Zsófia Edit Pápay1, Nóra Mike-Kaszás1, Petra Füredi1, Lívia Budai1, Annamária Kósa2, Béla Böddi2, István Antal1
1 Semmelweis University, Department of Pharmaceutics, Budapest
2 Eötvös Loránd University, Faculty of Sciences, Department of Plant Anatomy, Budapest
Introduction: The relevance of developing biocompatible particles, which delivering the active ingredients in a harmless and effective way, is increasing. The human body consists of several complex fluids therefore the viscosity of drug delivery systems can play an important role. It is well known that both locust bean gum and chitosan are biocompatible excipients and possess viscoleastic properties similarly to human lung fluid. The anticancer action of apigenin against lung carcinoma has proven. This bioactive flavonoid with poor water solubility was classified as BCS II. drug therefore enchancement of its solubility is essential.
Aims: The aims of this work were to prepare and characterize novel biocompatible and viscoelastic particles, loaded with apigenin.
Method: The human serum albumin and locust bean gum (HSA-LBG) conjugates in 1:3 and 1:6 molar ratios were prepared by Maillard reaction at 60°C and 80% relative humidity. The products were investigated by FTIR and fluorescence spectroscopy. As the next step, 1% chitosan (Ch) solution (pH 5.2) was added and high pressure homogenization was applied at 1250 bar for 5 and 10 cycles. The physical properties of the samples such as particle size, viscosity and drug loading efficiency were investigated.
Results: The Maillard reaction between HSA and LBG was verified by FTIR and fluorescence spectroscopy. Utilizing high pressure homogenization significantly decreased the particle size and the bioactive apigenin could be effectively loaded into the particles. High encapsulation efficiency could be achieved with 1:6 conjugate. Furthermore, rheological measurements demonstrated that the apigenin loaded HSA/LBG/Ch particles have viscoelastic properties.
Conclusion: The results indicate that the developed HSA/LBG/Ch particles with viscoelastic properties may have great potential for lung cancer therapy.
Supported by the ÚNKP-17-4-I-SE New National Excellence Program of the Ministry of Human Capacities.
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