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The use of chitosan as an effective carrier of theophylline – an anti-asthmatic drug

Aziz Noor Firas, Hussein-Al-Ali Samer Hasan, Ghareeb Mowafaq Mohammed, Nashwan Nashwan Abdallah

Polimery

2023

Vol. 68, nr 3

157--168

In order to solve the problem of frequent drug dosing and increase its effectiveness, theophylline (THP) was deposited on chitosan nanoparticles (CSNPs). THP-CSNPs nanocomposites with the composition of 50, 75, 100 or 150 mg of chitosan (CS) and 25, 50, 75, 100 or 200 mg of tripolyphosphate (TPP) at pH 4.0, 5.0, 6.0 and 6.5 were prepared, and a constant weight of THP of 100 mg. The nanocomposites were characterized by X-ray diffraction (PXRD), field emission scanning electron microscopy (FE-SEM), and Fourier transform infrared spectroscopy (FTIR). The rate of drug release was also tested. The Minitab 18 program was used to analyze the results. The independent variables were the CS, TPP, and pH, while loading efficiency, zeta potential, and particle size were the dependent variables. The nanocomposites successfully transported and protected the drug, providing its sustained release.

W celu rozwiązania problemu częstego dawkowania leku i zwiększenia jego efektywności teofilinę (THP) osadzono na nanocząstkach chitozanu (CSNPs). Przygotowano nanokompozyty THP-CSNPs o składzie 50, 75, 100 lub 150 mg chitozanu (CS) oraz 25, 50, 75, 100 lub 200 mg trójpolifosforanu (TPP) przy pH 4,0, 5,0, 6,0 i 6,5 oraz stałej masie THP wynoszącej 100 mg. Nanokompozyty charakteryzowano za pomocą dyfrakcji promieniowania rentgenowskiego (PXRD), skaningowej mikroskopii elektronowej z emisją polową (FE-SEM), spektroskopii w podczerwieni z transformacją Fouriera (FTIR). Zbadano również szybkość uwalniania leku. Do analizy wyników wykorzystano program Minitab 18. Niezależnymi zmiennymi były CS, TPP i pH, podczas gdy wydajność ładowania, potencjał zeta i wielkość cząstek były zmiennymi zależnymi. Nanokompozyty z powodzeniem transportowały i zabezpieczały lek, zapewniając jego przedłużone uwalnianie.

Multiobjective optimization of fluphenazine nanocomposite formulation using NSGA-II method

Abu Sharar Ahmed Adnan, Ramadan Saleem Z., Hussein-Al-Ali Samer Hasan

Materials Science Poland

2021

Vol. 39, No. 4

517--544

The World Health Organization (WHO, 2019) reports that schizophrenia affects approximately 20 million people worldwide, and the annual number of new cases is estimated at 1.5%/10,000 people. As a result, there is a demand for making the relevant medicines work better. Using a fluphenazine (FZN) drug delivery system that has been optimized using nanoparticles (NPs) technology is an important alternative treatment option for noncompliant patients with schizophrenia. Compared to the conventional delivery system, the NPs delivery system provides a controlled-release treatment, minimizes drug levels reaching the blood, and has fewer side effects as well. As a result of using the NPs delivery system, patients can obtain the benefits of reduced daily dosing and improved compliance. In this context, this study was performed to develop a mathematical model for FZN to optimize its nanocomposite delivery system using a mixture-process DoE and multiobjective optimization (MOO) approaches. The influences of NPs input fabrication parameters [i.e., FZN percentage, chitosan (CS) percentage, sodium tripolyphosphate (TPP) percentage, and pH] were investigated by mixture-designed experiments and analyzed by analysis of variance (ANOVA); subsequently, based on the results of the analysis, three regression models were built for size, zeta potential (ZP), and drug loading efficiency (LE%); and thereafter, these models were validated using 26 experiments with three replicates. The MOO approach was employed using a non-dominated sorting genetic algorithm (NSGA-II) to provide the optimal fitness value of each objective function by minimizing NPs size, maximizing ZP, and maximizing LE%. Test of hypotheses showed no statistical differences between the average observed values and the corresponding predicted values calculated by the regression models (126.6 nm, 18.7 mV, and 91.6%, respectively). As there is no benchmark available for the optimal NPs input fabrication parameters in the literature, the optimized formulation was further characterized using X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), polydispersity index (PdI), and differential scanning calorimetry (DSC). Those tests indicated that FZN was successfully encapsulated into the final nanocomposite. Furthermore, an in-vitro drug release study was carried out and showed that at least 5 days would be needed for FZN to be fully released from its nanocomposite in a sustained-release pattern. The nanocomposite could serve as a model for the controlled and extended delivery of many drugs.