Kahweol is an active diterpene with anti-inflammatory, antioxidant, and anticancer properties; however, its use may be limited by unfavorable pharmacokinetic characteristics. This study aimed to develop kahweol-loaded poly(lactic-co-glycolic acid) (PLGA) and red blood cell membrane-coated PLGA (RBC-PLGA) nanoparticles and evaluate their in vitro release behavior and in vivo pharmacokinetic profiles. Kahweol-loaded PLGA nanoparticles were prepared using the emulsification-solvent evaporation method and subsequently coated with rabbit erythrocyte membranes, a type of blood cell membrane, to obtain RBC-PLGA nanoparticles. Particle size, zeta potential, morphology, and encapsulation efficiency were characterized. In vitro release studies were performed using the dialysis bag method. Pharmacokinetic profiles of free kahweol, kahweol-loaded PLGA, and kahweol-loaded RBC-PLGA nanoparticles were evaluated in rabbits following intravenous administration (0.5 mg/kg), and plasma kahweol concentrations were analyzed by LC-MS/MS. PLGA and RBC-PLGA nanoparticles showed high encapsulation efficiency (>90%) and sustained biphasic release compared with the rapid burst release of free kahweol. Pharmacokinetic analysis demonstrated that PLGA and RBC-PLGA nanoparticles reduced peak plasma concentrations and prolonged systemic exposure. Among the nanoparticles, RBC-PLGA exhibited the most prolonged pharmacokinetic profile, with delayed time to maximum plasma concentration (Tmax), extended half-life, and increased overall exposure. The nanoparticles improved the pharmacokinetic profile of kahweol by enabling sustained release and prolonged systemic exposure, supporting their potential as delivery platforms for future applications.
Unilateral testicular torsion causes ischemia–reperfusion (I/R) injury, potentially impairing testicular structure and reproductive function. This study investigated the effects of kahweol, flurbiprofen, and their combination on testicular injury and vas deferens contractility following torsion/detorsion in rats. Eighty male Wistar albino rats were divided into five groups: sham, torsion/detorsion, kahweol, flurbiprofen, and combination. Following 2 h of unilateral testicular torsion, treatments were administered immediately after detorsion and continued for six days. Histopathological, biochemical, spermatological, and isolated organ bath analyses were performed on day 7. Torsion/detorsion caused severe ipsilateral histopathological damage, increased caspase-3 immunoreactivity, and impaired vas deferens contractility. All treatments reduced caspase-3 immunoreactivity but failed to significantly improve histopathological damage. Changes in inflammatory mediators and oxidative stress markers were variable, without consistent evidence of antioxidant protection. Flurbiprofen and combination treatment partially improved noradrenaline-induced contractions, while combined treatment enhanced electrical field stimulation-induced responses in the prostatic vas deferens. Spermatological findings were limited by sample availability and variability. These findings suggest that flurbiprofen, alone or combined with kahweol, may partially improve selected functional outcomes following testicular I/R injury, although substantial structural damage persists.
1 January 2024 in Ankara Universitesi Eczacilik Fakultesi Dergisi
Amaç: Farklı ilaç uygulamalarının etken maddelerin etkinliğini arttırabildiği bilinmesine rağmen hangi ilaç salım sisteminin daha iyi olduğu konusunda birçok çalışma bulunmaktadır. Bunun nedeninin etken maddenin özelliklerine göre bu uygulamaların daha büyük avantaj sağlamasıdır. Bu çalışmada piroksikam dilaltı polimerik film uygulamasının potansiyel kullanımı araştırılmıştır. Gereç ve Yöntem: Çalışmada piroksikam dilaltı maltodekstrin ve pullulan içeren filmler hazırlanmış ve sağlıklı tavşan in vivo modelinde ilacın plazma düzeyleri araştırılmıştır. Sonuç ve Tartışma: İn vivo sonuçlar, tek doz uygulamadan sonra 10 saat içinde piroksikamın en yüksek plazma konsantrasyonlarına ulaştığını göstermiştir. Ayrıca plazma ilaç profilinde olası gastrointestinal emilime karşılık gelen ikinci bir tepe noktası oluşmamıştır. Özetle, piroksikam yüklü dilaltı polimerik film uygulamasının analjezik etkinin sağlanması amacıyla kullanılabilir özellikte olduğu tespit edilmiştir.
19 May 2026 in Ankara Universitesi Eczacilik Fakultesi Dergisi
Objective: A simple, rapid, sensitive, and cost-effective high-performance liquid chromatographic (HPLC) method was developed for the pharmacokinetic study and determination of Piroxicam.Material and Method: The chromatographic separation was performed with a Agilent ZORBAX reversed-phase C18 column (250 mm × 4,6 mm ID × 5 μm). Mobile phase composition was 0.04 M KH2PO4: acetonitrile:methanol (50:40:10) at pH 3.8. The flow rate was adjusted as 0.9 mL/min.Result and Discussion: An isocratic method was used for the analysis. The UV detector was set at 360 nm, and a retention time of 7 minutes was obtained for piroxicam. The method showed linear performance over the concentration range of 0.1–4 mg/l.
Myocardial infarction remains a leading cause of heart failure owing to the limited regenerative capacity of adult cardiac tissue, underscoring the need for biomimetic therapeutic platforms that combine structural support with biological functionality. Accordingly, this study aimed to develop a multifunctional electrospun cardiac patch by integrating decellularized neonatal porcine myocardial extracellular matrix (dECM), gelatin, and microbiota-derived postbiotics for cardiac tissue engineering. The fabricated patches were comprehensively characterized in terms of their morphology, mechanical properties, biodegradation behavior, antibacterial activity, antioxidant capacity, and in vitro biocompatibility. Postbiotics derived from Lactiplantibacillus plantarum EIR/IF-1 exhibited potent antimicrobial activity against methicillin-resistant Staphylococcus aureus, strong antioxidant capacity, and significant anti-inflammatory activity through the suppression of pro-inflammatory mediators and upregulation of IL-10 expression. Moreover, they protected H9c2 cardiomyoblasts from oxidative stress, promoted COL1A1 expression, and supported ECM remodeling. The fabricated electrospun cardiac patches exhibited a homogeneous nanofibrous architecture, mechanically suitable properties (Young’s modulus ~4 MPa), controlled biodegradation over 7 days, favorable cell viability, and maintained the biological functionality of the incorporated postbiotics. Overall, the synergistic integration of tissue-specific dECM and microbiota-derived postbiotics yielded a multifunctional biohybrid cardiac patch with favorable structural and biological properties, supporting its potential as a promising platform for myocardial regeneration and next-generation cardiac tissue engineering.