Poowadon Muenraya

The cashew apple (Anacardium occidentale L.) is rich in antioxidant bioactive constituents that have anti-aging and wound healing properties. The objective of this study is to evaluate the biological activities of cashew apple extract (CAE) and to improve the issue involving the instability of ascorbic acid, the principal active compound, by encapsulating the extract in liposomes in order to enhance its stability and skin permeation for cosmetic applications. CAE was obtained from fresh cashew apple via ethanol maceration, solvent evaporation, and freeze-drying. Ascorbic acid content, total phenolic content (TPC), total flavonoid content (TFC), and total caffeoylquinic acid content (TCQAC) were determined. The ascorbic acid content and its tautomer in the extract were quantified using the LC-MS/MS method. Biological activities, including antioxidant, anti-tyrosinase, fibroblast collagen synthesis, cytoprotection against oxidative stress, wound healing, and cytotoxicity, were assessed. CAE was encapsulated in liposomes to enhance the stability of its inherent ascorbic acid and improve its skin in comparison to free-CAE. The CAE and liposomal-CAE were incorporated and formulated into a solution, and their physicochemical stability was assessed after storage. CAE appeared as a brown, viscous liquid with a characteristic sweet, fruity scent. Each gram of CAE contained 0.90 ± 0.05 mg of ascorbic acid, TPC, 81.40 ± 7.14 mg of gallic acid equivalents (GAE), TFC, 3.73 ± 0.30 mg of rutin equivalents (RE), and TCQAC, 4.48 ± 0.05 mg of chlorogenic acid equivalents (CGAE). CAE exhibited antioxidant properties (IC₅₀ = 282.19 ± 11.16 and 963.66 ± 3.95 µg/mL for DPPH and ABTS assay, respectively) and weak anti-tyrosinase activity (IC₅₀ = 4213.77 ± 138.97 µg/mL). It was non-cytotoxic to fibroblast and monocyte cells at a concentration of less than 1 mg/mL. In vitro wound healing assays demonstrated that CAE stimulated collagen production in a dose-dependent manner at CAE concentrations above 250 µg/mL. Additionally, CAE exhibited cytoprotective effects against H₂O₂-induced oxidative stress and did not induce inflammatory responses in immune cells. The liposomal formulation containing CAE achieved high encapsulation efficiency (79.75–84.55%) based on ascorbic acid content. In skin permeation studies, CAE-loaded liposomes demonstrated an enhancement ratio approximately two-fold greater than that of free-CAE. Stability testing over 3 months showed that the ascorbic acid content in CAE-loaded liposomes remained significantly higher than that in the free-CAE under both refrigerated and long-term conditions (30 °C/75% RH). CAE demonstrated potential anti-aging properties for improving aging skin. Liposomal incorporation markedly improved ascorbic acid stability and skin permeability.

BrSPR-20-P1 antimicrobial peptide (P1-AMP) is a novel antimicrobial peptide isolated from Brevibacillus sp. SPR-20 and has been developed as a liposomal in chitosan hydrogel. It has potential to be used as a topical antimicrobial agent.

Inhaled colistin is used to treat pneumonia and respiratory infections through nebulization or dry powder inhalers. Nevertheless, the development of a metered-dose inhaler (MDI) for colistin, which could enhance patient convenience and treatment efficacy, has not yet been developed. Colistin is known for its ability to induce cellular toxicity. Gold nanoparticles (AuNPs) can potentially mitigate colistin toxicity. Therefore, this study aimed to evaluate the antimicrobial effectiveness of colistin conjugated with chitosan-capped gold nanoparticles (Col-CS-AuNPs) and their potential formulation for use with MDIs to deliver the aerosol directly to the deep lung. Fourier-transform infrared spectroscopy, nuclear magnetic resonance, and elemental analysis were used to characterize the synthesized Col-CS-AuNPs. Drug release profiles fitted with the most suitable release kinetic model were evaluated. An MDI formulation containing 100 µg of colistin per puff was prepared. The aerosol properties used to determine the MDI performance included the fine particle fraction, mass median aerodynamic diameter, and geometric standard deviation, which were evaluated using the Andersen Cascade Impactor. The delivered dose uniformity was also determined. The antimicrobial efficacy of the Col-CS-AuNP formulation in the MDI was assessed. The chitosan-capped gold nanoparticles (CS-AuNPs) and Col-CS-AuNPs had particle sizes of 44.34 ± 1.02 and 174.50 ± 4.46 nm, respectively. CS-AuNPs effectively entrapped 76.4% of colistin. Col-CS-AuNPs exhibited an initial burst release of up to 60% colistin within the first 6 h. The release mechanism was accurately described by the Korsmeyer–Peppas model, with an R² > 0.95. The aerosol properties of the Col-CS-AuNP formulation in the MDI revealed a high fine particle fraction of 61.08%, mass median aerodynamic diameter of 2.34 µm, and geometric standard deviation of 0.21, with a delivered dose uniformity within 75–125% of the labeled claim. The Col-CS-AuNP MDI formulation completely killed Escherichia coli at 5× and 10× minimum inhibitory concentrations after 6 and 12 h of incubation, respectively. The toxicity of CS-AuNP and Col-CS-AuNP MDI formulations in upper and lower respiratory tract cell lines was lower than that of free colistin. The stability of the Col-CS-AuNP MDI formulation was maintained for at least 3 months. The Col-CS-AuNP MDI formulation effectively eradicated bacteria over a 12-h period, showing promise for advancing lung infection treatments.

Colistin is a potent peptide antibiotic that is effective against Gram-negative bacteria. However, nephrotoxicity limited its clinical use. Silver nanoparticles (AgNPs) have gained attention as a potential antimicrobial agent and nanodrug carrier. The conjugation of antibiotics and AgNPs has been found to increase the activity and decrease drug toxicity. In this study, colistin was conjugated with AgNPs (Col-AgNPs), which was confirmed by Fourier-transform infrared (FT-IR) and energy-dispersive X-ray (EDX) spectra. The optimized Col-AgNPs had the proper characteristics, including spherical shape, monodispersity, nanosized particle, high surface charge, and good stability. The powder X-ray diffraction (PXRD) pattern supported the crystallinity of Col-AgNPs and AgNPs. The drug loading of Col-AgNPs was 11.55 ± 0.93%. Col-AgNPs had higher activity against Gram-negative bacteria (Escherichia coli, Klebsiella pneumonia, and Pseudomonas aeruginosa) than AgNPs and colistin. The mechanism of actions of Col-AgNPs involved membrane disruption and genomic DNA damage. The Col-AgNPs and AgNPs were biocompatible with human red blood cells and renal cells at concentrations up to 16 µg/mL. Interestingly, Col-AgNPs exhibited higher cell survival than AgNPs and colistin at 32 µg/mL. Our results revealed that the Col-AgNPs could enhance the antimicrobial activity and cell biocompatibility more than colistin and AgNPs.

The aim of this study was to investigate the drug release behavior from bacterial cellulose (BC). Ibuprofen and propranolol hydrochloride were used as model drugs to represent low and highly water soluble drugs. The drug was loaded into the BC by immersing the partially swollen BC in a solution of drug concentrations ranging from 0.05 to 0.5 mg mL⁻¹ and then drying by two different methods: air-drying and freeze-drying. The results showed that the type of drug and the drying method influenced the drug loading efficiency and drug release behavior. For ibuprofen, high drug loading efficiency was found when loading the drug into BC at low concentration and vice versa for propranolol hydrochloride. The drug-loaded BC prepared by the freeze-drying method showed a sustained release regardless of drug type and drug-loaded amount. The sustained release followed the Higuchi and Korsmeyer–Peppas models. On the other hand, when using the air-drying method, BC loaded with ibuprofen showed immediate release at every drug-loaded amount. However, BC loaded with propranolol hydrochloride showed immediate release at the high drug-loaded amount but showed sustained release at the low drug-loaded amount. The release of drug from a drug-loaded BC prepared by air-drying method tended to follow first-order kinetics. In conclusion, the drug loading concentration and the drying method in the drug-loaded BC preparation influenced the drug release characteristics of the BC-based drug delivery system.

Sildenafil is a specific inhibitor of the phosphodiesterase type 5 (PDE-5) enzyme that protects cyclic guanosine monophosphate from breakdown by PDE-5. It is a biopharmaceutical categorization system Class II medication with low bioavailability because it is almost insoluble in water. The objectives of this study were to prepare sildenafil cocrystals with co-former molecules including aspirin (acetylsalicylic acid [ASA]), fumaric acid (FMA), and benzoic acid (BZA) to improve the water solubility of sildenafil. The cocrystals were prepared by antisolvent addition (AA) and slow solvent evaporation (SE) methods. The stoichiometric ratios of sildenafil and co-former molecules were varied. The obtained crystals were characterized by stereomicroscope, Fourier transformed infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR), and powder X-ray diffraction (PXRD). The water solubility of sildenafil cocrystals was compared with sildenafil base. In the AA method, the crystals only form in sildenafil-ASA reaction. These crystals were not cocrystals between sildenafil and ASA because they were formed to new substances that were confirmed by single-crystal X-ray diffraction. In the SE method, the cocrystals were successfully prepared in the reaction of sildenafil with ASA, FMA, and BZA which use acetone or ethyl acetate as a solvent. The obtained crystals are irregular shapes and their FT-IR, NMR, and PXRD results exhibited the characteristics of sildenafil and its co-former. The stoichiometric ratios of sildenafil and co-formers after cocrystallization were different from an initial of crystallization. The sildenafil cocrystals with ASA, FMA, and BZA by SE method had higher water solubility than sildenafil base. The sildenafil-FMA cocrystals had the highest water solubility and increased up to five times when compared with sildenafil base.