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Purpose: Physalis angulata Linn. (Ciplukan) is a plant widely used in traditional medicine in subtropical and tropical regions. Most studies focus on its antioxidant and anti-inflammatory activity. Many studies also reported its therapeutic potential for treating cancer, malaria, hepatitis, rheumatism, liver problems, and tumors, but few studies have reported its anti-fibrosis activity. Here, we aimed to investigate the potential of P. angulata as an antioxidant and anti-inflammatory that may be correlated with its anti-fibrosis action. Methods: In our study, we treated 3T3-L1 and TGF-ß-induced 3T3-L1 cells with an ethanol extract of P. angulata. We then monitored the cell's response, evaluated the antioxidant activity using an MTT assay, and observed the cells' migration using the cell scratch assay. We used RT-PCR to determine the expression of HIF-1α and IL-6 on TGF-ß-induced 3T3-L1 cells. Results: The ethanol extract of P. angulata showed antioxidant activity and promoted cell proliferation on 3T3-L1 cells. Interestingly, the extract inhibited the migration of TGF-ß-induced 3T3-L1 cells. Further analysis revealed that the extract could inhibit HIF-1α expression and suppress IL-6 expression on TGF-ß-induced 3T3-L1 cells. Conclusion: The ethanol extract of P. angulata showed antioxidant and anti-inflammation activities in 3T3-L1 cells. Both activities are associated with the antifibrotic activity of P. angulata's ethanol extract.
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Antioxidants are essential for reducing oxidative stress, protecting cells from damage, and supporting overall well-being. Functionalized mesoporous silica materials have garnered interest due to their flexible uses in diverse domains, such as drug delivery systems. This review aims to thoroughly examine and evaluate the progress made in utilizing functionalized mesoporous silica materials as a possible approach to enhancing antioxidant activity. The authors performed a thorough search of reliable databases, including Scopus, PubMed, Google Scholar, and Clarivate Web of Science, using precise keywords linked to functionalized mesoporous silica nanoparticles and antioxidants. The identified journals serve as the major framework for the main discussion in this study. Functionalized mesoporous silica nanoparticles have been reported to greatly enhance antioxidant activity by allowing for an increased loading capacity, controlled release behavior, the targeting of specific drugs, improved biocompatibility and safety, and enhanced penetration. The results emphasize the significant capacity of functionalized mesoporous silica (FSM) to bring about profound changes in a wide range of applications. FSM materials can be designed as versatile nanocarriers, integrating intrinsic antioxidant capabilities and augmenting the efficacy of current drugs, offering substantial progress in antioxidant therapies and drug delivery systems, as well as enhanced substance properties in the pharmaceutical field. Functionalized mesoporous silica materials are a highly effective method for enhancing antioxidant activity. They provide new opportunities for the advancement of cutting-edge treatments and materials in the field of antioxidant research. The significant potential of FSM materials to change drug delivery methods and improve substance properties highlights their crucial role in future breakthroughs in the pharmaceutical field and antioxidant applications.
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Drug-coformer systems, such as coamorphous and cocrystal, are gaining recognition as highly effective strategies for enhancing the stability, solubility, and dissolution of drugs. These systems depend on the interactions between drug and coformer to prevent the conversion of amorphous drugs into the crystalline form and improve the solubility. Furthermore, mesoporous silica (MPS) is also a promising carrier commonly used for stabilization, leading to solubility improvement of poorly water-soluble drugs. The surface interaction of drug-MPS and the nanoconfinement effect prevent amorphous drugs from crystallizing. A novel method has been developed recently, which entails the loading of drug-coformer into MPS to improve the solubility, dissolution, and physical stability of the amorphous drug. This method uses the synergistic effects of drug-coformer interactions and the nanoconfinement effect within MPS. Several studies have reported successful incorporation of drug-coformer into MPS, indicating the potential for significant improvement in dissolution characteristics and physical stability of the drug. Therefore, this study aimed to discuss the preparation and characterization of drug-coformer within MPS, particularly the interaction in the nanoconfinement, as well as the impact on drug release and physical stability.
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Nanopartículas , Dióxido de Silicio , Liberación de Fármacos , Dióxido de Silicio/química , Solubilidad , Agua/química , Nanopartículas/químicaRESUMEN
Low molecular weight chitosan (LMWC) has higher solubility and lower viscosity allowing for a wider pharmaceutical application compared to high molecular weight chitosan. LMWC chitosan can be obtained through a chitosan depolymerization process. This research aimed to produce LWMC using the combination of formic acid and ultrasonication method with the optimal condition of the depolymerization process. The chitosan depolymerization method was performed by combining formic acid and ultrasonication. The optimum conditions of the depolymerization process were obtained using the Box-Behnken design. The LMWC obtained from depolymerization was characterized to identify its yield, degree of deacetylation, the molecular weight, structure, morphology, thermal behavior, and crystallinity index. Results: The characterization results of LWMC obtained from the depolymerization process using the optimum conditions showed that the yield was 89.398%; the degree of deacetylation was 98.076%; the molecular weight was 32.814 kDa; there was no change in the chemical structure, LWMC had disorganized shape, there was no change in the thermal behavior, and LWMC had a more amorphous shape compared to native chitosan. Conclusion: The production of LWMC involving depolymerization in the presence of weak acid and ultrasonication can be developed by using the optimal condition of the depolymerization process.
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Investigation into the solid-state transition among drug polymorphs has been more intense lately. Many factors induce the transformation of polymorphs during manufacturing processes. Efavirenz (EFV), an AIDS therapy drug, has more than 23 polymorphs, but very little information has been reported on them. This study aimed to perform a characterisation of EFV polymorph properties and to predict the kinetics and mechanism of the polymorphic transformation of EFV during manufacturing processes. The bimorphism study was conducted by Differential Scanning Calorimetry (DSC) thermal analysis. The phase transition kinetics of the polymorphs was monitored by X-ray powder diffraction and the quantification of concomitant polymorphs was examined using Rietveld refinement with MAUD ver. 2.7 as a software aid. To predict the solid-state transition, correlation coefficients of solid-state kinetic models were fitted to the experimental data. The results show that Form I and Form II of EFV were thermodynamically shown to be monotropy related. By fitting the experimental data, it was found that isothermal treatment had the best model fit with the phase boundary reaction in the two-dimensional model (G2). Accordingly, by employing mechanical treatment (grinding), it was predicted that the transition mechanism is a second-ordered reaction (R2). The activation energy of the transition during isothermal treatment calculated by the Arrhenius plot was found to be 23.051 kJ mol-1; the half-lif of Form II at ambient temperature was 428.05 min (~7.1 h).
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Polymorphism occurs in pharmaceutical compounds affect to the physicochemical quality and goal of therapy. Thus, quality evaluation of different crystal forms should be assessed especially the solubility and dissolution behaviors among polymorphic forms, which correlate to bioavailability and therapy efficacy. To achieved the different of a polymorph various solvent were used such as acetonitrile, methanol, ethyl acetate, acetone, water, n-hexane, and n-heptane. All of the crystal modification resulted were characterized by a polarization light microscopy (PLM), Fourier-Transform Infrared (FTIR) differential scanning calorimetry (DSC) and powdered X-ray diffraction (PXRD). Besides that, nature of solubility in water (24 and 48 hours test times) and particulate dissolution profile (an hour test) were carried out. There were various polymorphs success resulted and have significant differences in morphology, definite spectral fingerprints, crystal structure and thermal behavior. From the solubility of the samples found the top three highest soluble forms i.e. Form 6, 2 and 3, respectively. But there are showed became in order reverse performance after 60 minutes dissolution (Form 3, 2 and 6, respectively). The polymorphic forms of EFV were successful to obtained by the solvents treatment. Therefore, the physicochemical properties of polymorphic forms from active pharmaceutical ingredients (APIs) should be carefully considered in dosage forms pre-formulation approaches.