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1.
Curr Pharm Des ; 29(11): 865-882, 2023.
Article in English | MEDLINE | ID: mdl-36967465

ABSTRACT

The insertion of topical antimicrobials in wound treatment represented an important role in patient management. Among these agents, silver sulfadiazine (AgSD), introduced in the therapy of wounds and burns in the 1960s, is considered the gold standard in treatment due to its mechanism of action, in addition to its proven efficacy and safety. The association of AgSD with polymers for the development of curative formulations has been reported. The evaluation of the physical-chemical properties of these systems with the aid of analytical techniques of characterization is essential for the determination of their activities, besides allowing the detection of possible incompatibilities between AgSD and polymers. Thus, this review presents the main techniques of physicochemical characterization used in the evaluation of systems containing AgSD with curative purposes in order to provide parameters to ensure the efficacy and safety of these new therapeutic options. Microscopic, thermoanalytical, and spectroscopic techniques, for example, provide information on system properties such as surface chemical composition, crystallinity, morphology, and thermal stability of curative formulations containing AgSD. These techniques are important in the selection of the most appropriate techniques during the development of a polymeric curative system containing AgSD, in addition to providing information for cost reduction of a possible scale-up and the establishment of methodologies for quality control of these systems to ensure their efficacy and safety.


Subject(s)
Anti-Infective Agents, Local , Silver Sulfadiazine , Humans , Silver Sulfadiazine/pharmacology , Silver Sulfadiazine/chemistry , Bandages , Polymers
2.
Lasers Med Sci ; 37(8): 3183-3191, 2022 Oct.
Article in English | MEDLINE | ID: mdl-35723829

ABSTRACT

This study aims to develop and characterize NCL loaded with ZnF16Pc (Pc) for application in antimicrobial photodynamic therapy. For the development of the NLC, the fusion-emulsification technique followed by sonication was applied. NLC and Pc-NLC were characterized in terms of mean diameter (Dm.n), polydispersity index (PdI), zeta potential (ZP), encapsulation efficiency (%EE), transmission electron microscopy (TEM), differential scanning (DSC), photobleaching and singlet oxygen generation in cellular systems (SOSG), and in vitro release assays performed by the beaker method, using dialysis membranes. Cell viability was performed by colony forming units (CFU/mL). The mean size of NLC and Pc-NLC was 158 nm ± 1.49 to 161.80 nm and showed PdI < 0.3 and ZP between -17.8 and -19.9, and stable during storage time (90 days). The TEM presented spherical particles, the Pc-NLC promoted the encapsulation of 75.57% ± 0.58. DSC analysis confirmed that there was no incompatibility between Pc and NLC. The analysis of the photodegradation profile proved to be photostable after encapsulation and this corroborates the data obtained by SOSG. In vitro release showed controlled and prolonged release. PDT Pc-NLC exhibited greater antifungal effect against C. albicans (3 log10 reduction) than Pc-NLC without light (1 log10 reduction). NLC can be an alternative to the application of Pc and improve the effect during PDT treatment.


Subject(s)
Candida albicans , Nanostructures , Antifungal Agents/pharmacology , Drug Carriers/chemistry , Drug Carriers/pharmacology , Indoles , Lipids/chemistry , Nanostructures/chemistry , Organometallic Compounds , Particle Size , Singlet Oxygen
3.
Polymers (Basel) ; 13(14)2021 Jul 17.
Article in English | MEDLINE | ID: mdl-34301102

ABSTRACT

Cellulose acetate (ACT) is one of the most important cellulose derivatives due to its biodegradability and low toxicity, presenting itself as one of the main substitutes for synthetic materials in the development of wound dressing films. The incorporation of a N-acylhydrazonic derivative (JR19), with its promising anti-inflammatory activity, may represent an alternative for the treatment of skin wounds. This work aims to develop and to physicochemically and mechanically characterize ACT films containing JR19. The films were prepared using the 'casting' method and further characterized by thermoanalytical and spectroscopic techniques. In addition, mechanical tests and morphological analysis were performed. Thermogravimetry (TG) and differential scanning calorimetry (DSC) analyses showed that the thermal events attributed to excipients and films were similar, indicating the absence of physical incompatibilities between ACT and JR19. Infrared spectroscopy showed that JR19 was incorporated into ACT films. The characteristic band attributed to C≡N (2279 to 2264 cm-1) was observed in the spectra of JR19, in that of the physical mixture of JR19/ACT, and, to a lesser extent, in the spectra of JR19 incorporated into the ACT film, suggesting some interaction between JR19 and ACT. X-ray diffraction (XRD) evidenced the suppression of the crystallinity of JR19 (diffraction peaks at 8.54°, 12.80°, 14.09°, 16.08°, 18.19°, 22.65°, 23.59°, 24.53°, 25.70°, 28.16° and 30.27°2θ) after incorporation into ACT films. The mechanical tests indicated the adequate integrity of the films and their resistance to bending. The morphological characterization showed JR19 crystals along with a homogeneously distributed porous structure throughout the surface of the films with an average diameter of 21.34 µm and 22.65 µm of the films alone and of those incorporating JR19F, respectively. This study was able to characterize the ACT films incorporating JR19, showing their potential to be further developed as wound healing dressings.

4.
Drug Deliv Transl Res ; 10(6): 1748-1763, 2020 12.
Article in English | MEDLINE | ID: mdl-32924099

ABSTRACT

The Melaleuca alternifolia essential oil (MEO) has been widely used due to its healing and antimicrobial action. Its incorporation into drug delivery systems is a reality, and numerous studies have already been developed for this purpose. In this regard, the aim of this work was to develop, characterize, and evaluate the in vivo pharmacological activity of bicontinuous microemulsions (BME) containing MEO. Through diagram construction, a formulation consisting of Kolliphor® HS 15 (31.05%), Span® 80 (3.45%), isopropyl myristate (34.5%), and distilled water (31%) was selected and MEO was incorporated in the proportion of 3.45% (v/v). Morphological analysis characterization confirms that the system studied herein is a BME. The evaluated formulation showed physicochemical characteristics that allow its topical use. Rheologically, samples were characterized as pseudo-plastic non-Newtonian thixotropic fluids. The chromatographic method developed is in accordance with the current recommendations. The extraction method used assured a 100% recovery of the pharmacological marker (terpinen-4-ol). In vivo studies suggest that BME loaded with MEO may contribute to the healing process of skin wounds. In addition, it demonstrated antibacterial activity for Gram-positive and Gram-negative bacteria. Therefore, the BME system loaded with MEO is promising as a healing and antimicrobial agent for skin wounds.Graphical abstract.


Subject(s)
Anti-Bacterial Agents , Melaleuca , Tea Tree Oil , Wound Healing/drug effects , Anti-Bacterial Agents/pharmacology , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Melaleuca/chemistry , Tea Tree Oil/pharmacology
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