Levocetirizine Dihydrochloride-Loaded Chitosan Nanoparticles: Formulation and <i>In Vitro</i> Evaluation

Abstract

Bu çalışmanın amacı, biyoyararlanımı iyileştirerek plazma ilaç konsantrasyonunu optimize etmek için uzatılmış etkiye ve yüksek yükleme kapasitesine sahip, mikron altı düzeyde levosetirizin dihidroklorür (LCD) yüklü kitosan nanopartijkülleri formüle etmektir. Gereç ve Yöntemler: Bu çalışmada LCD, oral uygulama amacı ile kitosan nanopartiküllerine püskürterek kurutma yöntemi kullanılarak yüklenmiştir. Nanopartiküllerin in vitro karakteristik özellikleri detaylıca incelenmiştir. Bulgular: LCD püskürterek kurutma yöntemi ile polimerik matrise başarıyla yüklenmiştir. Nanopartiküllerin karakterizasyonu yüklenme etkinliği, parçacık büyüklüğü, zeta potansiyel, morfoloji, polidisperslik indisi ve yüksek basınçlı sıvı kromatografisi ile LCD tayini dahil olmak üzere yapılmıştır. Nanopartiküllerden LCD salımı simüle edilmiş bağırsak vasatında (pH 6,8) diyaliz tübü kullanılarak gerçekleştirilmiştir. Nanopartiküllerden LCD salımına ait in vitro salım profilleri Korsmeyer-Peppas modeline uygunluk gösterek uzatılmış salım göstermiştir. Sonuç: Kitosan bazlı LCD yüklü polimerik nanopartiküllerin etkin madde için umut verici bir ilaç taşıyıcı sistem olduğu sonucuna varılabilir. Anahtar kelimeler: Levosetirizin dihidroklorür, kitosan, polimerik nanopartikül, püskürterek kurutma Objectives:The aim of the present study was to formulate levocetirizine hydrochloride (LCD)-loaded chitosan nanoparticles at submicron level with high entrapment efficiency and prolonged effect for optimizing the plasma drug concentration enhancing bioavailability. Materials and Methods: LCD was successfully incorporated into chitosan nanoparticles by spray drying for the purpose of oral application. In vitro characteristics were evaluated in detail. Results: LCD was successfully loaded into the polymeric matrices by spray drying. Characterization of the nanoparticles including encapsulation efficiency, particle size, zeta potential, morphology, polydispersity index, solid-state characterizations, and LCD quantification by high performance liquid chromatography was performed. The release pattern of LCD from the nanoparticles was determined using a dialysis tube in simulated intestinal fluid (pH 6.8). In vitro release profiles indicated prolonged release of LCD from the nanoparticles that followed the Korsmeyer-Peppas kinetic model. Conclusion:Chitosan-based LCD-loaded polymeric nanoparticles appear to be a promising drug delivery system for the active agent.

PLGA-based biodegradable microspheres in drug delivery: recent advances in research and application

“…The spray drying process usually includes four stages: atomization, droplet mixing with dry gas, solvent volatilization, and product separation, in which the technological conditions and parameters of the atomization process play a decisive role in the droplet size distribution (Ré, 2006 ; Liu et al, 2015 ; Deshmukh et al, 2016 ; Messa et al, 2020 ), such as the selection of atomizer, nozzle pressure, feed or air flow rate, etc (Bowey & Neufeld, 2010 ; Shi et al, 2020 ). The spray drying method can generate particles in one step quickly and continuously, eliminating the need for a separate drying process in other preparation methods (Helbling et al, 2020 ; Ozturk & Kiyan, 2020 ; Yurtdas & Ozturk, 2020 ). The entire preparation process is automated, and a relatively high encapsulation rate can be obtained (Calegari et al, 2020 ), which is suitable for the encapsulation of proteins or peptides (Aydin, 2020 ; Shi et al, 2020 ), plasmid DNA (Walter et al, 2001 ; Atuah et al, 2003 ; Jilek et al, 2004 ), and small molecule drugs (Waldron et al, 2014 ).…”

Preparation, Characterization, Antioxidant Activities, and Determination of Anti-Alzheimer Effects of PLGA-Based DDSs Containing Ferulic Acid

“…In the physical mixture, both the characteristic melting peaks of FA and the peaks belonging to the glass transition temperature of PLGA were observed. The disappearance of the FA melting peak in the A-FA coded NP formulation’s thermogram indicated that FA was diffused molecularly throughout the polymeric framework and contained in its amorphous state. , Furthermore, the thermogram demonstrated that FA and the polymers did not interact. These data obtained are important because the presence of the drug in molecular dispersion form helps with its extended-release feature …”

Therapeutic Targeting of Lung Adenocarcinoma with Mannose-Coated Chitosan/Copper Nanocluster–Levocetirizine Nanocomposite

“…14 The positively charged amino groups of chitosan can bind to the negatively charged mucosal membranes, thus prolonging the time of contact. 15 As chitosan nanoparticles tend to have different properties compared to those of the bulk material, the former can be modified to suit the desired parameters. They can also be fashioned into nanospheres, nanocapsules, and nanofibers according to the need.…”

“…Also, since it is a linear polymer of glucosamine and acetylglucosamine, it biodegrades into harmless amino sugars that are absorbed by the body . The positively charged amino groups of chitosan can bind to the negatively charged mucosal membranes, thus prolonging the time of contact . As chitosan nanoparticles tend to have different properties compared to those of the bulk material, the former can be modified to suit the desired parameters.…”