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1.
Pharmaceutics ; 16(6)2024 Jun 14.
Article in English | MEDLINE | ID: mdl-38931933

ABSTRACT

In this study, we present a new type of polymer-free hydrogel made only from nonionic surfactants, oil, and water. Such a system is produced by taking advantage of the physicochemical behavior and interactions between nonionic surfactants and oil and water phases, according to a process close to spontaneous emulsification used in the production of nano-emulsions. Contrary to the classical process of emulsion-based gel formulation, we propose a simple one-step approach. Beyond the originality of the concept, these nanoemulgels appear as very promising systems able to encapsulate and deliver various molecules with different solubilities. In the first section, we propose a comprehensive investigation of the gel formation process and its limits through oscillatory rheological characterization, characterization of the sol/gel transitions, and gel strength. The second section is focused on the follow-up of the release of an encapsulated model hydrophilic molecule and on the impact of the rheological gel properties on the release profiles.

2.
Pharmaceuticals (Basel) ; 17(5)2024 Apr 24.
Article in English | MEDLINE | ID: mdl-38794118

ABSTRACT

Miconazole nitrate (MCNR), an antifungal drug, is used to treat superficial infections. The objective of the current study was to assess the antifungal effectiveness of MCNR-loaded transethosomal gel (MNTG) against Candida albicans in an in vivo rat model. The outcomes were compared with those of the miconazole nitrate gel (MNG) and marketed Daktarin® cream (2%) based on histopathological and hematological studies. The results of the skin irritation test revealed the safety profile of the MNTG. The MNTG demonstrated the greatest antifungal activity in the histological analysis and the visible restoration of the skin, and the rats revealed an apparent evidence of recovery. Compared to the untreated group, the treated group's lymphocyte and white blood cells counts increased, but their eosinophil counts decreased. In conclusion, MNTG exhibited the greatest antifungal activity, which might be connected to the improved skin permeability of the transethosome's nanosized vesicles. Therefore, it could be considered a promising carrier for topical usage and the treatment of cutaneous candidiasis. More clinical research needs to be performed in order to demonstrate its effectiveness and safe usage in humans.

3.
J Ethnopharmacol ; 326: 117884, 2024 May 23.
Article in English | MEDLINE | ID: mdl-38350502

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Opuntia monacantha belongs to the cactus family Cactaceae and is also known by cochineal prickly pear, Barbary fig or drooping prickly pear. It was traditionally used to treat pain and inflammation. O. monacantha cladodes showed pharmacological effects such as antioxidant potential owing to the presence of certain polysaccharides, flavonoids, and phenols. AIM OF THE STUDY: This research aimed to evaluate the anti-inflammatory as well as the anti-arthritic potential of ethanol extract of Opuntia monacantha (E-OM). MATERIALS AND METHODS: In vivo edema in rat paw was triggered by carrageenan and used to evaluate anti-inflammatory activity, while induction of arthritis by Complete Freund's Adjuvant (CFA) rat model was done to measure anti-arthritic potential. In silico studies of the previously High performance liquid chromatography (HPLC) characterized metabolites of ethanol extract was performed by using Discovery Studio 4.5 (Accelrys Inc., San Diego, CA, USA) within active pocket of glutaminase 1 (GLS1) (PDB code: 3VP1; 2.30 Å). RESULTS: EOM, particularly at 750 mg/kg, caused a reduction in the paw edema significantly and decreased arthritic score by 80.58% compared to the diseased group. It revealed significant results when histopathology of ankle joint was examined at 28th day as it reduced inflammation by 18.06%, bone erosion by 15.50%, and pannus formation by 24.65% with respect to the diseased group. It restored the altered blood parameters by 7.56%, 18.47%, and 3.37% for hemoglobin (Hb), white blood count (WBC), and platelets, respectively. It also reduced rheumatoid factor RF by 13.70% with concomitant amelioration in catalase (CAT) and superoxide dismutase (SOD) levels by 19%, and 34.16%, respectively, in comparison to the diseased group. It notably decreased mRNA expression levels of COX-2, IL-6, TNF-α, IL-1, NF-κß and augmented the levels of IL-4 and IL-10 in real time PCR with respect to the diseased group and piroxicam. HPLC analysis previously performed showed that phenolic acids and flavonoids are present in E-OM. Molecular docking studies displayed pronounced inhibitory potential of these compounds towards glutaminase 1 (GLS1), approaching and even exceeding piroxicam. CONCLUSIONS: Thus, Opuntia monacantha could be a promising agent to manage inflammation and arthritis and could be incorporated into pharmaceuticals.


Subject(s)
Arthritis, Experimental , Opuntia , Rats , Animals , Cytokines/metabolism , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Plant Extracts/analysis , Glutaminase , Piroxicam/therapeutic use , Molecular Docking Simulation , Rats, Sprague-Dawley , Arthritis, Experimental/chemically induced , Arthritis, Experimental/drug therapy , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Ethanol/chemistry , Inflammation/drug therapy , Edema/chemically induced , Edema/drug therapy , Edema/metabolism , Flavonoids/therapeutic use
4.
BMC Plant Biol ; 23(1): 629, 2023 Dec 08.
Article in English | MEDLINE | ID: mdl-38062351

ABSTRACT

Chromium (Cr) toxicity significantly threatens sunflower growth and productivity by interfering with enzymatic activity and generating reactive oxygen species (ROS). Zinc quantum dot biochar (ZQDB) and arbuscular mycorrhizal fungi (AMF) have become popular to resolve this issue. AMF can facilitate root growth, while biochar tends to minimize Cr mobility in soil. The current study aimed to explore AMF and ZQDB combined effects on sunflower plants in response to Cr toxicity. Four treatments were applied, i.e. NoAMF + NoZQDB, AMF + 0.40%ZQDB, AMF + 0.80%ZQDB, and AMF + 1.20%ZQDB, under different stress levels of Cr, i.e. no Cr (control), 150 and 200 mg Cr/kg soil. Results showed that AMF + 1.20%ZQDB was the treatment that caused the greatest improvement in plant height, stem diameter, head diameter, number of leaves per plant, achenes per head, 1000 achenes weight, achene yield, biological yield, transpiration rate, stomatal conductance, chlorophyll content and oleic acid, relative to the condition NoAMF + No ZQDB at 200 mg Cr/kg soil. A significant decline in peroxidase (POD), superoxide dismutase (SOD), and catalase (CAT) while improvement in ascorbate peroxidase (APx), oil content, and protein content further supported the effectiveness of AMF + 1.20%ZQDB against Cr toxicity. Our results suggest that the treatment AMF + 1.20%ZQDB can efficiently alleviate Cr stress in sunflowers.


Subject(s)
Helianthus , Mycorrhizae , Quantum Dots , Mycorrhizae/physiology , Antioxidants/metabolism , Helianthus/metabolism , Chromium/toxicity , Chromium/metabolism , Soil , Plant Roots/metabolism
5.
Pharmaceutics ; 15(11)2023 Oct 27.
Article in English | MEDLINE | ID: mdl-38004517

ABSTRACT

Miconazole nitrate (MCNR) is a BCS class II antifungal drug with poor water solubility. Although numerous attempts have been made to increase its solubility, formulation researchers struggle with this significant issue. Transethosomes are promising novel nanocarriers for improving the solubility and penetration of drugs that are inadequately soluble and permeable. Thus, the objective of this study was to develop MCNR-loaded transethosomal gel in order to enhance skin permeation and antifungal activity. MCNR-loaded transethosomes (MCNR-TEs) were generated using the thin film hydration method and evaluated for their zeta potential, particle size, polydispersity index, and entrapment efficiency (EE%). SEM, FTIR, and DSC analyses were also done to characterize the optimized formulation of MCNR-TEs (MT-8). The optimized formulation of MCNR-TEs was incorporated into a carbopol 934 gel base to form transethosomal gel (MNTG) that was subjected to ex vivo permeation and drug release studies. In vitro antifungal activity was carried out against Candida albicans through the cup plate technique. An in vivo skin irritation test was also performed on Wistar albino rats. MT-8 displayed smooth spherical transethosomal nanoparticles with the highest EE% (89.93 ± 1.32%), lowest particle size (139.3 ± 1.14 nm), polydispersity index (0.188 ± 0.05), and zeta potential (-18.1 ± 0.10 mV). The release profile of MT-8 displayed an initial burst followed by sustained release, and the release data were best fitted with the Korsmeyer-Peppas model. MCNR-loaded transethosomal gel was stable and showed a non-Newtonian flow. It was found that ex vivo drug permeation of MNTG was 48.76%, which was significantly higher than that of MNPG (plain gel) (p ≤ 0.05) following a 24-h permeation study. The prepared MCNR transethosomal gel exhibited increased antifungal activity, and its safety was proven by the results of an in vivo skin irritation test. Therefore, the developed transethosomal gel can be a proficient drug delivery system via a topical route with enhanced antifungal activity and skin permeability.

6.
Gels ; 9(7)2023 Jul 06.
Article in English | MEDLINE | ID: mdl-37504430

ABSTRACT

PURPOSE: Numerous carbohydrate polymers are frequently used in wound-dressing films because they are highly effective materials for promoting successful wound healing. In this study, we prepared amikacin (AM)-containing hydrogel films through the cross-linking of chitosan (CS) with folic acid along with methacrylic acid (MA), ammonium peroxodisulfate (APS), and methylenebisacrylamide (MBA). In the current studies, an effort has been made to look at the possibilities of these materials in developing new hydrogel film wound dressings meant for a slow release of the antibiotic AM and to enhance the potential for wound healing. METHODS: Free-radical polymerization was used to generate the hydrogel film, and different concentrations of the CS polymer were used. Measurements were taken of the film thickness, weight fluctuation, folding resistance, moisture content, and moisture uptake. HPLC, FTIR, SEM, DSC, and AFM analyses were some of the different techniques used to confirm that the films were successfully developed. RESULTS: The AM release profile demonstrated regulated release over a period of 24 h in simulated wound media at pH 5.5 and 7.4, with a low initial burst release. The antibacterial activity against gram-negative bacterial strains exhibited substantial effectiveness, with inhibitory zones measuring approximately 20.5 ± 0.1 mm. Additionally, in vitro cytocompatibility assessments demonstrated remarkable cell viability, surpassing 80%, specifically when evaluated against human skin fibroblast (HFF-1) cells. CONCLUSIONS: The exciting findings of this study indicate the promising potential for further development and testing of these hydrogel films, offering effective and controlled antibiotic release to enhance the process of wound healing.

7.
Front Pharmacol ; 14: 1243742, 2023.
Article in English | MEDLINE | ID: mdl-38239191

ABSTRACT

Panicum antidotale has traditionally been used as a poultice to alleviate local inflammation and painful diseases. This study aimed to evaluate the anti-inflammatory, wound-healing, analgesic, and antipyretic potential of its ethanol extract (PAAPEE) in vivo for the first time. In vitro antioxidant assays of Panicum antidotale using a 2,2-diphenyl-1-picrylhydrazyl assay revealed that it showed IC50 of 62.50 ± 6.85 µg/mL in contrast to standard, ascorbic acid, that showed IC50 of 85.51 ± 0.38 µg/mL. Administration of PAAPEE at a dose of 500 mg/kg (PAAPEE-500) displayed 78.44% and 75.13% inhibition of paw edema in carrageenen and histamine-induced edema models. respectively, 6 h post-treatment compared to that of the untreated group. Furthermore, it showed 68.78% inhibition of Freund's complete adjuvant-induced edema 21 days after treatment. It reduced the animal's rectal temperature in the yeast-induced fever model to 99.45 during the fourth h post-treatment. It significantly inhibited abnormal writhing by 44% in the acetic acid-induced pain model. PAE-500 also showed enhancement in wound closure by 72.52% with respect to that of the untreated group on the 10th day post-treatment using the excision healing of wound model. Histopathological examination of skin samples confirmed this improvement, showing enhanced tissue architecture with minimal infiltration of inflammatory cells. High-performance liquid chromatography (HPLC) of PAAPEE revealed the presence of quercetin, gallic, p-coumaric, benzoic, chlorogenic, syringic, ferulic, cinnamic, and sinapic acids. Molecular docking of 5-lipoxygenase and glycogen synthase kinase-3 ß protein indicated their potential interaction within the active sites of both enzymes. Thus, P. antidotale serves as an effective natural wound-healing, anti-inflammatory, analgesic, and antipyretic agent.

8.
Int J Pharm ; 501(1-2): 278-99, 2016 Mar 30.
Article in English | MEDLINE | ID: mdl-26827920

ABSTRACT

Owing to their unique and interesting properties, extensive research round the globe has been carried out on carbon nanotubes and carbon nanotubes based systems to investigate their practical usefulness in biomedical applications. The results from these studies demonstrate a great promise in their use in targeted drug delivery systems, diagnostic techniques and in bio-analytical applications. Although, carbon nanotubes possess quite interesting properties, which make them potential candidates in the biomedical science, but they also have some inherent properties which arise great concern regarding their biosafety. In this comprehensive review, we have discussed different aspects of carbon nanotubes and carbon nanotube based systems related to biomedical applications. In the beginning, a short historical account of these tiny yet powerful particles is given followed by discussion regarding their types, properties, methods of synthesis, large scale production method, purification techniques and characterization aspects of carbon nanotubes. In the second part of the review, the functionalization of carbon nanotubes is reviewed in detail, which is not only important to make them biocompatible and stable in biological systems but also render them a great property of loading various biomolecules, diagnostic and therapeutic moieties resulting in diversified applications. In the final part of the review, emphasis is given on the pharmacokinetic aspects of carbon nanotubes including administration routes, absorption mechanisms, distribution and elimination of carbon nanotubes based systems. Lastly, a comprehensive account about the potential biomedical applications has been given followed by insights into the future.


Subject(s)
Nanotubes, Carbon , Animals , Biomedical Research , Humans , Molecular Structure , Nanotubes, Carbon/chemistry , Nanotubes, Carbon/toxicity , Pharmacokinetics
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