - 16 Jan 2022

Cited by 21 | Viewed by 3897

Abstract

IBD (Inflammatory Bowel Disease) is an inflammatory disease affecting the gastrointestinal tract that is common in both humans and veterinarians. Several studies have revealed the pharmacological properties of the oxazoline of palmitoylethanolamide (PEAOXA). Zebrafish larvae were exposed to sodium dextran sulphate (DSS) to [...] Read more.

IBD (Inflammatory Bowel Disease) is an inflammatory disease affecting the gastrointestinal tract that is common in both humans and veterinarians. Several studies have revealed the pharmacological properties of the oxazoline of palmitoylethanolamide (PEAOXA). Zebrafish larvae were exposed to sodium dextran sulphate (DSS) to induce enterocolitis and study the protective action of PEAOXA. After repetitive exposure with 0.25% DSS, larvae presented gut alteration with an increase in mucus production. Furthermore, DSS exposure induced an increase in the inflammatory pathway in the intestine, related to an increase in the Endoplasmic-reticulum (ER) stress genes. PEAOXA exposure at a concentration of 10 mg/L decreased the DSS-induced gut damage and mucus production, as well as being able to reduce the inflammatory and ER stress-related genes expression. In conclusion, our results demonstrate that the alterations induced by repeated exposure to DSS were counteracted by PEAOXA action that was able to inhibit the increase in inflammation and ER stress involved in the progression of enterocolitis. Full article

(This article belongs to the Special Issue Pharmaceutical Biotechnology)

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2 pages, 6646 KiB

Open AccessCorrection

Correction: Al-Qahtani et al. Self-Nanoemulsifying Drug Delivery System of 2-Methoxyestradiol Exhibits Enhanced Anti-Proliferative and Pro-Apoptotic Activities in MCF-7 Breast Cancer Cells. Life 2022, 12, 1369

by Salwa D. Al-Qahtani, Hawazen H. Bin-Melaih, Eman M. Atiya, Usama A. Fahmy, Lenah S. Binmahfouz, Thikryat Neamatallah, Fahad A. Al-Abbasi and Ashraf B. Abdel-Naim

Life 2023, 13(6), 1343; https://doi.org/10.3390/life13061343 - 8 Jun 2023

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In the original publication [...] Full article

(This article belongs to the Special Issue Pharmaceutical Biotechnology)

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